Zhu, Chen; Li, Xinwei; Zhao, Bangyi; Peng, Weiqing; Li, Wei; Fu, Wei published the artcile< Discovery of aryl-piperidine derivatives as potential antipsychotic agents using molecular hybridization strategy>, Product Details of C12H13FN2O, the main research area is hybridization aryl piperidine derivative preparation antipsychotic; 5-HT(2A) receptor antagonist; Antipsychotic; D(2) receptor antagonist; Molecular hybridization; Multi-target strategy.
Schizophrenia is a chronic, disabling mental disorder that affects about one percent of world’s population. Drugs acting on multiple targets have been demonstrated to provide superior efficacy in schizophrenia than agents acting on single target. In this study, based on FW01, a selective potent 5-HT1A receptor agonist discovered via dynamic pharmacophore-based virtual screening, mol. hybridization strategy was employed to optimize its in vitro activity over D2 and 5-HT2A receptors. The optimized compound 9f was found to show dual potent D2 and 5-HT2A receptors antagonistic activity. In addition, compound 9f showed good in vivo metabolic stability with t1/2 of 2 h in ICR mice and good capability to penetrate the blood-brain barrier with Kp value of 4.03. These results demonstrated that the dual D2 and 5-HT1A receptor antagonist 9f could serve as a promising lead compound to discover potent antipsychotic agents.
European Journal of Medicinal Chemistry published new progress about 5-HT2A antagonists. 84163-77-9 belongs to class benzisoxazole, and the molecular formula is C12H13FN2O, Product Details of C12H13FN2O.
Referemce:
Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics