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Effect of flecainide derivatives on sarcoplasmic reticulum calcium release suggests a lack of direct action on the cardiac ryanodine receptor

Bannister, Mark L., Alvarez-Laviada, Anita, Thomas, N. Lowri, Mason, Sammy A., Coleman, Sharon, du Plessis, Christo L., Moran, Abbygail T., Neill-Hall, David, Osman, Hasnah, Bagley, Mark C., MacLeod, Kenneth T., George, Christopher H. and Williams, Alan J. 2016. Effect of flecainide derivatives on sarcoplasmic reticulum calcium release suggests a lack of direct action on the cardiac ryanodine receptor. British Journal of Pharmacology 173 (15) , pp. 2446-2459. 10.1111/bph.13521

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Abstract

Flecainide is a use-dependent blocker of cardiac Na+ channels. The mechanisms involved in block were elucidated using fully charged (QX-FL) and neutral (NU-FL) derivatives of flecainide, establishing that Na+ channel block requires the cationic form of the molecule to enter the cytosolic vestibule of the open channel. Flecainide is also effective in the treatment of catecholaminergic polymorphic ventricular tachycardia (CPVT), however its mechanism of action is contentious. We investigated how flecainide derivatives influence RyR2-mediated Ca2+-release from the sarcoplasmic reticulum and whether this correlates with their effectiveness as blockers of Na+ channels and/or RyR2.

Item Type: Article
Date Type: Publication
Status: Published
Schools: Medicine
Subjects: R Medicine > R Medicine (General)
Publisher: Wiley
ISSN: 0007-1188
Funders: British Heart Foundation
Date of First Compliant Deposit: 15 June 2016
Date of Acceptance: 17 May 2016
Last Modified: 30 Jan 2020 13:30
URI: http://orca-mwe.cf.ac.uk/id/eprint/91718

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