Differential effects of BQ-123 against endothelin-1 and endothelin-3 on the rat vas deferens: evidence for an atypical endothelin receptor

Br J Pharmacol. 1993 Jul;109(3):736-8. doi: 10.1111/j.1476-5381.1993.tb13635.x.

Abstract

1. Endothelin-1 and endothelin-3 enhanced concentration-dependently the rat vas deferens twitch response to electrical stimulation, endothelin-1 being three times more potent. Sarafotoxin S6c was at least 200 times less active than endothelin-1. 2. The response to endothelin was antagonized in a competitive manner by the supposedly selective ETA receptor antagonist, BQ-123 (pA2:7.0 +/- 0.1). In contrast, the endothelin-1 concentration-response curve was only shifted two fold in the presence of 10 microM BQ-123, while no effect was observed at 1 microM. 3. This evidence suggests the rat vas deferens contains an endothelin receptor not conforming to the ETA/ETB receptor subtype classification so far proposed.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amino Acid Sequence
  • Animals
  • Electric Stimulation
  • Endothelins / antagonists & inhibitors*
  • In Vitro Techniques
  • Male
  • Molecular Sequence Data
  • Muscle Contraction / drug effects
  • Muscle, Smooth / drug effects*
  • Peptides, Cyclic / pharmacology*
  • Rats
  • Rats, Sprague-Dawley
  • Receptors, Endothelin / drug effects*
  • Vas Deferens / drug effects
  • Vasoconstrictor Agents / pharmacology
  • Viper Venoms / pharmacology

Substances

  • Endothelins
  • Peptides, Cyclic
  • Receptors, Endothelin
  • Vasoconstrictor Agents
  • Viper Venoms
  • sarafotoxins s6
  • cyclo(Trp-Asp-Pro-Val-Leu)