Limited induction of torsade de pointes by Terikalant (cas 132338-79-5) and erythromycin in an in vivo model

Add time:08/06/2019    Source:sciencedirect.com

The proarrhythmic activities of the selective IKr blocker erythromycin and the less selective K+ channel blockers, Terikalant (cas 132338-79-5) and clofilium, have been compared in an α1-adrenoceptor-stimulated, anaesthetized rabbit model. Terikalant (2.5, 7.5 and 25 nmol kg−1 min−1; n=10), erythromycin (133, 400 and 1330 nmol kg−1 min−1; n=8), clofilium (20, 60 and 200 mg kg−1 min−1; n=10) or vehicle (n=8) was infused intravenously over 19 min and there was a 15-min interval between each infusion. QT and QTc intervals, and epicardial monophasic action potential duration were prolonged significantly (and to a similar extent) only by clofilium and terikalant. The total incidences of torsade de pointes were 60%*, 20%, 0% and 0% in clofilium-, terikalant-, erythromycin- and vehicle-treated animals, respectively (*P<0.05 compared to vehicle control). In conclusion, terikalant exerted mild proarrhythmic activity though it prolonged repolarisation markedly. Despite being given in high doses, erythromycin neither prolonged repolarisation nor induced proarrhythmia.

We also recommend Trading Suppliers and Manufacturers of Terikalant (cas 132338-79-5). Pls Click Website Link as below: cas 132338-79-5 suppliers

Prev:Cellular electrophysiological effect of Terikalant (cas 132338-79-5) in the dog heart
Next:THE INHIBITORY EFFECTS OF Terikalant (cas 132338-79-5) ON THE CONTRACTILE ACTIVITY OF GALANIN IN ISOLATED RAT FUNDUS STRIPS)