CM 40907 - A STRUCTURALLY NOVEL ANTICONVULSANT IN MICE, RATS AND BABOONS

  • 1 January 1985
    • journal article
    • research article
    • Vol. 233  (3) , 836-844
Abstract
CM 40907 [3-(4-hydroxypiperidyl)-6-(2''-chlorophenyl)-pyridazine] is a chemically original compound which possesses the pharmacological properties of a potent, p.o. [per os] active anticonvulsant. The anticonvulsant activity of CM 40907 was examined in mice, rats and photosensitive P. papio baboons, and compared to that of phenobarbital, diphenylhydantoin, carbamazepine, Na 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, Na 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 P. papio baboons CM 40907 antagonized myoclonus and cortical paroxysmal discharges. In this model CM 40907 was .apprx. 1/4 as potent as phenobarbital, twice as potent as carbamazepine and 6 times more potent than Na valproate. In mice CM 40907, at anticonvulsant doses, increased the affinity of [3H]flunitrazepam for its central receptor site. CM 40907 is a potent and relatively nonsedative anticonvulsant and may be of therapeutic benefit in epileptic disorders.

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