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

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


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.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Animals
  • Biogenic Monoamines / metabolism*
  • Brain / metabolism*
  • Cloning, Molecular
  • Humans
  • Receptors, G-Protein-Coupled / chemistry
  • Receptors, G-Protein-Coupled / genetics
  • Receptors, G-Protein-Coupled / physiology*
  • Signal Transduction


  • Biogenic Monoamines
  • Receptors, G-Protein-Coupled
  • Trace amine-associated receptor 1