Celiprolol exerts microvascular dilatation by activation of beta 2-adrenoceptors

Naunyn Schmiedebergs Arch Pharmacol. 1992 Jul;346(1):27-31. doi: 10.1007/BF00167566.

Abstract

In order to clarify the question whether the beta 1-selective adrenoceptor antagonist celiprolol possesses vasodilating properties, isolated vascular networks were perfused with increasing concentrations of celiprolol (in a cumulative manner) ranging from 10(-8) to 10(-4) mol/l. The study was carried out using the isolated mesenteric vascular bed of the guinea pig mesenterium coli. Vascular diameters of four different vascular regions [vessels classified as G1 (585 +/- 30 microns), G2 (403 +/- 25 microns), G3 (282 +/- 27 microns) and G4 (197 +/- 13 microns)] were assessed by means of microscopic videoangiometry. Perfusion with celiprolol resulted in concentration dependent vasodilation which was more pronounced in G3 and G4 vessels. In addition, cumulative concentration-response curves were determined from responses obtained in the presence of 10(-8), 10(-7), 10(-6) and 10(-4) mol/l ICI 118,551 (a highly selective adrenoceptor antagonist). In the presence of ICI 118,551 at concentrations greater than or equal to 10(-6) mol/l, no celiprolol response could be observed. Lower concentrations of ICI 118,551 shifted the celiprolol concentration-response curve to the right in a concentration-dependent manner. Therefore, it is concluded (a) that celiprolol has a vasodilating effect, (b) that this vasodilation is produced by stimulation of beta 2-adrenoceptors and (c) that the vasodilating effect is more pronounced in smaller than in larger vessels (G3, G4 vs G1, G2).

MeSH terms

  • Adrenergic beta-Antagonists / pharmacology*
  • Animals
  • Antihypertensive Agents / pharmacology
  • Celiprolol / pharmacology*
  • Dose-Response Relationship, Drug
  • Guinea Pigs
  • In Vitro Techniques
  • Male
  • Mesenteric Arteries / drug effects
  • Microcirculation / drug effects*
  • Perfusion
  • Propanolamines / pharmacology
  • Receptors, Adrenergic, beta / drug effects*
  • Vasodilator Agents / pharmacology*

Substances

  • Adrenergic beta-Antagonists
  • Antihypertensive Agents
  • Propanolamines
  • Receptors, Adrenergic, beta
  • Vasodilator Agents
  • ICI 118551
  • Celiprolol