CM 40907: a structurally novel anticonvulsant in mice, rats and baboons
CM 40907 (3-(4-hydroxypiperidyl)-6-(2'-chlorophenyl)-pyridazine) is a chemically original compound which possesses the pharmacological properties of a potent, p.o. active anticonvulsant. The anticonvulsant activity of CM 40907 was examined in mice, rats and photosensitive Papio-papio baboons and compared to that of phenobarbital, diphenylhydantoin, carbamazepine, sodium valproate and ethosuximide. In mice, CM 40907 antagonized electroconvulsive shock and chemically induced seizures with an overall potency comparable to that of carbamazepine and a therapeutic ratio (ED50 rotorod/ED50 electroshock) superior to that of ethosuximide, sodium valproate, phenobarbital and carbamazepine. In the rat CM 40907 suppressed completed kindled amygdaloid seizures and was approximately as active as phenobarbital. In naturally photosensitive Senegalese Papio-papio baboons CM 40907 antagonized myoclonus and cortical paroxysmal discharges. In this model CM 40907 was approximately one-fourth as potent as phenobarbital, twice as potent as carbamazepine and 6 times more potent than sodium valproate. In mice CM 40907, at anticonvulsant doses, increased the affinity of (/sup 3/H)flunitrazepam for its central receptor site. Based on these results it is postulated that CM 40907 is a potent and relatively nonsedative anticonvulsant and may be of therapeutic benefit in epileptic disorders.
- Research Organization:
- Centre de Recherches Clin Midy, Montpellier, France
- OSTI ID:
- 5253828
- Journal Information:
- J. Pharmacol. Exp. Ther.; (United States), Vol. 3
- Country of Publication:
- United States
- Language:
- English
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Related Subjects
ANTICONVULSANTS
RECEPTORS
AFFINITY
APES
COMPARATIVE EVALUATIONS
EPILEPSY
IN VITRO
MICE
PYRIDAZINES
RATS
TRACER TECHNIQUES
TRITIUM COMPOUNDS
ANIMALS
AZINES
CENTRAL NERVOUS SYSTEM DEPRESSANTS
DISEASES
DRUGS
HETEROCYCLIC COMPOUNDS
ISOTOPE APPLICATIONS
LABELLED COMPOUNDS
MAMMALS
NERVOUS SYSTEM DISEASES
ORGANIC COMPOUNDS
ORGANIC NITROGEN COMPOUNDS
PRIMATES
RODENTS
VERTEBRATES
550201* - Biochemistry- Tracer Techniques