α-Phenyl-β-(3,4-dimethoxy)phenethylamines: Novel Inhibitors of Choline Acetyltransferase from Torpedo Electric Organ
作者:Ragab M. Shafik、Raafat Soliman、Soad A. El-Hawash、Mahmoud Morshedy、Nabil A. Mansour
DOI:10.1002/jps.2600731114
日期:1984.11
derivatives of alpha-phenyl-beta-(3,4-dimethoxy)phenethylamine that might bear a certain conformational resemblance to choline were prepared. The in vitro inhibition of cholineacetyltransferasefromTorpedoelectricorgan was investigated. These compounds gave variable degrees of inhibition; the most potent inhibitor was, N,N,N,-trimethyl-alpha-phenyl-beta-(3,4-dimethoxy)phenethylammonium++ + iodide,
制备了一些可能与胆碱具有类似构象的α-苯基-β-(3,4-二甲氧基)苯乙胺衍生物。研究了鱼雷电器官对胆碱乙酰基转移酶的体外抑制作用。这些化合物具有不同程度的抑制作用。最有效的抑制剂是N,N,N,-三甲基-α-苯基-β-(3,4-二甲氧基)苯乙铵++ +碘化物,I50为1.3 X 10(-5)M。抑制胆碱乙酰转移酶还确定了来自斜纹夜蛾幼虫脑的来源用于比较研究。前述化合物在来自该来源的胆碱乙酰基转移酶上的I50为9 X 10(-6)M。