Would eating mannitol before injecting or snorting the deschloro lope help? 
I've read that ~15 minutes after ingestion mannitol "opens" your blood brain barrier.

   I was strolling the internet the other day (surfing is just too energetic at times!) and I tripped over a few more interesting asides about oxycodone and its sibling naltrexone.

  It's one truly extraordinary example of how just a couple of atoms, tw0 oxygen and a few more hydrogen atoms in this particular case, can change a substance from a full agonist into a full antagonist!

 And howz this for nifty marketing  http://en.wikipedia.org/wiki/Targin 

A combination of the two, apparently the naltrexone (apparently!) helps stop the constipation caused by the oxycodone!

I wish they'd let me be this smart!  I want a pharmaceutical firm!

Please check out attached drawing...

1. Deschloro
2. alcoholysis with ethanol and sulfuric (which will require reflux for a long period of time to go, if at all.  Otherwise, triflic anhydride and pyridine added at -40° C, then ethanol- not as much fun)
3 Propionyl halide or anhydride, your preference.

BTW Lop HCl and it's HCl derivatives will prefer to go into DCM over water in an extraction (just like fentanyl).

Thanks a bunch!

I'm still trying to get this working.  Jon's apparently worked out the art of getting high off of lope, but I'm not very gifted when it comes to chemistry.  Just reading this site is about the learning equivalent of chem 101 though. 

this might get some sort of offtopic, but i would like to know if you dont ever experience side effects like depressive mood or else? Ive read somewhere about such effects from a person using plain naltrexone oral dosed for about 1 week and it felt according to that report like every natural endorphine induced mood simply is total surpressed, the first day without the antagonist felt on the other hand very good, the writer assumed because the long term endorphin depletion is gone sudden logically

dopeamine really came through on this joint venture i'd say pain killing drugs can be very helpful

Well, options are always nice.  Personally, I would prefer the CTH method that I posted at the top of the page, but certainly if you don't have Pd/C and you do have all of the above mentioned chems then that's another option. 

I made the deschloropropionyl-loperamide.  I believe at the time that I tried it I had a helluva tolerance to methadone so I think that explains why it didn't do a whole lot for me.  Also, dissolving a portion of my product in propylene glycol was a big mistake because it tastes HORRIBLE.  I would gag trying to choke that down.  Taking a measured mini-spoonful was much easier to get past the tongue and wash down but really putting it in capsules would be the best way to go.  I still plan on trying the 1,2,3 with 2 being the new modification of ethanolysis if deschloroloperamide but I've got higher priorities at the moment.  I'm finally no longer burned out from work and #1 is doing that cyclopropane ring opening of naltrexone (CTH once again) followed by adding a cinnamoyl group at the 14-OH position (assuming I am successful in making the cinnamic anhydride).

Thank you for that point about 14-cinnamoyl ester of naltrexone.  I actually goofed.  I meant to say hydrocinnamoyl.  I am very concerned about taking any sort of partial agonist/antagonist, so that is why I planned to first split open that cyclopropane ring via CTH.  Converting that N-cyclopropylmethyl into N-isobutyl makes a material which is supposedly roughly equal to morphine.  Then, I was hoping to make hydrocinnamic anhydride using hydrocinnamic acid and acetic anhydride (distilling off acetic acid), and finally reacting this to make the 14-hydrocinnamoyl ester. 

I was able to run this molecule in Chemdraw 3-D and get that aromatic ring perpendicular to and slightly below ring A after minimizing energy, which is supposed to be the ideal orientation for an agonist.  I can see how the 7,8 double bond could direct the orientation of the electron rich carbonyl group away in 14-cinnamoyl, thus helping to force the restricted chain downward, but the hydrocinnamoyl should have much better rotational freedom in order to attain the desired orientation, regardless of the orientation of the carbony group.  The idea was that while 14-phenylpropoxy is ideal, it's a bitch to make and the hydrocinnamoyl will hopefully be close enough.  But, due to my fear of there being any unreacted material after the esterification, the plan was to open up that cyclopropane ring first to make doubly sure that it will be an agonist.

As for your question regarding potency, I would say that 100 mg of propionyldeschloroloperamide wasn't all that thrilling.  It did keep withdrawal symptoms at bay but gave no euphoria.  At the time that I was trying it, I had a tolerance to methadone which may have affected the qualitative affects.  I have found that methadone-type opioids and morphinan-type opioids seem to have separate tolerances.  If I do not take methadone for a month, then 40 mg will be quite pleasant for the initial few days, regardless of how much my heroin intake has been.   Similarly, if I take a week or two off from heroin and only use methadone, then when I use heroin again I will experience euphoria for the first few days which had been previously lacking.  So, maybe there would be some euphoria experienced if propionyldeschloroloperamide were taken, but I've been taking methadone again recently so I wouldn't be able to conclusively answer that.  Either way, I think this molecule needs more/different modifications in order to be worth the trouble.  Hence why I suggested alcoholysis with ethanol to get rid of that damn amide group, which is likely causing so much of  the inactivity due to P-gp transport.

