Thromboxane A2 antagonistic action of a new anti-ulcer agent, azuletil sodium (KT1-32).

Abstract

The TXA2/PGH2 receptor antagonistic activity of azuletil sodium (KT1-32), a new anti-ulcer agent, was examined. KT1-32 competitively antagonized the contraction of canine gastric arteries induced by U-46619, PGF2 alpha, and PGE2, whereas it had no effect on the PGF2 alpha-, PGE2- and LTD4-induced contraction of guinea-pig ileum, which was not affected by U-46619. In anesthetized dogs, KT1-32 significantly reduced the U-46619-induced decrease in gastric arterial blood flow. Gastric contraction induced by U-46619 in anesthetized rats was markedly inhibited by KT1-32. KT1-32 showed no influence on TXA2 synthetase and cyclooxygenase activities. These results indicate that KT1-32 is a competitive TXA2/PGH2 receptor antagonist, which may be important as to the effectiveness of KT1-32 against gastric ulcer.

• Authors: S Mochizuki, S Wakabayashi, A Tomiyama, N Satake, S Shibata
• Journal: Scandinavian journal of gastroenterology. Supplement (Scand J Gastroenterol Suppl) Vol. 162 Pg. 194-7 ( 1989) ISSN: 0085-5928 [Print] England
• PMID: 2595296 (Publication Type: Journal Article)

Chemical References

• Anti-Ulcer Agents
• Azulenes
• Prostaglandin Endoperoxides, Synthetic
• Sesquiterpenes
• azulene SN
• Thromboxane A2
• 15-Hydroxy-11 alpha,9 alpha-(epoxymethano)prosta-5,13-dienoic Acid
• azuletil

Topics

• 15-Hydroxy-11 alpha,9 alpha-(epoxymethano)prosta-5,13-dienoic Acid
• Animals
• Anti-Ulcer Agents (pharmacology)
• Arteries
• Azulenes
• Dogs
• Guinea Pigs
• Male
• Muscle Contraction (drug effects)
• Prostaglandin Endoperoxides, Synthetic (antagonists & inhibitors, pharmacology)
• Pylorus (blood supply)
• Rats
• Rats, Inbred Strains
• Regional Blood Flow (drug effects)
• Sesquiterpenes (pharmacology)
• Stomach (blood supply, drug effects)
• Thromboxane A2 (antagonists & inhibitors)
• Vasoconstriction (drug effects)