Anti-inflammatory and analgesic effects of FK3311, a selective inhibitor of cyclooxygenase in inflamed tissues
FK3311 (4'acetyl-2'-「2, 4-difluorophenoxy」 methanesulfonanilide), is a neutral non-steroidal anti-inflammatory compound with improved gastrointestinal tolerance in rats. In in vivo models of adjuvant arthritis and yeast-induced hyperalgesia, FK3311 showed evident anti-inflammatory and anal...
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| Published in: | Japanese Journal of Pharmacology Vol. 61; no. suppl.2; p. 333 |
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| Main Authors: | , |
| Format: | Journal Article |
| Language: | English Japanese |
| Published: |
The Japanese Pharmacological Society
1993
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| Online Access: | Get full text |
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| Abstract | FK3311 (4'acetyl-2'-「2, 4-difluorophenoxy」 methanesulfonanilide), is a neutral non-steroidal anti-inflammatory compound with improved gastrointestinal tolerance in rats. In in vivo models of adjuvant arthritis and yeast-induced hyperalgesia, FK3311 showed evident anti-inflammatory and analgesic effects. FK3311 did not induce gastric lesions. FK3311 inhibited PGE_2 formation but not leukotrienes in adjuvant arthritic and yeast-induced rat paws ex vivo. In PGE_2 formation in gastric mucosa, the effect of FK3311 was 100 times less potent than that of indomethacin. In in vitro assay, FK3311 did not inhibit cyclooxygenase activity of sheep seminal vesicle, rabbit renal medulla and platelets. However, in zymosan-stimulated rat peritoneral neutrophils, FK3311 inhibited PGE_2 formation. These results suggest that FK3311 is a novel anti-inflammatory agent and a selective inhibitor of cyclooxygenase in inflamed tissues. |
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| AbstractList | FK3311 (4'acetyl-2'-「2, 4-difluorophenoxy」 methanesulfonanilide), is a neutral non-steroidal anti-inflammatory compound with improved gastrointestinal tolerance in rats. In in vivo models of adjuvant arthritis and yeast-induced hyperalgesia, FK3311 showed evident anti-inflammatory and analgesic effects. FK3311 did not induce gastric lesions. FK3311 inhibited PGE_2 formation but not leukotrienes in adjuvant arthritic and yeast-induced rat paws ex vivo. In PGE_2 formation in gastric mucosa, the effect of FK3311 was 100 times less potent than that of indomethacin. In in vitro assay, FK3311 did not inhibit cyclooxygenase activity of sheep seminal vesicle, rabbit renal medulla and platelets. However, in zymosan-stimulated rat peritoneral neutrophils, FK3311 inhibited PGE_2 formation. These results suggest that FK3311 is a novel anti-inflammatory agent and a selective inhibitor of cyclooxygenase in inflamed tissues. |
| Author | Hachiro Senoh Takehiro Ochi |
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| Title | Anti-inflammatory and analgesic effects of FK3311, a selective inhibitor of cyclooxygenase in inflamed tissues |
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