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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.

SUBMITTER: Snead AN 

PROVIDER: S-EPMC3609712 | biostudies-literature | 2008 Nov

REPOSITORIES: biostudies-literature

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

Snead Aaron N AN   Miyakawa Motonori M   Tan Edwin S ES   Scanlan Thomas S TS  

Bioorganic & medicinal chemistry letters 20080809 22


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 resul  ...[more]

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