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Synthesis and in vitro evaluation of salvinorin A analogues: Effect of configuration at C(2) and sub

Synthesis and in vitro evaluation of salvinorin A analogues: Effect of configuration at C(2) and sub

  1. Anonymous
    Cecile Beguin,a, Michele R. Richards, Jian-Guo Lib Yulin Wang, Wei Xu, Lee-Yuan Liu-Chen, William A. Carlezon, Jr. and Bruce M. Cohena


    Abstract—j-opioid receptor ligands have raised interest for their apparent effects on mood. The potent and selective j-agonist salvinorin
    A has short-lasting (15 min) depressive-like effects in rats in behavioral models used to study mood disorders. Two series of
    salvinorin derivatives modified at C(2) and C(18), respectively, were synthesized and their j-opioid receptor affinities, potencies, and
    efficacies were evaluated using in vitro receptor binding and biochemical functional assays. Modification at C(2) yielded potent
    j-agonists that are predicted to have improved metabolic stability (14a, 15a) or increased water solubility (10b). Our preliminary
    SAR study at C(18) suggested that this part of the molecule interacts with a tight lipophilic pocket of the j-receptor.