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巴氯芬可抑制不同惊厥处理诱导海马切片产生的爆发性活动。

Baclofen suppresses bursting activity induced in hippocampal slices by differing convulsant treatments.

作者信息

Ault B, Gruenthal M, Armstrong D R, Nadler J V, Wang C M

出版信息

Eur J Pharmacol. 1986 Jul 31;126(3):289-92. doi: 10.1016/0014-2999(86)90059-2.

Abstract

Epileptiform activity was induced in area CA3 of hippocampal slices by superfusion of medium containing 50 microM bicuculline and 3.5 mM K, 50 microM bicuculline and 5 mM K, 50 nM kainic acid and 3.5 mM K, or 7 mM K. Burst potentials were recorded at rates between 5 and 44/min, depending on the convulsant treatment. Baclofen reduced the frequency of burst firing in all slices tested in a dose-dependent manner, with little change in the morphology of individual bursts. Thus baclofen primarily affected the initiation of epileptiform discharges. IC50 values varied between 27 and 500 nM and were positively correlated with the rate of bursting. These experiments indicate that baclofen, at concentrations present in the CSF of patients treated for spasticity, has an anticonvulsant-like effect in the hippocampal formation and suggest that its mode of action is to reduce the excitability of pyramidal cells.

摘要

通过灌注含有50微摩尔荷包牡丹碱和3.5毫摩尔钾、50微摩尔荷包牡丹碱和5毫摩尔钾、50纳摩尔 kainic 酸和3.5毫摩尔钾或7毫摩尔钾的培养基,在海马切片的CA3区诱导癫痫样活动。根据惊厥治疗情况,爆发电位的记录频率在每分钟5至44次之间。巴氯芬以剂量依赖的方式降低了所有测试切片中爆发放电的频率,单个爆发的形态变化很小。因此,巴氯芬主要影响癫痫样放电的起始。IC50值在27至500纳摩尔之间变化,且与爆发率呈正相关。这些实验表明,对于接受痉挛治疗的患者,脑脊液中存在的浓度的巴氯芬在海马结构中具有类似抗惊厥的作用,并表明其作用方式是降低锥体细胞的兴奋性。

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