Design, synthesis and antidepressive activity of duloxetine derivatives.
- Author:
Yan-ping ZHANG
1
;
Rui XUE
;
Xin-hua HE
;
Yong-gang MENG
;
You-zhi ZHANG
;
Bo-hua ZHONG
Author Information
1. Institute of Pharmacology and Toxicology, Academy of Military Medical Sciences, Beijing 100850, China.
- Publication Type:Journal Article
- MeSH:
Animals;
Antidepressive Agents;
chemical synthesis;
chemistry;
pharmacology;
Duloxetine Hydrochloride;
Hindlimb Suspension;
Male;
Mice;
Mice, Inbred ICR;
Molecular Structure;
Serotonin 5-HT1 Receptor Antagonists;
pharmacology;
Structure-Activity Relationship;
Swimming;
Thiophenes;
chemical synthesis;
chemistry;
pharmacology
- From:
Acta Pharmaceutica Sinica
2010;45(7):869-873
- CountryChina
- Language:Chinese
-
Abstract:
In this paper, duloxetine was chosen as the lead compound. The pharmacophores with 5-HT(1A) antagonism activity were used to replace the naphthyl of duloxetine. A series of duloxetine derivatives had been designed and synthesized and whose structures were confirmed with elemental analysis, MS and H NMR. All synthesized compounds were tested by tail suspension test and forced swimming test in vivo. The test results revealed that most of the compounds have shown better activity than duloxetine at the same dosage. Some of them are worth to be studied further.
