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)