Sorry I've been away for so long, been working lots of overtime to pay off medical and other bills due to our medical insurance not covering a very important medical problem, it was not deemed "life or death" what a crock. I've got a lot of reading to do here, love all the posts and references at this place.
This is a culmination of several month experimentation & my own research complexing the novel new rare RC 25i-nbome psychedelic compound discovered in Berlin to hydroxy-propyl-beta-cyclodextrin (HPBCD) to achieve imho nearly 95% sublingual or buccal absorption in 20 minutes, negating the need for nasal application, "plugging", or IM shot. Years ago as an experiment I complexed a very small amount of the very hydrophobic compound testosterone freebase powder (0.033mg solubility in 1ml h2o) but when complexed to HPBCD (1 hour of stirring in solution of water and HPBCD) becomes 100% water soluble, a published study by Dr. Joseph Pitha showed 95% absorption of cyclodextrin complexed testosterone freebase in 20 minutes when applied sublingually. 25i-nbome is also very hydrophobic (water-fearing) just like testosterone. Amazingly, HPBCD can be used with not only the freebase drug version, but also the hcl drug version, as the cyclodextrin en-cages any lipophilic part of the molecule, still increasing the penetration effectiveness of even the HCL version of drugs according to a paper I've seen. I've read of lots of folks having an impossible time even getting the hcl version of this drug to dissolve into water at even 1mg per ml, many not even knowing if they have the freebase or hcl version, as vendors don't seem to be including this information. It does in my experience dissolve readily into alcohol/water mixtures with stirring however.
I really enjoy this psychedelic compound and can see it being a regular on my calendar forever. It is really very little like its 2c counterpart, instead having the OEV/CEV of DOI while sharing much of the same headspace of acid. Strangely at higher doses (550ug) I experienced ergoline/tryptamine morphing of things in my visual field very much the same as I have experienced on moderate doses of acid countless times. The trip is about 6 hours long (a couple hours shorter than an acid trip). I don't know if this has any relevance, but on page 511 of PIHKAL, Shulgin states that "The heaviest, iodine, was explored as the phenethylamine, as 2C-I, and as the amphetamine as DOI. These are the most potent. The next lighter is bromine, where the phenethylamine is 2C-B and the amphetamine is DOB. These two are a bit less potent, and are by far the most broadly explored of all the halides. Here, in the above recipe, we have the chlorine counterpart, 2C-C. There is also the corresponding amphetamine DOC. These are less potent still; and much less explored."
2-(4iodo2,5dimethoxyphenyl)-N-[(2methoxyphenyl)methyl]ethanamine is a derivative of the phenethylamine hallucinogen 2C-I, discovered in 2003 by Ralf Heim at the Free University of Berlin, and subsequently investigated in more detail by a team at Purdue University led by David Nichols.
The sublingually/buccally applied cyclodextrin complexed material (adhered on upper inner lip for 20 minutes in the form of blotter made out of a rectangle cut from #103 filter paper and held under tongue for 5 minutes) was so strong it could have fooled me, thinking I had taken it nasally (even though I didn't)...the comeup was fast, the energy ride up was intense, visuals near the equivalency of 200ug of acid, only in it's own special visual way, like being in a club full of whirling and strobing colored lights even though there are no lights on as she described it, yet still as the trip develops, the visuals are not just overlays as with 25c, (as I read someone write once) but with 25i, are more a part of your surroundings, seeming very similar in many ways to ergoline/tryptamine acid visuals during the peak and stages after that when you stare at images on a monitor or poster on a wall, the actual image morphs and changes into other things, and this continues over and over, the whole while colored energy glitter shooting to and fro in front of what you are seeing. There is incredible beauty seen in all living things and everything appears full of energy. Even though the visual portion was intense, thinking was still for the most part quite lucid to me the entire time and not confusing at any point like it can be with acid or especially ayahuasca, so that is how the mental part differs. Throw in some mescaline and the trip could become quite spiritual and transcendent, the additional 5-ht1a and 5-ht1e agonism from the mescaline will also have modulation effects on the 5-ht2a and 5-ht2c agonism of the 25i, causing not only well being and satisfaction feelings and thinking spiritually and otherwise, but possible modulation of the visuals as well, increasing their activity even more so, prompting not just visuals but actual visions modulation. The increased 5-ht2b agonism (quite strong) from the mescaline would only further serve to enhance the allready empathogenic and sensual 25i.
I found 25i to also have a very prominent empathogenic quality, very deep and transformative, having more meaning that the sort of shallow emotional bliss I feel on ecstasy. The feelings of ecstasy can be predictable while 25i allows me to explore different feelings & deep meaning, the sort of thing I experience on moderate doses of acid (around 175ug).
In the future will in dreams combine with 200mg of tan crystalline mescaline and give a report. If for some reason I've made it appear as if 25i needs a spiritual push, I didn't mean to do so, as stated before, it was the morning after my 2nd trip that I made changes in many of my behaviors and even stopped a 6 month long addiction that nothing else cured me of, the material is quite therapeutic, only it does it in it's own special way, powerful yet gentle, it brought up issues to me during not only my 2nd trip, but also my 1st trip, each trip bringing up some things that I needed to work on to become a better person, it seems to go straight for the therapeutic element, more so than some substances do. Even though I had been taking approximately 175ug of acid every few weeks for a while, surprisingly, it wasn't until I had the 25i trips, that I made actual changes to my behaviors and stopped an addiction, so that saids alot about the potent 5-ht2A and 5-ht2C target agonism of 25i...it is special with its therapeutic powers, very special, powerful yet gentle in its approach, just what I needed to make life long changes. Your mind and body are inter-connected as one, so if you keep yourself in good physical strong healthy shape, your mind should feel good as well, nurture your mind with spiritual Biblical teachings and think on a higher plane, these are things that my 2nd trip brought to the forefront, not to mention the changes in behavior, and teaching myself that I didn't need the chemical stimulant addiction at night that I had been pursuring for half a year. Mysterious powerful substances these psychedelics are. No other substance, stimulant or what have you can match the transcendent like powerful euphoria and empathy imho that this substance shows you that is allready inside yourself for a few short hours...it is a powerful tool...and when used properly, allows your mind to open and piece together new thoughts, to love your neighbors as you do yourself, creative and artistic insights, and think on a higher level, viewing your life from a new perspective. I wish that I would have ventured out side like I had done on 1st trip, but didn't get the chance as it was too dark.
Detailed trip report:
So we both had a third experiment in dreams last night. 550ug HPBCD (hydroxy-propyl-beta-cyclodextrin) complexed drug buccally applied was our most potent to date and kicked both our asses (especially hers), a +4 for her (except lacking spiritually) and an upper +3 for me with only 550ug applied to inner upper lip for 20 minutes, saliva and spit held in mouth for only 15 minutes, then swallowed, while strip allowed to sit an extra 5 minutes under tongue after being transferred. There is a characteristic faint "numbing" sensation of taste felt in the mouth at approximately 20 to 30 minutes after applying blotter that slowly fades away to nothing at the 45 minute point. After the 20 minute blotter soak on upper gum, we transferred it to under the tongue to hold it there for about 5 minutes as well.
Now, whether you have freebase or hcl 25i-nbome does not matter, as I have done more research and found that the cyclodextrin also increases the penetration and absorption of even hcl bound drug. It is useful for either the freebase or the salt. The cyclodextrin binds or entraps any lipohilic part of the molecule then transfers it easily in the saliva which it can then absorb into (as it has now been made very water soluble), to the surfaces of the mucosal where it then also increases penetration effectiveness many fold, some studies showing 95% absorption in 20 minutes when complexed to the very hydrophobic (water fearing) molecule testosterone. 25i-nbome is also hydro-phobic. HPBCD works miracles on improving the absorption of hydrophobic drugs.
I've found that it is best NOT to add extra hydroxy-propyl-beta-cyclodextrin powder on top the blotter piece, as it is not needed, it will only serve to obstruct the entry of the allready HPBCD complexed drug, using "too much" cyclodextrin is not advised. Just as the companie's websites who sell cyclodextrin advise, you want to use neither "too little" nor "too much" but just the right amount. I have found x9 times the CD (cyclodextrin) to drug as the manufacturer suggest to be the perfect amount, although you can use up to x20 the amount of cyclodextrin to drug as well, just don't go sprinkling on extra huge amounts of powder to the allready soaked and complexed blotter piece as I used to do in the past.
As the alcohol solution of cyclodextrin and drug on blotter dries in front of a fan heater over about a 10 minute period, during the last stages of evaporation, the cyclodextrin fully complexes to the drug, then it is ready for application sublingually (under tongue) or buccally (on upper inner lip).
anyhow, long ago, 100mg of 25i-nbome had been slowly sprinkled (added over a 5 minute period) to a spinning 100ml of 95% etoh (drinkable alcohol measured out on a tall 100ml volumetric cylinder) on a magnetic stirrer with stir bar. This was allowed to spin 12 hours.....then 900mg of HPBCD powder had been added as well over a 5 minute period, this complete solution was then allowed to spin for an additional 12 hours. Then after spinning, it was put into freezer in a jar, it has been kept like this for a couple months now, no loss of potency and should store like this indefinately. This gave me a soution of 100ug of drug to each 0.1 ml on the 1ml insulin syringe. If I were to mix this again, I would use only 50 ml of 95% etoh to give me a concentration of 200ug of drug per each 0.1ml, so that would mean less alcohol to evaporate from the blotter, meaning half the time to make/evaporate alcohol from blotter.
1. this was the most potent buccal experiment to date, it came on rapid, within only 1 hour of putting the 1.75" x 5/16" blotter strip above the inner lip (and letting it sit there for 20 minutes), we were both at full effects. I bet putting a square piece of soaked and fully dried blotter under tongue for 15 minutes would be very highly effective as well.
2. 550ug (0.55)ml of the solution from the jar was sucked up via insulin syringe, and the alcohol solution was slowly deposited back and forth on the blotter strip (similar to a cre*t whitening strip size), the blotter strip was then allowed to dry in front of a holmes fan heater for 10 minutes, it dried rather quickly since no extra cyclodextrin powder was sprinkled on top the blotter. If I were to mix this again, I would use only 50 ml of 95% etoh to give me a concentration of 200ug of drug per each 0.1ml, so that would mean less alcohol to evaporate from the blotter, meaning half the time to make/evaporate alcohol from blotter.
