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Trace amine-associated receptor (TAAR (for the class/family), individual members as TAAR1, TAAR2, etc.)

Target
TAAR (for the class/family), individual members as TAAR1, TAAR2, etc.
Molecular classification
G protein-coupled receptor (GPCR), Receptor
01

Overview

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].

Other names
trace amine receptorTARTATAARstrace amine-associated receptor 1 (TAAR1, most commonly studied subtype)
02

Mechanism of action

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

03

Biological functions

Signal transductionNeuromodulationOlfaction (esp. TAAR2–TAAR9)Modulation of monoamine neurotransmissionRegulation of cognitive processes and moodChemotaxis (in leukocytes)Homeostasis, Rheostasis
04

Disease associations

Neuropsychiatric disease (notably schizophrenia)Psychosis (Parkinson's disease psychosis)Substance use/addictionObesity/metabolic syndromeCancer (TAAR1 expression as a biomarker)
05

Safety considerations

Functional selectivity and species specificity: Different ligand binding and signaling profiles may limit direct translation to clinical utilityLimited efficacy/unknown long-term effects for TAAR1-targeting drugs in schizophrenia and other CNS disordersPossible off-target or mood/cognition effects due to widespread CNS/peripheral expression
06

Interacting drugs

Ulotaront (SEP-363856, TAAR1 agonist)

4 more in the full profile.

07

Biomarkers

TAAR1 expression (potential prognostic biomarker in cancers)

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