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nor-Binaltorphimine: K-Opioid receptor antagonist


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#1 Spectre

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Posted 29 April 2011 - 04:27 AM


Hey guys,

is anyone on here familiar with the research chemical "nor-Binaltorphimine"? It's a kappa opioid receptor antagonist and I'm interested in finding out more information (mainly the safety of use), and possibly using it to improve symptoms of my memory dysfunction brought on by dextromethorphan and salvinorin. Sulbutiamine has helped me quite a bit but I'm still not 100%. Both dxm and salvia are kappa opioid receptor agonists and I personally attest that the k opioid receptor activation is what caused my deja-vu/memory impairment (the way my brain interprets and forms memories is abnormal). I don't have access to a reputable neurologist so I doubt I could find a doctor that would be willing to try me out on this stuff, I doubt they would even know what it is in the first place. Does anyone here have knowledge or experience with this chemical? If this is safe I would be EXTREMELY interested in finding out how to obtain a very small amount to test on myself..risky, of course..but if this chemical could completely reverse the memory impairment I'm experiencing I think this would be a remarkable discovery and would lead to some great research in the field of psychopharmacology. So far the only sources I have found sell a minimum of 10mg per order (which is about $110-$150..I don't need that much, this stuff is active in the mcg range). Thanks for any input.

http://en.wikipedia....binaltorphimine

Norbinaltorphimine (nor-BNI) is an opioid antagonist used in scientific research. It is one of the few opioid antagonists available that is highly selective for the κ-opioid receptor, and blocks this receptor without affecting the μ- or δ-opioid receptors,[1] although it has less selectivity in vivo than when used in isolated tissues.[2] nor-BNI blocks the effects of kappa agonists in animal models,[3][4] and produces antidepressant effects.[5]


I'm also interested in JDTic, which is another selective kappa opioid receptor antagonist. If anyone has any in-depth knowledge or experience with these chemicals please let me know, thanks for any input.

http://en.wikipedia.org/wiki/JDTic

JDTic is a drug that acts as an opioid antagonist, which is highly selective for the κ-opioid receptor, and blocks this receptor without affecting the μ- or δ-opioid receptors.[1] It is a 4-phenylpiperidine derivative, distantly structurally related to analgesic drugs such as meperidine and ketobemidone, and more closely to the mu opioid antagonist alvimopan, and is structurally distinct from other kappa antagonists such as norbinaltorphimine.[2][3] It has a very long duration of action, with effects in animals seen for up to several weeks after administration of a single dose,[4] although its binding to the kappa opioid receptor is not irreversible and its long-acting effects are instead caused by altered activity of c-Jun N-terminal kinases.[5] Animal studies suggest that it may produce antidepressant and anxiolytic effects,[6] as well as having possible application in the treatment of addiction to cocaine and morphine.[7][8]


Edited by Spectre, 29 April 2011 - 04:36 AM.


#2 jadamgo

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Posted 29 April 2011 - 05:59 PM

It's fascinating -- I was just reading about this stuff a week ago. But unfortunately, it seems to only be available from chemical suppliers like the one you mentioned.

Do some research into other K-opioid antagonists. There are some currently available drugs that might do the trick, but watch out for the ones that have activity at the other opioid receptors as they can, of course, be habit forming. If you take one of those, take it at doses without noticeable mu- or delta-opioid effects. Ignore that suggestion at your own risk.

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#3 tdmonster99

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Posted 30 April 2011 - 02:08 AM

I too am also extremely interested in the kappa opioid receptor antagonists, especially nor-BNI. I believe I have a thread on here and Mind and Muscle about chronic depersonalization/derealization induced by an experience with DMT. Naltrexone has had some studies showing efficacy in treating DP/DR and it seems to be KOR antagonism that yields the therapeutic effects. My trial with naltrexone yielded some positive effects but the side effects such as sedation made me stop. The strict KOR antagonism of nor-BNI should potentially minimize side effects and maximize therapeutic potential.

I was able to find a supplier offering 10mg for about $77, maybe all those interested could do a bulk buy or something and distribute amongst or selves. But until then I'm very curious to see if anyone has personal experiences with KOR antagonists.




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