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 Lettjournal_title
Bioorganic & medicinal chemistry lettersauthors
Snead AN,Miyakawa M,Tan ES,Scanlan TSdoi
10.1016/j.bmcl.2008.08.013subject
Has Abstractpub_date
2008-11-15 00:00:00pages
5920-2issue
22eissn
0960-894Xissn
1464-3405pii
S0960-894X(08)00940-2journal_volume
18pub_type
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