Profile of anticonvulsant activity and minimal toxicity of methyl 4-[(p-chlorophenyl)amino]-6-methyl-2-oxo-cyclohex-3-en-1-oate and some prototype antiepileptic drugs in mice and rats.

Abstract	The anticonvulsant and toxic properties of methyl 4-[(p-chlorophenyl)amino]-6-methyl-2-oxocyclohex-3-en-1-oate (ADD 196022), were compared with those of phenytoin (PHT), carbamazepine (CBZ), and valproate (VPA). These compounds were evaluated in mice and rats using well-standardized anticonvulsant testing procedures. Results indicate that ADD 196022 is a very potent anticonvulsant in the maximal electroshock seizure (MES) model. The compound was effective in nontoxic doses after intraperitoneal (i.p.) administration in mice and oral administration in rats. In mice, i.p. administration of ADD 196022 resulted in an ED50 value of 26.2 mg/kg as compared with a value of 6.48 mg/kg for PHT in the same assay. ADD 196022 was more potent that PHT in the oral rat model, having an ED50 value of 5.79 mg/kg as compared to 23.2 mg/kg for PHT. ADD 196022 was ineffective in nontoxic doses against all other seizure models evaluated and thus has a pharmacologic profile similar to that of PHT.
Authors	D Mulzac, K R Scott
Journal	Epilepsia (Epilepsia) Vol. 34 Issue 6 Pg. 1141-6 ( 1993) ISSN: 0013-9580 [Print] United States
PMID	8243370 (Publication Type: Comparative Study, Journal Article, Research Support, Non-U.S. Gov't)
Chemical References	Anticonvulsants Cyclohexanecarboxylic Acids Cyclohexylamines ADD 196022 Carbamazepine Valproic Acid Phenytoin Pentylenetetrazole
Topics	Administration, Oral Animals Anticonvulsants (administration & dosage, pharmacology, toxicity) Carbamazepine (pharmacology) Cyclohexanecarboxylic Acids (administration & dosage, pharmacology, toxicity) Cyclohexylamines (administration & dosage, pharmacology, toxicity) Electroshock Epilepsy (chemically induced, prevention & control) Injections, Intraperitoneal Kindling, Neurologic (drug effects) Male Mice Pentylenetetrazole Phenytoin (pharmacology) Rats Rats, Sprague-Dawley Valproic Acid (pharmacology)

Join CureHunter, for free Research Interface BASIC access!

Take advantage of free CureHunter research engine access to explore the best drug and treatment options for any disease. Find out why thousands of doctors, pharma researchers and patient activists around the world use CureHunter every day.

Realize the full power of the drug-disease research graph!