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Potent and stereospecific anticonvulsant activity of 3-isobutyl GABA relates to in vitro binding at a novel site labeled by tritiated gabapentin.

作者信息

Taylor C P, Vartanian M G, Yuen P W, Bigge C, Suman-Chauhan N, Hill D R

机构信息

Department of Pharmacology, Warner-Lambert Co., Ann Arbor, MI 48105.

出版信息

Epilepsy Res. 1993 Jan;14(1):11-5. doi: 10.1016/0920-1211(93)90070-n.

DOI:10.1016/0920-1211(93)90070-n
PMID:8383597
Abstract

3-Isobutyl GABA is a derivative of the inhibitory neurotransmitter gamma-aminobutyric acid (GABA) and is also structurally related to the novel anticonvulsant gabapentin. The S(+) enantiomer of 3-isobutyl GABA blocks maximal electroshock seizures in mice and also potently displaces tritiated gabapentin from a novel high-affinity binding site in rat brain membrane fractions. The R(-) enantiomer is much less active in both assays, suggesting that the gabapentin binding site is involved in the anticonvulsant activity of 3-isobutyl GABA.

摘要

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