3. The blotter contained 4.9mg of cyclodextrin from the solution and 550ug of the drug from the solution (as there is x9 the amount of cyclodextrin to drug) remember as mixed above (550 x 9 = 4.9mg of cyclodextrin).
4. two of these blotter strips were made and each subject applied to upper lip, and it was allowed to adhere to the upper inner lip for 20 minutes, saliva and spit was help that was generated for 15 minutes, then swallowed, but the strip was still allowed to sit on upper inner lip for 5 more minutes.
5. energy come-up was felt within only 30 minutes, and by 1 hour, full effects were noted, the cyclodextrin-complexed drug came on quite quickly and felt nearly just like it had been nasally administered...the cyclodextrin not only allowed the drug to be absorbed very quickly via sublingual or buccal route, but also caused about 95% of it to be absorbed as opposed to approximately 50% or so normally (non-complexed) imho.
6. She was at a +4 within 1.5 hour, and I was at an upper +3 by 1.5 hour.
7. During the come-up her ego was softly relenquished and she lost the sense of who she was and what she was doing for a period, there was anxiety for her during the comeup portion as it was so strong in its effects but after the 2 hour comeup period she felt fully relaxed when all the anxiety had completely passed she told me. I on the other hand did not experience any anxiety as I was used to quite strong mind and come-up states such as this. I remember standing to the side of a mirror at one point and being able to observe myself as well as my reflection "from a third party" perspective which had never happened to me on a psychedelic trip before.
8. She was experiencing very heavy visuals, invisible smoke billing from the floors into the air, pink and purple colors forming in mid-air, glitter being seen everywhere and energy trails and shooters, patterns seen on skin...when looking into a computer monitor for me, the image on the screen morphed and changed into other things without any need for mind or eye tricks on my part, very similar to my acid tryptamine like visuals with things morphing and changing into other things, energy glitter sparklies were seen darting too and fro the whole time as well, in the other room, things were beginning to expand and shrink and grow. She saw lots of block patterning and geometric formations, it was almost "too visual" during the comeup for her, like walking through air castles of patterns and formations.
9. Music sounded absolutely outstanding and there was extreme empathy and a dominant euphoria was experienced during the first few hours by myself, it seemed to remind me of my first "E" experience of long ago, extreme empathy and heavy euphoria, just incredible bliss experienced by my self. Looking at TV, ugly faces were experienced as "more grotesque" and beautiful faces and bodies were experienced as "incredibly beautiful" just like with my tryptamine like visuals in the past with other substances. As the anxiety had passed for her, she was having a very enjoyable time, both subjects had a blast after the comeup period till the trip ended. For some reason the visual part of the trip had ended abruptly at only 4.5 hours after applying blotter, could have been that the cyclodextrin caused the drug to be absorbed nearly as fast (but not quite as totally fast) as when it have been nasally applied, so therefore a quicker comeup with a shorter plateau, anyhow, all the trips I have had with this stuff have been different from each one in different ways so I would not expect the length of the trips to always be the exact same either, not to mention I did not sprinkle on an extra 5 to 10mg of cyclodextrin on the blotter first before applying the alcohol/cyclodextrin/drug drops from the insulin needle, so by only using the proper amount of cyclodextrin to begin with (I avoided adding extra CD), the stuff came on rather quickly and with great absorption effectiveness. I'm not quite able to understand how this compound creates the incredible delightful best non-mdma euphoria that it does, but it has done it each time for me, really interesting.
10. For us to both experience (for her a +4) and for me an upper +3, the buccal cyclodextrin proved extremely effective. Don't add extra cyclodextrin to the blotter before applying, you don't want to overdo it, too much can obstruct effective absorption, but the proper amount used (x 9 times the amount of drug) is perfect, with unbelievable effectiveness. I could never imagine administering this 550ug amount nasally, the buccally applied cyclodextrin complexed stuff had the intensity of nasal allready with the imho same exact absorption effectivness (about 95% is absorbed when complexed to CD (cylodextrin)....I am apt to say "are you kidding....apply this via nasal???, no way!!" it was super potent and VERY intense with CD complxed applied buccally....there is no way I would want to go above this intensity, that would just be insane, the buccal was the most intensity we could both stand as is.
11. how did it seem like acid and differ from acid?
1. it had a slightly shorter duration of visual effects (for this trip anyways) due to the rapid absorption sublingually/buccally (quite similar to nasally applied, about exact same absorption percentage as nasal, but came on about 20 minutes later than as a nasally applied trip would begin), the heavy visuals were about 4.5 hours long, with only the headspace of the trip continuing beyond that.
2. The visuals would be more comparable as erny had stated long ago to the visuals of DOI, however I experienced very tryptamine like visuals (similar to acid visuals) when staring at images, as they would morph and change into other images over and over, with hidden images behind the main image that would form, and they too would morph and change, and so on and so into their own little worlds of visual life. energy glitter and "sparklies" would shoot too and fro constantly when looking at something, energy sparkles, lots of color and beauty and everything looked very alive and full of energy.
3. All sense of time was lost for both of us and it may have had the visuals of DOI and lots of visuals (similar for me) to acid visuals when staring at things, but the headspace felt like that of the acid headspace for the most part, very enjoyable with overflowing euphoria and empathy, the "human-ness" of humanity was experienced for the duration of the trip, feelings, empathy, connections, emotions amplified and complex. She found the visuals different from acid (for the most part) but she did comment that the headspace was very similar to that of acid headspace as well, but that the trip was way less spiritual for her than an acid trip. She also did not see the same typical mayan/archatypical patterning and imaging as she was used to seeing on acid, she missed seeing those images. Instead she saw way different types of patterning and "blocky/geometric" imaging, strobe flashes, smoke billowing and glitter with lots of purple and pink coloring everywhere. She remarked that she loved seeing the brilliant colored sparkly energized glitter darting around everywhere, and missed it when the visuals ended abruptly for both of us at the 4.5 hour point. I am not surprised at this fact since acid hits a whole dog-gone range of receptor sites along with 5-ht2A, 5-ht2C, 5-ht2B, 5-ht6 that 25i-nbome hits. The 5-ht1 sites which acid hits probably contribute to "well-being and satisfaction (spiritually?)" as opposed to 5-ht2a agonism. mescaline also hits 5-ht1a and 5-ht1e and it is also quite spiritual, I imagine combining a 25i-nbome trip with mescaline would give you tons of spiritual feelings and connections along with adding archetypical imaging (seeing lots of real archatypical images and even myan/tribal images, etc.) along with the typical 25i-nbome images. with eyes closed I saw plenty of movie type images of people going about business as well as fractal patterning. I need to explore the CEV's more in the future, but I was trying to pay attention to her trip more as well, so spent little time with eyes closed. During the 1st 2 hours of the comeup she remarked that the visuals were too much for her, she was relieved when the anxiety passed after 2 hours and the visuals were tolerable and she felt relaxed at last. She did remark that music & all sounds sounded just as extraordinary as it does on acid. At the peak, we both watched our favorite movie, and it was like seeing it for the first time, details were seen that we never paid attention to before, the plot and characters were felt as if we were there in the actors and actresses place sharing the experience with them & being emotionally drawn into their world, just an overall amazing experience, and every little sound and all music heard with crystal clear perception of the highest level, putting together new thoughts in your mind....sensory amplification & sensual enchantment. Never at any point was there any nausea, gastointestinal distress or other physical side effects for either one of us, zero body load as with acid. In contrast to her, with this substance, I enjoyed myself during the entire come-up portion as well, my ego was for the most part intact during the comeup & I had no anxiety, whereas hers was relinquished for a period.
4. 25i-nbome is "it's own special psychedelic" just as acid is "it's own special psychedelic" but I am extremely grateful that 25i-nbome shares much of the same headspace as acid along with the good humor (we laughed a lot at movies like funny or die, saw 4 episodes) and lots of empathy and euphoria/joy just like with acid. There were complex thoughts and art & music was amplified beyond comprehension, very fun and joyous after the comeup period. One of my previous experiences in dreams with 25i helped me to change certain behaviors and be an even better person, it has good entheogenic life changing qualities that you may not even notice the night of the trip, but may take hold of your thoughts the morning after. It leaves one with no headache the next day, in fact the next morning you have good energy and feel remarkably refreshed (just like a good acid trip) as if the "reset" button has been pressed on your serotonic brain, allowing you to "make a fresh start" and see things from a brand new perspective.
Erny (one of the first to try the NBome's):
Interesting Erowid report:
I have a feeling that combining this stuff with mescaline will give a trip that is extremely close to acid in many ways, however, 25i feels so darn close allready, or is so special in its own way that it really doesn't need anything to "complete it". However, mescaline hits the receptors that 25i lacks, and 25i hits the receptors that mescaline lacks...in other words, they overlap with remarkable precision. 25i is allready the closest thing to acid I've ever exprienced, I just feel that 25i needs a little extra "spiritual push" to complete it....If you get spiritual feelings from the extreme empathy and euphoria that 25i produces, then there is no need for mescaline, but if you really want to push the envelope, then mescaline is the ticket.
Kent's book "psychedelic information theory" states the following in general terms:
* 5-HT1 affinity is generally thought to work in contrast to 5-HT2A agonism to promote well-being and satisfaction. Mescaline, 5-MEO-DMT, DIPT, LSD all have a high 5-HT1 affinity. Mescaline hits (5-HT1A at 3.61, note this value is from an inverse chart, where 4.0 indicates maximum affinity), LSD hits (5-HT1A at 1.1, this is from the ki chart where 0.0 indicates maximum affinity). Mescaline hits (5-HT1E at 3.16, this is from the ki chart where 4.0 indicates maximum affinity). LSD hits (5-HT1E at 2.62, this is from the ki chart where 4.0 indicates maximum affinity). 25i lacks affinity for 5-HT1A and 5-HT1E.
