Discovery of Trace Amine-Associated Receptor 1 (TAAR1) Agonist 2-(5-(4′-Chloro-[1,1′-biphenyl]-4-yl)-4<i>H</i>-1,2,4-triazol-3-yl)ethan-1-amine (LK00764) for the Treatment of Psychotic Disorders

Discovery of Trace Amine-Associated Receptor 1 (TAAR1) Agonist 2-(5-(4′-Chloro-[1,1′-biphenyl]-4-yl)-4<i>H</i>-1,2,4-triazol-3-yl)ethan-1-amine (LK00764) for the Treatment of Psychotic Disorders

A focused in-house library of about 1000 compounds comprising various heterocyclic motifs in combination with structural fragments similar to β-phenylethylamine or tyramine was screened for the agonistic activity towards trace amine-associated receptor 1 (TAAR1). The screening yielded two closely re...

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Bibliographic Details
Main Authors: Mikhail Krasavin, Alexey Lukin, Ilya Sukhanov, Andrey S. Gerasimov, Savelii Kuvarzin, Evgeniya V. Efimova, Mariia Dorofeikova, Anna Nichugovskaya, Andrey Matveev, Kirill Onokhin, Konstantin Zakharov, Maxim Gureev, Raul R. Gainetdinov
Format: Article
Language:English
Published: MDPI AG 2022-11-01
Series:Biomolecules
Subjects:
schizophrenia
trace amine-associated receptor 1
agonism
1,2,4-triazoles
dopamine transporter knockout rats
dopamine
Online Access:https://www.mdpi.com/2218-273X/12/11/1650

Internet

https://www.mdpi.com/2218-273X/12/11/1650

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