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Synthesis and antiinflammatory, analgesic, and antipyretic testing of 4-[1-oxo-(3-substituted aryl)-2-propenyl]-3-phenylsydnones and of 3-[4-[3-(substituted aryl)-1-oxo-2-propenyl]phenyl]sydnones.

Two series of styrylcarbonyl 3-phenylsydnone derivatives, 4-[1-oxo-(3-substituted aryl)-2-propenyl]-3-phenylsydnones (series 1, 1-21) and 3-[4-[3-(substituted aryl)-1-oxo-2-propenyl]phenyl]sydnones (series II, 22-40), were synthesized and evaluated pharmacologically at a dose of 100 mg/kg po. Eleven compounds in series I plus one in series II and six in series I plus seven in series II were active in the carrageenan-induced edema and acetic acid-induced writhing assays, respectively. Compound 35 in the latter assay showed activity somewhat similar to that of the positive control drug, aspirin, administered at the same dosage. Compounds 11, 17, and 23 showed activity in both assays, and 23 also was active in the adjuvant-induced arthritis assay.

Acetates↗

[Analgesic and antipyretic effects of cyproheptadine].

Cyproheptadine-HCl raised the pain thresholds during hot plat test and writhing test in mice and tail flick test in rats, strengthened the hypnotic action by subthreshold dosage of sodium pentobarbital and chloral hydrate. The ED50 were 4.4 (3.2-5.7) and 12.4 (8.4-18.2) mg/kg 30 min after ip cyproheptadine in mice and rats, respectively. The ED50 was 0.14 (0.12-0.18) mg/kg 90 min after icv cyproheptadine in mice. Cyproheptadine po 20, 40 mg/kg and ip 10, 20 mg/kg showed significant antipyretic effects on yeast-induced pyrexia in rats.

Animals↗