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

journal contribution
posted on 2005-01-27, 00:00 authored by Thomas Munro, M A Rizzacasa, B L Roth, B A Toth, F Yan
Salvinorin A (1), from the sage Salvia divinorum, is a potent and selective Κ 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 μor δ opioid receptors.

History

Journal

Journal of Medicinal Chemistry

Volume

48

Issue

2

Pagination

345 - 348

ISSN

0022-2623

Publication classification

CN.1 Other journal article