Evidence that ICI 118, 551 is a potent, highly beta2-selective adrenoceptor antagonist and can be used to characterize beta-adrenoceptor populations in tissues

O'Donnell S.R. and Wanstall J.C. (1980) Evidence that ICI 118, 551 is a potent, highly beta2-selective adrenoceptor antagonist and can be used to characterize beta-adrenoceptor populations in tissues. Life Sciences, 27 8: 671-677. doi:10.1016/0024-3205(80)90008-9


Author O'Donnell S.R.
Wanstall J.C.
Title Evidence that ICI 118, 551 is a potent, highly beta2-selective adrenoceptor antagonist and can be used to characterize beta-adrenoceptor populations in tissues
Journal name Life Sciences   Check publisher's open access policy
ISSN 0024-3205
Publication date 1980-01-01
Sub-type Article (original research)
DOI 10.1016/0024-3205(80)90008-9
Volume 27
Issue 8
Start page 671
End page 677
Total pages 7
Language eng
Subject 3004 Pharmacology
Abstract pA values for a new ß-adrenoceptor antagonist, ICI 118, 551 (erythro-DL-1(7-methylindan-4-yloxy)-3-isopropylaminobutan-2-o1), have been obtained on intrinsic tone tracheal chain preparations and on spontaneously beating atrial preparations from guinea-pigs. Two different agonists, fenoterol (ß-selective) and noradrenaline (ß-selective) were used. The slopes of the Schild plots were not significantly different from 1.0. The antagonist was very potent (pA on trachea, fenoterol as agonist, was 8.69) and also highly ß-selective (pA on atria, noradrenaline as agonist, was only 6.96). On guinea-pig trachea (which contains ß- and ß-adrenoceptors) the potency was 44 times higher when fenoterol was the agonist than when noradrenaline was the agonist. On guinea-pig atria (which contains only ß-adrenoceptors) the pA value was the same whichever agonist was used. Thus ICI 118, 551 has been shown to be potent and the most ß-selective antagonist so far studied in our laboratory. In experiments carried out with selective agonists ICI 118, 551 distinguished clearly between tissues with a mixed ß-adrenoceptor population (different pA values) and those with a homogeneous population (single pA value). Therefore, ICI 118, 551 is a valuable addition to the group of ß-selective adrenoceptor antagonists.
Q-Index Code C1
Q-Index Status Provisional Code
Institutional Status Unknown

Document type: Journal Article
Sub-type: Article (original research)
Collection: Scopus Import
 
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