Methaqualone derivatives are potent noncompetitive AMPA receptor antagonists

…, FS Menniti, MJ Pagnozzi, KD Shenk, FE Ewing…

Index: Chenard; Menniti; Pagnozzi; Shenk; Ewing; Welch Bioorganic and Medicinal Chemistry Letters, 2000 , vol. 10, # 11 p. 1203 - 1205

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Citation Number: 28

Abstract

The 2-amino-3-(3-hydroxy-5-methyl-4-isoxazolyl)-propionate (AMPA) receptor mediates fast glutamatergic synaptic transmission in the central nervous system. Overactivation of AMPA receptors may play a role in epileptogenesis and glutamate-induced neuronal death. 1 Thus there is considerable interest in discovery of AMPA receptor antagonists and several classes of compounds have been identified. 2 These include compounds that competitively displace glutamate binding, ...