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A Review of Salvinorin Analogs and their Kappa-Opioid Receptor Activity

Jeremy J Roach, Ryan A Shenvi

Bioorganic & Medicinal Chemistry Letters March 12, 2018 DOI: 10.1016/j.bmcl.2018.03.029 (opens in new tab)

Study at a glance

AI-extracted from the abstract
Characteristics Review Peer reviewed
Topics Salvia divinorum
Key findings Extensive peripheral modifications of salvinorin A have yielded a trove of SAR information, and deeper structural changes are now possible through advances in chemical synthesis.

Abstract

The plant metabolite salvinorin A potently and selectively agonizes the human kappa-opioid receptor, an emerging target for next-generation analgesics. Here we review analogs of the salvinorin chemotype and their effects on selectivity, affinity and potency. Extensive peripheral modifications using isolated salvinorin A have delivered a trove of SAR information. More deep-seated changes are now possible by advances in chemical synthesis.

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