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新型抗过敏药物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)对纤毛运动的影响

Influence of 1-(2-ethoxyethyl)-2-(4-methyl-1-homopiperazinyl)benzimidaz ole difumarate (KB-2413), a new antiallergic, on ciliary movement.

作者信息

Fukuda T, Saito T, Yoshidomi M, Ito K

出版信息

Arzneimittelforschung. 1984;34(7):816-8.

PMID:6149756
Abstract

Influence of 1-(2-ethoxyethyl)-2-(4-methyl-1-homopiperazinyl)benzimidazol e difumarate (KB-2413), a new antiallergic agent, on tracheal ciliary movement of pigeons and its local anaesthetic effect were investigated in comparison with reference drugs. KB-2413 (0.3 and 3 mg/kg i.v.) did not affect ciliary movement, but ketotifen, diphenhydramine, chlorpheniramine, lidocaine and tetracaine showed a significantly inhibitory effect on ciliary movement at a dose of 3 mg/kg i.v. KB-2413 (4% solution) did not inhibit corneal reflex in guinea pigs, but ketotifen, diphenhydramine and chlorpheniramine inhibited corneal reflex at 1%, 1% and 4% solution, respectively. KB-2413 (5 X 10(-4) mol/l) did not inhibit action potentials of desheathed frog sciatic nerve fiber, but ketotifen, chlorpheniramine and diphenhydramine inhibited significantly action potentials at 5 X 10(-4) mol/l. These results suggested that KB-2413 did not influence tracheal ciliary movement because of having no local anaesthetic effect.

摘要

研究了新型抗过敏药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)对鸽子气管纤毛运动的影响及其局部麻醉作用,并与对照药物进行了比较。静脉注射KB-2413(0.3和3mg/kg)不影响纤毛运动,但静脉注射3mg/kg剂量时,酮替芬、苯海拉明、氯苯那敏、利多卡因和丁卡因对纤毛运动有显著抑制作用。KB-2413(4%溶液)不抑制豚鼠角膜反射,但酮替芬、苯海拉明和氯苯那敏分别在1%、1%和4%溶液浓度时抑制角膜反射。KB-2413(5×10(-4)mol/L)不抑制去鞘青蛙坐骨神经纤维的动作电位,但酮替芬、氯苯那敏和苯海拉明在5×10(-4)mol/L时显著抑制动作电位。这些结果表明,KB-2413由于没有局部麻醉作用,所以不影响气管纤毛运动。

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