Design, synthesis, and biological evaluation of piperazine derivatives involved in the 5-HT_1AR/BDNF/PKA pathway.

ABSTRACT: In this study, four series of piperazine derivatives were designed, synthesised and subjected to biological test, and compound 6a with potential antidepressant activity was obtained. An affinity assay of compound 6a with 5-hydroxytryptamine (serotonin, 5-HT)_1A receptor (5-HT_1AR) was undertaken, and the effects on the 5-HT level in the brains of mice were also tested. The results showed that compound 6a had the best affinity with 5-HT_1AR (K_i = 1.28 nM) and significantly increased the 5-HT level. The expression levels of 5-HT_1AR, BDNF, and PKA in the hippocampus were analysed by western blot and immunohistochemistry analyses. The results showed that the expression of 5-HT_1AR, BDNF, and PKA in the mo

SUBMITTER: Zhou H 

PROVIDER: S-EPMC11721615 | biostudies-literature | 2024 Dec

REPOSITORIES: biostudies-literature