Summary: We compared the anticonvulsant activity and neurotoxicity of 4‐amino‐N‐(2,6–dimethyl‐phenyl)phthalimide (ADD213063)with those of phenytoin (PHT), carbamazepine (CBZ), phenobarbital (PB), ethosuximide (ESM), valproate (VPA), and felbamate (FBM). Evaluation of anticonvulsant properties performed according to well‐established procedures in rats and mice showed that ADD 213063 is most effective in protecting animals against maximal electroshock seizures (MES). This anti‐MES activity is achieved with nontoxic doses, with the optimal effect recorded in rats dosed orally with anti‐MES ED, and protective index (PI) values of 25.2 FmoYkg and >75, respectively. ADD 213063 protects to a lesser extent against seizures induced by subcutaneous (s.c.) picrotoxin and subcutaneous pentylenetetrazol(FTZ) in mice dosed intraperitoneally and orally, respectively. The profile of anticonvulsant action of ADD 213063 closely parallels that of CBZ.

01 Jan 1994·Biomedicine & PharmacotherapyQ2 · MEDICINE

Anticonvulsant activity of some 4-amino-N-phenylphthalimides and N-(3-amino-2-methylphenyl)phthalimides

Q2 · MEDICINE

Article

Author: V. Bailleux ; J.P. Nuyts ; J. Vamecq ; L. Vallée

A series of fifteen N-phenylphthalimides including 12 4-amino-N-phenylphthalimides and three N-(3-amino-2-methylphenyl)phthalimides was prepared and evaluated for anticonvulsant properties. The compounds were tested against seizures induced by electroshock (MES) and pentylenetetrazol (scPTZ) in mice dosed intraperitoneally. Their neurologic toxicity was assessed using the rotorod assay procedure. The most potent 4-amino-N-phenylphthalimides against MES were those possessing small lipophilic groups in either 2 or 2 and 6 positions of the N-phenyl ring. They also exhibited some activity against scPTZ and were the most toxic of the series. By contrast, no activity against scPTZ or neurotoxicity could be observed up to 300 mg/kg for members of the N-(3-amino-2- methylphenyl)phthalimide series. In this series, the order of anti-MES activity appears to correspond to the phthalimide ring substitution pattern of 4-amino > H > 4-methyl. Quantitation of anticonvulsant properties and toxicity of 4-amino-N-(2,6-dimethylphenyl)phthalimide (ADD 213063) previously initiated in rats has been, here, extended to mice dosed intraperitoneally but also orally. The confrontation of the two modes of administration in mice suggests that ADD 213063 presents with a good bioavailability.

01 Jan 1993·Biomedicine & PharmacotherapyQ2 · MEDICINE

Original anticonvulsant properties of two N-phenylphthalimide derivatives

Q2 · MEDICINE

Article

Author: V. Bailleux ; J.P. Nuyts ; J. Vamecq ; L. Vallée

Two N-phenylphthalimide derivatives, ADD 213063 and ADD 219048, were shown to be extremely potent anticonvulsant agents after oral dosing.

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Indication	Highest Phase	Country/Location	Organization	Date
Epilepsy	Preclinical	France	-	-
Epilepsy	Preclinical	Belgium	-	-
Epilepsy	Preclinical	United States	-	-

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