Receptor | Trace Amine 1, TA1 |
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Previous names | TAR1, TRAR1, BO111, TAAR1 (approved human gene symbol) |
Structural information | 7TM |
Human: 339 aa (SwissProt Q96RJ0), chr 6q23.2 (Entrez 134864) | |
Rat: 332 aa (SwissProt Q923Y9), chr 1p12 (Entrez 113914) | |
Mouse: 332 aa (SwissProt Q923Y8) chr 10A3 (Entrez 111174) | |
Functional assays | COS-7/HEK293 cells transfected with TA1 and Gαs (Borowsky et al., 2001; Lindemann et al., 2005; Wolinsky et al., 2007); X. laevis oocytes cotransfected with TA1 and CFTR (Borowsky et al., 2001); CHO cells expressing TA1 and promiscuous Gα16 (Navarro et al., 2006) |
Endogenous agonists | Tyramine (pEC50 = 6.4–6.7), β-PEA (pEC50 = 6.2–7.0), (Borowsky et al., 2001; Wainscott et al., 2007; Barak et al., 2008) |
Antagonists | None currently commercially available |
Radioligand assays | COS-7 cells transiently transfected with human TA1 and rat Gαs (Borowsky et al., 2001) |
Radioligands | [3H]tyramine (pKD = 7.7) (Borowsky et al., 2001); [125I]-,[2H]-, [3H]3-iodothyronamine (Miyakawa and Scanlan, 2006) |
Transduction | Couples to Gαs (Borowsky et al., 2001; Lindemann et al., 2005; Wolinsky et al., 2007) and Gα16 (Navarro et al., 2006; Lewin et al., 2008) in vitro |
Receptor distribution | Studies in humans, RT-PCR showed mRNA encoding TA1 in stomach, amygdala, kidney, lung, small intestine, cerebellum, dorsal root ganglion, hippocampus, hypothalamus, liver, medulla, pancreas, pituitary, reticular formation, prostate, skeletal muscle, spleen (Borowsky et al., 2001), pancreatic islets (Regard et al., 2007), circulating leukocytes (D'Andrea et al., 2003), and intestinal mucosa/endothelium (Kidd et al., 2008); in rats, mRNA found in cardiac ventricles (Chiellini et al., 2007); in mice, in situ hybridization localized mRNA encoding TA1 to discrete CNS areas, including the mitral cell layer of the olfactory bulb, trigeminal nuclei, cerebellar Purkinje cells, spinal cord, amygdala, hippocampus, monoaminergic nuclei (Borowsky et al., 2001), and dopaminergic neurons of the substantia nigra (Xie et al., 2007) |
Tissue function | Inhibits uptake and induces efflux of monoamines at striatal and thalamic synapses (Xie et al., 2008; Xie and Miller, 2008) |
7TM, seven transmembrane; aa, amino acid(s); chr, chromosome; CFTR, cystic fibrosis transmembrane conductance regulator; CHO, Chinese hamster ovary; RT-PCR, reverse transcriptase polymerase chain reaction; CNS, central nervous system