Behavioral and biochemical stereoselectivity of sigma opiate/PCP receptors

Brain Res. 1984 Feb 27;294(1):174-7. doi: 10.1016/0006-8993(84)91326-x.

Abstract

The relative potencies of the stereoisomers of ketamine, N-allylnormetazocine and cyclazocine were determined at mu opiate and sigma opiate/phencyclidine (PCP) receptors in vitro in rat brain homogenates, as well as in a discriminative stimulus behavioral paradigm in rats trained to discriminate PCP from saline. In all cases the in vivo and in vitro data were in agreement. The (+)-isomers of N-allylnormetazocine and cyclazocine are highly specific sigma opiate/PCP ligands.

Publication types

  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Animals
  • Behavior, Animal / drug effects*
  • Brain / metabolism
  • Cyclazocine / pharmacology*
  • Hydromorphone / pharmacology*
  • In Vitro Techniques
  • Ketamine / pharmacology*
  • Male
  • Phenazocine / analogs & derivatives*
  • Phenazocine / pharmacology
  • Phencyclidine / pharmacology*
  • Rats
  • Rats, Inbred Strains
  • Receptors, Opioid / drug effects
  • Receptors, Opioid / physiology*
  • Stereoisomerism

Substances

  • Receptors, Opioid
  • Ketamine
  • SK&F 10047
  • Phenazocine
  • Phencyclidine
  • Cyclazocine
  • Hydromorphone