Wer have only limited knowledge of just how potent carfentanil is in man. While a TI of 10,600 is listed, that's based on animal models. Whle μ selective, I suspect that analgesic activity might be mediated by μ1 (supraspinal receptors) rather than μ2 (brain) but even this isn't certain. But I think the fact that it's μ2 agonism is what produces respiratory collapse has been established.
The handful of 'trip reports' suggest a longer duration of action. Now it wasn't clear if they meant the 'high' lasted longer or if the interval between doses could be longer (several report it stopped AWS for 12 hours) possibly because at least some of the metabolites are actives.
It IS highly lipopholic and more protein-bound that fentanyl and one or indeed both may explain that unexpected factor. Not one mentioned the term 'euphoric' and at least a few researchers have suggested that it is uniquely β-arrestin-biased so tachyphlaxis due to endocytosis may well be considered a positive to sellers since in essence, it's a one-way street. Renarcotising was observed and that would line up with high protein bound fraction and that LogP.
LONG occupany time with the specific warning that naloxone lacks the ability to reverse OD.
It's achiral - that's incrediby important to the 'cooks' who make these things. While derivatives of OHMEfentanil are more potent, three chiral centres so potency of mixture (coupled with synthetic complexity) makes it a leaas optimal target.
Note that MOST papers talk about case studies of fatalities.
You know, long ago I went to a lecture by Hardy, one of Bentley's team. Not only did they describe the infamous 'glass rod incident' but also being first-into-man for buprenorphine. 200μg IV made him puke for 24 hours.
Kenneth Bentley was a world authority on the chemistry of the morphine alkaloids, and made important advances in the treatment of pain and drug dependency. Derived from the opium poppy, morphine
www.thetimes.com
M-99 was imbibled but in a well resourced drug discovery laboratory, such potent things are always a hazard. That all survived a pot of tea stirred with a dry glass rod contaminated with the stuff sort of underlines how risky such compounds really are. Safety is a culture, not just a process.
I still think it ironic that Wildnil comes as a a two vial product. One a solution of carfentanil, the other a solution of diprenorphine. For one, Janssen has to pay McFarlen-Smith!
hdiac.dtic.mil
