Irreversible beta-adrenoceptor blockade of atrial rate and tension responses.

Abstract:

:The competitive reversible beta-adrenoceptor antagonist activity of Ro 03-5255 [1-(5-acetylaminobenzfuran-2-yl)-2-isopropylaminoethanol] upon isoprenaline-induced increases of the rate and tension of guinea-pig isolated atria is described. The chlorinated derivative [Ro 03-7894; 1-[5-chloracetylaminobenzfuran-2-yl)-2-isopropyl-aminoethanol] in contrast exhibited concentration-dependent non-competitive irreversible blocking activity as measured by depression of the maximum responses which were not restored by a washout period that successfully reversed Ro 03-5255. When orciprenaline was used as a weak agonist of low efficacy, the maximum responses were depressed to a greater extent. The blockade by Ro 03-7894 was relatively specific for beta-adrenoceptors since it did not antagonize histamine or calcium chloride. The depression of the maximum responses to orciprenaline was reduced by the presence of sodium thiosulphate. Sodium thiosulphate was ineffective in reversing an established blockade. The blockade by Ro 03-7894 was therefore assumed to involve irreversible binding to the beta-adrenoceptor after conversion to an appropriate electrophilic ligand. The significance of this is discussed.

journal_name

Eur J Pharmacol

authors

Nicholson CD,Broadley KJ

doi

10.1016/0014-2999(78)90278-9

subject

Has Abstract

pub_date

1978-12-01 00:00:00

pages

259-69

issue

3-4

eissn

0014-2999

issn

1879-0712

pii

0014-2999(78)90278-9

journal_volume

52

pub_type

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