Huang, Ling; Gao, Lanchang; Zhang, Xiaohua; Yin, Lei; Hu, Jintao; Song, Ting; Chen, Yin published the artcile< Synthesis and pharmacological evaluation of piperidine (piperazine)-amide substituted derivatives as multi-target antipsychotics>, Name: 6-Fluoro-3-(4-piperidinyl)-1,2-benzisoxazole, the main research area is piperidine piperazine amide derivative antipsychotic; Amide; Antipsychotic; Multi-target; Piperazine; Piperidine.
We report the optimization of a series of novel amide-piperidine (piperazine) derivatives using the multiple ligand approach with dopamine and serotonin receptors. Of the derivatives, compound 11 (I) exhibited high affinity for the D2, 5-HT1A, and 5-HT2A receptors, but low affinity for the 5-HT2C and histamine H1 receptors and human ether-a-go-go-related gene (hERG) channels. In vivo, compound 11 reduced apomorphine-induced climbing, MK-801-induced hyperactivity and DOI-induced head twitching without observable catalepsy, even at the highest dose tested. In addition, it exhibited suppression in a CAR test. Furthermore, in a novel object recognition task, it displayed pro-cognition properties. Therefore, compound 11 is a promising candidate multi-target antipsychotic.
Bioorganic & Medicinal Chemistry Letters published new progress about 5-HT1A receptors Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 84163-77-9 belongs to class benzisoxazole, and the molecular formula is C12H13FN2O, Name: 6-Fluoro-3-(4-piperidinyl)-1,2-benzisoxazole.
Referemce:
Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics