amine-associated receptor 1 (taar1)

RO5263397 is a TAAR1 specific agonist with oral activity that has been used in antidepressant studies. It has also been found to act as an inhibitor of the enzyme cyclooxygenase-2 (COX-2), which is involved in the synthesis of prostaglandins.

3-Methoxytyramine hydrochloride (3-O-methyl Dopamine hydrochloride) is an inactive metabolite of dopamine which can activate trace amine associated receptor 1 (TAAR1). 3-methoxytyramine can be found primarily in human brain and most tissues tissues; and in blood, cerebrospinal fluid (csf) or urine. Within a cell, 3-methoxytyramine is primarily located in the cytoplasm.

RO5256390 is a trace amine-associated receptor 1 (TAAR1) agonist, a highly conserved G-protein-coupled receptor that blocks psychostimulant-induced hyperarousal, and may be used in the study of neurological disorders.

SEP-363856 hydrochloride (SEP-856 hydrochloride) is an orally active, CNS-active psychotropic agent with a unique non-D2 5-HT2A mechanism of action, demonstrating antipsychotic-like effects and potential for schizophrenia treatment.

TAAR1 agonist 3 is a potent agonist of Trace Amine-Associated Receptor 1 (TAAR1) with a pEC50 value of 7.6. Additionally, it acts as a full agonist at the α2AR with a pEC50 of 6. TAAR1 agonist 3 is utilized in the research of neuropsychiatric disorders.

TAAR1 agonist 2 (compound 30), a full agonist at trace amine-associated receptor 1 (TAAR1) (pEC50=7.5), also displays agonistic properties at H1 receptors and activates various muscarinic acetylcholine receptors, including the M2 receptor (pEC50=5). This compound is utilized in researching neuropsychiatric diseases.

2-Phenylpropan-1-amine hydrochloride is a phenethylamine compound that acts as an agonist of the trace amine-associated receptor 1 (TAAR1) in humans.

RO5166017 is an orally active, potent and selective trace amine-associated receptor 1 (TAAR1) agonist for the study of conditioned taste aversion frontal nerve disorders.

Potent trace amine 1 (TA1) receptor agonist (EC50 values are 0.12, 35 and 17-85 nM for mouse, rat and human receptors, respectively). Increases wakefulness and reduces REM and NREM sleep duration in wild type mice. Inhibits spontaneous locomotor activity in dopamine transport (DAT) knockout mice. Espinoza et al (2018) Biochemical and functional characterization of the trace amine-associated receptor 1 (TAAR1) agonist RO5263397. Front.Pharmacol. 9 645 PMID:29977204 |Galley et al (2015) Discovery and characterization of 2-aminooxazolines as highly potent, selective, and orally active TAAR1 agonists. ACS.Med.Chem.Letts. 7 192 PMID:26985297 |Schwartz et al (2017) Trace amine-associated receptor 1 regulates wakefulness and EEG spectral composition. Neuropsychopharmacology. 42 1305 PMID:27658486

ZH8659 is a Gq agonist targeting the trace amine-associated receptor 1 (TAAR1) and has potential applications in schizophrenia research [1].

Ralmitaront (RO6889450) is a potent, orally active partial agonist of the trace amine-associated receptor 1 (TAAR1).

Ro 5212773 (Epptb) is a selective TAAR1 antagonist.