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. 2005 Oct 1;15(19):4169-73.
doi: 10.1016/j.bmcl.2005.06.092.

Synthesis and in vitro pharmacological studies of C(4) modified salvinorin A analogues

David Y W Lee  1 , Minsheng He, Leelakrishna Kondaveti, Lee-Yuan Liu-Chen, Zhongze Ma, Yulin Wang, Yong Chen, Jian-Guo Li, Cecile Beguin, William A Carlezon Jr, Bruce Cohen
Affiliations

Synthesis and in vitro pharmacological studies of C(4) modified salvinorin A analogues

David Y W Lee et al. Bioorg Med Chem Lett. .

Abstract

Salvinorin A is the most potent naturally occurring opioid agonist with a high selectivity and affinity for kappa-opioid receptor. To explore its structure-activity relationships, modifications at the C(4) position have been studied and a series of salvinorin A derivatives were prepared. These C(4)-modified salvinorin A analogues were screened for binding and functional activities at the human kappa-opioid receptor and several potent new agonists have been identified.

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