• N&PD Moderators: Skorpio | thegreenhand

Balanced Mu-Delta Agonist & Kappa Antagonist (and easy to synth)?

This has interested me as well. Looking at the difference between buprenorphine and norbuprenorphine, you'd think some similar Bentley compound near those could produce the desired effect with how they flip their affinities, and how bupe is partial mu agonist & kappa antagonist. Then again maybe not with regard to the morphology of the overall morphinan.
 
It has been done - 14-methoxymetopon being the obvious exmple. I've posted the link to a paper on the QSAR of opioids and MANY dual agonists. I hope it helps.
 
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