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PMID: 8991783 Published · ppublish English Journal Article

The effects of D-23129, a new experimental anticonvulsant drug, on neurotransmitter amino acids in the rat hippocampus in vitro.

Epilepsy research ·Vol. 22 ·No. 3 ·1995-11-00 ·Pages 167-73

Kapetanovic IM, Yonekawa WD, Kupferberg HJ

Abstract

D-23129 [N-(2-amino-4-(4-fluorobenzylamino)phenyl)carbamic acid ethyl ester] and D-20443 (dihydrochloride of D-23129) are promising anticonvulsant compounds with a broad spectrum activity in animal models of epilepsy. Their effects on de novo synthesis of excitatory (glutamate and aspartate) and inhibitory (GABA) amino acids were studied in rat hippocampal slices. Like phenytoin, carbamazepine, lamotrigine, losigamone, U54494A, and flupirtine, D-23129 and D-20443 were effective in preventing the effects of a chemoconvulsant, 4-aminopyridine, on de novo synthesis of the three amino acids. However, unlike the other compounds, D-23129 and D-20443 also preferentially increased the concentrations of newly synthesized GABA. Their effect on the neosynthesis of GABA was unique, dose dependent, and not tetrodotoxin sensitive. A total of 15 compounds (including standard, new and candidate anticonvulsants) either had no effect on new GABA or decreased it. Therefore, D-23129 and D-20443 exhibited two different effects on de novo synthesis of neurotransmitter amino acids, both of which could potentially be anticonvulsant in nature.

MeSH Terms
4-Aminopyridine/antagonists & inhibitors,pharmacology Animals Anticonvulsants/pharmacology Carbamates/pharmacology Hippocampus/drug effects,metabolism In Vitro Techniques Male Nerve Tissue Proteins/analysis,biosynthesis Neurotransmitter Agents/biosynthesis Phenylenediamines/pharmacology Rats Rats, Inbred Strains Tetrodotoxin/pharmacology gamma-Aminobutyric Acid/biosynthesis
Chemicals
Anticonvulsants Carbamates Nerve Tissue Proteins Neurotransmitter Agents Phenylenediamines ezogabine Tetrodotoxin gamma-Aminobutyric Acid 4-Aminopyridine
Authors & Affiliations
3 authors, click to expand affiliations / ORCID
Kapetanovic I M
National Institute of Neurological Disorders and Stroke, National Institutes of Health, Bethesda, MD 20892, USA. [email protected]
Yonekawa W D
Kupferberg H J
Article Info
Journal
Epilepsy research
Abbr.
Epilepsy Res
ISSN
0920-1211
Published
1995-11-00
Pages
167-73
Language
English
Region
Netherlands
NLM ID
8703089
Subset
IM
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