The sigma [corrected] ligand rimcazole antagonises (+)SKF 10,047, but not (+)3-PPP, in the mouse isolated vas deferens

Eur J Pharmacol. 1990 Jun 8;181(3):315-8. doi: 10.1016/0014-2999(90)90097-p.

Abstract

We have characterized the actions of several sigma receptor ligands on the electrically evoked, neurogenic contractions of the mouse isolated vas deferens. (-)SKF 10,047 was significantly more potent than (+)SKF 10,047 in potentiating twitch contractions and was equipotent with (+)3-PPP. Rimcazole (1 and 3 microM) antagonised the potentiation induced by 100 microM (+)SKF 10,047 and, to a lesser extent, that induced by 30 microM (-)SKF 10,047 but increased that elicited by (+)3-PPP (30 microM). This apparent contradiction may arise from sigma agonists acting in this tissue at both sigma and non-sigma sites.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antipsychotic Agents / pharmacology*
  • Carbazoles / pharmacology*
  • In Vitro Techniques
  • Male
  • Mice
  • Mice, Inbred DBA
  • Muscle, Smooth / drug effects*
  • Phenazocine / analogs & derivatives*
  • Phenazocine / antagonists & inhibitors
  • Phenazocine / pharmacology
  • Piperidines / antagonists & inhibitors*
  • Piperidines / pharmacology
  • Stereoisomerism
  • Vas Deferens / drug effects

Substances

  • Antipsychotic Agents
  • Carbazoles
  • Piperidines
  • SK&F 10047
  • preclamol
  • rimcazole
  • Phenazocine