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Studies toward the pharmacophore of salvinorin A, a potent kappa opioid receptor agonist.

Version 2 2024-06-12, 15:18
Version 1 2017-05-09, 15:06
journal contribution
posted on 2024-06-12, 15:18 authored by TA Munro, MA Rizzacasa, BL Roth, BA Toth, F Yan
Salvinorin A (1), from the sage Salvia divinorum, is a potent and selective kappa opioid receptor (KOR) agonist. We screened other salvinorins and derivatives for binding affinity and functional activity at opioid receptors. Our results suggest that the methyl ester and furan ring are required for activity but that the lactone and ketone functionalities are not. Other salvinorins showed negligible binding affinity at the KOR. None of the compounds bound to mu or delta opioid receptors.

History

Journal

Journal of Medicinal Chemistry

Volume

48

Pagination

345-348

Location

United States

ISSN

0022-2623

Language

eng

Publication classification

CN.1 Other journal article

Issue

2

Publisher

American Chemical Society