Reduction of exercise tachycardia in man after propranolol, atenolol and bisoprolol in comparison to beta-adrenoceptor occupancy
- 1 December 1987
- journal article
- clinical trial
- Published by Oxford University Press (OUP) in European Heart Journal
- Vol. 8 (suppl M) , 3-8
- https://doi.org/10.1093/eurheartj/8.suppl_m.3
Abstract
In a double blind, placebo controlled study, propranolol (240mg), atenolol (200mg) or bisoprolol (100mg) were administered as a single oral dose to groups of 6 healthy male volunteers. Exercise tachycardia was monitored for 84 hours after administration of the drugs to monitor beta blockade in vivo. Plasma samples drawn in parallel with these effects were used to detect beta1- or beta2-adrenoceptor occupancy in two subtype selective in vitro receptor binding assays. Reduction of exercise tachycardia parallels beta1-adrenoceptor occupancy. Furthermore, at comparable beta1-adrenoceptor occupancy, less beta2-adrenoceptor occupancy was observed after bisoprolol than after atenolol. The latter finding is in agreement with the two-fold higher beta1/beta2-selectivity ratio of bisoprolol (75-fold) versus atenolol {35-fold). It is concluded, that beta blockade observed via the reduction of exercise tachycardia can be delineated from the in vitro occupancy of beta1-adrenoceptors by an antagonist present in plasma samples.Keywords
This publication has 0 references indexed in Scilit: