1. Signaling Pathways
  2. GPCR/G Protein
  3. Trace Amine-associated Receptor (TAAR)

Trace Amine-associated Receptor (TAAR)

Trace amine associated-receptors (TAARs) are a class of G protein-coupled receptors that were discovered in 2001. Humans possess six functional isoforms (TAAR1, TAAR2, TAAR5, TAAR6, TAAR8, and TAAR9), whereas some fish species express over 100. It acts as an endogenous receptor for the trace amines. Trace amines are endogenous compounds classically regarded as comprising β-phenylethyalmine, p-tyramine, tryptamine, p-octopamine, and some of their metabolites.

Although all other TAARs serve predominantly or exclusively as chemosensory receptors in the main olfactory system, TAAR 1 has been demonstrated to be a novel modulator of dopaminergic, serotonergic and glutamatergic activity in the brain. And TAAR 1 has been identified as a novel therapeutic target for schizophrenia, depression, and addiction. In the periphery, TAAR1 regulates nutrient-induced hormone secretion, suggesting its potential as a novel therapeutic target for diabetes and obesity. TAAR1 may also regulate immune responses by regulating leukocyte differentiation and activation.

Trace Amine-associated Receptor (TAAR) Related Products (5):

Cat. No. Product Name Effect Purity
  • HY-110098
    Ro 5212773
    Ro 5212773 (EPPTB) is a potent and selective trace amine-associated receptor 1 (TAAR1) antagonist (Ki=0.9 nM for mouse TAAR1), with no significant effects on other TAARs. TAAR1 is a G protein-coupled receptor (GPCR) that is nonselectively activated by endogenous metabolites of amino acids.
  • HY-109157
    Ralmitaront (RO6889450), a potent and orally active partial agonist of the trace amine-associated receptor 1 (TAAR1), acts as a neuroleptic agent. Ralmitaront can be used for the research of neuro-related diseases, such as schizophrenia (SCZ), schizoaffective disorder, and negative symptoms.
  • HY-12700
    RO5256390 is an agonist of trace amine-associated receptor 1 (TAAR1), a highly conserved G-protein-coupled receptor (GPCR) bound by endogenous trace amines. RO5256390 can be used to reduce multiple behavioral effects of agents of abuse through their actions on the mesocorticolimbic system. RO5256390 is a modulator of monoaminergic neurotransmission, blocks psychostimulant-induced hyperactivity and produces a brain activation pattern reminiscent of the antipsychotic agent olanzapine, suggesting antipsychotic-like properties.
  • HY-108015
    RO5263397 is a potent, selective, and orally available TAAR1 agonist, with EC50s of 17 and 35 nM for human TAAR1 and rat TAAR1, respectively. RO5263397 regulates wakefulness and EEG spectral composition. Antidepressant-like effect.
  • HY-12699
    RO5166017 is an orally active and species-crosses TAAR1 agonist, with Ki values of 1.9 nM, 2.7 nM, 31 nM and 24 nM for mouse, rat, human and cynomolgus monkey, respectively.