Iorio M A, Reymer T P, Frigeni V
Laboratory of Pharmaceutical Chemistry, Istituto Superiore di Sanità, Rome, Italy.
J Med Chem. 1987 Oct;30(10):1906-10. doi: 10.1021/jm00393a037.
Some 4-phenyl-4-piperidinols, corresponding esters, and related compounds with a p-fluorobutyrophenone chain on nitrogen were synthesized and evaluated in in vitro and in vivo tests in order to examine their ability to interact contemporaneously with opioid and dopamine receptors. The propionyloxy derivatives showed a good combination of analgesic and neuroleptic activity. With a 3-methyl substituent on the piperidine ring, the beta-configuration was the more active form not only for analgesic activity, as expected from previous results on prodines, but also for neuroleptic activity. Haloperidol and its propionate were also tested as reference compounds.
合成了一些4-苯基-4-哌啶醇、相应的酯以及氮上带有对氟丁酰苯链的相关化合物，并进行了体外和体内试验评估，以考察它们同时与阿片受体和多巴胺受体相互作用的能力。丙酰氧基衍生物显示出良好的镇痛和抗精神病活性组合。在哌啶环上有一个3-甲基取代基时，β-构型不仅如之前对普罗迪类药物的研究结果所预期的那样，对镇痛活性更具活性，而且对抗精神病活性也更具活性。还测试了氟哌啶醇及其丙酸盐作为参考化合物。
