Author Topic: 2-methyl-butan-2-ol (and opioids-dihydrocodeine)-testing amylene hydrate  (Read 140 times)

Tsathoggua

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2-methyl-butan-2-ol (and opioids-dihydrocodeine)-testing amylene hydrate
« on: August 26, 2011, 02:52:40 PM »
This is still in progress, bear in mind, but I do not think the effects are going to change much given what I have read on 2-methyl-butan-2-ol.

My build is slight, no fat, although wiry and not physically weak either. Built sort of like a stick insect with metal wire wrapped round it (and no parthenogenetic procreative ability to the best of my knowledge) and sex is male. Age mid 20s (or alternatively it is ''none whatsoever please'', unless you are both classically autistic, and happen to be my 'lil dormouse, and she, does not come on this site, at least, not unless she still likes to do what originally she was, and stalk me, can't remember if I gave her my password here or not or if she just has most of my others)

Also bear in mind I have chronic pain, and have been on painkillers for nearly a decade now. Today I didn't expect to recieve the product and its just one of those days where as occasionally I do, choose to take a higher dose than what I need for pain relief...no...I take that back...a higher dose than I need to remain stable without causing withdrawal and allow me to walk or climb down the house stairs freely. My usual dose, 30mg DHC taken per os, QDS (without APAP, I told my doctor that I do not take it, and I don't, I see no point in doing so, since even given via an IV line, it is completely and utterly without any action whatsoever in me, no analgesia, or any other effect), truth be told, even taking a MUCH higher dose, as one dose, rather than QDS of my pain meds doesn't leave me anywhere like pain free, they do help though, even at my daily dose taken as a single bolus (which seems to leave me both stable and with at least some analgesia)

12x30mg dihydrocodeine tartrate tablets were taken earlier in the morning, not hugely earlier, by an hour or maybe two, I hadn't kept track of the time as I had no reason to do so when they were taken. Most likely somewhere inbetween. That was enough time to have the pills kick in some and get to the stage of a nice warm glow and relaxation.

Then what happened....my order of amylene hydrate popped through the door. Was expecting 40ml which I paid very little for, possibly wouldn't have bought it, except for novelty bioassay purposes, but I was not poorly off at the time, and besides, the ever-curious elder thing of amphibian aspect, he tells me he has some use for it too, in that he had some time ago, the novel concept enter his warty, venomous, fly-and/or-person-eating head of forming an isocyanate from the beckmann rearrangement product of a certain 3,4-methylenedioxy-ring substituted floral note chemical used in perfumery and subsequent reaction of this with an alcohol, yielding a carbamate, which would crack open in HCl to release MDA and the alcohol the carbamate corresponds to. This being sufficient, as long as no MDA byproduct from a wet alcohol/solvent etc. is allowed to remain in the reaction conditions.

Was expecting a nicely sized order of methoxetamine, along with some fresh syringes, 30ga. 1/2 inch needles and amps of sterile water to go with it. Having found out that intravenous methoxetamine is EXCELLENT for both the tendon and joint pain, as well as for the neuropathy I got left with, after having surgery, which aside from preventing the knee from locking, stopped neither pain, weakness, nor the affected leg collapsing occasionally entirely. Did lessen the frequency of it collapsing, but not eliminate it...this seems to be happening more and more often in the present time.

What the bloody buggers DID do however, was damage a nerve, most probably my medial sural cutaneous nerve, or possibly an ofshoot of my tibial. Left me with neuropathy and paraesthesia thats usually treated (to a degree) by pregabalin, although its not great, works a treat for potentiating opiate nods though. This is getting included because it does have a bearing on this report, despite my methoxetamine and injection supplies not yet getting here. I find methoxetamine fantastic for dealing with my pain, and altogether a most enjoyable recreational, and the afterglow the day after, and for a good few days post doses it provides a good increase in energy, motivation and a strong antidepressant-like mood lift, appears to be strongly anxiolytic also.

Its both a strong dissociative anaesthetic, and also, I believe a stronger mu opioid receptor agonist than people suspect, giving a distinct, pronounced, although not overwhelming rush on intravenous injection as well as being able to maintain this subject completely, without recourse to his dihydrocodeine at all being given by intravenous injection BD...not enough to make him nod until a dose is reached that makes MXE preclude that entirely, by putting him under a surgical plane of anaesthesia. Slight local anaesthetic properties also (I intend on testing something out, division of a good solid dose that would M-hole him without question into 2ml of sterile water for injection, and infiltrating a depot shot, subcut, of a quarter of the solution each shallowly over the patellar tendon, median sural cutaneous nerve, approximately equal to the middle point between the anterior cruciate ligaments and a little up and to the outer median side of the median sural cutaneous nerve to cover roughly the locality of the tibial nerves first major branch in the direction of the pelvis. Of course, its a given that said solution will be prepared with sterifilteration using an 0.22 micron filter...I think its not impossible there may be a non-centrally mediated analgesia possible that is not just the sum of the centrally mediated opioid and dissociative properties...at any rate, the mild local anaesthesia would without precluding walking, likely lessen pain significantly for a while)

Why am I including information about methoxetamine, which I have none of, and haven't as such, taken (no syringes to put one of the needles in my injection kit on either until they come) ? because ethanol is known to have a sizeable dissociative component to it, especially in larger doses, and an easily perceptible NMDA antagonist signature. I have used MXE heavily, been through around 6-7g spaced over a month or so, and more previous to that although having had a break from its use between the last two runs of use, I thus have a sizeable tolerance to dissociatives and can accurately assay this property of 2-methyl-butan-2-ol than I would otherwise be able to if I had no such tolerance, this is partially offset by somewhat negligent in frequency, dosing of piracetam (which will both counteract, and/or block the effects of NMDA antagonists, and given AMPA receptors feed forward glutamatergic signalling to cause expulsion of the magnesium ion responsible for the voltage and ligand-gated blockade of the NMDA receptor at resting potentials, which is responsible for the level of receptor expression and likely sensitivity to antagonists) but I have been lazy, and have little left right now.

What does appear to be the case, is that after dosing the quantity of amylene hydrate I have thus far my pain is lessened more than what I believe would be the case on merely the opioid. Still present though, but only MXE adequately completely eliminates it.

