期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 19, 期 20, 页码 5913-5914出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2009.08.058
关键词
Amiodarone; Human trace amine-associated receptor 1; hTAAR1; G protein-coupled receptors
资金
- NIDA [R01-DA016327]
The ability of amiodarone and its putative metabolites to activate unmodified human trace amine associated receptor 1 (hTAAR1) stably expressed in CHO cell lines was evaluated. Receptor activation was monitored by measuring the accumulation of cAMP, the putative hTAAR1 native second messenger, or calcium mobilization in cells where the receptor was coupled to the promiscuous Gq, G(alpha 16). Despite literature reports of activation of rodent TAAR1 by these agents, no response was seen in either cell line although robust activation was obtained with the endogenous ligand beta-phenethylamine. These results indicate that TAAR1 activation by amiodarone and its analogs is species specific. (C) 2009 Elsevier Ltd. All rights reserved.
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