Last update 01 Nov 2024

TAAR5

Last update 01 Nov 2024

Basic Info

Synonyms

hTaar5, PNR, Putative neurotransmitter receptor

+ [5]

Introduction

Olfactory receptor specific for trimethylamine, a trace amine. Also activated at lower level by dimethylethylamine. Trimethylamine is a bacterial metabolite found in some animal odors, and to humans it is a repulsive odor associated with bad breath and spoiled food. This receptor is probably mediated by the G(s)-class of G-proteins which activate adenylate cyclase.

Drugs associated with TAAR5

Salubrin-HF

Target

TAAR5

Mechanism

TAAR5 modulators

Active Org.

Pherin Pharmaceuticals, Inc.

Originator Org.

Pherin Pharmaceuticals, Inc.

Active Indication

Hot Flashes

Inactive Indication-

Drug Highest PhasePhase 2

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

HG-1149

Target

TAAR5

Mechanism

TAAR5 modulators

Active Org.-

Originator Org.

Human Genome Sciences, Inc.

Active Indication-

Inactive Indication

Nervous System Diseases

Drug Highest PhasePending

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

100 Clinical Results associated with TAAR5

100 Translational Medicine associated with TAAR5

0 Patents (Medical) associated with TAAR5

Literatures (Medical) associated with TAAR5

01 Sep 2024·Pharmacology Biochemistry and Behavior

Ligands of the trace amine-associated receptors (TAARs): A new class of anxiolytics

Review

Author: Alnefeesi, Yazen ; Sukhanov, Ilya ; Gainetdinov, Raul R

Most cases of anxiety are currently treated with either benzodiazepines or serotonin reuptake inhibitors. These drugs carry with them risks for a multitude of side effects, and patient compliance suffers for this reason. There is thus a need for novel anxiolytics, and among the most compelling prospects in this vein is the study of the TAARs. The anxiolytic potential of ulotaront, a full agonist at the human TAAR1, is currently being investigated in patients with generalized anxiety disorder. Irrespective of whether this compound succeeds in clinical trials, a growing body of preclinical literature underscores the relevance of modulating the TAARs in anxiety. Multiple behavioral paradigms show anxiolytic-like effects in rodents, possibly due to increased neurogenesis and plasticity, in addition to a panoply of interactions between the TAARs and other systems. Crucially, multiple lines of evidence suggest that the TAARs, particularly TAAR1, TAAR2, and TAAR5, are expressed in the extended amygdala and hippocampus. These regions are central in the actuation of anxiety, and are particularly susceptible to neurogenic and neuroplastic effects which the TAARs are now known to regulate. The TAARs also regulate the dopamine and serotonin systems, both of which are implicated in anxiety. Ligands of the TAARs may thus constitute a new class of anxiolytics.

01 Jan 2024·S.S. Korsakov Journal of Neurology and Psychiatry

Polymorphic variants in the cluster of genes encoding trace amine receptors and cognitive functioning in patients with schizophrenia spectrum disorders and healthy controls

Article

Author: Golimbet, V E ; Plakunova, V V ; Lezheiko, T V ; Alfimova, M V

OBJECTIVETo evaluate the association of polymorphisms in the TAAR1-9 gene cluster on chromosome 6 with cognitive functions in patients with schizophrenia spectrum disorders and healthy controls.MATERIAL AND METHODSPatients with schizophrenia spectrum disorders (n=216) and healthy people without a family history of mental disorders (n=240) completed a battery of cognitive tests, from which individual indices of cognitive functioning were derived. Associations of the cognitive index with 22 polymorphisms in the TAAR genes were assessed using ANCOVA controlling for sex, age, genetic structure of the sample, and polygenic risk scores of schizophrenia and intelligence.RESULTSAn interaction effect between group and genotype on the cognitive index was found at the rs3813355 site in the TAAR5 gene (F=6.68; p=0.010; η²_p=0.02). A post hoc analysis revealed genotype-related differences in the patient group. Homozygotes for the common A allele had a milder cognitive deficit than carriers of the minor G allele (t=2.75; p=0.032; Cohen's d=0.38). The effect of genotype on cognitive index remained significant after the inclusion of disease duration and negative symptoms in the model (F=7.99; p=0.005; η²_p=0.04). Of the individual cognitive indicators, associations with genotype were found for working memory and attention (F=8.25; p=0.005; η²p=0.05), cognitive flexibility (F=5.82; p=0.017; η²_p=0.05) and verbal episodic memory (F=6.75; p=0.011; η²_p=0.05).CONCLUSIONThe results are consistent with the assumption of the role of the TAAR5 genetic polymorphism in the variability of cognitive deficits in patients with schizophrenia.

13 Nov 2023·Journal of Chemical Information and Modeling

Structure-Based Discovery of Mouse Trace Amine-Associated Receptor 5 Antagonists

Article

Author: Nicoli, Alessandro ; Di Pizio, Antonella ; Weber, Verena ; Gainetdinov, Raul R ; Gustincich, Stefano ; Steuer, Alexandra ; Lang, Roman ; Espinoza, Stefano ; Bon, Carlotta

Trace amine-associated receptors (TAARs) were discovered in 2001 as new members of class A G protein-coupled receptors (GPCRs). With the only exception of TAAR1, TAAR members (TAAR2-9, also known as noncanonical olfactory receptors) were originally described exclusively in the olfactory epithelium and believed to mediate the innate perception of volatile amines. However, most noncanonical olfactory receptors are still orphan receptors. Given its recently discovered nonolfactory expression and therapeutic potential, TAAR5 has been the focus of deorphanization campaigns that led to the discovery of a few druglike antagonists. Here, we report four novel TAAR5 antagonists identified through high-throughput screening, which, along with the four ligands published in the literature, constituted our starting point to design a computational strategy for the identification of TAAR5 ligands. We developed a structure-based virtual screening protocol that allowed us to identify three new TAAR5 antagonists with a hit rate of 10%. Despite lacking an experimental structure, we accurately modeled the TAAR5 binding site by integrating comparative sequence- and structure-based analyses of serotonin receptors with homology modeling and side-chain optimization. In summary, we have identified seven new TAAR5 antagonists that could serve as lead candidates for the development of new treatments for depression, anxiety, and neurodegenerative diseases.

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TAAR5

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