Dosage and route of 2-M2B taken so far? 4.16g, per os, in gelcaps. The liquid is clear, and has, contrary to the description of 'minty and chemical' in wikipedia it has a pronounced and quite definate smell of either ether or THF. Tastes like ether too (drunk enough to be able to tell it when I taste it..and one of my favourite kinds of candy is flavoured with ether..or was, actually, since they took it out of the recipe I haven't bought a single tube of victory Vs, well, one, only needed to buy one to find out I was dissapointed with that stupid idea) It must have a low water content as it doesn't soften and melt the gelcaps in the time needed to empty the indometacin out of them, and add the weighed out amylene hydrate via a pipette.

To start with, being that a dose of opioids that would cause some respiratory depression was kicking in (although not dangerously depressing to my breathing rate or tidal volume) 1g, which is noted to be very, very much on the low side for this drug was taken, the gelcaps being washed down by a good slug of sort of flat coke. Within ten minutes then a warm glow was felt. Part of this was I believe, local in origin, the bursting of the gelcaps and release of something which was basically pure overproof alcohol in that respect being heating and a circulatory stimulant, also the beginnings of a warm glow of central origin had begun to manifest. Not so much subtle, but not overpowering and not strong. Just feelable, but not in the way or pushy.

First time with this drug, so its prudent to dose slowly until one can be reasonably sure one is where they want to be. A little then was inhaled also, inspired by the etherial scent, when I smell ether, that immediately makes me want to squirt some into a bottle and pull away on it, I love ether, but get to do it very rarely, as it will stink the house out if I do it inside :P

Don't want to waste the amylene hydrate though, so one of the small glass vials it was purchased in was held underneath the nose, as I have done with ether when taking it to parties, like a bottle of butyl nitrite poppers, one nostril closed, and inhaled repeatedly. No rapid onset of dissociative effects like with ether, but 2-methyl-butan-2-ol is known to be MUCH longer lasting, 8 hours or so.

Quite relaxing, added some euphoria that hadn't been reached by the opiates to the experience, around half an hour later, seeing as how its been taken quite slowly a second gram was taken, that ended up being 1.16g, but blowed it I see it as practical to take back 0.16g of a drug active in doses of multiple grams, I see more chance of accidentally knocking over a vial. I have more than one obviously, but all the same, I don't want to lose what I handed over perfectly legitimate and hard to come by currency for...and of course, ye olde toade wanteth some for his ministrations in the lab over whatever the hell he is up to this time, or get it spilled into the bowels of his milligram scale or inside his keyboard.

Again, rapid onset of effect, with the warmth signifified by absorption providing a herald of the effects.
This time...what was a relaxed, pleasant opioid experience with a hint of sedation from the 2-M2B turned into my nodding. Eyes closing every so often, suddenly jerking back to full conscousness in a myoclonic way as I find typical of opioid effects.

Around 3/4-1 hour ish were left before redosing this time. Some slowing of respiration is evident, but again, not threatening, just there. I probably wouldn't do a signifificantly strong dose of methoxetamine under this combination of this dose of DHC plus the amylene hydrate, had it arrived. Would do some, but would do the IV push very slowly, and carefully watch respiration rate and tidal volume to ensure comfort. Nodding pronounced now. Keep closing my eyes, in fact I cannot willfully force them to remain open 100% of the time, closed them, and was presented with the image of the stunning, grey-hazel eyed, brunnete, oxy-carbon subnitride flame intense beauty of my dear dormouse, coming closer as though to kiss me. definately a vote for my approval on this one then, regardless of any hangover, that said, I could be getting capsaicin injected into my eyeballs, and if I saw her face, then it would recieve a positive report.

 I really am shocked, by the effect she has on me, and the capacity she has to make me feel emotions intensely, I never knew I COULD feel things that intensely emotionally, all my life, until I came to realise just how much I treasure my dearest lady. She matters to me, more than anyone, or anyTHING else, ever has. If it took my selling or giving away every last material possession I had, keeping only my computer and phone to communicate with her to be by her side, then I would do it without a fraction of a second in hesitation. 

Thats not the drug talking, that is what I have long known I feel. I am a very, very very lucky man, in that I got to have a beautiful lady of her caliber stalking me, so shockingly, mindblowingly stunning, and so completely up front, brutally and unflinchingly honest, softly spoken, yet hyperintense of feeling of an classical autie girl, I think of her so many times throughout every day, the moment I wake up, I think of my dormouse, and as soon as I turn my computer on, the first thing I like to do, is look at a photo of her, lying down, on her bed, smiling. Sleek dark hair, grey eyes, and a smile that would melt molybdenum as easily as a fission-boosted, deuterium/tritium boosted fusion bomb would melt an icecube, twice my age, give or take a couple of years, at 44, but not looking it at all, I think of her often, all the time, can be walking down the road, eating, drinking, going to the loo, feeding my silvery grey rescue(ish) cat, working with the power tools or performing some sort of chemical synthesis/purification, and her face, her petite, slim, pale body with the waist-length hair, and her soft american accent walks into my mind again to make me crack a huge smile. I must look like I am on something plenty of times when I am on nothing but the bare minimum of painkillers to hold me and keep me properly mobile because of the way my mouth twists up into that huge grin, the same one thats as big or bigger as the one that would show on my face about 3 seconds after an IV push of methoxetamine or morphine sulfate. Hell, she has even actually woken me up before plenty of times, not being physically present, but just the thought of her, its enough to make me wake from a deep sleep, and curl u contentedly, smiling like a cat with a bowl of cream.  I'd do anything for her, give my life for her even if she needed it. I have never had to ask her if she means something shes said, never had to question her faithfulness, or her intensity of love for me, never had to doubt a single thing about her or from her.

Anyways, back on track...yes, obviously, it just happened again, and the thoughts of my dear dormouse came straight back into my mind, as so often they do.

