Pharmacological properties of N-methoxy-3-(3,5-ditert-butyl-4-hydroxybenzylidene)-2-pyrrolidone (E-5110), a novel nonsteroidal antiinflammatory agent.
The antiinflammatory activity of a novel pyrrolidone derivative E-5110 was investigated using anti-inflammatory, analgesic and antipyretic animal models in comparison to indomethacin (IND) and piroxicam (PIR). The acute antiinflammatory activity of E-5110 on carrageenin paw edema was similar to IND, and half of PIR. E-5110 inhibited the pleural exudate volume and leucocyte infiltration in a reversed passive Arthus reaction more potent than IND. The chronic inflammatory responses in the established adjuvant- and type II collagen-induced arthritis were suppressed by E-5110 similar to IND and PIR. The analgesic potency of E-5110 was similar to IND and PIR, but the antipyretic activity of E-5110 was more potent than that of IND, and slightly more potent than that of PIR. The ulcerogenic effect of E-5110 on rat gastric mucosa was less than that of the reference drugs.
D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal; D005334:Fever / Q000188:drug therapy; D007213:Indomethacin / Q000494:pharmacology / Q000633:toxicity; D007249:Inflammation / Q000188:drug therapy; D010146:Pain / Q000188:drug therapy; D010894:Piroxicam / Q000494:pharmacology / Q000633:toxicity; D011760:Pyrrolidinones / Q000494:pharmacology* / Q000633:toxicity; D051381:Rats; D013276:Stomach Ulcer / Q000139:chemically induced
D000894:Anti-Inflammatory Agents, Non-Steroidal; D011760:Pyrrolidinones; C054091:E 5110; D010894:Piroxicam; D007213:Indomethacin