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
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
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页码:11 / 15
页数:5
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