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巴比妥类衍生物HB-7在猫烯丙基甘氨酸诱导的癫痫模型中的抗惊厥活性。

Anticonvulsive activity of a barbiturate derivative HB-7 in a model of allylglycine-induced epilepsy in cats.

作者信息

Getova D, Moyanova S, Georgiev V, Ivanova V

机构信息

Experimental Pharmacology Department, Bulgarian Academy of Sciences, Sofia.

出版信息

Acta Physiol Pharmacol Bulg. 1990;16(3):43-9.

PMID:1966259
Abstract

With the aim of characterizing further the anticonvulsive activity of the newly-synthesized barbituric derivative 2-hydroxylamino-5-ethyl-5-sec. penthylbarbituric acid (HB-7), we studied its effects on allylglycine-induced epileptiform electrocorticogram (ECoG) in cats under acute conditions. Pentobarbital (PB) was used for comparison. Allylglycine (AG) was administered in a dose of 100 mg/kg i.v. to all cats. The control animals were treated with AG only. HB-7 and PB were applied in doses of 20 mg/kg i.p., about 60 min after AG. Intermittent light stimulation (ILS) at flash rate of 8/s and 25/s was applied to some animals. The ILS-stimulated animals were also divided in three groups: controls and animals treated with HB-7 or PB in the same dose. AG led to the appearance of paroxysmal ECoG activity: single and multiple spikes and spike-waves appeared first, to be followed later by generalized seizure activity. No AG-induced convulsions appeared in the cats treated with HB-7, but the AG-induced spikes and spike-waves remained unchanged. The effect of PB on the AG-induced paroxysmal ECoG activity was similar to that of HB-7, but the addition of PB provoked the appearance of slow waves and spindles, mixed with spikes and spike-waves. Although the paroxysmal character of the activity was more pronounced in the ILS-stimulated animals than in the group without ILS, HB-7 and PB (albeit to a lesser extent) inhibited the AG-induced discharges.(ABSTRACT TRUNCATED AT 250 WORDS)

摘要

为了进一步表征新合成的巴比妥衍生物2-羟氨基-5-乙基-5-仲戊基巴比妥酸(HB-7)的抗惊厥活性,我们研究了其在急性条件下对猫烯丙基甘氨酸诱导的癫痫样脑电图(ECoG)的影响。使用戊巴比妥(PB)作为对照。所有猫均静脉注射100mg/kg剂量的烯丙基甘氨酸(AG)。对照动物仅接受AG治疗。在AG给药约60分钟后,以20mg/kg腹腔注射HB-7和PB。对一些动物施加8次/秒和25次/秒闪光频率的间歇性光刺激(ILS)。接受ILS刺激的动物也分为三组:对照组以及接受相同剂量HB-7或PB治疗的动物。AG导致阵发性ECoG活动出现:首先出现单个和多个尖峰以及尖峰波,随后是全身性癫痫发作活动。接受HB-7治疗的猫未出现AG诱导的惊厥,但AG诱导的尖峰和尖峰波保持不变。PB对AG诱导的阵发性ECoG活动的影响与HB-7相似,但添加PB会引发慢波和纺锤波的出现,与尖峰和尖峰波混合。尽管在接受ILS刺激的动物中活动的阵发性特征比未接受ILS刺激的组更明显,但HB-7和PB(尽管程度较轻)抑制了AG诱导的放电。(摘要截断于250字)

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