* 5-HT2A & 5-HT2C are the most important receptors that all the main psychedelics hit, with the most potent psychedelics hitting them real hard...they are implicated in extreme visual activity and complex thinking. 25i-nbome hits these two receptors (5HT2A & 5-HT2C) harder than any other psychedelic out there. 25i hits (5-HT2A at 0.044) and hits (5-HT2C at 2.0), LSD is only able to hit (5HT2A at 3.5) and hits (5-HT2C at only 23.0). The lower the ki value, the greater the receptor binding.
* 5-HT2B is implicated with purely sensual or entactogenic effect. 25i hits (5-HT2B at 231), and LSD hits (5-HT2B at 25). Mescaline hits (5-HT2B at 3.97, this is from the inverse chart with 4.00 indicating maximum affinity). MDMA hits (5-HT2B at 3.64, this is from the inverse chart with 4.00 indicating maximum affinity).
DiPT, Mescaline, and MDMA have very poor 5-HT2A, 2C affinity, but all have a high 5-HT2B and adrenal affinity, cardiovascular activity, and acute sensuality. 5-HT2B affinity is quite high for all theses.
* 5-HT6 is implicated with ?. 25i hits (5-HT6 at 73.0), LSD hits (5-HT6 at 6.0).
* 5-HT7 is implicated with reward activity and overall transcendent psychedelic action, with the mystically popular DMT, 5-MEO-DMT, and LSD topping the affinity list for this receptor. LSD hits (5-HT7 at 6.0). Now neither 25i nor mescaline hit 5-HT7.
* adrenal-2a receptor is hit by mescaline at 2.92 (inverse chart), whereas LSD hits adrenal-2a at 2.93 (inverse chart), very similar.
* adrenal-2c receptor is hit by mescaline at 4.00 (inverse chart, maximum value), whereas MDMA hits adrenal-2c receptor at 3.21.
* 25i does not hit any of the adrenal receptors.
adrenal affinity is implicated (along with 5-HT2B) with effectivenss at stimulating serotonin production, cardiovascular activity, and acute sensuality.
So in other words, mescaline will target 5-HT1A, 5-HT1E and 5-HT2B receptors with extreme affinity....and the 25i will target the 5-HT2A, 5-HT2C, 5-HT6, and 5-HT2B with great affinity. Mescaline fills in the spiritual well-being and satisfaction void, and 25i fills in the extreme visual activity and complex thinking. Mescaline by also targeting the 5-HT2B receptor with even greater intensity than 25i, contributes to even greater increased sensual and entactogenic effect. Now, 25i is very empathogenic and sensual all on it's own, imho appearing in the trips I've had to be near equal to mdma in the euphoria it produces mentally, and 25i goes even deeper & feeling more natural than the substance mdma.
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So by adding mescaline along with 25i, we get the following:
5-HT1A, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT6, adrenal-2a, adrenal-2c
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Mescaline overlaps 25i perfectly, filling in the gaps needed while 25i overlaps mescaline filling in the gaps perfectly as well.
The only thing of importance really missing is 5-HT7 agonism, which LSD hits at 6.0 (regular ki chart, where 0.0 = maximum affinity)...5-HT5A, 5-HT5B, 5-HT1B, 5-HT1D, d1, d2 are the other receptors that acid hits, but little is known about the significance of these.
Take this all with a grain of salt, as psychedelic information theory is purely theoretical at this point.
Psychedelic Information Theory (Kent's book): http://psychedelic-information-theory.com/ebook/index.htm
I had totally forgoten that the book "Psychedelic Information Theory" by James Kent has a chapter on "Psychedelic Receptor Binding". He saids that the substances that have the most Hallucinogenic potency have very high 5-HT2A affinity as well as 5-HT2C affinity...
TABLE 1 from Kent's book
In comparison, mescaline has very poor affinity for 5-HT2A or 5-HT2C, he saids this explains why it is largely considered a non-visual psychedelic, along with 5-meo-dmt, dipt, and mdma. To me, 25i-nbome is visually more spectacular than acid (in it's own distinct way however). I disagree with his non-visual statement about mescaline because to me, mescaline is visual at high doses, causing not just visuals but visions as well.
From last paragraph of Nichol's paper:
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There are actually a couple places (outside of auction sites ) that directly have Hydroxypropyl Beta Cyclodextrin. In any case, there are hundreds of research papers on the science of HPBCD, "Trappsol" and other fancy sounding brand names are currently used for the stuff these days it seems.
this is an important study (below) from the cyclodextrin mega-expert Dr. Joseph Pitha, and explains in more
detail the theory behind my preparation of the Nbome blotter that we both tried using a 95% drinkable alcohol (ethanol) solution....ie a solution of 100ml of 95% etoh, 100mg of 25i-nbome, and 900mg of HPBCD, which had been pre-spun for 24 hours.
http://www.sciencedirect.com/science...78517392902816
hxxp://www.sciencedirect.com/science/article/pii/0378517392902816
This is a culmination of several month experimentation & my own research complexing the novel new rare RC 25i-nbome psychedelic compound discovered in Berlin to hydroxy-propyl-beta-cyclodextrin (HPBCD) to achieve imho nearly 95% sublingual or buccal absorption in 20 minutes, negating the need for nasal application, "plugging", or IM shot. Years ago as an experiment I complexed a very small amount of the very hydrophobic compound testosterone freebase powder (0.033mg solubility in 1ml h2o) but when complexed to HPBCD (1 hour of stirring in solution of water and HPBCD) becomes 100% water soluble, a published study by Dr. Joseph Pitha showed 95% absorption of cyclodextrin complexed testosterone freebase in 20 minutes when applied sublingually. 25i-nbome is also very hydrophobic (water-fearing) just like testosterone. Amazingly, HPBCD can be used with not only the freebase drug version, but also the hcl drug version, as the cyclodextrin en-cages any lipophilic part of the molecule, still increasing the penetration effectiveness of even the HCL version of drugs according to a paper I've seen. I've read of lots of folks having an impossible time even getting the hcl version of this drug to dissolve into water at even 1mg per ml, many not even knowing if they have the freebase or hcl version, as vendors don't seem to be including this information. It does in my experience dissolve readily into alcohol/water mixtures with stirring however.
I really enjoy this psychedelic compound and can see it being a regular on my calendar forever. It is really very little like its 2c counterpart, instead having the OEV/CEV of DOI while sharing much of the same headspace of acid. Strangely at higher doses (550ug) I experienced ergoline/tryptamine morphing of things in my visual field very much the same as I have experienced on moderate doses of acid countless times. The trip is about 6 hours long (a couple hours shorter than an acid trip). I don't know if this has any relevance, but on page 511 of PIHKAL, Shulgin states that "The heaviest, iodine, was explored as the phenethylamine, as 2C-I, and as the amphetamine as DOI. These are the most potent. The next lighter is bromine, where the phenethylamine is 2C-B and the amphetamine is DOB. These two are a bit less potent, and are by far the most broadly explored of all the halides. Here, in the above recipe, we have the chlorine counterpart, 2C-C. There is also the corresponding amphetamine DOC. These are less potent still; and much less explored."
2-(4iodo2,5dimethoxyphenyl)-N-[(2methoxyphenyl)methyl]ethanamine is a derivative of the phenethylamine hallucinogen 2C-I, discovered in 2003 by Ralf Heim at the Free University of Berlin, and subsequently investigated in more detail by a team at Purdue University led by David Nichols.
The sublingually/buccally applied cyclodextrin complexed material (adhered on upper inner lip for 20 minutes in the form of blotter made out of a rectangle cut from #103 filter paper and held under tongue for 5 minutes) was so strong it could have fooled me, thinking I had taken it nasally (even though I didn't)...the comeup was fast, the energy ride up was intense, visuals near the equivalency of 200ug of acid, only in it's own special visual way, like being in a club full of whirling and strobing colored lights even though there are no lights on as she described it, yet still as the trip develops, the visuals are not just overlays as with 25c, (as I read someone write once) but with 25i, are more a part of your surroundings, seeming very similar in many ways to ergoline/tryptamine acid visuals during the peak and stages after that when you stare at images on a monitor or poster on a wall, the actual image morphs and changes into other things, and this continues over and over, the whole while colored energy glitter shooting to and fro in front of what you are seeing. There is incredible beauty seen in all living things and everything appears full of energy. Even though the visual portion was intense, thinking was still for the most part quite lucid to me the entire time and not confusing at any point like it can be with acid or especially ayahuasca, so that is how the mental part differs. Throw in some mescaline and the trip could become quite spiritual and transcendent, the additional 5-ht1a and 5-ht1e agonism from the mescaline will also have modulation effects on the 5-ht2a and 5-ht2c agonism of the 25i, causing not only well being and satisfaction feelings and thinking spiritually and otherwise, but possible modulation of the visuals as well, increasing their activity even more so, prompting not just visuals but actual visions modulation. The increased 5-ht2b agonism (quite strong) from the mescaline would only further serve to enhance the allready empathogenic and sensual 25i.
I found 25i to also have a very prominent empathogenic quality, very deep and transformative, having more meaning that the sort of shallow emotional bliss I feel on ecstasy. The feelings of ecstasy can be predictable while 25i allows me to explore different feelings & deep meaning, the sort of thing I experience on moderate doses of acid (around 175ug).