An hour or so past the second dose, a third dose of 2-CH3-2-butanol, 2g this time, was taken, again, like the others, pipetted into gelcaps, sealed, and swallowed with a drink. A fleeting nausea was experienced on them bursting, but no more than a minute or two, with the warmth and heat being felt strongly this time, more so than before. This quickly subsided though in a mere handful of minutes. Nodding strongly now, no nausea. A little drymouth, although I attribute this to the DHC. I can, tolerance to the 3-MeO-eticyclidine notwithstanding, I feel a taste of dissociative signature. I find this quite distinctive, as much as so as a cannabinoid containing bong hit, or the rush of an intravenous opioid, if its there, I will realise it, as easily as I would know the taste of salt or sweetness. Respiration rate slow, steady, and a taste on the breath, especially breathing out through the nose, that is the same as I get after having swallowed a shot of diethyl ether.

That will be my report for now, more updates will be done though as and when appropriate, probably not for a while though. This is a euphoric substance, not the intense, shallow, ecstatic euphorigenic effect of enteral GBL, but a slower, long lasting, very relaxed euphoria. I am, however, hungry, so I am going to go out and buy something to eat. Then come home, eat, think of my dormouse while curled up on my bed with some music on, nodding, stick on some music, and think of my girl some more.

After eating, I think I will dose a little more amylene hydrate, I think I might plug 1-1.5ml. This is NOTHING like alcohol, at least in as far as I can tell while I'm on a decent  dose of DHC also. I don't MIND alcohol especially, but in moderation. i don't really appreciate anything more than a light, warming buzz, or a good few drinks at the end of a long, long day hiking through the woods on AMT with a light meal. EtOH feels otherwise...dirty if that makes sense, and there are less pleasant qualitities about it that just don't render it a suitable recreational or relaxant substance on the whole. Diuretic effect of 2-methyl-2-butanol unlike with C2H5OH seem not just reduced, but absent, not merely proportionally but entirely. If there are any they are slight. I could use a piss right now, but opioids also, I would feel the need to urinate frequently if it were alcohol, but experience urinary retention due to bladder sphincter myorelaxation which would make it more difficult.

Could use a cigar, I quit smoking fags (well occasionally I will go to a gaybar with my revolver and brainsmoke a few of those bastards in the toilets as they sit on the dunny ;D) after my first, inadvertently bloody well very heavy AMT experience but I do enjoy the occasional tin of short, strong panatellas, and the very occasional treat of one or two of my favourite large, cuban oscuro corona de lux...this desire right now is not because I crave nicotine and am dependent, but because I feel it would add the experience and be just the thing. Other than that...just curl up and picture every last expression, every last hair, skin tone and curve on my dearest one.
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Tsathoggua

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Re: 2-methyl-butan-2-ol (and opioids-dihydrocodeine)-testing amylene hydrate
« Reply #1 on: August 30, 2011, 06:11:53 PM »
Obviously long acting, many hours. Very rapid onset. Minutes. I downed half a 10ml vial of the stuff last night as I woke up in opiate withdrawl...thanks knee injury, thanks a twatting bunch, just lovely. Not. My pain meds won't kick in until quite some time after taking them, nor will any benzos, my pregabalin, the fastest acting relief I have available is chlormethiazole, which comes as the freebase, at least my particular prescription for it does, the ethanedisulfonate salt is available as a syrup. Thats fast acting when given rectally. But nowhere near as quick as amylene hydrate.

It reminds me of GBL in that respect. Fast acting, hard hitting, and unlike what some people have said, no hangover.

It would be quite impossible to slip into somebody's drink surreptitiously, they would immediately spit it out and likely thump the person responsible.

Contrary to other reports, I find the statement that it 'smells minty' quite erroneous. In actual fact it smells like diethyl ether or THF. In fact I originally wondered if I had in fact been sent vials of EtOEt or THF after smelling it. 2-methyl-2-butanol smells NOTHING like mint, it smells, and tastes, like a slurry of soil in diethyl ether. I've never drunk a slurry of dirt in ether, but thats what it tastes like nevertheless. The dose of last night is still active. Tailing off, very slowly, but still active.

After swallowing a dose, one can expect, I think, to wait a maximum of 10 minutes before being hit like a train wreck victim. Tastes disgusting, tastes like diethyl ether mixed with dirt. The dirt bit making it revolting. I love the taste of ether, I'll drink EtOEt in preference to vodka, neat. But amylene hydrate tastes absolutely foul. I can still taste it if I belch, and I can still feel it. Currently I have to check my typing before posting because its coming out all squirrely.

Oh, and it makes a very effective remedy for opioid induced constipation. Backed up....unmentionables, can be quite effectively partially dissolved by using a 30ml syringe to thoroughly mix 5-10ml (depends on how well one tolerates the drug to begin with) of 2-methyl-butan-2-ol in as mucb further water as the syringe will hold, then sticking it where the sun don't shine.

After the 5ml dose last night, it hit FAST, this was orally. Warms going down, stings in the mouth. But that is rapidly remedied by swilling out with a soft drink. It appears to be compatible with metronidazole. The original doses were taken on the tail end of a course of the latter. I suspected as much. Being a tertiary alcohol it shouldn't go through an intermediate aldehyde via hepatic metabolism courtesy of alcohol dehydrogenase. This would explain the VASTLY longer half life than EtOH, and the lack of a disulfiram-like reaction on intake of a few ml of 2-methyl-butan-2-ol.

Still no sign of diuretic properties. That is one thing I really quite dislike about ethanol. Its impossible to enjoy an intoxication, which in the case of EtOH, feels dirty anyway, whilst having to take a leak every ten bloody minutes! None of that here. I feel comparisons with EtOH aren't very meaningful, but nevertheless must be made because other people will make them. If I had to compare it with another drug it would be GBL. Comparing amylene hydrate to ethanol isn't very smart IMO, because it ISN'T ethanol. An alcohol, yes, but not THE alcohol. Personally I prefer it by a great deal to EtOH. Ethanol is way too short acting to be of value to me, one has to keep redosing constantly, or continuously drinking.

It is at least, tasteless, thats the only downside I have yet discovered to 2-methyl-2-butanol. The taste. Its awful. If it tasted like diethyl ether, great, I would drink it just for the flavour, but tasting like a slurry of ether and dirt? no thanks, it is quite revolting. I think I will save my last 10ml vial, split it equally between two empty small glass vials (it came in these...rather handy I must say, perfect if one is going to go out somewhere and plans to dose or transport a substance of some sort).

