Related Experiment Video
Updated: Jun 20, 2026

Dual-Dye Optical Mapping of Hearts from RyR2R2474S Knock-In Mice of Catecholaminergic Polymorphic Ventricular Tachycardia
Published on: December 22, 2023
Amiodarone and its putative metabolites fail to activate wild type hTAAR1
Anita H Lewin1, Hernán A Navarro, Brian P Gilmour
1Center for Organic and Medicinal Chemistry, RTI International, PO Box 12194, Research Triangle Park, NC 27709, USA. ahl@rti.org
None:
The ability of amiodarone and its putative metabolites to activate unmodified human trace amine associated receptor 1 (hTAAR1) stably expressed in CHO cell lines was evaluated. Receptor activation was monitored by measuring the accumulation of cAMP, the putative hTAAR1 native second messenger, or calcium mobilization in cells where the receptor was coupled to the promiscuous Gq, Galpha16. Despite literature reports of activation of rodent TAAR1 by these agents, no response was seen in either cell line although robust activation was obtained with the endogenous ligand beta-phenethylamine. These results indicate that TAAR1 activation by amiodarone and its analogs is species specific.
More Related Videos
Related Concept Videos
Antiarrhythmic Drugs: Class III Agents as Potassium Channel Blockers
Heart Failure Drugs: Inotropic Agents
Antiarrhythmic Drugs: Class II Agents as β-Adrenergic Blockers
Antiarrhythmic Drugs: Class I Agents as Sodium Channel Blockers
Class 1A Antiarrhythmic Drugs: These drugs work by moderately blocking sodium channels,...
Heart Failure Drugs: Inhibitors of Renin-Angiotensin System
Antiarrhythmic Drugs: Class IV Agents as Calcium Channel Blockers
Verapamil, a calcium channel blocker, inhibits calcium movement across myocardial cell membranes and vascular smooth muscle. This results in the dilation of coronary and...

