Selective and non-selective ET antagonists reveal an ETB receptors mediated ET-1-induced behavioural effect in conscious rats

Life Sci. 1996;58(10):PL 177-80. doi: 10.1016/0024-3205(96)00023-9.

Abstract

The injection of endothelin-1 (ET-1) (1 pmol/rat) into the dorsolateral periaqueductal gray (PAG) area of freely moving rats induced rotation along the long axis of the body (barrel-rolling). Preinjection (10 min before) of BQ-788 (an ETB receptor selective antagonist; 5 nmol) or bosentan (an ETA/ETB receptor non-selective antagonist; 10 nmol) to the PAG reduced the behavioral response to ET-1. In contrast, pretreatment with FR139317 (an ETA receptor selective antagonist; 5 nmol) did not affect the ET-1-induced barrel-rolling. These results suggest that barrel-rolling induced by microinjection of ET-1 into the PAG area is predominantly mediated via ETB-like receptors.

MeSH terms

  • Animals
  • Azepines / pharmacology
  • Behavior, Animal / drug effects
  • Behavior, Animal / physiology*
  • Bosentan
  • Consciousness
  • Endothelin Receptor Antagonists*
  • Endothelins / antagonists & inhibitors
  • Endothelins / pharmacology*
  • Indoles / pharmacology
  • Male
  • Oligopeptides / pharmacology
  • Periaqueductal Gray / drug effects
  • Periaqueductal Gray / ultrastructure
  • Piperidines / pharmacology
  • Rats
  • Rats, Sprague-Dawley
  • Receptor, Endothelin A
  • Receptor, Endothelin B
  • Receptors, Endothelin / physiology*
  • Sulfonamides / pharmacology

Substances

  • Azepines
  • Endothelin Receptor Antagonists
  • Endothelins
  • Indoles
  • Oligopeptides
  • Piperidines
  • Receptor, Endothelin A
  • Receptor, Endothelin B
  • Receptors, Endothelin
  • Sulfonamides
  • FR 139317
  • BQ 788
  • Bosentan