Amiodarone and its putative metabolites fail to activate wild type hTAAR1.
Basic Information
ID: ALA1156046
Journal: Bioorg Med Chem Lett
Title: Amiodarone and its putative metabolites fail to activate wild type hTAAR1.
Authors: Lewin AH, Navarro HA, Gilmour BP.
Abstract: 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, Galpha16. 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.
CiteXplore: 19740654
DOI: 10.1016/j.bmcl.2009.08.058
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