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