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Synthesis and in vitro pharmacological evaluation of salvinorin A analogues modified at C(2)

Synthesis and in vitro pharmacological evaluation of salvinorin A analogues modified at C(2)

  1. Anonymous
    Cecile Beguin, Michele R. Richards, Yulin Wang, Yong Chen, Lee-Yuan Liu-Chen,
    Zhongze Ma, David Y. W. Lee, William A. Carlezon, Jr.d and Bruce M. Cohena,

    Abstract—Salvinorin A is the only known non-nitrogenous and specific j-opioid agonist. A series of salvinorin A derivatives were
    prepared and tested for in vitro activity at the j-opioid receptor. Unsubstituted carbamate 9 was a potent j-agonist (EC50 = 6.2 nM)
    and should be more stable than salvinorin A toward metabolic transformations. Compound 10, containing an N-methyl carbamate
    at C(2), showed partial agonist activity with 81% efficacy when compared with the full agonist U50,488H. No antagonist ligands
    were observed.