2. Signaling Pathways
  3. GPCR/G Protein
  4. 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 (11):

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-110098
    Ro 5212773
    		99.85%
    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.
    Ro 5212773
  • HY-12700
    RO5256390
    		98.75%
    RO5256390 is an orally effective trace amine associated receptor 1 (TAAR1) agonist. RO5256390 exhibits pro-cognitive and antidepressant-like properties in rodent and primate models, showing similar brain activation patterns to Olanzapine (HY-14541). RO5256390 can reduce various behavioral effects of abuse of active molecules through the action of active molecules on the mesocortical system. RO5256390 blocks compulsive overeating behavior in rats. RO5256390 can inhibit ATP (HY-B2176)-induced TNF secretion in mouse bone marrow-derived macrophages .
    RO5256390
  • HY-109157
    Ralmitaront
    		Agonist 99.92%
    Ralmitaront (RO6889450) is an orally active agonist of trace amine-associated receptor 1 (TAAR1) with a EC50 value of 110.4 nM. Ralmitaront has antipsychotic, cognitively improvement, and antidepressant activity in rodents. Ralmitaront can be used as a neurosuppressant in the study of neuro-related diseases, such as schizophrenia (SCZ), schizoaffective disorder.
    Ralmitaront
  • HY-12699
    RO5166017
    		99.48%
    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.
    RO5166017
  • HY-108015
    RO5263397
    		98.87%
    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.
    RO5263397
  • HY-W909173
    TAAR1 agonist 2
    		Agonist
    TAAR1 agonist 2 (compound 30) is a full agonist of trace amine-associated receptor 1 (TAAR1) (pEC50=7.5). TAAR1 agonist 2 also exhibits agonist activity at H1 receptors and activates several members of the muscarinic acetylcholine receptor family, such as the M2 receptor (pEC50=5). TAAR1 agonist 2 can be used in the study of neuropsychiatric diseases.
    TAAR1 agonist 2
  • HY-W909149
    TAAR1 agonist 3
    		Agonist
    TAAR1 agonist 3 is a trace amine-associated receptor 1 (TAAR1) agonist (pEC50=7.6). TAAR1 agonist 3 is also a full agonist of the α2A receptor (pEC50=6). TAAR1 agonist 3 can be used in the study of neuropsychiatric diseases.
    TAAR1 agonist 3
  • HY-42346
    ZH8651
    		Agonist 99.71%
    ZH8651 is an agonist of TAAR1 which can activate both Gs and Gq signal pathway. ZH8651 can used in study schizophrenia.
    ZH8651
  • HY-161317
    Gαq/11 protein-IN-1
    		Agonist
    Gαq/11 protein-IN-1 (compound F33) is an inhibitor of Gαq/11 protein with an IC50 value of 9.4 μM. Gαq/11 protein-IN-1 has antitumor activity.
    Gαq/11 protein-IN-1
  • HY-157955A
    TAAR1 agonist 1 hydrochloride
    		Agonist
    TAAR1 agonist 1 hydrochloride (6e·HCl) is a novel G-protein-coupled receptor TAAR1 agonist. TAAR1 agonist 1 hydrochloride is used in the study of schizophrenia.
    TAAR1 agonist 1 hydrochloride
  • HY-157955
    TAAR1 agonist 1
    		Agonist
    TAAR1 agonist 1 (compound 6E) is a potent TAAR1 agonist with a potent TAAR1-Gs/Gq dual-pathway activation property. TAAR1 agonist 1 significantly alleviates MK-801-induced schizophrenia-like cognitive phenotypes.
    TAAR1 agonist 1