A study of some propranolol analogues for selective beta-adrenoceptor antagonism using A2 values on isolated trachea and atria from guinea-pig

British Journal of Pharmacology
S R O'DonnellJ C Wanstall

Abstract

1 PA2 values for beta-adrenoceptor antagonists were obtained on isolated preparations of guinea-pig trachea (intrinsic tone) and atria (rate), with isoprenaline, noradrenaline (beta 1-selective) and fenoterol (beta 2-selective) as agonists. Uptake mechanisms and alpha-adrenoceptors were inhibited. The antagonists studied were (+/-)-threo-alpha-methylpropranolol. (+/-)-1(4-benzimidazoloxy)-3-isopropylamino-2-propanol (4-BIP) and (+/-)-1-(5-benzimidazoloxy)-3-isopropylamino-2-propanol (5-BIP). 2 4-BIP was a potent beta-adrenoceptor antagonist but it was not selective for trachea (pA2 on trachea 7.88 and on atria 7.73, fenoterol as agonist). 5-BIP was less than one tenth as active as 4-BIP and was therefore not studied in detail. 3 alpha-Methylpropranolol was potent and it was also selective for trachea (pA2 on trachea 8.24 and on atria 7.56, fenoterol as agonist). This selectivity was not seen with isoprenaline as agonist. In tracheal preparations contracted by carbachol the slope of the Schild plot for alpha-methylpropranolol was less than 1.0 (isoprenaline as agonist). 4 alpha-Methylpropranolol, although not highly selective for beta 2-adrenoceptors, is considerably more potent than the alternative beta 2-selective antagonists ...Continue Reading

References

Nov 1, 1978·Clinical and Experimental Pharmacology & Physiology·J D Fitzgerald, S R O'Donnell
Mar 1, 1959·British Journal of Pharmacology and Chemotherapy·O ARUNLAKSHANA, H O SCHILD

Related Concepts

Adrenergic beta-Antagonists
Metazoa
Cavia porcellus
Inotropism
Myocardial Contraction
Tissue Specificity
Phenoxybenzamine Hydrochloride
Rexigen
Trachea
In Vitro [Publication Type]

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