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

…, M He, LY Liu-Chen, L Kondaveti, Z Ma, Y Wang…

Index: Lee, David Y.W.; Karnati, Vishnu V.R.; He, Minsheng; Liu-Chen, Lee-Yuan; Kondaveti, Leelakrishna; Ma, Zhongze; Wang, Yulin; Chen, Yong; Beguin, Cecile; Carlezon Jr., William A.; Cohen, Bruce Bioorganic and Medicinal Chemistry Letters, 2005 , vol. 15, # 16 p. 3744 - 3747

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Citation Number: 62

Abstract

Salvinorin A is the most potent naturally occurring opioid agonist yet discovered with high selectivity and affinity for κ-opioid receptor. To explore its structure and activity relationships, a series of salvinorin A derivatives modified at the C (2) position were prepared and studied. These salvinorin A derivatives were screened for binding and functional activities at the human κ-opioid receptor. Compound 4, containing a methoxymethyl group at the 2- ...