Abstract
AHR-10037 is an anti-inflammatory compound possessing analgesic and antipyretic properties and a high therapeutic index. AHR-10037 was comparable to indomethacin in suppressing acute (Evans blue-carrageenan pleural effusion) and chronic (adjuvant-induced arthritis) inflammation. There was a delayed onset of antipyresis (yeast-induced hyperthermia in rats), analgesia (acetylcholine-induced abdominal constriction in mice) and inhibition of caster oil-induced diarrhea in rats. Antipyresis occurred 3 hours after administration of AHR-10037, 4 mg/kg, PO, vs 1 hour after administration of acetylsalicylic acid, 100 mg/kg, PO; maximum analgesic activity (ED50-4.1 mg/kg) occurred at 4 hours. AHR-10037 was inferior to indomethacin in suppressing castor oil-induced diarrhea in rats. The therapeutic index of AHR-10037 (relating acute anti-inflammatory potency to gastric toxicity potency relative to indomethacin) ranged from 56–91. The pharmacological profile suggests that AHR-10037 is a prodrug convertedin vivo to a cyclooxygenase inhibitor.
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Sancilio, L.F., Nolan, J.C., Wagner, L.E. et al. AHR-10037, a non-steroidal anti-inflammatory compound of low gastric toxicity. Agents and Actions 31, 117–126 (1990). https://doi.org/10.1007/BF02003231
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DOI: https://doi.org/10.1007/BF02003231