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1,6 - 二甲基 - 4 - 氧代 - 1,6,7,8,9,9a - 六氢 - 4H - 吡啶并[1,2 - a]嘧啶 - 3 - 甲酰胺(奇诺因 - 127),一种强效非麻醉性镇痛和抗炎剂。

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.

作者信息

Knoll J, Gyires K, Mészáros Z

出版信息

Arzneimittelforschung. 1979;29(5):766-73.

PMID:315232
Abstract

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.

摘要

1,6 - 二甲基 - 4 - 氧代 - 1,6,7,8,9,9a - 六氢 - 4H - 吡啶并[1,2 - a]嘧啶 - 3 - 甲酰胺(奇诺因127),一种具有强效抗炎活性的非麻醉性镇痛药被描述。在热板法、兰德尔 - 塞利托法和扭体试验中,奇诺因 - 127作为镇痛药比乙酰水杨酸(ASA)更有效,并且在一系列用于测量抗炎活性的试验(角叉菜胶、高岭土和右旋糖酐诱导的大鼠足肿胀、诺思弗试验、角叉菜胶诱导的脓肿、植入棉球法、佐剂性关节炎)中是一种有效的抗炎剂。发现PG合成抑制剂(吲哚美辛、舒洛芬)没有镇痛活性,并且观察到它们的抗炎作用有很大的试验依赖性差异。它们在诺思弗试验中被证明是无活性的。通过同时给予奇诺因127和吲哚美辛,在角叉菜胶诱导的大鼠足肿胀试验中可获得不同寻常程度的抑制。

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