New analgesic drugs derived from phencyclidine.
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.
D000700:Analgesics / Q000138:chemical synthesis*; D000818:Animals; D055598:Chemical Phenomena; D002621:Chemistry; D007928:Lethal Dose 50; D008297:Male; D051379:Mice; D009043:Motor Activity / Q000187:drug effects; D010622:Phencyclidine / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology; D011930:Reaction Time / Q000187:drug effects
D000700:Analgesics; D010622:Phencyclidine