Dorfman R I
Arzneimittelforschung. 1975 Feb;25(2A):278-81.
The need for a nonsteroidal anti-inflammatory agent effective in rheumatoid arthritis, osteoarthritis, gout, ankylosing spondylitis and related diseases with reduced side effects when compared to existing drugs led us to develop naproxen: d-2-(6'-methoxy-2'-naphthyl)-propionic acid. This new agent is a highly effective anti-inflammatory, analgetic, and antipyretic agent in the rodent administered orally. In a rat paw edema test for anti-inflammatory activity naproxen was 55 times more active than aspirin. Analgetic activity was assessed by three different assay procedures. In the mouse phenylquinone writhing test naproxen was 7 times as effective as aspirin. In the rat yeast-induced paw edema and the rat carrageenin paw edema analgetic assays the test compound was 10 and 20 times more effective than aspirin, respectively. A yeast-induced pyresis model in the rat indicated that naproxen was 22 times more potent than the standard aspirin. The relative potency of naproxen to phenylbutazone and indometacin is presented.
由于需要一种对类风湿性关节炎、骨关节炎、痛风、强直性脊柱炎及相关疾病有效的非甾体抗炎药,且与现有药物相比副作用更小,我们研发了萘普生:d - 2 -(6'-甲氧基 - 2'-萘基)-丙酸。这种新药在经口给药的啮齿动物中是一种高效的抗炎、镇痛和解热药物。在大鼠足爪水肿抗炎活性试验中,萘普生的活性比阿司匹林高55倍。通过三种不同的测定方法评估镇痛活性。在小鼠苯醌扭体试验中,萘普生的效果是阿司匹林的7倍。在大鼠酵母诱导的足爪水肿和大鼠角叉菜胶足爪水肿镇痛试验中,受试化合物的效果分别比阿司匹林高10倍和20倍。大鼠酵母诱导发热模型表明,萘普生的效力比标准阿司匹林高22倍。文中给出了萘普生相对于保泰松和吲哚美辛的相对效力。