Itzhak Y, Kalir A, Weissman B A, Cohen S
J Med Chem. 1981 May;24(5):496-9. doi: 10.1021/jm00137a004.
Several esters of 1-(1-phenylcyclohexyl)-4-piperidinol (3), 1-(1-phenylcyclohexyl)-4-phenyl-4-piperidinol (10) and its propionate (11), and 1-(1-phenylcyclohexyl)-4-phenylpiperidine (13) were prepared and characterized. The new compounds, which are derived from phencyclidine, exerted analgesic activity in mice. The most potent is 10, which is twice as active as morphine. The antinociceptive activity of 10, 11, and 13 could be well correlated with their potency in the mouse vas deferens bioassay, and both were completely reversed by naloxone.
制备并表征了1-(1-苯基环己基)-4-哌啶醇(3)、1-(1-苯基环己基)-4-苯基-4-哌啶醇(10)及其丙酸盐(11)以及1-(1-苯基环己基)-4-苯基哌啶(13)的几种酯类化合物。这些衍生自苯环己哌啶的新化合物在小鼠体内具有镇痛活性。其中活性最强的是10，其活性是吗啡的两倍。10、11和13的抗伤害感受活性与其在小鼠输精管生物测定中的效力密切相关，且两者均可被纳洛酮完全逆转。
