TAAR1

TAAR1 agonists and antagonists act on trace amine-associated receptor 1 (TAAR1), a receptor for trace amines. A family of mammalian G protein-coupled receptors (GPCRs) that respond to trace amines such as tyramine and β-phenylethylamine was described in 2001. In the same year, amphetamine and 3,4-methylenedioxymethamphetamine (MDMA) were shown to activate the rat receptor. TAAR1 couples mainly to Gs proteins and raises cyclic adenosine monophosphate (cAMP) inside the cell. In the brain it modulates the firing of dopamine and serotonin neurons. Its ligands are therefore studied in models of psychosis, addiction and metabolic control. Listed agonists include RO5256390, RO5263397, RO5203648 hydrochloride and ralmitaront, while Ro 5212773 is listed as a TAAR1 antagonist.

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