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Title: CM 40907: a structurally novel anticonvulsant in mice, rats and baboons

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. 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.

Authors:
; ; ; ; ; ;
Publication Date:
Research Org.:
Centre de Recherches Clin Midy, Montpellier, France
OSTI Identifier:
5253828
Resource Type:
Journal Article
Journal Name:
J. Pharmacol. Exp. Ther.; (United States)
Additional Journal Information:
Journal Volume: 3
Country of Publication:
United States
Language:
English
Subject:
59 BASIC BIOLOGICAL SCIENCES; 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

Citation Formats

Chambon, J P, Brochard, J, Hallot, A, Heaulme, M, Brodin, R, Roncucci, R, and Biziere, K. CM 40907: a structurally novel anticonvulsant in mice, rats and baboons. United States: N. p., 1985. Web.
Chambon, J P, Brochard, J, Hallot, A, Heaulme, M, Brodin, R, Roncucci, R, & Biziere, K. CM 40907: a structurally novel anticonvulsant in mice, rats and baboons. United States.
Chambon, J P, Brochard, J, Hallot, A, Heaulme, M, Brodin, R, Roncucci, R, and Biziere, K. 1985. "CM 40907: a structurally novel anticonvulsant in mice, rats and baboons". United States.
@article{osti_5253828,
title = {CM 40907: a structurally novel anticonvulsant in mice, rats and baboons},
author = {Chambon, J P and Brochard, J and Hallot, A and Heaulme, M and Brodin, R and Roncucci, R and Biziere, K},
abstractNote = {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.},
doi = {},
url = {https://www.osti.gov/biblio/5253828}, journal = {J. Pharmacol. Exp. Ther.; (United States)},
number = ,
volume = 3,
place = {United States},
year = {Sat Jun 01 00:00:00 EDT 1985},
month = {Sat Jun 01 00:00:00 EDT 1985}
}