N-Allyl analogs of phencyclidine: chemical synthesis and pharmacological properties
作者:Asher Kalir、Shoshana Teomy、Adina Amir、P. Fuchs、Sung A. Lee、Elzbieta J. Holsztynska、Wieslaw Rocki、Edward F. Domino
DOI:10.1021/jm00376a006
日期:1984.10
Several N-allyl derivatives of 1-phenylcyclohexylamine (PCA) were prepared, and their pharmacology was briefly characterized. The mono- and diallyl derivatives had phencyclidine-like activities in mice but were less potent behaviorally than phencyclidine (PCP). None were PCP antagonists. In vitro these compounds were competitive inhibitors of butyrylcholinesterase (BChE) and protected against inhibition
制备了1-苯基环己胺(PCA)的几种N-烯丙基衍生物,并对其药理进行了简要表征。单和二烯丙基衍生物在小鼠中具有苯环利定样活性,但行为却不如苯环利定(PCP)。没有人是五氯苯酚拮抗剂。在体外,这些化合物是丁酰胆碱酯酶(BChE)的竞争性抑制剂,并受到DFP的抑制作用。此外,这些药物从小鼠脑匀浆中取代了ti化的N-甲基-4-哌啶基苯甲酸三tri化N-甲基-4-哌啶基苯并抑制了乙酰胆碱对分离的豚鼠回肠的作用。这些体外作用均与小鼠体内PCP样行为活动无关。