Endothelins stimulate phosphoinositide breakdown in the rat spinal cord through ETA receptors

J Cardiovasc Pharmacol. 1995:26 Suppl 3:S148-9.

Abstract

In rat spinal cord slices, endothelin-1 (ET-1) and -3 (ET-3), sarafotoxin 6c (STX-6c), and the ETB receptor agonist IRL-1620 produced increases of [3H]inositol phosphate (IP) accumulation with the following rank order of potency: ET-1 > ET-3 >> STX-6c = IRL-1620. The ET-1- and ET-3-induced IP accumulations were blocked by BQ-123, a selective ETA antagonist, with a similar inhibition constant (IC50 16.7 +/- 3.4 microM and 8.0 +/- 1.6 microM, respectively) whereas BQ-788, a selective ETB antagonist, was inactive. These data indicate that ET-induced IP accumulation in rat spinal cord is mediated by an ETA receptor. The present study is in agreement with ETA receptor-mediated cardiovascular changes induced by intrathecal injection of ET-1 in the conscious rat.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Endothelins / pharmacology*
  • In Vitro Techniques
  • Male
  • Phosphatidylinositols / metabolism*
  • Rats
  • Rats, Wistar
  • Receptor, Endothelin A
  • Receptors, Endothelin / physiology*
  • Spinal Cord / drug effects*
  • Spinal Cord / metabolism

Substances

  • Endothelins
  • Phosphatidylinositols
  • Receptor, Endothelin A
  • Receptors, Endothelin