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Biochem Pharmacol. 2009 Nov 1;78(9):1095-104. doi: 10.1016/j.bcp.2009.05.031. Epub 2009 May 29.

Trace amine-associated receptor 1 as a monoaminergic modulator in brain.

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  • 1Division of Neuroscience, New England Primate Research Center, Harvard Medical School, One Pine Hill Drive, Southborough, MA 01772, USA.


Brain monoaminergic systems play critical roles in mood, cognition, emotion, reward, learning and attention, and aberrance in brain monoaminergic activity is associated with a variety of neuropsychiatric disorders/diseases. The present commentary focuses on trace amine-associated receptor 1 (TAAR1) and its potential regulatory roles in brain monoaminergic systems. TAAR1 was discovered in 2001 and has been established to be a G-protein-coupled receptor signaling through the cAMP pathway. This receptor is activated by a broad spectrum of agonists, although there are notable species differences in ligand efficacy and potency. TAAR1 is expressed and widely distributed in brain monoaminergic systems and co-localized with the dopamine transporter in a subset of dopaminergic neurons in rhesus monkey and mouse brain substantia nigra. TAAR1 activation by the common biogenic amines, the trace amine beta-phenylethylamine and methamphetamine alters the monoamine transporter function in both mouse and rhesus monkey brain synaptosomes, suggesting a modulatory role for this receptor in the presynaptic regulation of monoaminergic activity. However, little is known about other functional roles of TAAR1 in the brain. With a purpose to promote further studies on this receptor, we herein discuss the recent findings that provide insights into the functional significance and biological relevance of this receptor as a modulator in brain monoaminergic systems.

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