In the future will in dreams combine with 200mg of tan crystalline mescaline and give a report. If for some reason I've made it appear as if 25i needs a spiritual push, I didn't mean to do so, as stated before, it was the morning after my 2nd trip that I made changes in many of my behaviors and even stopped a 6 month long addiction that nothing else cured me of, the material is quite therapeutic, only it does it in it's own special way, powerful yet gentle, it brought up issues to me during not only my 2nd trip, but also my 1st trip, each trip bringing up some things that I needed to work on to become a better person, it seems to go straight for the therapeutic element, more so than some substances do. Even though I had been taking approximately 175ug of acid every few weeks for a while, surprisingly, it wasn't until I had the 25i trips, that I made actual changes to my behaviors and stopped an addiction, so that saids alot about the potent 5-ht2A and 5-ht2C target agonism of 25i...it is special with its therapeutic powers, very special, powerful yet gentle in its approach, just what I needed to make life long changes. Your mind and body are inter-connected as one, so if you keep yourself in good physical strong healthy shape, your mind should feel good as well, nurture your mind with spiritual Biblical teachings and think on a higher plane, these are things that my 2nd trip brought to the forefront, not to mention the changes in behavior, and teaching myself that I didn't need the chemical stimulant addiction at night that I had been pursuring for half a year. Mysterious powerful substances these psychedelics are. No other substance, stimulant or what have you can match the transcendent like powerful euphoria and empathy imho that this substance shows you that is allready inside yourself for a few short hours...it is a powerful tool...and when used properly, allows your mind to open and piece together new thoughts, to love your neighbors as you do yourself, creative and artistic insights, and think on a higher level, viewing your life from a new perspective. I wish that I would have ventured out side like I had done on 1st trip, but didn't get the chance as it was too dark.
Detailed trip report:
So we both had a third experiment in dreams last night. 550ug HPBCD (hydroxy-propyl-beta-cyclodextrin) complexed drug buccally applied was our most potent to date and kicked both our asses (especially hers), a +4 for her (except lacking spiritually) and an upper +3 for me with only 550ug applied to inner upper lip for 20 minutes, saliva and spit held in mouth for only 15 minutes, then swallowed, while strip allowed to sit an extra 5 minutes under tongue after being transferred. There is a characteristic faint "numbing" sensation of taste felt in the mouth at approximately 20 to 30 minutes after applying blotter that slowly fades away to nothing at the 45 minute point. After the 20 minute blotter soak on upper gum, we transferred it to under the tongue to hold it there for about 5 minutes as well.
Now, whether you have freebase or hcl 25i-nbome does not matter, as I have done more research and found that the cyclodextrin also increases the penetration and absorption of even hcl bound drug. It is useful for either the freebase or the salt. The cyclodextrin binds or entraps any lipohilic part of the molecule then transfers it easily in the saliva which it can then absorb into (as it has now been made very water soluble), to the surfaces of the mucosal where it then also increases penetration effectiveness many fold, some studies showing 95% absorption in 20 minutes when complexed to the very hydrophobic (water fearing) molecule testosterone. 25i-nbome is also hydro-phobic. HPBCD works miracles on improving the absorption of hydrophobic drugs.
I've found that it is best NOT to add extra hydroxy-propyl-beta-cyclodextrin powder on top the blotter piece, as it is not needed, it will only serve to obstruct the entry of the allready HPBCD complexed drug, using "too much" cyclodextrin is not advised. Just as the companie's websites who sell cyclodextrin advise, you want to use neither "too little" nor "too much" but just the right amount. I have found x9 times the CD (cyclodextrin) to drug as the manufacturer suggest to be the perfect amount, although you can use up to x20 the amount of cyclodextrin to drug as well, just don't go sprinkling on extra huge amounts of powder to the allready soaked and complexed blotter piece as I used to do in the past.
As the alcohol solution of cyclodextrin and drug on blotter dries in front of a fan heater over about a 10 minute period, during the last stages of evaporation, the cyclodextrin fully complexes to the drug, then it is ready for application sublingually (under tongue) or buccally (on upper inner lip).
anyhow, long ago, 100mg of 25i-nbome had been slowly sprinkled (added over a 5 minute period) to a spinning 100ml of 95% etoh (drinkable alcohol measured out on a tall 100ml volumetric cylinder) on a magnetic stirrer with stir bar. This was allowed to spin 12 hours.....then 900mg of HPBCD powder had been added as well over a 5 minute period, this complete solution was then allowed to spin for an additional 12 hours. Then after spinning, it was put into freezer in a jar, it has been kept like this for a couple months now, no loss of potency and should store like this indefinately. This gave me a soution of 100ug of drug to each 0.1 ml on the 1ml insulin syringe. If I were to mix this again, I would use only 50 ml of 95% etoh to give me a concentration of 200ug of drug per each 0.1ml, so that would mean less alcohol to evaporate from the blotter, meaning half the time to make/evaporate alcohol from blotter.
1. this was the most potent buccal experiment to date, it came on rapid, within only 1 hour of putting the 1.75" x 5/16" blotter strip above the inner lip (and letting it sit there for 20 minutes), we were both at full effects. I bet putting a square piece of soaked and fully dried blotter under tongue for 15 minutes would be very highly effective as well.
2. 550ug (0.55)ml of the solution from the jar was sucked up via insulin syringe, and the alcohol solution was slowly deposited back and forth on the blotter strip (similar to a cre*t whitening strip size), the blotter strip was then allowed to dry in front of a holmes fan heater for 10 minutes, it dried rather quickly since no extra cyclodextrin powder was sprinkled on top the blotter. If I were to mix this again, I would use only 50 ml of 95% etoh to give me a concentration of 200ug of drug per each 0.1ml, so that would mean less alcohol to evaporate from the blotter, meaning half the time to make/evaporate alcohol from blotter.
3. The blotter contained 4.9mg of cyclodextrin from the solution and 550ug of the drug from the solution (as there is x9 the amount of cyclodextrin to drug) remember as mixed above (550 x 9 = 4.9mg of cyclodextrin).
4. two of these blotter strips were made and each subject applied to upper lip, and it was allowed to adhere to the upper inner lip for 20 minutes, saliva and spit was help that was generated for 15 minutes, then swallowed, but the strip was still allowed to sit on upper inner lip for 5 more minutes.
5. energy come-up was felt within only 30 minutes, and by 1 hour, full effects were noted, the cyclodextrin-complexed drug came on quite quickly and felt nearly just like it had been nasally administered...the cyclodextrin not only allowed the drug to be absorbed very quickly via sublingual or buccal route, but also caused about 95% of it to be absorbed as opposed to approximately 50% or so normally (non-complexed) imho.
6. She was at a +4 within 1.5 hour, and I was at an upper +3 by 1.5 hour.
7. During the come-up her ego was softly relenquished and she lost the sense of who she was and what she was doing for a period, there was anxiety for her during the comeup portion as it was so strong in its effects but after the 2 hour comeup period she felt fully relaxed when all the anxiety had completely passed she told me. I on the other hand did not experience any anxiety as I was used to quite strong mind and come-up states such as this. I remember standing to the side of a mirror at one point and being able to observe myself as well as my reflection "from a third party" perspective which had never happened to me on a psychedelic trip before.
8. She was experiencing very heavy visuals, invisible smoke billing from the floors into the air, pink and purple colors forming in mid-air, glitter being seen everywhere and energy trails and shooters, patterns seen on skin...when looking into a computer monitor for me, the image on the screen morphed and changed into other things without any need for mind or eye tricks on my part, very similar to my acid tryptamine like visuals with things morphing and changing into other things, energy glitter sparklies were seen darting too and fro the whole time as well, in the other room, things were beginning to expand and shrink and grow. She saw lots of block patterning and geometric formations, it was almost "too visual" during the comeup for her, like walking through air castles of patterns and formations.
9. Music sounded absolutely outstanding and there was extreme empathy and a dominant euphoria was experienced during the first few hours by myself, it seemed to remind me of my first "E" experience of long ago, extreme empathy and heavy euphoria, just incredible bliss experienced by my self. Looking at TV, ugly faces were experienced as "more grotesque" and beautiful faces and bodies were experienced as "incredibly beautiful" just like with my tryptamine like visuals in the past with other substances. As the anxiety had passed for her, she was having a very enjoyable time, both subjects had a blast after the comeup period till the trip ended. For some reason the visual part of the trip had ended abruptly at only 4.5 hours after applying blotter, could have been that the cyclodextrin caused the drug to be absorbed nearly as fast (but not quite as totally fast) as when it have been nasally applied, so therefore a quicker comeup with a shorter plateau, anyhow, all the trips I have had with this stuff have been different from each one in different ways so I would not expect the length of the trips to always be the exact same either, not to mention I did not sprinkle on an extra 5 to 10mg of cyclodextrin on the blotter first before applying the alcohol/cyclodextrin/drug drops from the insulin needle, so by only using the proper amount of cyclodextrin to begin with (I avoided adding extra CD), the stuff came on rather quickly and with great absorption effectiveness. I'm not quite able to understand how this compound creates the incredible delightful best non-mdma euphoria that it does, but it has done it each time for me, really interesting.
10. For us to both experience (for her a +4) and for me an upper +3, the buccal cyclodextrin proved extremely effective. Don't add extra cyclodextrin to the blotter before applying, you don't want to overdo it, too much can obstruct effective absorption, but the proper amount used (x 9 times the amount of drug) is perfect, with unbelievable effectiveness. I could never imagine administering this 550ug amount nasally, the buccally applied cyclodextrin complexed stuff had the intensity of nasal allready with the imho same exact absorption effectivness (about 95% is absorbed when complexed to CD (cylodextrin)....I am apt to say "are you kidding....apply this via nasal???, no way!!" it was super potent and VERY intense with CD complxed applied buccally....there is no way I would want to go above this intensity, that would just be insane, the buccal was the most intensity we could both stand as is.
11. how did it seem like acid and differ from acid?
1. it had a slightly shorter duration of visual effects (for this trip anyways) due to the rapid absorption sublingually/buccally (quite similar to nasally applied, about exact same absorption percentage as nasal, but came on about 20 minutes later than as a nasally applied trip would begin), the heavy visuals were about 4.5 hours long, with only the headspace of the trip continuing beyond that.
2. The visuals would be more comparable as erny had stated long ago to the visuals of DOI, however I experienced very tryptamine like visuals (similar to acid visuals) when staring at images, as they would morph and change into other images over and over, with hidden images behind the main image that would form, and they too would morph and change, and so on and so into their own little worlds of visual life. energy glitter and "sparklies" would shoot too and fro constantly when looking at something, energy sparkles, lots of color and beauty and everything looked very alive and full of energy.
