Potent and stereospecific anticonvulsant activity of 3-isobutyl GABA relates to in vitro binding at a novel site labeled by tritiated gabapentin
Epilepsy ResearchPublished 1 January 1993
Charles P. Taylor, Mark G. Vartanian, Po‐wai Yuen, Christopher Bigge, Nirmala Suman‐Chauhan, David R. Hill
Citations148
SJR quartileQ2
SJR score0.69
SNIP0.81
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TL;DR
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.
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.
Keywords
ChemistryNeurosciencePharmacology, Toxicology and Pharmaceutics
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