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Pharmacological properties of N-methoxy-3-(3,5-ditert-butyl-4-hydroxybenzylidene)-2-pyrrolidone (E-5110), a novel nonsteroidal antiinflammatory agent

  • Antiinflammatory/Antiarthritic Agents
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Abstract

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.

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Authors and Affiliations

  1. Eisai Research Laboratories, Eisai Co., Ltd., Tokodai 5-chome, Toyosato-machi, Tsukuba-gun, 300-26, Ibaraki, Japan

    H. Shirota, K. Katayama, H. Ono, K. Chiba, S. Kobayashi, K. Terato, H. Ikuta & I. Yamatsu

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  1. H. Shirota
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  2. K. Katayama
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  3. H. Ono
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  4. K. Chiba
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  5. S. Kobayashi
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  6. K. Terato
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  7. H. Ikuta
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  8. I. Yamatsu
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Shirota, H., Katayama, K., Ono, H. et al. Pharmacological properties of N-methoxy-3-(3,5-ditert-butyl-4-hydroxybenzylidene)-2-pyrrolidone (E-5110), a novel nonsteroidal antiinflammatory agent. Agents and Actions 21, 250–252 (1987). https://doi.org/10.1007/BF01966481

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  • DOI: https://doi.org/10.1007/BF01966481

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