• N&PD Moderators: Skorpio | thegreenhand

Viminol

I think the only form actually in use is the racemate. Although the 2R isomer is x5 morphine (in animal models), the mixture comes as 75mg tablets which are purported to be around the same efficacy as 10mg morphine sulfate. Some further research revealed that the o-F & o-CF3 were twice as active and had a much higher TI (the original paper had stated o-Cl was optimal).

The pyrrole ring has also been substituted with a lactam. This is interesting because the =O is in the same spatial position as the 6 position in the phenanthracene scaffold. I seem to remember that some of them were rather potent.
If nothing else, the N-di(sec)butyl moiety is totally unique (activity drops off rather steeply when this pattern is modified). I have, in moments of true boredom, wondered if this pattern has ever been applied to the 3,3 diphenyl heptanones (for example) because the piperidine analogues of viminol were actually reasonably active. I don't think any antagonists in the methadone class have been discovered yet... it may just yield a little more insight into the pharmocore.

Unusual chemically & possibly useful in opioid detoxification but I don't think they have any subjective effects to make them worthy of detailed investigation.

BTW Viminol seems to have acute toxicity similar to that of other opioids although the analogues with different ortho substitutions had much, much higher LD50 values in the animal models at least.
 
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i take it that as usual we have plenty of theoretical but no practical?
as a mu agonist you would expect at least some "button pushing" if not euphoria even from the racemic?
has anyone ACTUALLY tried this?
 
If you are looking for something recreational, don't bother. It's good for detoxing though. Doubt any serious junk head could maintain on it for long.
 
thanks for the info, nice to hear some empirical.
looking at the ah's.
look a lot more promising.
 
I came across a 'viminolo' containing preparation in a Naples pharmacy some 5 or so years ago. It was OTC, but I did not buy it (as the pharmacist recommended a superior alternative). The structure is certainly one of interest, and with some 'persuasion', the racemate could be.......well......

In a country with a relative abundance of opiates and semi-synthetics, Italy has come up with a number of interesting opioids (most pertinent to the nature of the discussion would be compounds such as azaprocin, etc).
 
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