Synthesis, in vitro acetylcholine-storage-blocking activities, and biological properties of derivatives and analogs of trans-2-(4-phenylpiperidino) cyclohexanol ( …

…, SM Parsons, DC Anderson, LM Nilsson…

Index: Rogers, Gary A.; Parsons, Stanley M.; Anderson, D. C.; Nilsson, Lena M.; Bahr, Ben A.; et al. Journal of Medicinal Chemistry, 1989 , vol. 32, # 6 p. 1217 - 1230

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Citation Number: 235

Abstract

Eighty-four analogues and derivatives of the acetylcholine-storage-blocking drug trans-2-(4- phenylpiperidino)-cyclohexanol (vesamicol) were synthesized, and their potencies were evaluated with the acetylcholine active-transport assay utilizing purified synaptic vesicles from Torpedo electric organ. The parent drug exhibits enantioselectivity, with (-)-vesamicol being 25-fold more potent than (+)-vesamicol. The atomic structure and absolute ...