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) Agonists (5)

Trace Amine-associated Receptor (TAAR) Related Products (9):

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 (K_i=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	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.

HY-12700

RO5256390		98.75%
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-12699

RO5166017		99.48%
RO5166017 is an orally active and species-crosses TAAR1 agonist, with K_i values of 1.9 nM, 2.7 nM, 31 nM and 24 nM for mouse, rat, human and cynomolgus monkey, respectively.

HY-108015

RO5263397		99.26%
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-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.

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.

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.

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.

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