Amiodarone and its putative metabolites fail to activate wild type hTAAR1.
Amiodarone and its putative metabolites fail to activate wild type hTAAR1.
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DOI：
10.1016/j.bmcl.2009.08.058
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发表时间：
2009-10-15
影响因子：
2.7
通讯作者：
Gilmour BP
中科院分区：
文献类型：
--
作者：
Lewin AH;Navarro HA;Gilmour BP
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, Gα16. 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 β-phenethylamine. These results indicate that TAAR1 activation by amiodarone and its analogs is species specific.
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