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