New analgesic drugs derived from phencyclidine

J Med Chem. 1981 May;24(5):496-9. doi: 10.1021/jm00137a004.

Abstract

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.

MeSH terms

  • Analgesics / chemical synthesis*
  • Animals
  • Chemical Phenomena
  • Chemistry
  • Lethal Dose 50
  • Male
  • Mice
  • Motor Activity / drug effects
  • Phencyclidine / analogs & derivatives*
  • Phencyclidine / chemical synthesis
  • Phencyclidine / pharmacology
  • Reaction Time / drug effects

Substances

  • Analgesics
  • Phencyclidine