Bibliographic Information

Design, anticonvulsive, and neurotoxic properties of retrobenzamides. N-(nitrophenyl)benzamides and N-(aminophenyl)benzamides.     Bourhim, Mustapha; Poupaert, Jacques H.; Stables, James P.; Vallee, Louis; Vamecq, Joseph.    Laboratoire Ext,  CERTIA,  Villeneuve d'Ascq,  Fr.    Arzneimittel-Forschung  (1999),  49(2),  81-87.  CODEN: ARZNAD  ISSN: 0004-4172.  Journal  written in English.    CAN 130:291033    AN 1999:157263    CAPLUS  

Abstract

Design, anticonvulsant properties in maximal electroshock-induced seizures [MES] and seizures induced by s.c. administration of pentetrazole (scPtz), and neurotoxicity of retrobenzamides (N-(nitrophenyl)benzamides and N-(aminophenyl) benzamides) are reported.  These data are further compared with those on carbamazepine, phenytoin, ameltolide, and other ref. compds.  Studies on retrobenzamides in mice dosed i.p. point out a good anticonvulsant potential in the MES test for the amino derivs. (N-(aminophenyl)benzamides) and moderate activity for corresponding "nitro" derivs.  In rats dosed orally, aminoretrobenzamides were less active in the MES test than in mice dosed i.p.  Differences between exptl. animal species and administration routes lead to hypothesize rapid metabolization of compds., reduced intestinal resorption, and increased removal from body.  The presence of a Me substitution on the N-Ph moiety of aminoretrobenzamides attenuated these discrepancies between mice and rats.  Present results indicate that pharmacol. values, including the dose offering anticonvulsant protection in 50% of tested animals (ED50) and protective indexes, obtained on some retrobenzamides may compete with phenytoin and carbamazepine values.  By contrast with phenytoin, some retrobenzamides further exhibit activity in the scPtz test.  

Indexing -- Section 1-1  (Pharmacology)