Hirakawa K, Unno T, Ogino F, Takebe H, Iino T, Nose T
Arzneimittelforschung. 1982;32(9):1071-7.
Diethyl 4-(benzothiazol-2-yl)benzylphosphonate (KB-944), a new Ca-antagonist, in the dose range of 25--200 mg/kg/day, was orally administered to Jcl:SD rats for five consecutive weeks and the following results were obtained. Neither death nor inhibition of body weight gain nor any toxic symptoms of the drug were noted in rats but an increase in water intake was found in the rats treated with over 100 mg/kg/day of KB-944. In plasma there was a decrease in alkaline phosphatase activity, creatinine level and cholinesterase activity and an increase in GPT activity and total cholesterol level in rats given a higher dosage of the drug. Weight gain of the liver, kidneys, heart, adrenals and ovaries, and degeneration in the epithelium of the renal proximal tubule were observed. However, none of these changes were serious and the maximum non-toxic dose of KB-944 was 25 mg/kg/day.
4-（苯并噻唑-2-基）苄基膦酸二乙酯（KB-944）是一种新型钙拮抗剂，以25-200毫克/千克/天的剂量范围连续五周口服给予Jcl:SD大鼠，得到以下结果。大鼠未出现死亡、体重增加受抑制或该药物的任何毒性症状，但每天给予超过100毫克/千克KB-944的大鼠饮水量增加。给予较高剂量该药物的大鼠血浆中碱性磷酸酶活性、肌酐水平和胆碱酯酶活性降低，谷丙转氨酶活性和总胆固醇水平升高。观察到肝脏、肾脏、心脏、肾上腺和卵巢的重量增加，以及肾近端小管上皮细胞变性。然而，这些变化均不严重，KB-944的最大无毒剂量为25毫克/千克/天。
