Anti-inflammatory and safety profile of DuP 697, a novel orally effective prostaglandin synthesis inhibitor.

摘要: DuP 697 (5-bromo-2[4-fluorophenyl]-3-[4-methylsulfonylphenyl]-thiophene) is a potent inhibitor of paw swelling in nonestablished and established adjuvant arthritis rats (ED50 = 0.03 0.18 mg/kg/day, respectively). had no effect on phenylquinone writhing greater than 100 mg/kg), but was analgetic against inflammation-related pain the Randall-Selitto assay (ED30 3.5 mg/kg) very antipyretic agent 0.05 mg/kg). The drug not ulcerogenic at single doses up to 400 mg/kg. (5 mg/kg i.v.) did alter renal blood flow or vascular response angiotensin II furosemide-pretreated, volume-depleted rats. In contrast, indomethacin decreased potentiated these animals. moderate bull seminal vesicle prostaglandin (PG) synthesis (IC50 2.4 X 10(-5) M) rat brain PG 4.5 10(-6) ineffective kidney 7.5 M). These differential effects by various tissues may account for its high potency as an anti-inflammatory minimal toxicity profile.