Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 17, Issue 22, Pages 6111-6115Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2007.09.050
Keywords
kappa; salvinorin A; Salvia divinorum; opioid; antagonist
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Funding
- NIDA NIH HHS [R01 DA018151, DA 018151, R01 DA018151-01A2] Funding Source: Medline
- NIGMS NIH HHS [T32 GM067795] Funding Source: Medline
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Modification of the C-1 ketone of salvinorin A (2a) produces analogues with opioid antagonist properties. Of particular significance is the finding that 1-deoxo-1,10-dehydrosalvinorin A (11a) is a moderately potent antagonist at all three opioid receptor subtypes, and that herkinorin (2b), a mu agonist, is converted to a weak antagonist by removal of the C-1 ketone (3b and 11b). These observations suggest that the ketone of 2b is a key structural feature responsible for p agonist activity. (C) 2007 Elsevier Ltd. All rights reserved.
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