Abstract
Salvia divinorum (Lamiaceae) has drawn much attention in recent years due to its psychopharmacological properties. The active ingredient salvinorin A, is a potent κ-opioid receptor (KOR) agonist [1]. Since its discovery, numerous synthetic analogues of salvinorin A have been reported at KOR, µ-opioid receptor (MOR) and δ-opioid receptor (DOR) [2]. The current objective is to use the knowledge about salvinorin A-KOR interactions to rationally design salvinorin A derivatives with different pharmacological profiles and therapeutic potential. Previous work on the KOR model and analysis of the mode of binding of RB-64 (22-thiocyanatosalvinorin A) suggest that Cys-315 may be a good anchoring amino acid at the binding site in KOR [3]. Considering the fact that Michael acceptors may strongly bind with thiol group of Cys-315 of KOR, we synthesized a series of Michael-acceptor type of salvinorin A derivatives, and evaluated for their binding affinity at κ-, µ-, and δ-opioid receptors.
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