3. All sense of time was lost for both of us and it may have had the visuals of DOI and lots of visuals (similar for me) to acid visuals when staring at things, but the headspace felt like that of the acid headspace for the most part, very enjoyable with overflowing euphoria and empathy, the "human-ness" of humanity was experienced for the duration of the trip, feelings, empathy, connections, emotions amplified and complex. She found the visuals different from acid (for the most part) but she did comment that the headspace was very similar to that of acid headspace as well, but that the trip was way less spiritual for her than an acid trip. She also did not see the same typical mayan/archatypical patterning and imaging as she was used to seeing on acid, she missed seeing those images. Instead she saw way different types of patterning and "blocky/geometric" imaging, strobe flashes, smoke billowing and glitter with lots of purple and pink coloring everywhere. She remarked that she loved seeing the brilliant colored sparkly energized glitter darting around everywhere, and missed it when the visuals ended abruptly for both of us at the 4.5 hour point. I am not surprised at this fact since acid hits a whole dog-gone range of receptor sites along with 5-ht2A, 5-ht2C, 5-ht2B, 5-ht6 that 25i-nbome hits. The 5-ht1 sites which acid hits probably contribute to "well-being and satisfaction (spiritually?)" as opposed to 5-ht2a agonism. mescaline also hits 5-ht1a and 5-ht1e and it is also quite spiritual, I imagine combining a 25i-nbome trip with mescaline would give you tons of spiritual feelings and connections along with adding archetypical imaging (seeing lots of real archatypical images and even myan/tribal images, etc.) along with the typical 25i-nbome images. with eyes closed I saw plenty of movie type images of people going about business as well as fractal patterning. I need to explore the CEV's more in the future, but I was trying to pay attention to her trip more as well, so spent little time with eyes closed. During the 1st 2 hours of the comeup she remarked that the visuals were too much for her, she was relieved when the anxiety passed after 2 hours and the visuals were tolerable and she felt relaxed at last. She did remark that music & all sounds sounded just as extraordinary as it does on acid. At the peak, we both watched our favorite movie, and it was like seeing it for the first time, details were seen that we never paid attention to before, the plot and characters were felt as if we were there in the actors and actresses place sharing the experience with them & being emotionally drawn into their world, just an overall amazing experience, and every little sound and all music heard with crystal clear perception of the highest level, putting together new thoughts in your mind....sensory amplification & sensual enchantment. Never at any point was there any nausea, gastointestinal distress or other physical side effects for either one of us, zero body load as with acid. In contrast to her, with this substance, I enjoyed myself during the entire come-up portion as well, my ego was for the most part intact during the comeup & I had no anxiety, whereas hers was relinquished for a period.
4. 25i-nbome is "it's own special psychedelic" just as acid is "it's own special psychedelic" but I am extremely grateful that 25i-nbome shares much of the same headspace as acid along with the good humor (we laughed a lot at movies like funny or die, saw 4 episodes) and lots of empathy and euphoria/joy just like with acid. There were complex thoughts and art & music was amplified beyond comprehension, very fun and joyous after the comeup period. One of my previous experiences in dreams with 25i helped me to change certain behaviors and be an even better person, it has good entheogenic life changing qualities that you may not even notice the night of the trip, but may take hold of your thoughts the morning after. It leaves one with no headache the next day, in fact the next morning you have good energy and feel remarkably refreshed (just like a good acid trip) as if the "reset" button has been pressed on your serotonic brain, allowing you to "make a fresh start" and see things from a brand new perspective.
Erny (one of the first to try the NBome's):
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NBOMe-2C-I was the first of them I have tried myself and the first one to appear on an illicit market here under the brand name "Solaris", late summer 2007. Currently this name refers to any NBOMe on a glycine tablet (a common cheap innocuous medicine for sublingual administration).
David's NBOMe-2C-I is a true gem. Basically it resembles PEAs, but is much like acid in some of it's effects, especially in the emotional area. It is full with the deep glowing LSD-like empathy that is uncommon within phenylethylamines.
The activity of bomamines in humans are sometimes inverted: NBOMe-2C-I requires 500-1000 mkg for a trip. When insufflated or injected i/m, they need a full hour to come up, even 1,5 hours in the case of NBOMe-2C-I.
NBOMe-2C-I seem a little like DOI and a little like LSD, NBOMe-2C-C seem a little like DOC and a little like DOI, NBOMe-2C-B - a little like DOB, NBOMe-2C-N seem a little like DON and a little like DMT if you wish to know that.
I do not get what is 2C-I and DOI nastiness you are talking about, I see those two as a remarkable visual experience and something that is easy on the mind (not paranoid, not frightening etc), but little else than that. One may also find there some good humour and an an opened, euphoric state of mind good for social tripping, reminiscent of empathogens or acid. This effect is barely noticeable in these two however, and not really reproducible, but is the one that shines to its full extent in NBOMe-2C-I and makes it very special.
NBOMe-2C-I is amasingly positive and is a clear empathogen in an LSD manner, i. e. somewhat deeper and feeling more natural than things like MDMA. An overflowing, exuberant joy, yet not as jittery as MDMA is. This state of mind is uncommon in PIHKAL phenylethylamines and is much closer to a good LSD trip.
NBOMe-2C-I has very few side effects past the come-up, the fact that made me to regard all of them as chemicals that are easy on the body at first, unfortunatly this is not true. there is no heavyness to pull you down and pin to a single place, the body feels weightless. Like the rest, it doesn't suppress appetite, probably due to it's low affinity to 5-HT2C receptor. Yet it is mildly vasoconstrictive and thus may give you a headache shortly after returning to baseline, just like PIHKAL.
It is, of course, visually rich, like it's relatives with iodine in PIHKAL. NBOMes have less distinctive visual patterns that would repeat in every trip like those in PEAs. Besides simple visual "noise" I rarely pay attention to and don't remember well, visuals there are generally more variable. There is one distinctive visual effect, however - caleidoscopic images, like in a real caleidoscope, or, with a higher dose, true fractals, i. e. structures with self-similarity and not just any geometrical visual mesh. Those are present in NBOMe-2C-I as well, of course, and make this similarity with acid even greater.
If we are talking about 2C-I-NBOMe in regular doses, there is no anxiety at all and the overall discomfort is moderate to weak. Mushrooms are much more anxious during the come-up than 2C-I, even plain 2C-B is more anxious. Unless 2C-I is taken in a huge dose. 60 mg may make you anxious. Same is true for NBOMe-2C-I, or any other psychedelic, and taking into consideration it is much more potent not only in terms of dosage, you may guess now what was the real source of that anxiety.
I've heard such complaints about 2C-I, as well, as it's being a sort of "psychedelic speed", etc, but never heard anything like that about NBOMe-2C-I. The frequency of the appearance of negative reactions to this chemical seems to be much lower than that of any other well explored NBOMe molecule (those are B, C and N), and lower than with most of the DOX.
After-effects I was talking about are not real after-effects, it's just the chemical that haven't left the body completely. I was actually still tripping. With a regular dose you will feel almost normal yet not completely at the baseline during this time, and most probably will be able to sleep.
Question "Did you find this substance to be similar to 2C-I qualitatively?"
Somewhat. But more so to DOI in regard its CEV/OEV and LSD - in mindset.
Doses above one-two milligram(s) have produced ...some usual phenomena of an overdose mostly similar with that of any other psychedelic drug.
Doses of more than three milligrams may produce seizures and doses of less than ten milligrams may be fatal. Reality is a little more complicated of course. One of the reports on worryfying overdoses I was able to find was about a man who took 1 mg of NBOMe-2C-I by insufflation. He literally fell as if shot five minutes later, lost consciousness and had seisures.
But I also had a memorable overdose if we are talking on that subject now. At the beginning of it all in 2007 I couldn't killed myself with 30 milligrams (this isn't a typo and was accurately weighed) of NBOMe-2C-B i/m, when accidentally mislabeled packages. I was able to return to this plane of reality unharmed, without any lasting consequences of this misfortune to speak about. There were several lethal doses in it - if we are to estimate them the proposed way. Nevertheless, I am alive and feeling fine, and I can't do anything about this fact. What's worse, I am not at all unique in being so tough. There is a number of reports about similar accidents found at several russian thematic web-resourses. Their story is always the same: someone accidentially overdoses with 5-10 mgs of NBOMe-2C-C/B/I, and after suffering extreme DMT-like trip gets off with only a scare. People like me or these others who won't die from what was called a "lethal" dose in the citation aren't a rarity, it looks more like this is a norm (or one of several norms to be more precise). For us who are the toughest ones in this regard, NBOMe molecules are nearly as safe as the least toxic structures among 2C-X PEAs (that seem to be the safest psychedelic phenylethylamines I am aware of).
This shouldn't serve as a cause for optimism towards phentanyl-like structures we are talking about here. There are also people, who are also quite numerous, for whom their safety margin appears to be closer to that of DOX. For them a suicide by means of 20x-30x NBOMe-2C-X overdose isn't necessarily impossible. And there are also individuals, not as numerous (but it makes no difference; that they exist is just enough), who will find NBOMe-2C-X to have the safety closer to that of benzodifurans like bromo-dragonfly (it would probably be better to say they have no safety reserve at all). These latter individuals will be the first to get into dangerous or even lethal accidents, if we are to see such in the near future.
While there is no way to find out beforehand who is who, or what may happen if somebody will take one of these chems.
Interesting Erowid report:
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Tears of Joy
2C-I-NBOMe
by p3ych0n4ught
DOSE: T+ 0:00 smoked 2C-I-NBOMe (powder / crystals)
T+ 0:20 smoked 2C-I-NBOMe (powder / crystals)
BODY WEIGHT: 185 lb
After ordering from a reliable vendor I received 1 gram of 25I NBOME as a fluffy white powder. Unaware if this was the salt or freebase I proceeded to do a simple solubility test. The compound proved to insoluble in H20 leading me to believe that it was the freebase. I decided that vaporization would be the most effective route of administration. I had planned to use volumetric measurement but was unable to get the chemical to dissolve after several different attempts. (I later discovered that 25I NBOME freebase is soluble in 91% Isopropyl alcohol) But, this time around I had no accurate way of measuring at a ug dose so I prepared a dose as small as I could (eyeballing a dose this small is not recommended and dangerous). This was vaporized.
