Receptor binding and antinociceptive properties of phencyclidine opiate-like derivatives

Eur J Pharmacol. 1981 Jul 10;72(4):305-11. doi: 10.1016/0014-2999(81)90568-9.

Abstract

The relative potencies of a new series of phencyclidine (PCP) analogs for the displacement of [3H] morphine binding from rat brain homogenates are well correlated with the relative antinociceptive potencies in the test of writhing induced by acetic acid (0.6%). One group of compounds exerts a completely naloxone-reversible analgesic effect, while the effects of a second group are partially reversed by naxolone. These findings and the structural differences between the two groups suggest that their analgesic is mediated through different opiate receptors.

MeSH terms

  • Analgesics*
  • Animals
  • Brain / metabolism*
  • Chemical Phenomena
  • Chemistry
  • Dose-Response Relationship, Drug
  • Male
  • Mice
  • Mice, Inbred ICR
  • Naloxone / pharmacology
  • Phencyclidine / analogs & derivatives*
  • Phencyclidine / metabolism
  • Phencyclidine / pharmacology
  • Rats
  • Receptors, Opioid / metabolism*
  • Structure-Activity Relationship

Substances

  • Analgesics
  • Receptors, Opioid
  • Naloxone
  • Phencyclidine