Synthesis of 7, 8-(Methylenedioxy)-1-phenyl-3, 5-dihydro-4 H-2, 3-benzodiazepin-4-ones as Novel and Potent Noncompetitive AMPA Receptor Antagonists

…, VI Ilyin, KE Vanover, RB Carter, E Weber…

Index: Wang, Yan; Konkoy, Christopher S.; Ilyin, Victor I.; Vanover, Kimberly E.; Carter, Richard B.; Weber, Eckard; Keana, John F. W.; Woodward, Richard M.; Cai, Sui Xiong Journal of Medicinal Chemistry, 1998 , vol. 41, # 14 p. 2621 - 2625

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Citation Number: 27

Abstract

A group of 7, 8-(methylenedioxy)-1-phenyl-3, 5-dihydro-4 H-2, 3-benzodiazepin-4-ones was synthesized and assayed for antagonism of rat brain α-amino-3-hydroxy-5-methylisoxazole- 4-propionic acid (AMPA) receptors expressed in Xenopus oocytes. The benzodiazepinones inhibited AMPA-activated membrane current responses in a manner consistent with noncompetitive, allosteric inhibition of the receptor-channel complex. The most potent ...