Trace amine-associated receptor 1 (TAAR1) is activated by amiodarone metabolites
Trace amine-associated receptor 1 (TAAR1) is activated by amiodarone metabolites
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DOI：
10.1016/j.bmcl.2008.08.013
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发表时间：
2008-11-15
影响因子：
2.7
通讯作者：
Scanlan, Thomas S.
中科院分区：
文献类型：
--
作者：
Snead, Aaron N.;Miyakawa, Motonori;Scanlan, Thomas S.
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. (C) 2008 Elsevier Ltd. All rights reserved.
