A comparative study of the antiinflammatory activity of fentiazac and its major metabolite, p-hydroxy fentiazac.

Abstract

Wy-25,110, the p-OH metabolite of fentiazac was approximately 100 times less potent than fentiazac after oral administration in rat carrageenan edema and 100-130 times less potent as an inhibitor of prostaglandin synthesis by mouse peritoneal macrophages. In addition, Wy-25,110 was one twelfth as active as fentiazac against immunologic-induced inflammation on day 16 in rat adjuvant arthritis. Wy-25,110 was also much less potent than fentiazac when administered intravenously, suggesting that inadequate oral absorption does not account for its lack of potency. Thus it seems unlikely that the p-OH metabolite contributes greatly to the antiinflammatory properties of fentiazac.

• Authors: J Chang, R P Carlson, A J Lewis
• Journal: Agents and actions (Agents Actions) Vol. 15 Issue 3-4 Pg. 443-7 (Oct 1984) ISSN: 0065-4299 [Print] Switzerland
• PMID: 6441470 (Publication Type: Comparative Study, Journal Article)

Chemical References

• Acetates
• Anti-Inflammatory Agents
• Arachidonic Acids
• Thiazoles
• fentiazac
• Arachidonic Acid
• Wy 25110

Topics

• Acetates (pharmacology, therapeutic use)
• Animals
• Anti-Inflammatory Agents (pharmacology, therapeutic use)
• Arachidonic Acid
• Arachidonic Acids (metabolism)
• Arthritis (drug therapy)
• Arthritis, Experimental (drug therapy, metabolism)
• Macrophages (drug effects, metabolism)
• Male
• Rats
• Rats, Inbred Strains
• Thiazoles (pharmacology, therapeutic use)