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Discovery and In Vivo Efficacy of Trace Amine-Associated Receptor 1 (TAAR1) Agonist 4-(2-Aminoethyl)-<i>N</i>-(3,5-dimethylphenyl)piperidine-1-carboxamide Hydrochloride (AP163) for the Treatment of Psychotic Disorders.

Author: EfimovaEvgeniya V, GainetdinovRaul R, GureevMaxim, KanovEvgeny V, KomarovaKristina, KrasavinMikhail, KuvarzinSavelii R, LukinAlexey, MurtazinaRamilya Z, OnokhinKirill, PeshkovAnatoly A, SmirnovaDaria, VinogradovaLyubov, ZakharovKonstantin

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.

Overview

This study investigated the activity of a set of analogs based on a 4-(2-aminoethyl)piperidine core as potential modulators of trace amine-associated receptor 1 (TAAR1). The study identified one compound (AP163) that displayed a statistically significant and dose-dependent reduction in hyperlocomotion in DAT-KO rats, suggesting its potential as a novel treatment option for disorders associated with increased dopaminergic function, such as schizophrenia.
Paper Details　
Original Abstract of the Article :
Starting from a screening hit, a set of analogs was synthesized based on a 4-(2-aminoethyl)piperidine core not associated previously with trace amine-associated receptor 1 (TAAR1) modulation in the literature. Several structure-activity relationship generalizations have been drawn from the observed ...See full text at original site
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引用元：
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9569940/

データ提供：米国国立医学図書館（NLM）

TAAR1 Agonist as a Potential Treatment for Psychotic Disorders

The study delves into the exciting world of [trace amine-associated receptor 1 (TAAR1)] modulation as a potential therapeutic avenue for [psychotic disorders]. Researchers have identified a novel TAAR1 agonist, AP163, which shows promise for treating disorders characterized by increased dopaminergic function. The research team employed a combination of [chemical synthesis], [structure-activity relationship studies], and [in vivo testing] to evaluate the efficacy of this compound.

AP163: A Promising Lead for Treating Psychotic Disorders

The study reports that AP163 exhibited a significant and dose-dependent reduction in hyperlocomotion in a rat model of dopamine-dependent hyperlocomotion. This suggests that AP163 has the potential to effectively manage psychotic disorders by targeting dopamine signaling pathways. Further preclinical characterization of AP163 is warranted to explore its potential as a novel therapeutic option.

TAAR1 Modulation: A New Frontier in Psychotic Disorder Treatment

The discovery of TAAR1 agonists like AP163 opens up new avenues for treating psychotic disorders. This research provides compelling evidence for the potential of TAAR1 modulation as a therapeutic strategy. As we navigate the complex landscape of mental health, this research offers a glimmer of hope for developing more effective and targeted treatments for patients.

Dr.Camel's Conclusion

Just like a camel navigating a scorching desert, scientists are exploring novel pathways to treat complex brain disorders. The identification of AP163 as a potential TAAR1 agonist offers a promising oasis in the search for effective treatments for psychotic disorders. This research represents a significant step towards understanding the intricate workings of the brain and finding solutions for those in need.

Date :
  1. Date Completed 2022-10-17
  2. Date Revised 2022-10-19
Further Info :

Pubmed ID

36232878

DOI: Digital Object Identifier

PMC9569940

Related Literature

Article Analysis
・Effective treatment of psychotic disorders
SNS
PICO Info
in preparation
Languages

English

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