In depth pharmacological characterization of endothelin B receptors in the rat middle cerebral artery

Neurosci Lett. 2001 Nov 13;314(1-2):69-72. doi: 10.1016/s0304-3940(01)02293-5.

Abstract

Whereas the endothelin A receptor is generally believed to mediate vasoconstriction; the endothelin B receptor seems elusive; both dilative and constrictive responses have been reported. Using the in vitro arteriograph, a method allowing compartmentalized study of vessel segments, segments of rat middle cerebral artery were cannulated with micropipettes, pressurized and luminally perfused. Vessel diameters were evaluated using a microscope equipped with an imaging system. Both intra- and extraluminal applications of endothelin-1 produced constriction. Intraluminal administration of a selective endothelin B receptor agonist sarafotoxin 6c in precontracted cerebral arteries and in the presence of the endothelin A receptor blocker FR139317 caused vasodilation in a concentration-dependent manner. Inhibition of nitric oxide synthase significantly reduced the dilation induced by sarafotoxin 6c, whereas inhibition of cyclooxygenase and endothelium-derived hyperpolarizing factor did not.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Azepines / pharmacology
  • Blood Pressure / drug effects
  • Blood Pressure / physiology
  • Charybdotoxin / pharmacology
  • Dose-Response Relationship, Drug
  • Endothelin Receptor Antagonists
  • Endothelin-1 / metabolism*
  • Endothelin-1 / pharmacology
  • Enzyme Inhibitors / pharmacology
  • Indoles / pharmacology
  • Male
  • Middle Cerebral Artery / drug effects
  • Middle Cerebral Artery / metabolism*
  • Muscle, Smooth, Vascular / drug effects
  • Muscle, Smooth, Vascular / metabolism*
  • Rats
  • Rats, Sprague-Dawley
  • Receptor, Endothelin B
  • Receptors, Endothelin / agonists
  • Receptors, Endothelin / metabolism*
  • Transducers, Pressure
  • Vasoconstriction / drug effects
  • Vasoconstriction / physiology*
  • Vasoconstrictor Agents / pharmacology
  • Viper Venoms / pharmacology

Substances

  • Azepines
  • Endothelin Receptor Antagonists
  • Endothelin-1
  • Enzyme Inhibitors
  • Indoles
  • Receptor, Endothelin B
  • Receptors, Endothelin
  • Vasoconstrictor Agents
  • Viper Venoms
  • sarafotoxins s6
  • Charybdotoxin
  • FR 139317