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

Bioorg Med Chem Lett. 2006 Nov 1;16(21):5498-502. doi: 10.1016/j.bmcl.2006.08.051.

David Y W Lee ¹, Minsheng He, Lee-Yuan Liu-Chen, Yulin Wang, Jian-Guo Li, Wei Xu, Zhongze Ma, William A Carlezon Jr, Bruce Cohen

Affiliations

Affiliation

1 Bioorganic and Natural Products Laboratory, McLean Hospital, Harvard Medical School, 115 Mill Street, Belmont, MA 02478, USA.

PMID: 16945525 DOI: 10.1016/j.bmcl.2006.08.051

Abstract

Salvinorin A, a compound isolated from the plant Salvia divinorum, is a potent and highly selective agonist for the kappa Opioid Receptor. For exploration of its structure and activity relationships, further modifications, such as reduction 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 new full agonists have been identified.

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