Vernakalant-d6 hydrochloride

Vernakalant-d6 (hydrochloride) is deuterium labeled Vernakalant.

Research Areas >> Cardiovascular Disease

Signaling Pathways >> Membrane Transporter/Ion Channel >> Potassium Channel

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].

[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.

[2]. Dorian, Paul MD et al. The Effect of Vernakalant (RSD1235), an Investigational Antiarrhythmic Agent, on Atrial Electrophysiology in Humans. Journal of Cardiovascular Pharmacology:July 2007 - Volume 50 -Issue 1 - pp 35-40.

[3]. Jodene Eldstrom et al. The Molecular Basis of High-Affinity Binding of the Antiarrhythmic Compound Vernakalant (RSD1235) to Kv1.5 Channels. Molecular Pharmacology December 2007 vol. 72 no. 6 1522-1534

[4]. Vernakalant. Too dangerous in atrial fibrillation.Prescrire Int. 2012 May;21(127):119-22.

[5]. Blomstr?m-Lundqvist C, Blomstr?m P.Safety and efficacy of pharmacological cardioversion of atrial fibrillation using intravenous vernakalant, a new antiarrhythmic drug with atrial selectivity.Expert Opin Drug Saf. 2012 Jul;11(4):671-9. Epub 2012 May 26.

[6]. Bash LD, Buono JL, Davies GM, Martin A, Fahrbach K, Phatak H, Avetisyan R, Mwamburi M.Systematic review and meta-analysis of the efficacy of cardioversion by vernakalant and comparators in patients with atrial fibrillation.Cardiovasc Drugs Ther. 2012 Apr;26(2):167-79.