Pharmacological studies on EB-382, a new non-steroidal antiinflammatory agents: mode of action of the analgesic effects.

Abstract

The analgesic mechanism of (+/-)-2-[p-[(2-methylallyl)amino]phenyl]propionic acid (EB-382), a new non-steroidal antiinflammatory agent, was studied. EB-382 exerted a potent analgesic effect on yeast-induced hyperalgesia in rats and bradykinin-induced writhing in mice, and its potency was superior to that of ibuprofen. EB-382 had a comparatively weak inhibitory effect on the prostaglandin E2 production from arachidonic acid in sheep seminal vesicle microsomal fraction in vitro. EB-382 exhibited a dose-dependent inhibitory effect on the phospholipase A2 activity in 3T3 mouse fibroblast cells with a different mechanism from steroidal agents, although indomethacin and ibuprofen did not reveal any significant inhibition. EB-382 did not affect the bradykinin-induced contraction of isolated rat uterus. Intracisternal injection of EB-382 did not affect the acetic acid-induced writhing response in mice. From these results, it is suggested that the analgesic effect of EB-382 in inflammation is exerted through its direct peripheral action, and inhibition of prostaglandin biosynthesis via phospholipase A2, rather than cyclooxygenase.

• Authors: T Fujiyoshi, H Iida, M Murakami, M Kuwashima, T Uematsu
• Journal: Chemical & pharmaceutical bulletin (Chem Pharm Bull (Tokyo)) Vol. 37 Issue 3 Pg. 775-7 (Mar 1989) ISSN: 0009-2363 [Print] Japan
• PMID: 2787705 (Publication Type: Journal Article)

Chemical References

• Anti-Inflammatory Agents, Non-Steroidal
• Propionates
• alminoprofen

Topics

• Animals
• Anti-Inflammatory Agents, Non-Steroidal (pharmacology)
• Female
• Male
• Mice
• Mice, Inbred Strains
• Propionates (pharmacology)
• Rats
• Rats, Inbred Strains
• Sheep