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Trace amine-associated receptors are a family of G protein-coupled receptors, discovered in 2001, that mediate the effects of endogenous trace amines such as phenethylamine, tyramine, and tryptamine, as well as various psychostimulants and metabolites of neurotransmitters[5][1][4]. TAAR1, the most clinically validated subtype, is widely expressed in the central nervous system and several peripheral tissues, where it modulates monoamine signaling, influences mood, cognition, and metabolism, and mediates chemotactic responses in immune cells[5][6][2]. Other subtypes function mainly as olfactory receptors sensing volatile amine odorants[5][3]. TAAR1 is a rapidly emerging drug target in neuropsychiatric conditions, notably schizophrenia, and may have implications for metabolic diseases, addiction, and cancer[2][4][6]. Several drugs, including ulotaront and amphetamines, function as TAAR1 agonists and are in clinical or preclinical phases for CNS disorders[2][5][6].
Agonism: Activation of TAAR1 or other TAAR subtypes by trace amines, pharmaceutical agonists, and psychostimulants, leading to G protein-mediated intracellular signaling (Gs, Gq) Modulation of cAMP signaling and K⁺ channels Regulation of monoamine transporter activity
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