[iem-2062、丙戊酸钠和美曼汀在戊四唑点燃大鼠模型中的慢性抗惊厥活性和安全性比较]。

V E Gmiro, S E Serdyuk, O S Veselkina
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引用次数: 0

摘要

IEM-2062[1-(6-氨基己胺)-1-苯基环己基二盐酸]引起NMDA和AMPA受体的联合阻断,分别以0.3和3 mg/kg剂量慢性口服后,戊四氮点燃大鼠的抗惊厥作用最大,因为完全点燃大鼠的数量减少了100%,并且使阵挛-强直性点燃发作的平均严重程度降低了2.5-3.3倍。em -2062在最广泛的剂量范围内(1-48毫克/公斤)产生显著的抗- 299毒性作用,是美金刚(12-20毫克/公斤)和丙戊酸钠(100-200毫克/公斤)的24-22倍。丙戊酸钠和美金刚在“开阔场”试验中引起显著的运动活动紊乱,在引火大鼠中引起最大的抗惊厥作用。同时,IEM-2062仅在92 mg/kg的非常高剂量时才引起运动活动障碍,超过点燃大鼠最大抗惊厥作用剂量的30.7倍。因此,em -2062降低点燃癫痫发作的严重程度比丙戊酸钠和美金刚强1.7-1.9倍,比丙戊酸钠和美金刚安全30.7倍。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
[COMPARISON OF CHRONIC ANTICONVULSANT ACTIVITY AND SAFETY OF IEM-2062, SODIUM VALPROATE AND ME-MANTINE IN THE PENTYLENETETRAZOL KINDLING MODEL IN RATS].

IEM-2062 [1-(6-aminohexylamino)-1-phenylcyclohexyl dihydrochloride], causing a combined block NMDA and AMPA receptors, after chronic oral administration in doses, respectively, 0.3 and 3 mg/kg, induce maximal anticonvulsant effect in the pentylenetetrazol kindling rats because decrease the number of completely kindling rats by 100 %, and also decrease in 2.5-3.3 times the average severity of clonic-tonic kindling seizures. IEM-2062 causes significant anticon- 299 vulsant effects in the widest range of doses, 1-48 mg/kg, which is 24-22 times more than that of memantine (12-20 mg/kg) and sodium valproate (100-200 mg/kg). Sodium valproate and memantine cause significant disturbances of locomotor activity in the «open field» test in doses causing maximal anticonvulsant effect in the kindling rats. At the same time IEM-2062 cause disturbance of locomotor activity only in very high dose of 92 mg/kg, which exceeds in 30.7 times the dose causing the maximum anticonvulsive effect in the kindling rats. Thus, IEM-2062 reduces the severity of kindling seizures in 1.7-1.9 times stronger than sodium valproate and memantine and also by 30.7 times is safer than sodium valproate and memantine.

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