Set: I am in the middle of a cross roads in my life. I was living in the woods/ on the streets for a while and I am trying to make the right decision about reintegrating into society. I recently quit smoking Marijuana, JWH-018, and Cigarettes after long habitual use to try to clear my mind. I have been completely sober 30 days when I decide to take this trip.
I consider psychedelics to be some of the greatest teachers I have had and I consider myself to have a complex relationship with each I have used. Feeling lost I returned to LSD earlier this year. I went in with an open mind and open heart yet, I heard nothing. All I got was visuals. I turned to DMT and had the exact same experience. It was purely sensory and superficial.
I seek out a psychologist who is unable to help me see clearly how I can live within a class-based society without compromising my core values of basic human equality.
Setting: A CRAZY HOT summer day.
0:00 The smoke had a chemical taste as expected but it was such a small amount of smoke that it was easily forgotten.
0:01 The onset is quick. I feel euphoric and a sensation similar to previous experiences with 2C-E.
0:02 I feel a vibrating sensation move through my body. It continues and extends seamlessly to the room I am in as a rippling patter on the walls. Colors are more vibrant and my pupils are dilated.
0:05 – 0:10 My head space is very clear and I am lucid. The rush subsides and I reach a plateau. I am at a ++.
0:20 There is no change form 0:10 and I decide to re-dose with the smallest amount I can measure. This dose is vaporized.
0:21 The vibrating sensation becomes very powerful and the rippling pattern on the walls turns into solid bars of color which create dramatic swirls. I am at a +++. My room looks nothing like what it looks like normally. I can think clearly and decide to listen to some music.
0:22 The solid bar patterns on the walls begin to dance as I experience strong synesthesia. The proportions of everything in the room grow and shrink with the music. I am experience strong time dilation. The visuals are as intense as previous 500ug LSD trips but lack the geometric patterning. Unlike LSD even with this high level of visual distortion I can still think relatively clearly and continue to preform simple tasks like searching through songs on my iPod.
0:30 The visual distortion is very intense and music sounds beautiful. The trip seems to plateau again. But, this is not what I seek from this chemical. I see chemicals like this as an extension of the creativity of nature and I am looking to this chemical to help resolve a complex cognitive dissonance within me. ===> I believe we should all live as equals but I am dependent upon a society, that distributes socio/economic power unevenly, for things like health care, and the science that has created this beautiful chemical, and the computer I write this report on. I am disappointed but the trip is still euphoric and up-beat. I accept it for what it is, swirly patterns and bright lights. I don't expect much more.
0:40 I decide to go for a long walk outside to enjoy the sun. I change clothes and put on my shoes with ease. I am surprised my fine motor skill are as enacted as they are. If I were on LSD or DMT with this level of visual distortion the thought distortion would be to intense for me to walk around much, let alone tie my shoes.
1:00 Music is beautiful. I am completely content. I walk for another hour.
2:00 I get back home and realize the trip is still at a solid +++. I take a shower. Every drop of water that hits my body makes a radiant multi colored circle on the wall, ceiling, or floor.
4:00 I decide to go for another walk.
5:00 It's dusk, the visuals are beginning to subside. I'm still listening to music when suddenly the euphoria in my body shifts to a powerful empathy. I can suddenly see everything in my life independent of my emotions, fears, hopes, aspirations. It reminds me a lot of MDMA. I realize how distracting the music I’ve been listening to for so long is and I take my headphones out, lay down next to the path I am on and just listen to the world around me. I hear my neighbor's dogs barking and cars driving by. It was like everything I was trying to figure out in my life, my internal monologue, everything just shut down and in thinking about nothing I suddenly understood everything. The tidal pool of emotions and ideas within me was suddenly a placid lake and in that lake I could see myself reflected as I truly was. I simply lay there not happy or sad but completely at peace. I don't know for how long. Time simply did not exist for me.
Out of 50+ trips I can say that this was one of only 2 times that I have ever reached what I would call a ++++. I realized that I should not spend my life trying to run from the crazy society we live in to live in my own idealized world. Instead I should grow where I am planted and accept the world and its complexities as the divine embodiment of nature's creativity ever evolving. Always as it is meant to be. It was time for me to stop arrogantly imposing my ideals about the way things should be in a world too complex for any one man/woman to understand. To stop trying to change everything around me and instead “be the change I want to see in the world” from where I am.
Eventually I get up and decide to walk home. My mind is so clear, it's like a chalk board that has just been wiped clean. I start to cry tears of joy for the first time in a long time.
Sleep came easy that night and I woke up the next morning feeling refreshed.
This experience ended a powerful depression I had been in instantaneously. I don't know how and I can't explain it. It just happened. This chemical has changed my life.
Exp Year: 2010
I have a feeling that combining this stuff with mescaline will give a trip that is extremely close to acid in many ways, however, 25i feels so darn close allready, or is so special in its own way that it really doesn't need anything to "complete it". However, mescaline hits the receptors that 25i lacks, and 25i hits the receptors that mescaline lacks...in other words, they overlap with remarkable precision. 25i is allready the closest thing to acid I've ever exprienced, I just feel that 25i needs a little extra "spiritual push" to complete it....If you get spiritual feelings from the extreme empathy and euphoria that 25i produces, then there is no need for mescaline, but if you really want to push the envelope, then mescaline is the ticket.
Kent's book "psychedelic information theory" states the following in general terms:
* 5-HT1 affinity is generally thought to work in contrast to 5-HT2A agonism to promote well-being and satisfaction. Mescaline, 5-MEO-DMT, DIPT, LSD all have a high 5-HT1 affinity. Mescaline hits (5-HT1A at 3.61, note this value is from an inverse chart, where 4.0 indicates maximum affinity), LSD hits (5-HT1A at 1.1, this is from the ki chart where 0.0 indicates maximum affinity). Mescaline hits (5-HT1E at 3.16, this is from the ki chart where 4.0 indicates maximum affinity). LSD hits (5-HT1E at 2.62, this is from the ki chart where 4.0 indicates maximum affinity). 25i lacks affinity for 5-HT1A and 5-HT1E.
* 5-HT2A & 5-HT2C are the most important receptors that all the main psychedelics hit, with the most potent psychedelics hitting them real hard...they are implicated in extreme visual activity and complex thinking. 25i-nbome hits these two receptors (5HT2A & 5-HT2C) harder than any other psychedelic out there. 25i hits (5-HT2A at 0.044) and hits (5-HT2C at 2.0), LSD is only able to hit (5HT2A at 3.5) and hits (5-HT2C at only 23.0). The lower the ki value, the greater the receptor binding.
* 5-HT2B is implicated with purely sensual or entactogenic effect. 25i hits (5-HT2B at 231), and LSD hits (5-HT2B at 25). Mescaline hits (5-HT2B at 3.97, this is from the inverse chart with 4.00 indicating maximum affinity). MDMA hits (5-HT2B at 3.64, this is from the inverse chart with 4.00 indicating maximum affinity).
DiPT, Mescaline, and MDMA have very poor 5-HT2A, 2C affinity, but all have a high 5-HT2B and adrenal affinity, cardiovascular activity, and acute sensuality. 5-HT2B affinity is quite high for all theses.
* 5-HT6 is implicated with ?. 25i hits (5-HT6 at 73.0), LSD hits (5-HT6 at 6.0).
* 5-HT7 is implicated with reward activity and overall transcendent psychedelic action, with the mystically popular DMT, 5-MEO-DMT, and LSD topping the affinity list for this receptor. LSD hits (5-HT7 at 6.0). Now neither 25i nor mescaline hit 5-HT7.
* adrenal-2a receptor is hit by mescaline at 2.92 (inverse chart), whereas LSD hits adrenal-2a at 2.93 (inverse chart), very similar.
* adrenal-2c receptor is hit by mescaline at 4.00 (inverse chart, maximum value), whereas MDMA hits adrenal-2c receptor at 3.21.
* 25i does not hit any of the adrenal receptors.
adrenal affinity is implicated (along with 5-HT2B) with effectivenss at stimulating serotonin production, cardiovascular activity, and acute sensuality.
So in other words, mescaline will target 5-HT1A, 5-HT1E and 5-HT2B receptors with extreme affinity....and the 25i will target the 5-HT2A, 5-HT2C, 5-HT6, and 5-HT2B with great affinity. Mescaline fills in the spiritual well-being and satisfaction void, and 25i fills in the extreme visual activity and complex thinking. Mescaline by also targeting the 5-HT2B receptor with even greater intensity than 25i, contributes to even greater increased sensual and entactogenic effect. Now, 25i is very empathogenic and sensual all on it's own, imho appearing in the trips I've had to be near equal to mdma in the euphoria it produces mentally, and 25i goes even deeper & feeling more natural than the substance mdma.
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So by adding mescaline along with 25i, we get the following:
5-HT1A, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT6, adrenal-2a, adrenal-2c
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Mescaline overlaps 25i perfectly, filling in the gaps needed while 25i overlaps mescaline filling in the gaps perfectly as well.
The only thing of importance really missing is 5-HT7 agonism, which LSD hits at 6.0 (regular ki chart, where 0.0 = maximum affinity)...5-HT5A, 5-HT5B, 5-HT1B, 5-HT1D, d1, d2 are the other receptors that acid hits, but little is known about the significance of these.
Take this all with a grain of salt, as psychedelic information theory is purely theoretical at this point.
Psychedelic Information Theory (Kent's book): http://psychedelic-information-theory.com/ebook/index.htm
I had totally forgoten that the book "Psychedelic Information Theory" by James Kent has a chapter on "Psychedelic Receptor Binding". He saids that the substances that have the most Hallucinogenic potency have very high 5-HT2A affinity as well as 5-HT2C affinity...
TABLE 1 from Kent's book
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25iNbome has 0.044 affinity for 5-HT2A (the highest ever recorded for a psychedelic, higher than acid even) and 2.0 affinity for 5-HT2C (much higher than acid), this may help explain the wild visuals that I experienced.
In this chart, a value of 4.00 indicates high affinity at that target; any value under 2.00 should be considered imperceptible. From Ray, 2010(3).