indeed the amide group facilitates peptide bonding with PGP just like any other amide would form h bonds with a protien.  i think the problem is that the 3 rings are equatorial to one another unable to adopt that perpindicular orientation the potency can't rise to the level of super opiods.  i looked at the model for hydrocinnamyl naltrexone and it's actually about 80 degrees in relation to ring A.  the phenyl propyl ring that is i still think that were in the right ballpark for agonist activity with that ester after modeling it umpteenth times. a little naltrexone won't hurt things i mixed microgram quantities up with the big H and found that it reversed tolerance. so if this stuff is orders of magnitude of potency related to morphine the small dose of residual naltrexone will actually reverse  tolerance. it's been my experience it does all the way up to 1 mg then it starts to act like an antagonist i mixed up probably less than 100 mcg with .25 gram smack and the results were astonishing. people with tolerance would have to do the whole bit to get high after adding , mcg quantities of naltrexone they got to nodding off just 1/4 th of that amount you should really try it the only way to fuck it up is to go over 1 milligram. but 5 dollars getting someone with a  hell of a tolerance to nod out, convinced me it works like advertised. if you don't believe me just look up ultra low dose naltrexone.  i'm thinking you've been on methadone so long it strongly binds to mu receptors and it's crowding out other opiods you try so you may want to think about switching to heroin then try the des chloro ester.it can be very potent just the fun wears off real quick. tachyphylaxis is what it's called. it gets boring fast but a nice fall back opiate.   anyway thanks dopeamine for concluding this research with loperamide i'm glad you made the effort (with a little assistance from yours truly) i found i could handle up to 400 mg/day of the plain ester it did'nt have the calcium channel blocking properties that loperamide has at that dose. that was over the course of a day i've done 1/2 gram heroin or more in a single day so you can't  say it is all that bad.

to answer your question about pinacol borohydride there are methods for removing halogens from aromatic rings galore (why it took me so long to narrow it down to pd/c) it's given in the literature this is the best way and a little more research indicates CTH under certain conditions is even more convenient and higher yeilding also so i would'nt go on any wild goose chases when we know what works.

yep it's a miracle to the high tolerance junkie it allows them to escape spending more and more on heroin when they can just adjust tolerance.
i think there is an on off interaction of antagonist ultra low dose that allows for virgin tolerances to be had
5 mcg's is what you strive for 1-5 micrograms.

Hey guys.  I have to make an apology.  I was wrong about that deschloropropionyl-Lop!  I think I just hadn't been taking enough. Previously I had been alternating between heroin (.5 g black tar- sadly) and methadone (40-50 mg) every coupla days or so.  Then I decided to give the DCP-Lop another try.  So in the evening I packed a #4 gelcap with ~100-125 mg of some of the remaining material which I hadn't dissolved in propylene glycol.  I woke up the next morning feeling pretty damn good.  But as with other methadone-type drugs, ya really got to allow for it to build in your system, so I took another gelcap of roughly the same amount (not sure what time), and other gelcaps followed.  I can't really say what the dosage schedule went like and it doesn't really matter.  What is of significance is that, just like methadone, after about 48-72 hrs the fun dropped off to basically unnoticeable plus I was getting down to last scrapings of the flask.    But, I can tell you that while I was at the peak of it I had moments where I had to close one eye in order to be able to focus on stuff.   

So, I dunno whether there is a cross tolerance between DCP-Lop and methadone and I just overwhelmed it by taking a much larger dose or whether this is just the dosage needed for an opiate lover like myself (I tend to have a higher tolerance than others even if I've gone a month or more without).  Given that the patent states that the deschloro-Lop is half the strength of morphine and we don't know what increase the propionyl ester brings to the table, maybe this dosage is just about what it ought to be.  Here's the Borohydride discussion which led us down this path: http://forum.opiophile.org/archive/index.php/t-34565.html?s=1170095548a680afaca8870c1283fddd  I really wanna talk to that dude or at least get him over onto this site.  I have mad respect for his knowledge and creativity when it comes to opioids (Piglet too). 

So, to sum up I believe that CTH dehalogenation followed by esterification with propionyl bromide is a viable route to some decent material.  I really wonder what would happen if one were to insert ethanolysis of the dimethylamide in between the two reactions.  Kinda depends on whether you look at it as a pethidine or a methadone analog. Boro would seem to disagree: "the dimethylamide was the only other moiety other than pyrrolidinyl that gave good activity in the moramide skeleton".   But, who knows whether his information factors in the P-gp transport issue.  It's too bad that there isn't an easy way to add a beta alkyl group on the ethyl as that definitely would make things a lot more fun!

One last note:  Do not put this material in propylene glycol.  I did this in the hopes of inhibiting P-gp as well as improving oral absorption http://www.aapsj.org/abstracts/AM_2005/AAPS2005-003075.pdf.  The problem is that it tastes so goddamn awful that I would almost puke if that shit hit my tongue!  Powder in a capsule is the way to go.  The HCl salt seemed to work fine but maybe the citrate or some other would be better.  (Like fentanyl HCl, DCP-Lop HCl is non-polar to the extent that it will preferentially go into DCM over water.  The solution I used for making aqueous fentanyl HCl was using an ultrasonic bath.)

Jon: Great to hear from ya!  I wanted to reply to your message but it seems that I'm blocked from being able to message you.  Could ya look into that?  I would love to chat with you again.