That last vial, is for next time I go mushroom hunting in a favourite spot of mine, which has since I discovered the substane, also become my favourite spot for low-medium dose AMT trips to work out personal issues if ever I feel that need. Only got the one vial of amylene hydrate left, so I think I will try combining the two when I reach the little woodland clearing I head to once I have finished harvesting whatever I can find, and want to rest. Last time on just AMT, I more or less curled up there and stayed for hours. I have a feeling I might just be staying for quite some time:D

This substance produces significant ataxia....unfortunately....I managed to go flying, and knock one of my favourite bits of lab glass onto the floor, right where one of my sets of weights were, a 5ml pear shaped flask, built into a microscale condenser, and still head. Luckily it broke the very top end of the condenser clean off, so I think its still useable if I fuse it with a propane torch.

I think I might just contact a chemical company, rather than an 'RC' company, to aquire a little more of this, rather than paying by the 10ml, I don't want a huge amount around, I could see it becoming addictive to my personality type, but it would be nice to have a couple of hundred ml about, I think it would be just the thing for when I've finished hiking in the woods. Neck a pre-prepared 5ml 'shot', before I head to the little tapas bar I like to pop into for the little concoction I like to have the barmaid make me. not on the menu, but y'pays yer money.....try this, people...a double shot of tia maria into a very strong, black espresso or filter coffee.

Its just the thing when you have been hiking all day, for 12 hours straight through the woods, sniffing and nibbling at fungi in the hopes of finding some that are suitable for taking home and eating. All I have been finding there are tawny grisettes (Amanita fulva) of late, never eaten them, they seem too fragile to withstand cooking into something worth eating..although I saw a bunch of blushers (Amanita rubescens) in somebody's garden while I was walking past the other day, which suggests to me that the fly agaric season, the season for peppery boletes, and the season for brown birch boletes is now fully here. Already the fly agarics are out..sorty of...been looking, but only seen ONE, a while back...now its time to go hunting in earnest.

He won't be pleased.
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I'm hyperbolic, hypergolic, viral, chiral. So motherfucking twisted my laevo is on the right side.

Sedit

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Re: 2-methyl-butan-2-ol (and opioids-dihydrocodeine)-testing amylene hydrate
« Reply #2 on: August 30, 2011, 08:09:34 PM »
Thank you for this, I have been looking into this myself as an alcohol substitute. I considered chloral but then came across this. I have much apprehension about it as I would with EtOH if not for the fact that everyone drinks alcohol and I started when I was young.

This seems great given its unable to form the aldehyde and due to the possibility people have discussed on Blue light on mixing this with cyclodextrines to form a dry easy to dose power which would release the t-Amyl alcohol in vivo.
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Tsathoggua

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Re: 2-methyl-butan-2-ol (and opioids-dihydrocodeine)-testing amylene hydrate
« Reply #3 on: August 30, 2011, 08:30:25 PM »
I wouldn't bother wasting the cash for cyclodextrins. To hell with chloral, its a real bastard on the G.I tract. Has to be safer than GBL. And there I am considering the neurotoxicity issue of the latter. Chloral hydrate has been shown to have mutagenic/possibly carcinogenic properties. I have a gut hunch that those chlorine atoms aren't good for us bipedal mammalian critters when attatched to an alcohol intended for ingestion just as they are not when attatched to a hydrocarbon. With a halogenated alcohol, at least the body then has a big polar handle to grab hold of and throw away.

I give the thumbs up for amylene hydrate though, and I can tentatively, by bioassay, confirm that it is indeed unable to form the aldehyde, or else I would have had to knock myself out with an anaesthetic and not bee here for a while, due to beeing on metronidazole at the time.

It is easy enough to dose as it is, without conjugation with a cyclodextrin binder, I just pour out what I want into a 10ml vial (you will NOT need 10ml, of that, I assure you...not without a tolerance to ethanol which means you should give up fucking drinking in the first place!!! no way in hell....t-pentanol is POTENT. 5ml per os had me staggering accross the room and flopping down on my bed like a ragdoll)

There is also, I believe, the possibility for it to build up in the body, and hit you much harder than you either expected or wanted if you drink for several sessions in a row. Its much longer lasting than alcohol, as I said. Much longer. Really does a number on motor coodrination too. Think your a bad driver after twenty pints of dilute ethanolic fermentation byproduct? you really got a shock coming...and so did a ten mile long, thin streak of pedestrian, on this stuff :D

Don't treat it like alcohol...it ISN'T alcohol, well, only if your a chemist...and speaking from a chemist's viewpoint. Treat it like it was GBL, it is highly potent, very fast acting, wrecks motor coordination, and unlike ethanol you wake up feeling refreshed and full of energy. Thus the potential for significant addictive properties in my view.

And for the sake of completenes, the lack of a disulfiram reaction with the metronidazole does NOT prove that its unable to form an aldehyde in-vivo...I had a fucking awful night not long ago when everything went to hell and back, and 'accidentally' downed a pint. I say accidentally, but more like on purpose, without thinking, I was still taking the antibiotics at the time. No coprine-like reaction, no evidence of flushing, tachycardia, nausea, etc. I thought 'oh fucking SHITE..I've just gone and poisoned myself...just when I thought things could get no worse whatsofuckingever', but I was fine


It is easy to dose, without cyclodextrin, so I really wouldn't bother. I imagine it would mess with the speed of onset, having to be liberated from a substrate. Thats one thing I actually like about it..the way it hits like a freight train. I don't care for ethanol much at all, but I did like GBL (much more so than I did GHB, I think the pharmacokinetic properties play a large role in that, GBL being much more lipophilic, and absorbed faster.)

I just measure it out, tip back, wash down, swear profusely, job done.

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I'm hyperbolic, hypergolic, viral, chiral. So motherfucking twisted my laevo is on the right side.

