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

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 recepto...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry 2008-11, Vol.18 (22), p.5920-5922
Main Authors: Snead, Aaron N., Miyakawa, Motonori, Tan, Edwin S., Scanlan, Thomas S.
Format: Article
Language:English
Subjects:
Amiodarone
Amiodarone - chemical synthesis
Amiodarone - chemistry
Amiodarone - pharmacology
Animals
Anti-Arrhythmia Agents - pharmacology
Arrhythmias, Cardiac - drug therapy
Biological and medical sciences
Combinatorial Chemistry Techniques
G protein-coupled receptors
Humans
Medical sciences
Mice
Miscellaneous
Molecular Structure
Pharmacology. Drug treatments
Rats
Receptors, G-Protein-Coupled - drug effects
TAAR 1
Trace amine-associated receptor 1
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Summary: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). 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.
ISSN:0960-894X
0968-0896
1464-3405
1464-3391
DOI:10.1016/j.bmcl.2008.08.013