Novel synthetic method and analgesic activity of tepoxalin.
- Author:
Xiao-he GUO
1
;
Hong-wei ZHANG
;
Le TAO
;
Yu-jiang LI
;
Ping-an WANG
;
Shu-yang WANG
;
Qiang WANG
;
Li-hong DONG
;
Jun-biao CHANG
Author Information
1. High & New Technology Research Center of Henan Academy of Sciences, Zhengzhou, China. drzhangguo@sina.com
- Publication Type:Journal Article
- MeSH:
Administration, Oral;
Analgesics;
administration & dosage;
chemical synthesis;
pharmacology;
Animals;
Anti-Inflammatory Agents, Non-Steroidal;
administration & dosage;
chemical synthesis;
pharmacology;
Cyclooxygenase Inhibitors;
administration & dosage;
chemical synthesis;
pharmacology;
Diclofenac;
pharmacology;
Imidazoles;
chemistry;
Ionic Liquids;
chemistry;
Lipoxygenase Inhibitors;
administration & dosage;
chemical synthesis;
pharmacology;
Mice;
Pain Measurement;
drug effects;
Pyrazoles;
administration & dosage;
chemical synthesis;
pharmacology;
Random Allocation
- From:
Acta Pharmaceutica Sinica
2010;45(10):1260-1264
- CountryChina
- Language:Chinese
-
Abstract:
Tepoxalin is a potent inhibitor of both the cyclooxygenase and lipoxygenase pathways of the arachidonic acid cascade, as well as a potent anti-inflammatory and control-pain (postoperation, arthritis et. al.) agent. The new method about the use of novel synthesis reagents and the first using ionic liquid as reactive solvent to synthesize tepoxalin were presented in this paper. The ionic liquid can be easily recycled and reused for several runs efficiently. The analgesic activity of tepoxalin was detected by acetic acid test on mice. The analysis of variance showed that oral administration of tepoxalin could significantly inhibit the number of writhing response within 1 hour and prolong the latent time in a dose dependent manner as compared with CMC control group (P < 0.05). At the same time, tepoxalin had the same analgesic activity as diclofenac sodium.