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加巴喷丁作用机制的新观点

Emerging perspectives on the mechanism of action of gabapentin.

作者信息

Taylor C P

机构信息

Department of Neuroscience Pharmacology, Parke-Davis Research, Division of Warner-Lambert Co., Ann Arbor, Michigan 48105.

出版信息

Neurology. 1994 Jun;44(6 Suppl 5):S10-6; discussion S31-2.

PMID:7517515
Abstract

Significant advances have been made in understanding the molecular and cellular mechanisms underlying seizure disorders and the actions of antiepileptic drugs. Agents with new mechanisms of action or enhanced activity via known mechanisms might provide improved seizure control or more selective therapy for specific epilepsies. Gabapentin is a new antiepileptic drug that is structurally similar to the neurotransmitter GABA and the endogenous amino acid L-leucine. The mechanism of action of gabapentin is not fully understood, but its distinct profile of anticonvulsant activity in animal seizure models and its lack of activity at many drug binding sites associated with other antiepileptic drugs indicate that its mechanism of action is novel.

摘要

在理解癫痫疾病的分子和细胞机制以及抗癫痫药物的作用方面已经取得了重大进展。具有新作用机制或通过已知机制增强活性的药物可能会改善癫痫控制或为特定癫痫提供更具选择性的治疗。加巴喷丁是一种新型抗癫痫药物,其结构与神经递质γ-氨基丁酸(GABA)和内源性氨基酸L-亮氨酸相似。加巴喷丁的作用机制尚未完全明确,但其在动物癫痫模型中独特的抗惊厥活性特征以及在许多与其他抗癫痫药物相关的药物结合位点缺乏活性,表明其作用机制是新颖的。

相似文献

1
Emerging perspectives on the mechanism of action of gabapentin.加巴喷丁作用机制的新观点
Neurology. 1994 Jun;44(6 Suppl 5):S10-6; discussion S31-2.
2
Gamma-aminobutyric acid type B receptors with specific heterodimer composition and postsynaptic actions in hippocampal neurons are targets of anticonvulsant gabapentin action.具有特定异二聚体组成且在海马神经元中具有突触后作用的γ-氨基丁酸B型受体是抗惊厥药加巴喷丁作用的靶点。
Mol Pharmacol. 2001 Jan;59(1):144-52.
3
Mechanisms of action of gabapentin.加巴喷丁的作用机制。
Rev Neurol (Paris). 1997;153 Suppl 1:S39-45.
4
The anticonvulsant, antihyperalgesic agent gabapentin is an agonist at brain gamma-aminobutyric acid type B receptors negatively coupled to voltage-dependent calcium channels.抗惊厥、抗痛觉过敏药物加巴喷丁是一种作用于脑内与电压依赖性钙通道负偶联的B型γ-氨基丁酸受体的激动剂。
J Pharmacol Exp Ther. 2001 Jul;298(1):15-24.
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Cellular and molecular action of the putative GABA-mimetic, gabapentin.假定的γ-氨基丁酸模拟物加巴喷丁的细胞与分子作用
Cell Mol Life Sci. 2003 Apr;60(4):742-50. doi: 10.1007/s00018-003-2108-x.
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Antiepileptic drug mechanisms of action.抗癫痫药物的作用机制。
Epilepsia. 1993;34 Suppl 5:S1-8. doi: 10.1111/j.1528-1157.1993.tb05918.x.
7
Gabapentin actions on Kir3 currents and N-type Ca2+ channels via GABAB receptors in hippocampal pyramidal cells.加巴喷丁通过海马锥体细胞中的GABAB受体对Kir3电流和N型Ca2+通道的作用。
Synapse. 2003 Nov;50(2):95-109. doi: 10.1002/syn.10247.
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Antiepileptic drug mechanisms of action.抗癫痫药物的作用机制。
Epilepsia. 1995;36 Suppl 2:S2-12. doi: 10.1111/j.1528-1157.1995.tb05996.x.
9
Mechanisms of action of currently prescribed and newly developed antiepileptic drugs.当前处方用及新研发抗癫痫药物的作用机制。
Epilepsia. 1994;35 Suppl 4:S41-50. doi: 10.1111/j.1528-1157.1994.tb05955.x.
10
Effects of gabapentin on release of gamma-aminobutyric acid from slices of rat neostriatum.加巴喷丁对大鼠新纹状体切片中γ-氨基丁酸释放的影响。
Arzneimittelforschung. 1993 Jun;43(6):636-8.

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An in vitro electrophysiological study on the effects of phenytoin, lamotrigine and gabapentin on striatal neurons.苯妥英钠、拉莫三嗪和加巴喷丁对纹状体神经元作用的体外电生理研究
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