Anticonvulsant activity of 4,9-dioxo-5,10-diazatetradecane (CM 40142), a new GABA derivative, in mice and photosensitive baboons).

Abstract

The authors describe the anticonvulsant activity of a new gamma-amino-butyric acid (GABA) derivative in several animal models of generalized epilepsy including photoepileptic baboons. In all the studies, 4,9-dioxo-5,10-diazatetradecane (CM 40 142) revealed potencies against chemically, electrically and photic-induced seizures very similar to those observed with sodium valproate. In chemically elicited seizures in mice, CM 40142 exhibited a higher potency than sodium valproate in antagonizing anti-GABAergic agents. Although CM 40142 was synthesized as a compound which would cross the blood-brain barrier and liberate GABA within the central nervous system, preliminary biochemical investigations in mice failed to demonstrate a rise in brain GABA levels after treatment with CM 40142. Furthermore, CM 40142 increased spontaneous motility in mice at anticonvulsant doses. The data suggest that CM 40142 could be a broad spectrum nonsedative antiepileptic agent.

• Authors: J P Chambon, J C Molimard, R Calassi, J Maruani, D Rodier, G Sigault, R Leyris, R Roncucci, K Bizière
• Journal: Arzneimittel-Forschung (Arzneimittelforschung) Vol. 34 Issue 9 Pg. 1017-21 ( 1984) ISSN: 0004-4172 [Print] Germany
• PMID: 6439227 (Publication Type: Journal Article)

Chemical References

• Anticonvulsants
• gamma-Aminobutyric Acid
• Valproic Acid
• 4,9-dioxo-5,10-diazatetradecane
• 3-Mercaptopropionic Acid
• Strychnine
• Pentylenetetrazole
• Bicuculline

Topics

• 3-Mercaptopropionic Acid (pharmacology)
• Animals
• Anticonvulsants (pharmacology)
• Behavior, Animal (drug effects)
• Bicuculline (pharmacology)
• Electroshock
• Female
• Male
• Mice
• Motor Activity (drug effects)
• Papio
• Pentylenetetrazole (pharmacology)
• Photic Stimulation
• Seizures (prevention & control)
• Strychnine (pharmacology)
• Valproic Acid (pharmacology)
• gamma-Aminobutyric Acid (analogs & derivatives, pharmacology, physiology, toxicity)