Bioorganic & Medicinal Chemistry Letters published new progress about 5-HT1A receptors Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Recommanded Product: (9Z,12Z)-Methyl octadeca-9,12-dienoate.
Shi, Wenqiang; Wang, Yu; Wu, Chunhui; Yang, Feipu; Zheng, Wei; Wu, Song; Liu, Yongjian; Wang, Zhen; He, Yang; Shen, Jingshan published the artcile< Synthesis and biological investigation of triazolopyridinone derivatives as potential multireceptor atypical antipsychotics>, Recommanded Product: (9Z,12Z)-Methyl octadeca-9,12-dienoate, the main research area is triazolopyridinone derivative preparation multireceptor atypical antipsychotic agent; 5-HT1A receptor; Antipsychotic; Multireceptor; Triazolopyridinone.
A series of triazolopyridinone derivatives originating from the antidepressant trazodone was designed and pharmacol. evaluated. Most of the compounds with a multireceptor functional profile exhibited high potency at the D2, 5-HT1A, and 5-HT2A receptors. Compounds 2-(4-(4-(benzo[b]thiophen-4-yl)piperazin-1-yl)butyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2 H)-one, 2-(4-(4-(benzo[b]thiophen-4-yl)piperazin-1-yl)butyl)-8-fluoro-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one, 2-(4-(4-(benzo[b]thiophen-4-yl)piperazin-1-yl)butyl)-5-methoxy-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one and 2-(4-(4-(benzo[b]thiophen-4-yl)piperazin-1-yl)butyl)-3-oxo-2,3-dihydro-[1,2,4]triazolo[4,3-a]pyridine-6-carbonitrile were selected for further evaluation of druggable potential. Among these compounds, 2-(4-(4-(benzo[b]thiophen-4-yl)piperazin-1-yl)butyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one, as a D2 receptor partial agonist, demonstrated very potent inhibition of quipazine-induced head-twitch response, which validated its 5-HT2A receptor antagonistic efficacy in vivo. 2-(4-(4-(Benzo[b]thiophen-4-yl)piperazin-1-yl)butyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2-H)-one also demonstrated a dose-dependent effect on PCP-induced hyperactivity when administered orally. Thus, 2-(4-(4-(benzo[b]thiophen-4-yl)piperazin-1-yl)butyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one endowed with a triazolopyridinone scaffold represents a valuable lead for the development of novel atypical antipsychotics.
Bioorganic & Medicinal Chemistry Letters published new progress about 5-HT1A receptors Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Recommanded Product: (9Z,12Z)-Methyl octadeca-9,12-dienoate.
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