Maruyama Y, Anami K, Katoh Y
Arzneimittelforschung. 1978;28(11):2102-7.
Analgesic and antipyretic activities of 2-(4-(2-imidazo-[1,2-a]pyridylphenyl)propionic acid (Y-9213) were studied with various experimental models. The analgesic activity of Y-9213 was found to be more potent than that of indometacin and morphine in the silver nitrate, Randall-Selitto, and phenylquinone writhing tests. Y-9213 also showed an analgesia in the tail pinch and electric stimulation test. On the warm water induced foot withdrawal reflex, Y-9213 was more effective in spinal-sectioned mice than in intact mice similarly to mephenesin and diazepam. Y-9213 was also proved to possess antipyretic activity as potent as indometacin and to be devoid of morphine-like property. Y-9213 exhibited little effect on the respiration and cardiovascular system in dogs. Y-9213 was found to be rapidly absorbed and eliminated from the blood with a half-life of about 2.5 h in rats. These findings indicate that Y-9213 may be an effective and well tolerated antipyretic and analgesic agent.
利用多种实验模型研究了2-(4-(2-咪唑并-[1,2-a]吡啶基苯基)丙酸(Y-9213)的镇痛和解热活性。在硝酸银、兰德尔-塞利托和苯醌扭体试验中，发现Y-9213的镇痛活性比吲哚美辛和吗啡更强。Y-9213在夹尾和电刺激试验中也显示出镇痛作用。在温水诱导的足部退缩反射试验中，与美芬辛和地西泮类似，Y-9213对脊髓切断的小鼠比完整小鼠更有效。还证明Y-9213具有与吲哚美辛相当的解热活性，且不具有吗啡样特性。Y-9213对犬的呼吸和心血管系统影响很小。在大鼠中发现Y-9213能迅速从血液中吸收和消除，半衰期约为2.5小时。这些发现表明Y-9213可能是一种有效且耐受性良好的解热镇痛药。