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Re: 2-methyl-butan-2-ol (and opioids-dihydrocodeine)-testing amylene hydrate
« Reply #4 on: August 30, 2011, 09:34:21 PM »
This stuff sounds ok but its still not within the range of potancy im looking for. EtOH is a great cure for chronic anxiety however it comes with way to many side effects. The loss of motor control is just one of them. I Also dislike the idea of any decent amount of solvent in my body hence the reason im looking for an alcohol replacement. Benzodiazepines are great however there relatively long onset I find lacking. I just wish weed made me feel like it use to  :-\.
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Re: 2-methyl-butan-2-ol (and opioids-dihydrocodeine)-testing amylene hydrate
« Reply #5 on: August 30, 2011, 10:58:13 PM »
Just how potent do you want it to get, sedit? a dose of 5ml to flatten someone....and flatten me it bloody did, they are not going to GET much more potent, for this sort of drug.

As an alcohol replacement, although I haven't tested it, perhaps 1-ethynylcyclohexan-1-ol, production of that is simple enough. I have read reports on bluelight suggesting that it causes alkylation of various hepatic cytochrome pathways. Apparently this is not uncommon in pharmaceutical drugs however.....you better read up on that one before you stick your head straight in there.

As an anxiolytic, needs are different entirely. Alcohol is NOT suited to use as an anxiolytic drug, not at all. A social lubricant in smaller quantities yes, but an anxiolytic agent? no. Ideally an anxiolytic should leave one cleanly functional, and otherwise just sit there in the background doing its thing, and otherwise not even being noticeable. Although some people, after having used benzos, barbs, or whatthehellever else they might have used for that purpose in the past, come to associate anxiolysis with the feeling a GABAergic drug gives them. Without the sloppy, inebriated all over the place sensation they got from benzos, a clean anxiolytic might not be so effective for that subset of users.

Difficult issue to solve in that case.

Depends how much effort you are willing to go to to get it (I.e make it) but the area of investigation I would suggest are subtype-selective GABAa positive modulators. That would deal, I think, with the issue of motor control, and also of being able to target those agents which show less memory impairment.

A subtype-selective partial agonist might be very useful, depends entirely on the patient, for anxiolysis without functional impairment. There are even some mixed subtype selective weak partial inverse agonist/agonists, that are inverse agonists at alpha1 and alpha5 subunits of the GABAa heteropentamer (agonists here result in potent amnestic agents and ataxia) but agonists at other sites. Alpha2 and alpha3 are probably the ones to look for a selective ligand for.

http://en.wikipedia.org/wiki/Bretazenil This one looks interesting. Its been suggested as an alcohol replacement too.

http://en.wikipedia.org/wiki/TP-003 Likely to be very selective, but with all those fluorines on there, might be damned hard to actually make.

http://en.wikipedia.org/wiki/TP-13 Same family, less accidental self-fluorination.

http://en.wikipedia.org/wiki/L-838,417 Another alpha3 subunit-preferring GABAa positive modulator, again a non-benzodiazepine.

Fast onset I think is the key issue here. There are not THAT many compounds with anxiolytic/recreational GABAergic properties with that rapid onset. Most of the ones that are really fast acting, in current use, are fast acting because they are given via injection. Such as etomidate, propofol, the ultrashort-acting thiobarbiturates etc. These are of course not suitable for self-medication, prescription drug or otherwise.

For that incredibly rapid speed of onset, without injection (and thus both increased acute lethality, and also increased susceptibility to addiction to the substance in question, whatever it may be), I see no other option, than a liquid, that is very lipophilic, and has a high degree of potency on a per weight basis. Something with physiochemical properties similar to GBL, amylene hydrate, alcohol, paraldehyde, or something similar to those.

It will have to cross mucous membranes quickly after exposure, and enter the bloodstream quickly, which is where the high weight potency comes in.

One other thing.....from somebody who has dealt with multiple GABAergic dependencies....you can either have anxiolytic or you can have recreational. You cannot have both. Take it, or leave it. That is your choice.
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Re: 2-methyl-butan-2-ol (and opioids-dihydrocodeine)-testing amylene hydrate
« Reply #6 on: August 30, 2011, 11:43:22 PM »
Im looking along the line of drops. If each drop was as strong as a shot so to speak I would be a happy camper.

"Without the sloppy, inebriated all over the place sensation they got from benzos,"

I never got that off of benzos unless they where combined with something. If I am smoking weed my tolerance for benzodiazapines goes into some crazy uncharted territory with no ill effects yet at the same time the antianxiety aspects of it can be felt off of a very small amount of .5 of so from xanax and what not. Not all benzos are any good, only Xanax and Lorazapam have truely shown effectiveness for me the reasons which I don't fully understand.

There are better ways that for some reason are not making it to the market often and that is alpha 2,3 subtype selective GABAa PAMs which is where the anti anxiety effects are modulated. 

Not only that but there are recent advancements being made that show so much promise I am trying not to get myself to excited over them so they are not a let down incase I get to try them. They are in the class of b-Carbolines I believe and they are a2, a3 agonist with antagonist properties at the Alpha 5 receptor causing the EXACT opposite to benzodiazapine memory loss.

I am dying to try Abecarnil  or one of the b-carboline drugs but I even have trouble finding reports online of there use just invitro assays that speak very little about the drugs true flavor so to speak. The only issue I have mostly with them is the fact that many times the indolic nitrogen is left unalkylated and I can't help to wounder if these are only partial agonist due to them antagonizing themselves. The indole Nitogen is needed to bind with the hydrogen acceptor and this alone is what makes antagonist of the GABAa receptor. If they align vertically they are agonist, if they align horizontally they are antagonist due to the hydrogen donator.
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Re: 2-methyl-butan-2-ol (and opioids-dihydrocodeine)-testing amylene hydrate
« Reply #7 on: August 31, 2011, 03:02:53 AM »
'Im looking along the line of drops. If each drop was as strong as a shot so to speak I would be a happy camper'

This would make an awful drug. It would lend itself both to compulsive dosing and to overdosing.
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Re: 2-methyl-butan-2-ol (and opioids-dihydrocodeine)-testing amylene hydrate
« Reply #8 on: August 31, 2011, 04:17:49 AM »
Possibly, I think it has more to do with the reason the person is using in the first place however.

For example anxiety melts away at far below the recreational dosage of EtOH for me. A mere 12 oz of brew could greatly change my life IF it where not for the fact that day time drinking is generally frowned upon so calming my nerves and clearing my mind first thing in the morning is out of the question. Also with EtOH you get primary effects for about 1 hour and then about 24 hours of side effects making it a rather worthless drug. For now insufflation of the increasingly harder to acquire benzodiazapines will have to do but there broad range of activity over the GABAa receptors makes them riddled with unwanted side effects and lowers there therapeutic range.

