1,6-Dimethyl-4-oxo-1,6,7,8,9,9a-hexahydro-4H-pyrido [1,2-a] pyrimidine-3-carboxamide (Chinoin-127), a potent non-narcotic analgesic and antiinflammatory agent.
1,6-Dimethyl-4-oxo-1,6,7,8,9,9a-hexahydro-4H-pyrido[1,2-a]pyrimidine-3-carbamide (Chinoin 127), a non-narcotic analgesic with potent antiinflammatory activity is described. Chinoin-127 is more potent as an analgesic in the hot plate, Randall-Selitto and writhing tests than is acetylsalicylic acid (ASA) and an effective antiphlogistic agent in a battery of tests (carrageenin, kaolin and dextran induced rat paw edema, Northover test, carrageenin induced abscess, implanted cotton pellet method, adjuvant arthritis) used for measuring antiinflammatory activity. The PG-synthesis inhibitors (indometacin, suprofen) were found to be devoid of analgesic activity, and great test-dependent variations in their antiinflammatory effect were observed. They proved to be inactive in the Northover test. Unusual grade of inhibition in the carrageenin-induced rat paw edema test was obtainable by the simultaneous administration of Chinoin 127 and indometacin.
D000038:Abscess / Q000503:physiopathology; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal; D001169:Arthritis, Experimental / Q000503:physiopathology; D002199:Capillary Permeability / Q000187:drug effects; D002351:Carrageenan; D003911:Dextrans; D004487:Edema / Q000139:chemically induced / Q000503:physiopathology; D005260:Female; D006099:Granuloma / Q000503:physiopathology; D007616:Kaolin; D008297:Male; D051379:Mice; D011453:Prostaglandins / Q000096:biosynthesis; D011744:Pyrimidinones / Q000494:pharmacology* / Q000633:toxicity; D051381:Rats; D013276:Stomach Ulcer / Q000139:chemically induced
D000894:Anti-Inflammatory Agents, Non-Steroidal; D003911:Dextrans; D011453:Prostaglandins; D011744:Pyrimidinones; D007616:Kaolin; D002351:Carrageenan