Irreversible u-opioid agonists

[resorcinol]

Drugs like this are just fascinating. This is one of them --

http://upload.wikimedia.org/wikipedia/en/thumb/f/f1/Oxymorphazone.png/240px-Oxymorphazone.png
oxymorphazone

It's about 1/2 the potency of oxymorphone, and is a full agonist. What's unique about it is how it binds to the receptors.

Almost all opioids, and almost all psychoactive drugs in general, form easily reversible bonds with their target receptor. Coordinate covalent bonds, hydrophobic interactions, dipole dipole interactions, etc. Even very potent opioids like fentanyls form reversible bonds with the u receptor.

Oxymorphazone is something I would never take no matter how sick I was.

Oxymorphazone forms a full on covalent bond with the mu opioid receptor. This bond CANNOT BE REVERSED. I don't care how powerful of an antagonist you have, you can never unseat this agonist from the receptor. The body has to internalize and destroy the receptor and make new ones to end the effects of this drug. The very idea of this happening makes me nervous. It's akin to what Nardil and Parnate do to MAO... although with MAO I don't get as nervous, it's an enzyme that the body has been show to easily remake in a few weeks. Mu opioid receptors are not something I'm comfortable with permanently altering, I guess, even if new ones will be made.

The scariest thing of all... when the nitrogen is substituted with an allyl group ala naloxone, guess what you get....

an irreversible ANTAGONIST. That's horrifying to even think about... I really hope the horrid possibilities there never emerge in the minds of the prohibitionists. Precipitated w/d that no amount of heroin could ever stop... that no amount of ETORPHINE or CARFENTANIL could ever stop! And who knows how long it would take the body to create new functional mu receptors to a degree that would allow for happiness again or to get high again.

[pharmboy]

The shit makes me nervouse too what with our sick ass government.

[EleusisII]

Sweet Jesus!

I got's to get me some of that!
So basically, you'd be permanent high?

How hard is this to synthesize? ;)

It doesn kinda sound like one of those super-evil drugs that they sometimes have in sci-fi movies (And which usually threatens to topple society and make people insane).

[resorcinol]

Lasts about 48 hours.... the body destroys the receptors and makes new ones to end the effects. So no, unfortunately no perma opioid high. Hell, a perma high might ruin the fun of it.

What scares me is that these drugs (whether agonist or *shudders* antagonist) ruin the mu receptor they bind to. The body should make new ones, but idk how perfectly my body would execute the process. Might take a long-ish time to go completely back to the way it was before taking the drug.

[Narkotikon]

an irreversible ANTAGONIST. That's horrifying to even think about... I really hope the horrid possibilities there never emerge in the minds of the prohibitionists. Precipitated w/d that no amount of heroin could ever stop... that no amount of ETORPHINE or CARFENTANIL could ever stop! And who knows how long it would take the body to create new functional mu receptors to a degree that would allow for happiness again or to get high again.

That is really scary, especially considering what they sometimes do in the penal system. I was watching some kind of documentary a year or so ago, about addicts in prison, and I remember some of the opiate / heroin addicts in there (who were caught using repeatedly in the prison) were implanted with a Revia / naltrexone pellet. I mean, they weren't given a choice. It was forced upon them. And it was implanted, so it couldn't be easily removed. That's fucked up. I have no idea how they get away with that. I mean, people have the right to refuse any medication when in a psych setting, maybe it's different in prisons. I'm not sure. But I thought that was scary in itself. So, yeah, it wouldn't surprise me if they tried to pass a law mandating this someday. If they ever did, I certainly wouldn't be staying around. I'd be on the first flight to Canada or Europe I could find.

Also, what exactly are the point of these drugs? I'm assuming that these aren't actually used as medicines, but rather drugs that scientists just come across while working in labs, and they get cataloged. I mean, I can't see this being useful as a medication. How do you find out about these?

[resorcinol]

I think they find these when they do studies on SAR (Structure Activity Relationships) of drugs. They're most likely just the product of academic interest. Lets hope it stays that way. The potential for governmental abuse of irreversable mu antagonists is really high.

I'm always on the lookout for new opioids. Journal articles, google searches, wikipedia, all great resources.

I'm particularly enamored with substitution of the 14 position of phenanthrene core opioids (morphine-like structured opioids). It seems to confer greater potency (confirmed) without dilution of euphoria or overly heavy sedation. Oxycodone is the common example.

[Armegeddon73]

In lay-man's terms...? Thanks. Peace.
ARM

[Hoss]

The potential for governmental abuse of irreversable mu antagonists is really high.

:mad: Dammit.

I'm always on the lookout for new opioids. Journal articles, google searches, wikipedia, all great resources.

Thank you Res!

I'm particularly enamored with substitution of the 14 position of phenanthrene core opioids (morphine-like structured opioids). It seems to confer greater potency (confirmed) without dilution of euphoria or overly heavy sedation. Oxycodone is the common example.

Ahh yes... :: DROOL :: for the possible possibilities ;)