PMID: 9181049Jan 1, 1997Paper

Anticonvulsant and neurotoxicological properties of 4-amino-N-(2-ethylphenyl)benzamide, a potent ameltolide analogue

Biomedicine & Pharmacotherapy = Biomédecine & Pharmacothérapie
O DioufJ Vamecq

Abstract

A well documented study on the anticonvulsant properties of 4-amino-N-(2-ethylphenyl)benzamide (4-AEPB) is here provided. Initial screening in mice dosed intraperitoneally and rats dosed orally indicated that 4-AEPB is active against maximal electroshock-induced seizures (MES), but does not protect animals against subcutaneous pentylenetetrazole (sc Ptz)-induced seizures. Quantitative evaluation of anti-MES activity and neurotoxicity of 4-AEPB given intraperitoneally to mice provided ED50 and TD50 values amounting to 28.6 and 96.3 mumol/kg respectively, resulting in a protective index (PI = TD50/ED50) equal to 3.36. Further quantitative evaluation in rats dosed orally indicated that the respective ED50 and TD50 values for 4-AEPB were 29.8 and more than 1,530 mumol/kg, resulting in a very high PI value of over 51. Comparison anticonvulsant properties and neurotoxicity of 4-AEPB with those previously reported in the literature for two 4-aminobenzamide derivatives, 4-amino-N-(2,6-dimethylphenyl)benzamide (or ameltolide, an antiepileptic drug prototype developed by Eli Lilly), and phenytoin, underlines the value of 4-AEPB for future pharmacological development. In this perspective, an additional favorable element is represented by ...Continue Reading

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Citations

Jan 1, 2010·Acta Crystallographica. Section E, Structure Reports Online·Islam Ullah KhanEdward R T Tiekink
Jan 1, 2010·Acta Crystallographica. Section E, Structure Reports Online·Islam Ullah KhanOrhan Büyükgüngör
Jan 8, 2015·Seizure : the Journal of the British Epilepsy Association·Eunice S M Yuen, Iñaki F Trocóniz
Nov 9, 2019·Bioorganic Chemistry·Cemre Acarİlkay Yıldız

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