New analgesic drugs derived from phencyclidine

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Abstract
Phencyclidine [1-(1-phenylcyclohexyl)piperidine, PCP], a major drug of abuse, was initially considered a safe general anesthetic. Several esters of 1-(1-phenylcyclohexyl)-4-piperidinol, 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 PCP, 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.

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