Chan C C, Farmer P S, McKenzie G, Robertson H
College of Pharmacy, Dalhousie University, Canada.
Pharmazie. 1987 Jun;42(6):369-71.
Five related derivatives of 2-(2-piperidinoethyl)tetralin have been synthesized as partially rigid analogs of the neuroleptic butyrophenones. Their in vitro dopamine receptor binding properties and in vivo inhibition of dexamphetamine-induced locomotor activity are described. 1-Phenyl-2-(2-piperidinoethyl)-3,4-dihydronaphthalene hydrochloride (8) is about 1% as potent as haloperidol.
已合成了2-(2-哌啶基乙基)四氢萘的五种相关衍生物，作为抗精神病药物丁酰苯类的部分刚性类似物。描述了它们的体外多巴胺受体结合特性以及体内对右旋苯丙胺诱导的运动活性的抑制作用。1-苯基-2-(2-哌啶基乙基)-3,4-二氢萘盐酸盐（8）的效力约为氟哌啶醇的1%。