Another requirement for what Im looking for is a wide therapeutic range which is one of the reasons that GHB is of little value. I would not want to go from happy and relaxed to a stumbling staggering fool just because I decided a tiny tiny bit more would help. Also the fact of needing to make Sodium Nitrite every time I want it would make it impractical.

I know it all sounds like a tall order and it indeed is meaning a highly subselective BZR ligand will need to be found. In the mean time motivation to do so lacks more and more and I would like an alternative in the mean time.

I'm relatively interested in GABA esters and im really curious as to what an ester of amylene hydrate with GABA would produce. Given that the ethyl and mainly octyl ester of GABA have shown to increase brain concentrations of GABA I could only imagine the effects the ester of amyl alcohol would produce as it was cleaved in the brain to make amylene hydrate and GABA.
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Re: 2-methyl-butan-2-ol (and opioids-dihydrocodeine)-testing amylene hydrate
« Reply #9 on: September 01, 2011, 05:08:49 PM »
That is a very interesting idea. I would imagine that the reason GABA doesn't make it into the brain, instead binding only to peripheral receptors, is the polar nature of the the carboxylic acid. Wish I knew just what determines BBB penetrability, I mean, you see the exact same bunch of functional groups on all sorts of drugs and poisons that DO cross, as you see on ones that do not.

Wouldn't surprise me if it did cross though. What it would do once it got there is any bugger's guess.  Probably a real broad-spectrum receptor slut. I have a hunch that the closer one gets to the native, endogenous neurotransmitter with a drug, the more prone to noxious side effects. Look at the increased frequency of side effects such as BP increase, tachycardias, etc. that one sees with 5-position methoxylated tryptamines. Or bufotenine, even better example, although I did not personally dislike bufotenine. Closer to serotonin means likely hitting more of the different receptor subfamilies for that neurotransmitter.

GABA might be different though, being an inhibitory and fairly simple neurotransmitter. Personally I think GABAb agonists feel pretty shitty as far as an excuse for a recreational substance goes. And in general for that matter, GHB being the exception. But I won't touch GHB now, there is a paper out that suggests it may well possess substantial neurotoxicity (excitotoxic damage mediated via glutamate release after stimulation of the excitatory GHB receptor)

You are quite right, a subtype selective GABAa PAM for the benzo-sensitive binding sites is likely your only option. Or possibly a positive modulator binding the loreclezole site. The actives in Valerian bind the loreclezole binding site, and valerian has shown use as a safe, effective anxiolytic (if a bit pongy)

Tried lemon balm tea? easy to obtain the plant, easier still to grow it, and its both calming, very gently sedating and anxiolytic. Harmless also. I've reccomended it to quite a few people lately actually. And it has things in there that modulate cholinergic neurotransmission and apparently, improve the memory. If nothing else though, trying it will produce no ill effects. Tasty too, in fact I think I'm going to go out and pick some to make tea with now before I have a load of cleaning to do (fuelled by desoxypipradrol, perfect to get around to actually doing what needs to be done :D)

If you try the balm, its best fresh, made with boiled, but not boiling water, so as not to volatilize the terpenes and the like that give it flavour.

My SAR predictions for an amylene hydrate GABA ester? I imagine it would likely cross the BBB, amylene hydrate is obviously quite lipophilic in and of itself, I did 5ml out of a 10ml vial as a shot, washed it down with dandelion and burdock, swore profusely, and let it take effect. Later I decided it stung and made my throat sore a little, not much, just a little when drunk as shots, neat, so I tried diluting it with water. Temperature of the water used was not taken...just tap water, neither very hot, nor very cold. The amylene hydrate floated on the surface, like chloroform in reverse.

Vigorous shaking did temporarily make a cloudy, pale suspension, but this quickly resolved into a bilayer again. It feels like spirits on the skin, yet its oily in character...sort of like ether...which it smells and tastes like. That is, if I GOT amylene hydrate, and not either ether or THF. I wouldn't like to think that I have been drinking shots of THF :P

Shite.....it just occurred to me to test the flammability of the substance. All 40ml have been consumed, but, there are dregs left in the vials. I just ignited a match, and after capping a vial with my thumb for a few moments, brought the match closer. Result was a flash thats much more forceful than ignition of an aq. EtOH solution. I suspect that either amylene hydrate has a very low flash point, and a volatility uncharacteristic of both its molecular weight, and bulk or I got fucked by the company sending it me.

I'm going to go look up the flash point of t-pentanol. My sample, that this report is based on, does NOT smell mintlike, or even close. It smells exactly like either EtOEt or THF. And the intoxication it produces at a 5-10ml dose is similar in character to oral administration of either diethyl or diisopropyl ether. Definate NMDA antagonist signature to it, so has EtOH though, just not so pronounced.

It should be born in mind, that if this is indeed tert-pentanol, then it is very, very flammable. Smoke around this stuff, or after a spill of more than mililiter aliquots, and your face is going to come off in pieces.

Its the lack of any mint-like smell, instead having a distinct and strong etherial odour that makes me wonder. From weighing the stuff out into the vial caps using a pipette, a weight of ROUGHLY 800mg/ml seems about correct, but the weight of diethyl ether is very close, 0.713g/ml and that of THF is a little higher. I do not believe my sample to be THF though. Not sure what THF tastes like, but its known to be miscible in H2O.

So....It COULD be ether, that I have, but it doesn't seem as volatile. Flash points are too low for both substances to give much of an indication. It wouldn't have occurred to me, having always got good service (not to discuss specific vendors or sources) from where it came from, an RC type business rather than a chemical supply business. Only their email inbox is full, phone appears dead, not tried the mobile line they have listed yet though, and something that should have come with the same order, didn't.

