Trace amine-associated receptor 1 (TAAR1) is activated by amiodarone metabolites.

Authors: Snead AN, Miyakawa M, Tan ES, Scanlan TS.
Publisher/Year: Bioorg Med Chem Lett. 2008 Nov 15;18(22):5920-2. Epub 2008 Aug 9.
Pub Med ID/Journal ID: PMID:18752950


Amiodarone (Cordarone, Wyeth-Ayerst Pharmaceuticals) is a clinically available drug used to treat a wide variety of cardiac arrhythmias. We report here the synthesis and characterization of a panel of potential amiodarone metabolites that have significant structural similarity to thyroid hormone and its metabolites the iodothyronamines. Several of these amiodarone derivatives act as specific agonists of the G protein-coupled receptor (GPCR) trace amine-associated receptor 1 (TAAR(1)). This result demonstrates a novel molecular target for amiodarone derivatives with potential clinical significance.