5HT--
2c-E = 1A (2.91), 1B (3.00), 1D (3.54), 1E (2.60), 2A (3.76), 2B (4.00), 2C [3.38], 5A (0.00), 6 (1.93), 7 (2.77), D1 (0.00)
2C-B = 1A (2.75), 1B (3.11), 1D (3.71), 1E (3.05), 2A (3.69), 2B (4.00), 2C [3.18], 5A (0.00), 6 (2.63), 7 (2.81), D1 (0.00)
LSD = 1A (3.73), 1B (4.00), 1D (3.70), 1E (2.62), 2A (3.54), 2B (3.11), 2C (3.11), 5A (3.64), 6 (3.75), 7 (3.70), D1 (2.34)
DOI = 1A (0.00), 1B (2.31), 1D (3.00), 1E (2.66), 2A (3.44), 2B (3.13), 2C (4.00), 5A (0.00), 6 (2.34), 7 (1.90), D1 (1.67)
DMT = 1A (0.00), 1B (0.00), 1D (3.91), 1E [3.28], 2A [2.58], 2B (0.00), 2C (3.42), 5A (3.16), 6 (3.35), 7 (4.00), D1 (3.51)
psilocin = 1A [2.88], 1B (2.19), 1D (3.40), 1E (3.03), 2A (2.14), 2B (4.00), 2C (2.52), 5A (2.83), 6 (2.82), 7 (2.82), D1 (3.37)
5meodmt = 1A (4.00), 1B (2.41), 1D [3.48], 1E (1.72), 2A [0.98], 2B (0.69), 2C (1.55), 5A (1.84), 6 (2.73), 7 (3.69), D1 [2.38]
DIPT = 1A (4.00), 1B (0.00), 1D (2.51), 1E (0.00), 2A (0.00), 2B [3.48], 2C (0.00), 5A (0.00), 6 (0.00), 7 (0.00), D1 (0.00)
mescaline = 1A (3.61), 1B (0.00), 1D (0.00), 1E (3.16), 2A (0.00), 2B (3.97), 2C (0.00), 5A (0.00), 6 (0.00), 7 (0.00), D1 (0.00)
MDMA = 1A (0.00), 1B (0.00), 1D (0.00), 1E (0.00), 2A (0.00), 2B (3.64), 2C (0.00), 5A (0.00), 6 (0.00), 7 (0.00), D1 (0.00)
Ray, TS: "Psychedelics and the Human Receptorome". PLoS One. 2010; 5(2): e9019.
In comparison, mescaline has very poor affinity for 5-HT2A or 5-HT2C, he saids this explains why it is largely considered a non-visual psychedelic, along with 5-meo-dmt, dipt, and mdma. To me, 25i-nbome is visually more spectacular than acid (in it's own distinct way however). I disagree with his non-visual statement about mescaline because to me, mescaline is visual at high doses, causing not just visuals but visions as well.
From last paragraph of Nichol's paper:
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The ligand 25i-Nbome had low affinity for most receptors, with the following reported Ki values (nM) for receptors where it had significant affinity: (remember the lower the number, the greater the binding):
5-HT2a (0.044)
5-HT2c (2)
5-HT6 (73, +/-12)
5-HT2B (231, +/-73)
u opiate (82, +/-14)
H1 (189, +/-35)
kappa opiate (288 +/-50)
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LSD:From "Psychedelic Information Theory" by James Kent:
5-HT1A = 1.1
5-HT1B = 90
5-HT1D = 11
5-HT1E = 93
5-HT2A = 3.5
5-HT2B = 25
5-HT2C = 23
5-HT5A = 7
5-HT5B = 5
5-HT6 = 6
5-HT7 = 6
d1 = 27
d2 = 6.4
d3 = 261
d4 = 230
d5 =
adrenergic = 37
histamine H1 = 1083
The significance of 5-HT5A, 5-HT6, and 5-HT7 receptors are unknown, but psychedelic tryptamines such as psilocin or DMT do have significant affinity for 5-HT1A receptors.
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Breadth of Psychedelic Receptor BindingInteresting as 25i-nbome also agonizes u opiate and kappa-opiate to a small limited degree. This might have explaind my feelings of weightlessness when walking outside in a garden at the peak of one of my first trips.
Table 1 lists the binding strength of popular psychedelic drugs at many 5-HT receptor sites, listed in order of 5-HT2A affinity.(3). This table should be an accurate representation of hallucinogenic potency of various psychedelics in descending order. From subjective reports all substances at the top of this list are very hallucinogenic, but DMT, which is often considered to be the most hallucinogenic, actually falls somewhere in the middle. If we also look at 5-HT2c affinity, which is implicated in hallucination, we can see that all substances at the top of the list also have high 5-HT2C affinity, with DMT and DOI having slightly higher affinity than the rest. 5-HT7 receptor affinity, which stimulates cAMP activity and the reward system, also seems to be implicated in overall transcendent psychedelic action, with the mystically popular DMT, 5-Meo-DMT, and LSD topping the affinity list for these receptors.
In contrast, there are four non-visual psychedelics at the bottom of the list, 5-Meo-DMT, DiPT, Mescaline, and MDMA. These substances have very poor 5-HT2A, 2C affinity, but all have a high 5-HT2B and adrenal affinity; this indicates they are effective at stimulating serotonin production, cardiovascular activity, and acute sensuality. 5-HT2B affinity is quite high for all samples in this list with the exception of DMT and 5-MeO-DMT, making 5-HT2B affinity a good indicator for purely sensual or entactogenic effects. It is interesting to note that DiPT, Mescaline, and 5-MeO-DMT all have a high 5-HT1A affinity, which is generally thought to work in contrast to 5-HT2A agonism to promote well-being and satisfaction. DiPT is unusual because it produces distinct audio hallucinationa and little or no visual hallucinations, and predictably does not bond with 5-HT2A, 2C receptors implicated in visual hallucination.
By analyzing this affinity table it seems possible to predict the relative potency and effect of any hallucinogen based soley on binding profiles, though the three control molecules at the bottom of the list (6-F-DMT, Lisuride, 4C-T-2) are reportedly non-hallucinogenic despite high 5-HT receptor promiscuity; this is likely because they are not active as agonists, they are antagonists, or their binding profiles are not synergistic and somehow cancel each other out.
Salvia divinorum interrupts kappa-Opiod tactile sensory pathways; these pathways mediate pain, gravity awareness, and sensation for determining physical orientation in space."
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There are actually a couple places (outside of auction sites ) that directly have Hydroxypropyl Beta Cyclodextrin. In any case, there are hundreds of research papers on the science of HPBCD, "Trappsol" and other fancy sounding brand names are currently used for the stuff these days it seems.
this is an important study (below) from the cyclodextrin mega-expert Dr. Joseph Pitha, and explains in more
detail the theory behind my preparation of the Nbome blotter that we both tried using a 95% drinkable alcohol (ethanol) solution....ie a solution of 100ml of 95% etoh, 100mg of 25i-nbome, and 900mg of HPBCD, which had been pre-spun for 24 hours.
http://www.sciencedirect.com/science...78517392902816
hxxp://www.sciencedirect.com/science/article/pii/0378517392902816
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"Effects of ethanol on formation of inclusion complexes of hydroxypropylcyclodextrins with testosterone or with methyl orange"Dazed (bodybuilding expert):
by Josef Pitha and Teruhiko Hoshinoa
National Institutes of Health, National Institute on Aging/GRC, Baltimore, MD 21224 U.S.A.
Received 21 June 1991;
revised 9 October 1991;
accepted 25 October 1991.
Available online 4 November 2002.
Abstract
Gradual additions of ethanol decreased and eventually abolished the formation of inclusion complexes of testosterone with hydroxypropylcyclodextrins in aqueous solutions. With hydroxypropyl-?-cyclodextrin this occured through two mechanisms. At low concentrations of ethanol (less than 30 percent), the solvent primarily acted as a competing guest compound; at higher concentrations the dissociation primarily occurred through non-specific solvent effects. With hydroxypropyl-?-cyclodextrin only the dissociation through nonspecific solvent effects was observed. Surprisingly, when ethanolic solutions containing fully dissociated complexes were evaporated, the solid residues had properties characteristic of complexed species, i.e., they showed the rapid and complete dissolution characteristic of complexes prepared by freeze drying of aqueous solutions. That inclusion complexes were formed during the final stages of evaporation of ethanolic solution of components was confirmed by measurements of circular dichroic spectra of a methyl orange: hydroxypropyl-?-cyclodextrin combination. In this combination the spectra of included species were highly characteristic and were recorded both in aqueous solutions and in solid state after the evaporation of ethanolic solutions but not in concentrated ethanolic solutions.
Keywords: Cyclodextrin; Hydroxypropylcyclodextrin; Inclusion complexation; Solvent effect; Testosterone
Quote
The conventional penetration enhancers like alcohols or polyethylene glycol act by disrupting the lipid layers of membranes.(3) That is a big source of irritation from the old formula, and this irritation can thus be avoided by the use of CD’s (cyclodextrins). Another advantage is, once administered, the steroid is rapidly absorbed sublingually. Nearly 95% of the steroid will be absorbed within 20 minutes. This also causes the need for multiple doses throughout the day.
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1. Water
HPBCD is very soluble in water. Substitution of the hydroxyl groups of the BCD disrupts the network of hydrogen bonding around the rim of the BCD. As a result of disruption of the hydrogen-bonding network, the hydroxyl groups interact much more strongly with water resulting in increased solubility compared to BCD. Solubilities of HPBCD are typically listed at >60% at amnbient temperature. As the concentraion becomes higher, viscosity begins to increase and solubility determinations become difficult to perform due to slow filtration rates and at very high solids levels, slow dissolution because of high viscosities making mixing difficult.
Solvents
HPBCD is more soluble in solvents than BCD, but extensive work has not been done to characterize the solubility of HPBCD in solvents. The table below shows the solubility in selected alcohols.
