Trace amine-associated receptor 1 (TAAR1) is activated by amiodarone metabolites.
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.
Snead
Aaron N
AN
Graduate Program in Chemistry and Chemical Biology, University of California at San Francisco, 600 16th Street, San Francisco, CA 94143, USA.
Miyakawa
Motonori
M
Tan
Edwin S
ES
Scanlan
Thomas S
TS