Propranolol stereoselectively inhibits alpha-adrenoceptor-mediated vasoconstriction in mesenteric arterial beds of rats

J Auton Pharmacol. 1996 Jun;16(3):125-9.

Abstract

1. The optical isomers of propranolol were compared for their effects on pressor responses to adrenergic and non-adrenergic vasoconstrictors in mesenteric arterial beds of rats. 2. R(+)-propranolol (10(-7)-10(-5) M) had no effect on vessel preparations stimulated with noradrenaline, methoxamine, or arginine-vasopressin. 3. S(-)-propranolol 10(-7) M did not alter pressor responses to noradrenaline. However, S(-)-propranolol 10(-6) and 10(-5) M inhibited vasoconstriction induced by noradrenaline. This effect was similar in the presence of indomethacin 3 x 10(-6) M. 4. S(-)-propranolol 10(-5) M also inhibited vasoconstriction induced by methoxamine, shifting the dose-response curves to the right, but did not affect pressor responses to arginine-vasopressin. 5. Schild analysis for equilibrium vasoconstrictor responses to methoxamine indicated stereoselective competitive alpha-adrenoceptor antagonism by propranolol. 6. These data suggest selective inhibition of alpha-adrenoceptor-mediated vasoconstriction by S(-)-propranolol at higher concentrations by competitive alpha-adrenoceptor antagonism.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adrenergic alpha-Agonists / pharmacology*
  • Adrenergic beta-Antagonists / pharmacology*
  • Analysis of Variance
  • Animals
  • Dose-Response Relationship, Drug
  • Male
  • Mesenteric Arteries
  • Methoxamine / antagonists & inhibitors*
  • Norepinephrine / antagonists & inhibitors*
  • Propranolol / pharmacology*
  • Rats
  • Rats, Sprague-Dawley
  • Stereoisomerism*
  • Vasoconstriction / drug effects*
  • Vasoconstrictor Agents / antagonists & inhibitors*

Substances

  • Adrenergic alpha-Agonists
  • Adrenergic beta-Antagonists
  • Vasoconstrictor Agents
  • Propranolol
  • Methoxamine
  • Norepinephrine