Solubility (g/100ml)
95% ethanol 225g/100ml
isopropanol 152g/100ml
solubility of HPBCD in ethanol-water mixtures:
0% ethanol concentration: 360g/100ml
20% ethanol concentration: 340g/100ml
40% ethanol concentration: 320g/100ml
60% ethanol concentration: 295g/100ml
80% ethanol concentration: 265g/100ml
95% ethanol concentration: 225g/100ml
Quote
What are cyclodextrins?
Cyclodextrins are a form of linked carbohydrates. They're formed by an enzymatic synthesis that begins with starch. The enzymes, called transglycosidases, are derived from bacteria. What these enzymes do is couple the starch molecules together to form a truncated, conical, molecular structure with a hollow cavity inside.
The inside of this cyclodextrin "cone" is just about the perfect shape and volume to accommodate a steroid molecule. It's also a non-polar molecule, which means that it has some of the same properties as a fat or oil. The steroid molecule doesn't just sit inside the cone, it actually attaches to the inside of it. Also, it won't dissolve in water. However, while the inside of the cyclodextrin cone is non-polar, the outside is polar, which means that it will dissolve in water. What's the significance of all of this? When a steroid molecule and a cyclodextrin molecule hook up, they form a 1:1 complex. So, while the steroids themselves won't dissolve in water, a cyclodextrin/steroid complex will. The upshot is that steroid complexes become more absorbable through the oral mucosa.
A lot of clinical research has been published on the use of sublingual cyclodextrin complexes (SCCs) in humans. At the forefront of much of this research has been Josef Pitha of the US Department of Health and Human Services. Pitha has several patents on sublingual cyclodextrin complexes. He's also authored a journal article where he details the results of an SCC of testosterone on men. In a nutshell, Pitha found that an SCC containing 10mg of testosterone per tablet raised testosterone levels astronomically high (900% over baseline at one hour) and at two hours the levels were still elevated 485%. Compare that with another study that used regular testosterone at 20 times the dosage used in Pitha's study. Regular testosterone - not complexed with cyclodextrin - only raised testosterone around 500% at the peak.
Another study performed by Stuenkel et.al. showed that testosterone SCCs of 2.5 and 5.0mg raised testosterone levels in hypogonadal men 2341% and 4270% (absolute increases of 1765 ng/dL and 2406 ng/dL) respectively! It took an average of 20 to 30 minutes to achieve maximum blood testosterone levels, but even after eight hours post-dose, the testosterone levels were still elevated 126% for the 2.5mg dose and 195% for the 5.0mg dose. Interestingly enough, the peak levels for estradiol only increased 300% and 340% over baseline, respectively. Remarkable, considering that one usually sees estradiol levels increase proportionally with testosterone levels when other forms of administration are used (i.e. injectable esters and TU)
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HPBCD BasicsDazed:
By David Tolson
Introduction
One of the primary issues concerning steroids and prohormones is that of optimal delivery. While most drugs and supplements are taken orally, there are a number of reasons why this method is largely ineffective with most prohormones. When taken orally, these compounds are extensively metabolized in the liver, making the dose used much larger than the amount that gets through. This may also place undue stress on the liver, especially with certain substances. Because of this, other delivery methods, such as transdermal, sublingual, and intranasal, have all become popularized, and each has advantages and disadvantages. This article discusses the compound hydroxypropyl-beta cyclodextrin (HPBCD), which can be used to facilitate prohormone delivery in a number of ways.
Cyclodextrins are a group of compounds that are commonly used in medicine to increase the aqueous solubility of drug substances by complexation [1]. Cyclodextrins are cyclic oligosaccarides, or sugars, which contain alpha-1,4 linked glucopyranose units (in the case of beta-cyclodextrins, seven of these units) in a truncated cone shape [2]. This results in a molecule that has an internal cavity that is hydrophobic and easily forms a complex with a steroid/prohormone molecule, while the outer surface of the cyclodextrin is hydrophilic, and this makes the complex easily dissolvable in water [2-4]. This renders prohormones much more bioavailable, and cyclodextrins are capable of enhancing nasal, sublingual, and transdermal delivery [5-6], among others. Moreover, cyclodextrins will cause much less irritation than other methods [3, 7].
The cyclodextrin of choice for prohormone delivery is HPBCD. When compared to other testosterone beta-cyclodextrin complexes, HPBCD was 1,533 percent more soluble in water, while another study found that HPBCD-steroid complexes were effective while beta-cyclodextrin-steroid complexes were not [4]. HPBCD also has an excellent safety profile.
Sublingual delivery
Sublingual delivery (administered under the tongue) presents an attractive alternative to traditional oral administration. Because of the limited surface area, the amount of prohormone that can be absorbed at one time appears to be 25 milligrams or less. However, when compared to oral delivery, even this amount is advantageous. One study found that a cyclodextrin complex containing 10 mg of testosterone delivered sublingually raised testosterone levels by 900% over baseline, with a 485% elevation at the two hour point. In contrast, even 200 mg of oral testosterone only raises levels by around 500% at the peak. A study comparing oral and cyclodextrin complexed 4-androstenediol also found that the sublingual version lead to a 261% greater increase in testosterone with one quarter of the dose, with the peak levels at 40 as opposed to 90 minutes. [4]
All in all, sublingual delivery is much more effective than oral for the amount used, but it does require more frequent dosing. Sublingual prohormones are usually taken 3-5 times daily.
Intranasal delivery
Intranasal delivery takes the trend of sublingual delivery even further. It is doubtful that more than 20 mg at a time will be absorbed using this method, and blood levels quickly spike 15 minutes after delivery and then dissipate to baseline by 90 minutes. Running a cycle using this method is impractical, as one has to dose up to 10 times daily. However, bioavailability is further increased – intranasal delivery has the highest bioavailability of all prohormone delivery methods, short of injection [7]. Additionally, intranasal delivery provides the most direct route to the brain [6, 7]. For these reasons, this method has become popular for pre-workout stimulant purposes. Many people report increased workout intensity from intranasal prohormones. DHT precursors are best suited to this purpose, although some other prohormones may make effective pre-workout stimulants as well.
Conclusion
HPBCD complexes can allow for a number of novel effective prohormone delivery methods. Each one has unique advantages and disadvantages. For further information, as well as information on creating your own cyclodextrin complexed prohormones, I recommend the following article:
Alternative Steroid Delivery Systems, by Dazed
If you have any questions or comments regarding this article
No part of this article may be reproduced in any form without the permission of David Tolson or Mike McCandless.
References
1. Eur J Pharm Sci. 2003 Oct;20(2):197-200. Driving forces and the influence of the buffer composition on the complexation reaction between ibuprofen and HPCD. Perlovich GL, Skar M, Bauer-Brandl A.
2. Int J Pharm. 2003 Sep 16;263(1-2):173-81. The effect of beta-cyclodextrins on the permeation of diclofenac from supersaturated solutions. Dias MM, Raghavan SL, Pellett MA, Hadgraft J.
3. Mind and Muscle Magazine Issue #9. Alternative Steroid Delivery Systems by Dazed.
4. Super Andro: Cyclodextrin Technology Shatters the Absorption Barrier by Patrick Arnold and David Garrett.
5. Int J Pharm. 2003 Mar 6;253(1-2):1-11. Mechanistic studies of the effect of hydroxypropyl-beta-cyclodextrin on in vitro transdermal permeation of corticosterone through hairless mouse skin. Shaker DS, Ghanem AH, Li SK, Warner KS, Hashem FM, Higuchi WI.
6. Int J Pharm. 2002 Oct 10;246(1-2):25-35. The effects of water-soluble cyclodextrins on the histological integrity of the rat nasal mucosa. Asai K, Morishita M, Katsuta H, Hosoda S, Shinomiya K, Noro M, Nagai T, Takayama K.
7. The Scoop on Intranasal Prohormones by Patrick Arnold
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The best tool available to make nasal and sublingual steroids are derivatives of beta cyclodextrins. The one that is most readily available is hydroxypropyl-beta cyclodextrin (HPBCD). (Note: Plain beta-cyclodextrin is of little use) In case you have not heard of these, cyclodextrins are cyclic oligosaccarides (sugars) that have a hydrophilic outer surface and a hydrophobic inner surface.(3)
They can be thought of as a doughnut, with the center capable of having a steroid molecule stuck inside it. The hydrophilic outer surface makes the cyclodextrin soluble in water, and when it is combined with a steroid, it can make the poorly water soluble steroid soluble as well.(3)
In addition to making steroids soluble, cyclodextrins have very other important properties that make them ideal for our purpose. Cyclodextrins are known to enhance steroid delivery through biological membranes.(3) The large CDs themselves are very bad at permeating biological membranes, but they deliver the steroid to the membrane, where it partitions into the membrane, leaving the CD on the outside of the membrane.(3)
The conventional penetration enhancers like alcohols or polyethylene glycol act by disrupting the lipid layers of membranes.(3) That is a big source of irritation from the old formula, and this irritation can thus be avoided by the use of CD’s. Another advantage is, once administered, the steroid is rapidly absorbed. Nearly 95% of the steroid will be absorbed within 20 minutes. This also causes the need for multiple doses throughout the day.
Complexation:
It seems that hardly anyone out there knows how to complex a steroid with a cyclodextrin. One procedure I saw on a different company’s steroid column was laughable. It was pretty obvious that whoever wrote that procedure knew very little about cyclodextrins. It is really fairly easy to do. There are multiple ways to do it, but I will tell you three methods to try, depending on what resources you have available. In all instances, you need a ratio of 9g of HPBCD to 1g of steroid. Complexation occurs because the steroid is more energetically stable inside the CD than outside of it. It is an equilibrium process, but the equilibrium lies much more on the side of complexation.(3) Water is essential for complexation to occur. It is removed from the inner cavity to allow for the steroid to enter, but even normal room humidity is sufficient for complexation if the mix is given sufficient time.(4)
Method1
For the first method we will formulate it for a total of 2g of steroid.
Dissolve 18g of HPBCD in 80ml saline in a beaker on a stir plate. Once this is dissolved, slowly add the 2g of steroid over about 5 minutes. Let this stir overnight. Filter out any insoluble particles. This provides a 25mg/ml solution.
Method 2
For the second method, we w

