Pirisino R, Bianchini F, Banchelli G, Ignesti G, Raimondi L, Pecori-Vettori L, Rafanelli D
Pharmacol Res Commun. 1986 Mar;18(3):241-56. doi: 10.1016/0031-6989(86)90122-0.
The activity of 2-phenylpyrazolo-4-ethyl-4,7-dihydro [1,5a]pyrimidin-7-one (FPP028), a non-acidic, analgesic, antipyretic, and anti-inflammatory compound, was investigated in a number of pharmacological tests performed in rats. The anti-inflammatory properties of FPP028 were evaluated through the carrageenan induced paw edema and the cotton pellet induced granuloma and compared with the activity of indomethacin, phenylbutazone, and isoxicam; as a result, the activity of FPP028 was shown to be similar to that of the latter compounds. To assess the analgesic properties of FPP028 in comparison with indomethacin and phenylbutazone, the Randall and Sellitto and the mouse-writhing tests were used; in both tests, FPP028 demonstrated a significant analgesic activity. FPP028 was shown to possess antipyretic properties in the test of yeast-induced pyrexia. The gastro-erosive activity of phenylbutazone and FPP028 was studied in restraint-stressed rats; in such test the ulcerogenic activity of phenylbutazone appeared to be dose-related; conversely, FPP028 demonstrated a gastro-protective effect since the number of gastric lesions induced either by stress or phenylbutazone treatment was decreased bu FPP028. Our data show that FPP028 is endowed with most of the pharmacological properties of the classic antiinflammatory drugs. Further studies are however needed to more fully elucidate its mechanism of action because our in-vivo data indicate that FPP028 is not an inhibitor of prostaglandin biosynthesis.
2-苯基吡唑并[1,5-a]嘧啶-7-酮(FPP028)是一种非酸性、具有镇痛、解热和抗炎作用的化合物,我们在大鼠身上进行了多项药理试验,对其活性进行了研究。通过角叉菜胶诱导的爪肿胀和棉球诱导的肉芽肿来评估FPP028的抗炎特性,并与吲哚美辛、保泰松和异恶酰胺的活性进行比较;结果表明,FPP028的活性与后几种化合物相似。为了评估FPP028与吲哚美辛和保泰松相比的镇痛特性,采用了兰德尔-塞利托试验和小鼠扭体试验;在这两种试验中,FPP028均表现出显著的镇痛活性。在酵母诱导发热试验中,FPP028显示出解热特性。在束缚应激大鼠中研究了保泰松和FPP028的胃糜烂活性;在该试验中,保泰松的致溃疡活性似乎与剂量相关;相反,FPP028表现出胃保护作用,因为应激或保泰松治疗诱导的胃损伤数量因FPP028而减少。我们的数据表明,FPP028具有经典抗炎药物的大多数药理特性。然而,由于我们的体内数据表明FPP028不是前列腺素生物合成的抑制剂,因此需要进一步研究以更全面地阐明其作用机制。