Ahh..well...if they turn out to have screwed me...I will screw them by reversing the payment entirely, for all items :P

So an ester of the stuff with GABA....I have mixed feelings about its subjective effects. I wonder if it would possess a muscimol-like effect. Muscimol binds the GABA binding site on the GABAa receptor (also its quite a potent agonist for the GABAc/GABAa-rho receptors, but I am completely ignorant, I must say, of the role they play in the CNS...it is known they have a significant degree of expression within the eye however) With it not being possible to get large quantities of GABA past the BBB, and also, with the existence of active transporters and catabolic enzymes with the capability to clear out any GABA administered by injection bloody quickly (an injection which anyway would be localised, and thus hit a single, or at least very restricted range of targets within the brain) it would be interesting to see what sorts of effects DO happen with the administration of tert-pentyl gamma-aminobutyrate. A systemically deliverable, continuously releasing source of GABA itself....that would be interesting.

I've long wanted to try other orthosteric agonists for the GABAa receptor for the GABA binding site. I like muscimol and find it useful enough to go out every fly agaric season and rake in as large a harvest as I can from a place that usually produces quite a lot of them. Only seen one this year though, luckily I have some dried from the previous year, if I find no more. Gaboxadol looked interesting...but apparently one company purporting to sell it, I don't know which, somebody bought some, and luckily, had analytical capability, because it turned out to be fucking ibotenic acid!

On that tangent...a new idea, as far as potential anxiolytics go...small doses of fly agaric. SMALL doses, not psychedelic, or dream/trance state inducing doses, that might just be one to consider. Its got very different properties in low doses to the classical dissociative/euphoriant/inebriant effect usually sought. And it appears to completely kill the ability to fear.

After taking it to help me resist the winter, I don't think I would be afraid enough to back down if a well-built, well trained kickboxer started a fight with me. Chances are I would run like hell if my own martial arts training wasn't enough, but it would be common sense that was motivating me to do a runner, not fear.

I bet something like isonipecotic acid, or isoguvacine might make a decent potential therapeutic for evaluation. Those are the two areas at least, in terms of GABAergic agents, which I think have promise, either highly subtype-selective benzo-site binding positive modulators, or direct GABA-site orthosteric agonists.

Fly agaric is certainly obtainable. I'm contemplating having some of my dried ones now in tea, then going out to search for more for a meal (yes, prepared right they are also good for food, but they have to be prepared carefully, if one doesn't want a big surprise)

Other potential ideas.....serotonergic agents. 5HT1a agonists are both strongly anxiolytic and apparently, very potently analgesic. 5HT2c agonists are anxiogenic, and inducers of migraines, so it stands to reason, that an antagonist might well do the opposite, and chances are, without the potential for a very serioues and nasty withdrawal syndrome that the GABA modulators have (muscimol seems to be very little prone to this however).

I think a serotonergic drug might be safer in the long run, certainly safer than a benzo and DEFINATELY more so than alcohol (including, I imagine, amylene hydrate), there is also that mitochondrial translocation pore thingy to think about as a target. Or all sorts of various neuropeptides. I wouldn't limit your horizons to just GABA as a neurotransmitter.
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Re: 2-methyl-butan-2-ol (and opioids-dihydrocodeine)-testing amylene hydrate
« Reply #10 on: September 02, 2011, 02:14:57 AM »
Short on time will read later,,,,


Look at this deity,

Picamilon the Niacin GABA amide. This is the future of direct GABA manipulation. iImagine GHB in place of GABA here. you would get B3 which is a BZ-PAM with very lsight afinity in itself and GHB as the main products formed.

Sorry so shot rides hee.
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Re: 2-methyl-butan-2-ol (and opioids-dihydrocodeine)-testing amylene hydrate
« Reply #11 on: September 02, 2011, 08:55:22 PM »
Quote
That is a very interesting idea. I would imagine that the reason GABA doesn't make it into the brain, instead binding only to peripheral receptors, is the polar nature of the the carboxylic acid. Wish I knew just what determines BBB penetrability, I mean, you see the exact same bunch of functional groups on all sorts of drugs and poisons that DO cross, as you see on ones that do not.


Its got a lot to do with polarity but you got to understand that just because it has this or that functional group it does not so much mean its polar or non polar. Also many substances cross the BBB because the are taken up by the active transporter enzymes used by endogenous substances meaning some things that normally would not make it there will because they are carried there by specific proteins.

I would like to share this little piece of gold that I am going to give its own thread too when I get a chance. You will not be disappointing as its a great patent.
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Re: 2-methyl-butan-2-ol (and opioids-dihydrocodeine)-testing amylene hydrate
« Reply #12 on: September 03, 2011, 07:37:08 PM »
Yes I am aware of that. I know of active transport/efflux. Makes the most sense, amongst the huge variety of active drugs/poisons/inactive yet BBB penetrant compounds, that the aminoacids, or some of them will cross. Being essential for protein synthesis for one, neurotransmitter precursors such as tryptophan*

With active transport and efflux to consider, BBB penetrance predictability presumably, for a substrate without detailed studies of a given substrate, or at least studies of the SAR of some chemically similar relatives or the existence of a isosteric molecule, becomes much more difficult.

And always, there have to be a few curveballs thrown in, like for instance, the brain having a load of wiring in place to rapidly remove excess glutamate, and prevent excitotoxicity from exogenous dietary glutamate, whilst generating it for use within the CNS, my reading that contrary to my expections, and some other peoples similar opinion as to what would be the case, the excitotoxin ibotenic acid not only crosses but apparently does so by being actively transported if taken systemically. 

