Synthetic studies and pharmacological evaluations on the MDMA ('Ecstasy') antagonist nantenine

…, S Chaudhary, SM Zimmerman, WE Fantegrossi…

Index: LeGendre, Onica; Pecic, Stevan; Chaudhary, Sandeep; Zimmerman, Sarah M.; Fantegrossi, William E.; Harding, Wayne W. Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 2 p. 628 - 631

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Citation Number: 11

Abstract

The naturally occurring aporphine alkaloid nantenine, has been shown to antagonize behavioral and physiological effects of MDMA in mice. We have synthesized (±)-nantenine via an oxidative cyclization reaction with PIFA and evaluated its binding profile against a panel of CNS targets. To begin to understand the importance of the chiral center of nantenine with regards to its capacity to antagonize the effects of MDMA in vivo,(R)-and (S ...