Anticonvulsant activity of 4,9-dioxo-5,10-diazatetradecane (CM 40142), a new GABA derivative, in mice and photosensitive baboons).
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.
D015097:3-Mercaptopropionic Acid / Q000494:pharmacology; D000818:Animals; D000927:Anticonvulsants / Q000494:pharmacology*; D001522:Behavior, Animal / Q000187:drug effects; D001640:Bicuculline / Q000494:pharmacology; D004597:Electroshock; D005260:Female; D008297:Male; D051379:Mice; D009043:Motor Activity / Q000187:drug effects; D010215:Papio; D010433:Pentylenetetrazole / Q000494:pharmacology; D010775:Photic Stimulation; D012640:Seizures / Q000517:prevention & control; D013331:Strychnine / Q000494:pharmacology; D014635:Valproic Acid / Q000494:pharmacology; D005680:gamma-Aminobutyric Acid / Q000031:analogs & derivatives* / Q000494:pharmacology / Q000502:physiology / Q000633:toxicity
D000927:Anticonvulsants; D005680:gamma-Aminobutyric Acid; D014635:Valproic Acid; C043616:4,9-dioxo-5,10-diazatetradecane; D015097:3-Mercaptopropionic Acid; D013331:Strychnine; D010433:Pentylenetetrazole; D001640:Bicuculline