*Starting on topic, going off on an off topic tangent, at least, certainly regarding my OP at least...
(with 5-OH-tryptophan having vastly lesser ability to cross compared, from what i read, to tryptophan itself, so even when an active transporter system is present it appears that a close structural derivative of an aminoacid essential for normal natural neurologic function, when rendered significantly more polar by the derivatization being in the guise of the 5-OH, as is paralleled, it seems, by the differences between bufotenine, and 5HT amongst the amines, although there are in that case other complex interactions between secondary, tertiary significant biological and chemical factors, for instance, MAO-a and logically intuiting that whilst an n,n-dimethylated tryptamine that is otherwise simple structurally and in relationship to the corresponding 5-OH-T homolog that MAO-a is pretty much designed specifically, along with a couple of other neurotransmitters and common exogenous pressor thingies like tyramine and the like to chew up and spit right out again, it wouldn't surprise me, if it were the case, given that extending one amino substituent of an tert. tryptamine* )

I have long been curious to know, of why serotonin itself doesn't pass the BBB, MAO aside, while tryptamine itself, if given IV to enable it living long enough to reach the brain although extremely short lived is psychedelic, or presumably to a greater extent/life with a MAOI (safety of this in practise would have to be very carefully assessed of course if to be done in an animal or a human) certainly does, bufotenine does, and the fairly dramatic differences seen when comparing psilocin, etc. The relationship, in short, between BBB penetration of structurally close, MAO-substrate, hydroxytryptamines orally active and orally inactive but very active when not so orally when given IV, with parenteral 5HT (rather, lack thereof, removing the possibility of active transport)

Would be useful and interesting to know what sort of factors govern, active transport aside BBB permeability of compounds. Polarity obviously, but what figures specifically likely grant or likely deny entry, logP value I know has something to do with it, but what there tips the balance towards either result, and what other than polarity, active transporter system existing are involved? I specifically am not counting the existence of enzymatic systems being present that, like the case of MAO-a and DMT, unless given via a non-oral route, inactivate a drug before it ever has a chance to get to the brain, things like that example, the extremely microscopically short half life of adenosine (for chemical cardioversion where its appropriate as the agent chosen for use, it is torn to pieces so quickly, that it has to be given either  via bolus as close to the circulation reaching the heart as possible, or via a rapid intraosseous push!) 

*A tertiary amine, being pretty much requisite for activity as a psychedelic in a tryptamine, with notable exceptions being alpha-alkyl tryptamines, in which case a primary amine is quite active both as an entactogenic agent following with the close structural similarities to amphetamine, MDMA, and the main two other monoamine neurotransmitters, and resultant properties as a monoamine release agent, yet is definately also active as a psychedelic (can confirm that one personally...interestingly, MDxx seems really shallow, hollow and indeed enough so to make me pretty uncomfortable with the changes in emotive processing and....*cough..gag..evacuate stomach contents in both vertical directions..choke on tongue...turn blue, push up a few daisies and feed a host of worms, bacteria, insect life, fungi and probably a few larger carnivores* pro-social interactive drive existing temporarily.

AMT has a great deal of similarity to MDxx in my personal experience of AMT, MDMA and beta-C=O-MDMA, as well as the more obvious psychedelics sensu stricto, yet thus far, more emotional depth than other tryptamines ever tested have, with the exceptions of individual experiences, recurrent on a given substance or not,  and and at the same time, changing my normal lack of value for spontaneous, or seeking out social interactions, whilst in common with the other entactogens tried, and found wanting, it still does not make me NEED to interact in any way with other people.

What I don't get there, I really do not, is exactly what the reason is that while it comes across as very plainly obvious to me that I am completely comfortable with who I am psychologically, and more than just comfortable, but very pleased by exactly what it is, that is one of the defining things about my neurological and resultant psychological wiring thats played a large part in shaping that. Quite literally, I would, if not for the case that I wouldn't be able to know what I was missing out on, be pretty fucking well horrified it I wasn't autie.

 And that, is certainly what makes me uncomfortable with MDMA, not why I find it emotionally shallow I don't think, but the pro-social properties very much so, with them feeling forced into being by artifice, and not a part of who and what I am, yet in the case of AMT...that same property feels subjectively as though it is simply activating something that has always been there, but whilst used without the influence of any psychotropic agent at all sometimes has never been needed, or something that would be missed if having made use of voluntary interaction, forming a friendship, I suddenly no longer had it.

Shows how subtle and complex the interplay of various factors in both a subjects basic biology, the physical and biological chemistry of an exogenous bioactive compound, and where relevant, neurology and psychological factors gets...and how little, in some cases, especially concerning the aim towards a grand, unified theory of psychedelic action are.

Bloody hell, as if, having spent several 12 hour stretches of intensive research  journal studying, requesting, medical questioning of someone should I not know that much full well, seeing how detailed a set of information must be, to be of value, when aimed towards with the combination of a pretty rare mitochondrial encephalomyopathy, epilepsy, a whole bloody bunch of meds, some really funky unique neuroendocrine idiosyncrasies and Rett syndrome (an autism spectrum variant, although much less common than the others, attended with other medical issues that is unusual in both having a known single gene cause and being universally embryonic lethal in a male with the condition, or not long post birth with the exception of YX(Xn) karyotype males), to help track down everything I can about the neurological, hormonal and metabolic profile of the individual given a thorough grounding in everything she knows (and thanks to extensive and pretty detailed medical DX and treatment history, coupled with a very good understanding of neurology, endocrinology, MRI-interpretation and the like on their part and pretty much brilliant intellect in general

Ideas and theories can be easily evolved together, when helping the person have available enough information about every even possibly significant factor for them to be able to make an informed choice about weather their testing of a psychedelic compound is possible, when carefully titrating from doses certain to be subclinical in all its details, can be done with responsible safety, given the strong chance that there is potential for some very majorly significant beneficial results if done right.....complicated....don't I fucking well know it! Makes the likes of active transport/efflux into/out of the BBB, thinking about it, seem like I should have been taught how to think in such a way before I was 5 by someone else as part of an early education curriculum rather than autodidactic learning in comparison :P

I'm pretty well read all round, epecially when it comes to biology/pharmacology/toxicology, as well as various natural history disciplines, I always find, when I learn something new worth knowing, either out of use, interest, or both, that getting an answer to a question is good, learning HOW to answer a question is much, much more useful, and that either of the two mean a legion of other ones that need to be figured out (and for that matter, that trying to figure them out, or finding out why nobody has a ghost of a clue on the matter in question still turns up a whole bunch of entirely new areas of interest)

Makes me think, that despite human brains basically being very complex, multistate logic processing organic computers, that if ever a sentient computer were made (and I've seen enough sci-fi movies to realise that I want to be nowhere near if that ever succeeds:D), with the speed of automated calculation available even today, it must surely result in the first ever denial of service suicide, at least if it happens to have an enquiring, or faster yet, if it happens to have a autie/aspie processor it might just DOS itself with the BIOS boot sequence with the tendency to flit from chain of thought to chain of thought and back as fast as they usually do)
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