Shibata R, Ishii T, Nishiguchi Y, Iwakura K, Sumi N
Kannami Laboratory, Bozo Research Center Inc., Shizuoka, Japan.
J Toxicol Sci. 1995 Dec;20 Suppl 2:335-40. doi: 10.2131/jts.20.supplementii_335.
A vascular irritability study of montirelin hydrate (NS-3) injection, a new drug for the treatment of disturbance of consciousness, was conducted in Japanese white rabbits. The concentration of montirelin hydrate was 4 mg/ml. Saline and 0.75% acetic acid were used as negative and positive control, respectively. In a part of the ear vein, 0.05 ml of each compound was allowed to remain for 3 min after intravenous injections once a day for 8 days. Inflammation in peri-venous region and thrombus were macroscopically observed in injection sites of rabbits with the montirelin hydrate injection group. However, no changes were seen with the negative control group. Histopathological examination revealed periphlebitis, desquamation of endothelial cells and thrombus in rabbits given montirelin hydrate injection or saline. But incidence and degree of periphlebitis caused by montirelin hydrate injection were higher than those caused by saline. On the other hand, the irritating changes caused by 0.75% acetic acid were severer than those by montirelin hydrate injection. These results show that montirelin hydrate injection has a very weak vascular irritability in the ear of rabbits.
在日本白兔身上进行了水合蒙替瑞林（NS-3）注射液的血管刺激性研究，水合蒙替瑞林是一种用于治疗意识障碍的新药。水合蒙替瑞林的浓度为4mg/ml。分别使用生理盐水和0.75%乙酸作为阴性和阳性对照。在耳静脉的一部分，每天静脉注射一次，每次注射0.05ml每种化合物，持续8天，注射后让每种化合物在注射部位留存3分钟。在水合蒙替瑞林注射液组的兔子注射部位，肉眼观察到静脉周围区域有炎症和血栓形成。然而，阴性对照组未见变化。组织病理学检查显示，注射水合蒙替瑞林或生理盐水的兔子出现静脉周围炎、内皮细胞脱落和血栓形成。但水合蒙替瑞林注射液引起的静脉周围炎的发生率和程度高于生理盐水组。另一方面，0.75%乙酸引起的刺激性变化比水合蒙替瑞林注射液更严重。这些结果表明，水合蒙替瑞林注射液在兔耳中具有非常弱的血管刺激性。
