A comparison of the anti-arrhythmic actions of I.C.I. 50172 and (--)-propranolol and their effects on intracellular cardiac action potentials and other features of cardiac function.

Abstract:

:1. I.C.I. 50172 had marked quinidine-like effects on intracellular cardiac action potentials at concentrations above 20 mg/l. (6.61 x 10(-5)M). The rate of rise and overshoot of the action potential, conduction velocity and contractions were decreased. (-)-Propranolol had similar effects at less than 1/30 this concentration.2. I.C.I. 50172 had 1/100 the activity of (-)-propranolol as a local anaesthetic. Since this is also the ratio of their in vitro beta-receptor blocking activities, I.C.I. 50172 provides no net increase in specificity of beta-receptor blockade.3. In contrast, the in vivo activity of I.C.I. 50172 in protecting anaesthetized guinea-pigs against ouabain-induced ventricular fibrillation was 40% that of (-)-propranolol.4. Structure-activity relations of beta-receptor blocking drugs are discussed.

journal_name

Br J Pharmacol

authors

Papp JG,Williams EM

doi

10.1111/j.1476-5381.1969.tb10576.x

subject

Has Abstract

pub_date

1969-10-01 00:00:00

pages

391-9

issue

2

eissn

0007-1188

issn

1476-5381

journal_volume

37

pub_type

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