新型解热镇痛药1,4 - 二氢 - 1 - 乙基 - 7 - 苯基吡咯并[1,2 - a]嘧啶 - 4 - 酮的药理特性
The pharmacological properties of 1,4-dihydro-1-ethyl-7-phenylpyrrol (1,2-a)-pyrimidine-4-one, a new antipyretic and analgesic drug.
作者信息
Evangelista S, Pirisino R, Perretti F, Fantozzi R, Brunelleschi S, Malmberg-Aiello P, Bartolini A
机构信息
Pharmacology Department, Menarini Pharmaceuticals, Florence, Italy.
出版信息
Drugs Exp Clin Res. 1987;13(8):501-8.
The antipyretic, analgesic, antinflammatory and antiulcerogenic properties of a new compound 1,4 dihydro-1-ethyl-7-phenylpyrrol (1,2-a)-pyrimidine-4-one (V33) are described. V33 on a mg/kg basis possesses antipyretic and analgesic properties at doses lower than paracetamol and which do not produce hypothermia or motor impairment. V33 possesses antiinflammatory activity and decreases the production of LTB4 from inflammatory exudates without affecting PGE2 content. V33 is not only devoid of gastric ulcerogenic properties but exerts antiulcer activity toward various ulcerogenic stimuli. Lethal dose 50% (LD50) of V33 is higher that of paracetamol.
描述了一种新化合物1,4-二氢-1-乙基-7-苯基吡咯并[1,2-a]嘧啶-4-酮（V33）的解热、镇痛、抗炎和抗溃疡特性。以毫克/千克为基础，V33在低于对乙酰氨基酚的剂量下具有解热和镇痛特性，且不会引起体温过低或运动障碍。V33具有抗炎活性，可降低炎症渗出物中白三烯B4的产生，而不影响前列腺素E2的含量。V33不仅没有致胃溃疡的特性，而且对各种致溃疡刺激具有抗溃疡活性。V33的半数致死剂量（LD50）高于对乙酰氨基酚。
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