Anticonvulsant activity of 3,4-dicarboxyphenylglycines in DBA/2 mice

The 3,4-dicarboxyphenylglycines (3,4-DCPG) inhibit sound-induced seizures in DBA/2 mice with the racemate being notably more potent than either isomer (ED 50 (nmol, i.c.v.)): (RS)-3,4-DCPG (0.004; 86 mg/kg, i.p.)>>the mGlu 8 agonist (S)-3,4-DCPG (0.11)>the AMPA antagonist (R)-3,4-DCPG (0.38...

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Bibliographic Details
Published in:Neuropharmacology 2001-04, Vol.40 (5), p.732-735
Main Authors: Moldrich, Randal X., Beart, Philip M., Jane, David E., Chapman, Astrid G., Meldrum, Brian S.
Format: Article
Language:English
Subjects:
(RS)-4-phosphonophenylglycine (RS)-PPG
3,4-Dicarboxyphenylglycine
3,4-dicarboxyphenylglycine (3,4-DCPG)
Acoustic Stimulation
Animals
Anticonvulsant
Anticonvulsants - pharmacology
Anticonvulsants. Antiepileptics. Antiparkinson agents
Benzoates - pharmacology
Biological and medical sciences
DBA/2 mice
Dose-Response Relationship, Drug
Epilepsy
Epilepsy, Tonic-Clonic - chemically induced
Excitatory Amino Acid Antagonists - pharmacology
Female
Glycine - analogs & derivatives
Glycine - pharmacology
Male
Medical sciences
mGluRs
Mice
Mice, Inbred DBA
Neuropharmacology
Pharmacology. Drug treatments
Receptors, AMPA - drug effects
Receptors, Metabotropic Glutamate - metabolism
Stereoisomerism
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Summary:The 3,4-dicarboxyphenylglycines (3,4-DCPG) inhibit sound-induced seizures in DBA/2 mice with the racemate being notably more potent than either isomer (ED 50 (nmol, i.c.v.)): (RS)-3,4-DCPG (0.004; 86 mg/kg, i.p.)>>the mGlu 8 agonist (S)-3,4-DCPG (0.11)>the AMPA antagonist (R)-3,4-DCPG (0.38). A potentiation of anticonvulsant activity between AMPA and mGlu 8 receptors was confirmed by combining (R)-3,4-DCPG with the mGlu 8 agonist (RS)-4-phosphonophenylglycine. This potentiating mechanism provides a novel strategy for the treatment of epileptic seizures.
ISSN:0028-3908
1873-7064
DOI:10.1016/S0028-3908(01)00002-8