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. 2005 Aug 15;15(16):3744-7.
doi: 10.1016/j.bmcl.2005.05.048.

Synthesis and in vitro pharmacological studies of new C(2) modified salvinorin A analogues

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

Synthesis and in vitro pharmacological studies of new C(2) 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 yet discovered with high selectivity and affinity for kappa-opioid receptor. To explore its structure and activity relationships, a series of salvinorin A derivatives modified at the C2 position were prepared and studied. These salvinorin A derivatives were screened for binding and functional activities at the human kappa-opioid receptor. Compound 4, containing a methoxymethyl group at the 2-position, was a full kappa-agonist with an EC50 value at 0.6 nM, which is about 7 times more potent than salvinorin A.

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