Pharmacology - Oxymorphazone - an "irreversible" opiate agonist.

[Dickon]

I just used the fucking search engine, and found that the only reference to oxymorphazone on DF were my own. It was an interesting "find" on wiki, so I thought I'd start a thread to bring it to the attention of others here, and perhaps accumulate some information.

Originally Posted by wiki: links removed

Oxymorphazone is an opioid analgesic drug related to oxymorphone. Oxymorphazone is a potent and long acting μ-opioid agonist which binds irreversibly to the receptor, forming a covalent bond which prevents it from detaching once bound. This gives it an unusual pharmacological profile, and while oxymorphazone is only around half the potency of oxymorphone, with higher doses the analgesic effect becomes extremely long lasting, with a duration of up to 48 hours. However with repeated doses, tolerance to the effects develops rapidly, as chronically activated opioid receptors are rapidly internalised by β-arrestins, in a similar manner as occurs with non-covalent binding by agonists with extremely high binding affinity such as lofentanil.

As if that isn't enough there also exist chlornalrexamine, an irreversible mixed agonist-antagonist and naloxamine an irreversible μ-opioid antagonist. That's something to threaten a junky with if he's giving you gyp!

I wonder how euphoric and/or addictive this might be. Any further information would be useful. If I have time I'll chase up the links from wiki at some point. I'd be curious if the stuff was easy to synthesise.

Dickon