加巴喷丁作用机制的微透析研究

A microdialysis study on the mechanism of action of gabapentin.

作者信息

Timmerman W, Bouma M, De Vries J B, Davis M, Westerink B H

机构信息

Department of Medicinal Chemistry, University Center for Pharmacy, Ant. Deusinglaan 1, 9713 AV, Groningen, The Netherlands.

出版信息

Eur J Pharmacol. 2000 Jun 9;398(1):53-7. doi: 10.1016/s0014-2999(00)00309-5.

DOI:10.1016/s0014-2999(00)00309-5

PMID:10856447

Abstract

To gain insight into the mechanism of action of the anti-epileptic, gabapentin, the effects of gabapentin on the in vivo extracellular gamma-aminobutyric acid (GABA) levels in the rat substantia nigra reticulata were studied using microdialysis. In order to investigate possible interference with different GABA-ergic compartments in the substantia nigra reticulata, we studied the effects of gabapentin under basal, K(+)-, nipecotic acid- and glutamate-stimulated conditions. Intraperitoneally (i.p.) administered gabapentin, at a dose of 100 mg/kg, did not significantly affect extracellular GABA levels under any condition. Thus, our data do not support the involvement of nigral GABA release in the mechanism of action of the anti-epileptic gabapentin.

摘要

为深入了解抗癫痫药物加巴喷丁的作用机制，采用微透析技术研究了加巴喷丁对大鼠黑质网状部体内细胞外γ-氨基丁酸（GABA）水平的影响。为了研究加巴喷丁对黑质网状部不同GABA能区室的潜在干扰，我们研究了在基础、钾离子、尼克酸和谷氨酸刺激条件下加巴喷丁的作用。腹腔注射（i.p.）剂量为100mg/kg的加巴喷丁，在任何条件下均未显著影响细胞外GABA水平。因此，我们的数据不支持黑质GABA释放参与抗癫痫药物加巴喷丁的作用机制。