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THE CARDIOVASCULAR EFFECTS OF ICI 118,587: A β 1 ‐ADRENOCEPTOR PARTIAL AGONIST
Author(s) -
NUTTALL A.,
SNOW H.M.
Publication year - 1982
Publication title -
british journal of pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.432
H-Index - 211
eISSN - 1476-5381
pISSN - 0007-1188
DOI - 10.1111/j.1476-5381.1982.tb09309.x
Subject(s) - partial agonist , agonist , adrenergic beta antagonists , medicine , pharmacology , endocrinology , receptor , propranolol
1 In a preparation in which cardiovascular reflexes were prevented from occurring, ICI 118,587 (1‐( p ‐hydroxyphenoxy)‐3‐β‐(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/d t max.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 β 1 ‐adrenoceptor partial agonist.