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Unless otherwise stated all data on this page refer to the human proteins. Gene information is provided for human (Hs), mouse (Mm) and rat (Rn).
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More detailed introduction
Trace amine-associated receptors were discovered from a search for novel 5-HT receptors [1], where 15 mammalian orthologues were identified and divided into two families. The TA1 receptor (nomenclature as agreed by the NC-IUPHAR Subcommittee for the Trace amine receptor [4]) has affinity for the endogenous trace amines tyramine, β-phenylethylamine and octopamine in addition to the classical amine dopamine [1]. Emerging evidence suggests that TA1 is a modulator of monoaminergic activity in the brain [8] with TA1 and dopamine D2 receptors shown to form constitutive heterodimers when co-expressed [3]. In addition to trace amines, receptors can be activated by amphetamine-like psychostimulants, and endogenous thyronamines.
TA1 receptor
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Database page citation (select format):
Concise Guide to PHARMACOLOGY citation:
Alexander SP, Christopoulos A, Davenport AP, Kelly E, Mathie A, Peters JA, Veale EL et al. (2021) THE CONCISE GUIDE TO PHARMACOLOGY 2021/22: G protein-coupled receptors. Br J Pharmacol. 176 Suppl 1:S27-S156.
In addition to TA1, in man there are up to 5 functional TAAR genes (TAAR2,5,6,8,9). See [1] for detailed discussion. The product of the gene TAAR2 (also known as GPR58) appears to respond to β-phenylethylamine > tyramine and to couple through Gs [1].
TAAR3, in some individuals, and TAAR4 are pseudogenes in man, although functional in rodents. The signalling characteristics and pharmacology of TAAR5 (PNR, Putative Neurotransmitter Receptor: TAAR5, O14804), TAAR6 (Trace amine receptor 4, TaR-4: TAAR6, 96RI8), TAAR8 (Trace amine receptor 5, GPR102: TAAR8, Q969N4 ) and TAAR9 (trace amine associated receptor 9: TAAR9, 96RI9) are lacking. The thyronamines, endogenous derivatives of thyroid hormone, have affinity for rodent cloned trace amine receptors, including TA1 [6]. An antagonist EPPTB has recently been described with a pKi of 9.1 at the mouse TA1 but >5.3 for human TA1 [7].