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Updated: Jul 19, 2026

Methods for the Discovery of Novel Compounds Modulating a Gamma-Aminobutyric Acid Receptor Type A Neurotransmission
Published on: August 16, 2018
Trace amine-associated receptors and their ligands
R Zucchi1, G Chiellini, T S Scanlan
1Dipartimento di Scienze dell'Uomo e dell'Ambiente, University of Pisa, Pisa, Italy. r.zucchi@med.unipi.it
Trace amine-associated receptors (TAARs) are a novel class of G protein-coupled receptors (GPCRs) that interact with trace amines and other ligands. Research reveals TAARs
Area of Science:
- Neuroscience and Pharmacology
- Endocrinology
Background:
- Classical biogenic amines (e.g., adrenaline, serotonin) signal through G protein-coupled receptors (GPCRs).
- Trace amines (e.g., p-tyramine, tryptamine) are present at low concentrations and traditionally thought to modulate aminergic pathways.
- The discovery of trace amine-associated receptors (TAARs) revealed novel GPCRs specifically responsive to trace amines.
Purpose of the Study:
- To explore the ligands and functions of the trace amine-associated receptor (TAAR) family.
- To investigate the role of TAARs in physiological and pathological processes.
Main Methods:
- In vitro pharmacological characterization of TAAR subtypes with various amine ligands.
- In vivo studies assessing the physiological effects of novel TAAR ligands.
- Analysis of TAAR gene expression patterns in mammalian tissues.
- Examination of genetic associations between TAARs and neuropsychiatric disorders.
Main Results:
- Several TAAR subtypes exhibit unique ligand specificities beyond classical trace amines.
- 3-iodothyronamine, a thyroid hormone derivative, acts as an endogenous ligand for TAAR1, inducing hypothermic and cardiodepressive effects in vivo.
- TAARs are expressed in various tissues, including the olfactory epithelium, and respond to volatile amines.
- TAAR1 is a target for psychotropic drugs, and the TAAR gene locus is linked to schizophrenia and bipolar disorder susceptibility.
Conclusions:
- TAARs represent a distinct GPCR subfamily with diverse endogenous and exogenous ligands.
- TAARs, particularly TAAR1, are implicated in regulating physiological functions and are associated with neuropsychiatric conditions.
- Further research into TAARs may yield novel therapeutic targets for metabolic and neurological disorders.
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