C8813

[Canis aureus]

I was thinking are these novel compounds in their way to medical scene or are there some fundamental problems in that way...? Of course I was thinking also possible rc's but mostly just inventions to usual pharm field.

I think that Lednicer said something about upjohn and toxicities appearing somewhere in tests in bromidol or aryl-cyclohexanones... and that thus upjohn ended all tests.

And about methadone. There are some patients who are on quite high doses (because as you know methadone has infinitely cumulative effects), but doses are always low in the beginning of the programs. It is also true that some people get cardiac problems with it, but not all; I think that it is quite marginal phenomenon after all...

To the question that could these potent opioids ever hit the markets of usual pharmaceutical compounds...? Do we have any room there anymore? Are there true needs for novel aand hellishly potent opioids?

 

[haribo1]

Lednier said that the company showed no interest in the product. By the time he was doing his work (1979) Both Etorphine & Carfentanil had the market for animals and who would use something so potent on humans? (Well, the Chinese actually, they use Dihydro Etorphine)

 

[fencamfamine]

I'm pretty sure that the analog which Holy Cow was hinting at was the analog with a amide side-chain on the p-ethoxy benzyl. This class seems to bind to the MOR2 sub-receptor far too much for my liking. In any case, there were tests with etonitazene & 1mg of it equated to 60mg of morphine sulphate.

The Lednicer class of cyclohexanols seems stronger if the p-Br is replaced with a p-methyl. At least with the simpler cyclohexanones, the p-methyl was x2 more potent. If the morphinan/fentanyl QSAR is anything like the BDPC->C8813 then the 2-furanylethyl should be the most potent (now that's sticking my neck out - because nobody has made the stuff AFAIK). I should really throw them all into Chem Office & look at the predicted electronic characteristics.

As I have commented before, opioids make interesting structures & have a large QSAR database but they are generally pretty bad news. Once you have taken them for pain, there is no fun to be had (maybe a good thing, in truth).