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A review of salvinorin analogs and their kappa-opioid receptor activity.

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.

SUBMITTER: Roach JJ 

PROVIDER: S-EPMC5912166 | biostudies-literature | 2018 May

REPOSITORIES: biostudies-literature

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A review of salvinorin analogs and their kappa-opioid receptor activity.

Roach Jeremy J JJ   Shenvi Ryan A RA  

Bioorganic & medicinal chemistry letters 20180312 9

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. ...[more]

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