The cardiovascular effects of ICI 118,587: A beta 1-adrenoceptor partial agonist

Br J Pharmacol. 1982 Oct;77(2):381-8. doi: 10.1111/j.1476-5381.1982.tb09309.x.

Abstract

1 In a preparation in which cardiovascular reflexes were prevented from occurring, ICI 118,587 (1-(p-hydroxyphenoxy)-3-beta-(morpholinocarbonamido) ethylamino-2-propranol fumarate) caused dose-dependent positive chronotropic and inotropic effects upon the dog heart. 2 The increase in heart rate brought about by ICI 118,587 was about 43% of the maximum increase produced by isoprenaline. 3 For a given chronotropic effect produced by either ICI 118,587 or isoprenaline, each compound produced a similar inotropic effect as indicated by an increase in LV dp/dtmax. 4 In contrast to the direct stimulant action of ICI 118,587 on the heart no direct effects on vascular smooth muscle were observed. 5 ICI 118,587 was shown to be a competitive antagonist of the chronotropic and vasodilator effects of isoprenaline on the heart and blood vessels and of the chronotropic effects of noradrenaline on the heart. 6 It is concluded that ICI 118,587 is a selective beta 1-adrenoceptor partial agonist.

MeSH terms

  • Adrenergic beta-Agonists / pharmacology*
  • Animals
  • Blood Pressure / drug effects
  • Dogs
  • Electric Stimulation
  • Female
  • Heart Rate / drug effects
  • Hemodynamics / drug effects*
  • Hindlimb / blood supply
  • In Vitro Techniques
  • Male
  • Myocardial Contraction / drug effects
  • Propanolamines / pharmacology*
  • Regional Blood Flow / drug effects
  • Sympathetic Nervous System / physiology
  • Xamoterol

Substances

  • Adrenergic beta-Agonists
  • Propanolamines
  • Xamoterol