Anticonvulsant effect of vigabatrin(.-vinyl GABA)

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Effect of vigabatrin (gamma-vinyl GABA) on amino acid levels in CSF of epileptic patients.

Vigabatrin (gamma-vinyl GABA) is a new anticonvulsive drug that irreversibly inhibits the activity of GABA transaminase. The effect of vigabatrin on neurotransmission-related amino acids in CSF of 28 epileptic patients was studied and the relationship between the amino acid pattern and clinical response during 7 months of administration of vigabatrin. Of this study population, 46% had more than...

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Vigabatrin induces tonic inhibition via GABA transporter reversal without increasing vesicular GABA release.

Two forms of GABAergic inhibition coexist: fast synaptic neurotransmission and tonic activation of GABA receptors due to ambient GABA. The mechanisms regulating ambient GABA have not been well defined. Here we examined the role of the GABA transporter in the increase in ambient [GABA] induced by the anticonvulsant vigabatrin. Pretreatment of cultured rat hippocampal neurons with vigabatrin (100...

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Vigabatrin and tiagabine are pharmacologically different drugs. A pre-clinical study

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GABA transaminase inhibition induces spontaneous and enhances depolarization-evoked GABA efflux via reversal of the GABA transporter.

The GABA transporter can reverse with depolarization, causing nonvesicular GABA release. However, this is thought to occur only under pathological conditions. Patch-clamp recordings were made from rat hippocampal neurons in primary cell cultures. Inhibition of GABA transaminase with the anticonvulsant gamma-vinyl GABA (vigabatrin; 0.05-100 microm) resulted in a large leak current that was block...

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ژورنال

عنوان ژورنال: Japanese Journal of Pharmacology

سال: 1988

ISSN: 0021-5198

DOI: 10.1016/s0021-5198(19)57088-3