Trace amine-associated receptor 1 (TAAR1) is activated by amiodarone metabolites

Aaron N. Snead, Motonori Miyakawa, Edwin S. Tan, Thomas S. Scanlan

Research output: Contribution to journalArticle

15 Scopus citations

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 (TAAR1). This result demonstrates a novel molecular target for amiodarone derivatives with potential clinical significance.

Original languageEnglish (US)
Pages (from-to)5920-5922
Number of pages3
JournalBioorganic and Medicinal Chemistry Letters
Volume18
Issue number22
DOIs
StatePublished - Nov 15 2008

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Keywords

  • Amiodarone
  • G protein-coupled receptors
  • TAAR
  • Trace amine-associated receptor 1

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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