Saito T, Fukuda T, Tajima S, Sukamoto T, Yamashita A, Kanazawa T, Morimoto Y, Shimohara K, Nishimura N, Yokota K
Pharmaceuticals Research Center, Kanebo Ltd., Osaka, Japan.
Arzneimittelforschung. 1988 Feb;38(2):267-72.
Effects of 1-(2-ethoxyethyl)-2(4-methyl-1-homopiperazinyl)benzimidazole difumarate (KB-2413) on the circulation and the other systems were compared with those of ketotifen and chlorpheniramine. 1. Among the effects on the circulation and the respiratory system, KB-2413 as well as ketotifen and chlorpheniramine transiently inhibited respiration at 3 mg/kg i.v. and slightly decreased blood pressure in dogs. KB-2413 slightly decreased heart rate in dogs, but ketotifen slightly increased it. 2. KB-2413 at 100 mg/kg p.o. slightly decreased the volume of gastric juice in rats and dose-dependently increased biliary secretion in rats in the dose range of 10-100 mg/kg i.d. On the other hand, ketotifen and chlorpheniramine decreased biliary secretion. 3. KB-2413 inhibited the spontaneous movements of various isolated smooth muscles at a high concentration of 10(-4) g/ml. 4. The autonomic system in cats and the motor nervous system in rats were not influenced by KB-2413 at 3 mg/kg i.v. 5. The blood clotting system, blood sugar level, urine volume and urinary electrolytes in rats were not affected by KB-2413 in the dose range of 10-100 mg/kg p.o. 6. KB-2413 inhibited carrageenin-induced rat paw edema at 100 mg/kg p.o. In conclusion, KB-2413 showed a less potent effect on the circulation and the other systems than ketotifen and chlorpheniramine, and no results suggested serious side effects of KB-2413.
比较了1-(2-乙氧基乙基)-2-(4-甲基-1-高哌嗪基)苯并咪唑二富马酸盐(KB-2413)对循环系统和其他系统的作用与酮替芬和氯苯那敏的作用。1. 在对循环系统和呼吸系统的作用中，静脉注射3mg/kg时，KB-2413以及酮替芬和氯苯那敏均会短暂抑制犬的呼吸，并使犬的血压略有下降。KB-2413会使犬的心率略有下降，而酮替芬会使其略有上升。2. 口服100mg/kg的KB-2413会使大鼠胃液分泌量略有减少，腹腔注射10-100mg/kg剂量范围内的KB-2413会使大鼠胆汁分泌量呈剂量依赖性增加。另一方面，酮替芬和氯苯那敏会减少胆汁分泌。3. KB-2413在10(-4)g/ml的高浓度下会抑制各种离体平滑肌的自发运动。4. 静脉注射3mg/kg的KB-2413对猫的自主神经系统和大鼠的运动神经系统没有影响。5. 口服10-100mg/kg剂量范围内的KB-2413对大鼠的血液凝固系统、血糖水平、尿量和尿电解质没有影响。6. 口服100mg/kg的KB-2413可抑制角叉菜胶诱导的大鼠足爪肿胀。总之，KB-2413对循环系统和其他系统的作用比酮替芬和氯苯那敏弱，且未发现表明KB-2413有严重副作用的结果。
