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.

journal_name

Bioorg Med Chem Lett

authors

Snead AN,Miyakawa M,Tan ES,Scanlan TS

doi

10.1016/j.bmcl.2008.08.013

subject

Has Abstract

pub_date

2008-11-15 00:00:00

pages

5920-2

issue

22

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(08)00940-2

journal_volume

18

pub_type

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