POTENT AND STEREOSPECIFIC ANTICONVULSANT ACTIVITY OF 3-ISOBUTYL GABA RELATES TO INVITRO BINDING AT A NOVEL SITE LABELED BY TRITIATED GABAPENTIN

被引：140

作者：

TAYLOR, CP

VARTANIAN, MG

YUEN, PW

BIGGE, C

SUMANCHAUHAN, N

HILL, DR

机构：

[1] WARNER LAMBERT PARKE DAVIS,DEPT CHEM,DIV RES,ANN ARBOR,MI 48105

[2] PARKE DAVIS NEUROSCI RES CTR,CAMBRIDGE CB2 2QB,ENGLAND

来源：

EPILEPSY RESEARCH | 1993年 / 14卷 / 01期

关键词：

MAXIMAL ELECTROSHOCK; MICE; RATS; RECEPTOR BINDING;

D O I：

10.1016/0920-1211(93)90070-N

中图分类号：

R74 [神经病学与精神病学];

学科分类号：

摘要：

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

引用

页码：11 / 15

页数：5

共 16 条

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