Synthesis and antidepressant activities of aryl alkanol piperidine derivatives.
- Author:
Yong-yong ZHENG
1
;
Kai GAO
;
Zhi-jie WENG
;
Jian-qi LI
Author Information
1. State Key Laboratory of New Drug and Pharmaceutical Process, Shanghai Institute of Pharmaceutical Industry, Shanghai 200040, China.
- Publication Type:Journal Article
- MeSH:
Animals;
Antidepressive Agents;
chemical synthesis;
chemistry;
pharmacology;
Dopamine;
metabolism;
Male;
Mice;
Molecular Structure;
Motor Activity;
drug effects;
Neurotransmitter Uptake Inhibitors;
chemical synthesis;
chemistry;
pharmacology;
Norepinephrine;
metabolism;
Piperidines;
chemical synthesis;
chemistry;
pharmacology;
Random Allocation;
Rats;
Rats, Sprague-Dawley;
Serotonin;
metabolism;
Structure-Activity Relationship;
Swimming;
Synaptosomes;
metabolism
- From:
Acta Pharmaceutica Sinica
2010;45(3):324-329
- CountryChina
- Language:Chinese
-
Abstract:
To explore novel monoamine reuptake inhibitor with antidepressant activity, a series of substituted aryl alkanol piperidine derivatives were designed and synthesized. All of them were new compounds, and their structures were confirmed with 1H NMR and HR-MS. The results showed that compounds 4, 5 and 8 displayed strong 5-HT, NA and DA reuptake inhibiting activities in vitro. Among the tested compounds, 4, 5 and 13 exhibited potent antidepressant activities in the mice forced swimming test. Compounds 4 and 5 have potent antidepressant activities and are worth further development.
