N&PD Moderators: Skorpio
Is anything known about the pharmacology of Thebaine?
JackiesBabyy
Bluelighter
I know it's a poison and causes death on its own but I've also heard thebaine is sitmulating rather than sedating like the morphine/codeine in the opium, and that oxycodone is stimulating because it's derived from thebaine.
endotropic
Bluelight Crew
I don't know much about this compound but your question got me curious so I ran a few searches. I wasn't able to find much about mechanisms except that it's a mu partial agonist with micromolar affinity:
http://www.ncbi.nlm.nih.gov/pubmed/17616524
The convulsive action makes me think delta agonism but I can't find any evidence for or against that. It also seems to be weakly rewarding (not surprising), and doesn't precipitate opiate withdrawals.
http://www.ncbi.nlm.nih.gov/pubmed/7255516
JackiesBabyy
Bluelighter
Hmm, so could a sub-convulsive dose be recreational if you were able to get your hands on pure thebaine? (For the love of god don't lecture me, I'm not actually going to try this.)
sekio
Bluelight Crew
I was under the impression that thebaine shares the same mode of toxicity with e.g. acetylcodeine, that is, it releases histamine from mast cells and can cause anaphylactic or seizure-like activity.
JackiesBabyy
Bluelighter
So (dumb question) how come you don't hear of people smoking opium, seizing out and suffocating. Is this because they find a way to take thebaine out or would you die of morphine OD before the thebaine could cause that?
sekio
Bluelight Crew
There's not enough thebaine in typical narcotic opium - it's generally less than 5%.
JackiesBabyy
Bluelighter
Interesting, I still wonder what a low dose of (subconvulsive) thebaine would feel, it must provide somewhat of a mood lift seeing as how it's "rewarding".
endotropic
Bluelight Crew
Can anyone find a source for Thebaine's action at sites other than mu? My searches have turned up nothing.
Limpet_Chicken
Bluelighter
http://www.sciencedirect.com/science/article/pii/0306449279901382
This appears to confirm my suspicions-that its an antagonist at strychnine-sensitive glycine receptors. Appears not to be too specific or important in binding to GABAa (lack of interaction with bicuculline and picrotoxin)
I'd imagine it easiest to look at accounts of the (now old fashioned in the extreme) use of strychnine as a stimulant to get an idea about the subjective effects of isolated thebaine.
I thought that it's action is more like strychnine.
Opium is much more stimulating than morphine, might be the thebaine. I think when opium's smoked all the thebaine vaporizes, but only half the morphine does. The morphine stays trapped in the dross.
Thebaine also counteracts some of the respiratory depression of morphine, especially mixed with narcotine.
Supposedly strychnine not that bad in very low doses, but god what a horrible way to go in an OD. I've wondered if that's the reason strychnine's put in #3 heroin, to give a more opium-like high for former hopheads.
Limpet_Chicken said:
nabollocks
Bluelighter
P A
Bluelighter
But if thebaine's bioavailability is roughly equivalent to that of morphine or codeine, opium smokers would be seizing left and right. Morphine is found in variable concentrations in dry samples, but unless you're getting primo-quality dope, the morphine-thebaine ratio doesn't seem high enough to guarantee safety (if thebaine is indeed as potent a convulsant as is being claimed). Unless morphine's anticonvulsant properties are fortuitously compensating for the untoward effects of the thebaine, I'm not sure how to account for the inconsistency...
asecin
Bluelighter
suboxone is thebaine derivative, does it explain why i cant get good high on it from high doses but it makes me horribly confused and dissoriented and not really experiencing the "euphoria" from typical opiates ? im saying this knowing it counters opiates because its used for opiate addiction but i did it on its own without using opiates. still same shit high. some say its that fucking naloxone the anti-opiate add on but im not even sure if thebaine is ever good for use to get high at all.
sekio
Bluelight Crew
No, oxycodone is technically a thebaine derivative, but it lacks the convulsant properties and people abuse it fr fun all the time.
Thebaine is used as a feedstock for producing things like oxycodone, oxymorphone et cetera simply because it's easy to convert it. Opioids derived from thebaine are no more toxic or convuslant than if they were derived frokm codeine.
Suboxone is a shitty opioid because it's only a mu partial agonist, it doesn't produce the same activation of the receptor that morphine does.
But they are more stimulating?
IME for oxycodone and buprenorphine, yes. Hydrocodone not so much.
It's probably for different reasons than being derived from thebaine, though chemically buprenorphines a little closer to thebaine. Bupe still is very different from thebaine in it's mode of action.
sekio
Bluelight Crew
Thebaine is just another poppy alkaloid, it's just one that doesn't bind well to mu-OR. Hydrocodone, oxycodone etc can be derived from thebaine. This does not mean they are intimately related, nor is it the only way of preparing them - hydrocodone/oxycodone can be produced from codeine just as easily. It's just another feedstock. The mere fact that they are derived from thebaine does not instill any sort of "stimulatory" qualities. It just so happens that thebaine is conveniently converted into oxycodone etc in the lab, and since it is much less divertable it is the "preferred" feedstock.
Hydrocodone, etc are probably more "stimulating" just because they are less "dirty" than morphine in terms of their action - more selective for mu-OR. Either that of they have more affinity for histamine release.
