Ito K, Kagaya H, Fukuda T, Yoshino K, Nose T
Arzneimittelforschung. 1982;32(1):49-55.
2-(5-Ethylpyridin-2-yl)benzimidazole (KB-1043) is a new benzimidazole derivative with marked antiinflammatory, analgesic and antipyretic properties. KB-1043 possesses potent inhibitory activities on the acute inflammatory edema induced by chemical and physical irritants in the hind paw of rats, but almost ineffective (similar to tiaramide) against adjuvant-induced polyarthritis in the rat. The antagonistic effects of KB-1043 on increased vascular permeability are more potent than those of phenylbutazone, and the analgesic effects of KB-1043 on the pain induced by chemical and mechanical stimulations were nearly equal to, or slightly less potent than, those of tiaramide and phenylbutazone. The fevers induced by brewer's yeast and polysaccharide from Pseudomonas fluorescens (T.T.G.) were lowered by KB-1043. THe ulcerogenic activity of KB-1043 was weaker than those of tiaramide and phenylbutazone. The therapeutic index of KB-1043 therefore is superior to those of tiaramide and phenylbutazone.
2-(5-乙基吡啶-2-基)苯并咪唑(KB-1043)是一种新型苯并咪唑衍生物，具有显著的抗炎、镇痛和解热特性。KB-1043对大鼠后爪由化学和物理刺激诱导的急性炎性水肿具有强效抑制活性，但对大鼠佐剂诱导的多关节炎几乎无效(类似于替拉米特)。KB-1043对血管通透性增加的拮抗作用比保泰松更强，且KB-1043对化学和机械刺激诱导的疼痛的镇痛作用几乎与替拉米特和保泰松相当，或略弱于它们。KB-1043可降低啤酒酵母和荧光假单胞菌多糖(T.T.G.)诱导的发热。KB-1043的致溃疡活性比替拉米特和保泰松弱。因此，KB-1043的治疗指数优于替拉米特和保泰松。
