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Non-acidic pyrazoles: Inhibition of prostaglandin production, carrageenan oedema and yeast fever

  • Immunosuppression and Inflammation
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Abstract

Prostaglandin production from mouse peritoneal macrophages was elicited by the tumour promotor 12-O-tetradecanoyl-phorbol-13-acetate (TPA). The inhibitory potency (IC50) of metamizole and its major metabolites as well as other non-acidic pyrazoles was defined in this system. A reliable IC50-value could not be assigned to metamizole. Isopropylaminophenazone was as active as acetylsalicylic acid while aminophenazone and methylaminophenazone, the major metabolites of metamizole, were about 10 times and phenazone 100 times less potent than acetylsalicylic acid, The major excretion products of metamizole, 4-formyl- and 4-acetyl-aminophenazone were inactive. The IC50-values obtained agree with those necessary for manifestation of anti-inflammatory effects in rats but are up to 10 times higher than those measurable in human plasma after administration of analgesic-antipyretic doses.

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Authors and Affiliations

  1. Department of Pharmacology, University of Erlangen, Universitätstraße 22, D-8520, Erlangen

    Kay Brune

  2. Department of Pharmacology, Hoechst AG, D-6230, Frankfurt, Germany

    Hans Alpermann

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  1. Kay Brune
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  2. Hans Alpermann
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Brune, K., Alpermann, H. Non-acidic pyrazoles: Inhibition of prostaglandin production, carrageenan oedema and yeast fever. Agents and Actions 13, 360–363 (1983). https://doi.org/10.1007/BF01971489

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  • DOI: https://doi.org/10.1007/BF01971489

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