• N&PD Moderators: Skorpio | thegreenhand

mu opioid agonist + DRI

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Bluelighter
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Apr 12, 2013
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https://imgur.com/F6e9wAm

People might recognize this as the reversed-ester of nortilidine. It overlays nortilidine precisely. It also overlays N-methyl cypenamine (the active isomer). I have heard people say nortilidine is stimulating and I suspect the cypenamine scaffold is to blame. How much potency increase the reversed ester causes I don't know but I contacted the gentleman who patented the material and he classed it in the prodine range (trans isomers). People wondering about that o-substitution. I think a methyl is likely to work. I noted that in pethidine and isopethidine, it conferred rigidity to the rotation of the aromatic. I think the most potent opioid I've ever seen had a meta xylene as the aromatic and Chemoffice showed it stopped rotation.

It's novel, it's interesting and it isn't another highly potent, highly hazardous fentanyl analogues and homologues. It makes me mad that the people buying that class do not consider that 1000% profit is enough. Synthesis poses interesting problems but after much research, a 2-step route from cyclopent-1-en-1ylbenzene is possible at bench scale but I bet scaling isn't possible (my synthetic route is that their is no cheap, safe, high-yield route so it's a dead end.

I thought it worth mentioning because the QSAR is almost unresearched. I have research it and a couple of friends did say that the approach was 'sane' but not being super-potent and can be eyeballed is of no concern to the scum poisoning H. If a limited number of opioids became legal, I would lobby for this one to be one item of the small set that might usefully be included.
 
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