Synthesis and excitatory amino acid pharmacology of a series of heterocyclic-fused quinoxalinones and quinazolinones

…, DO Calligaro, PJ O'Malley, D Lodge…

文献索引：McQuaid; Smith; South; Mitch; Schoepp; True; Calligaro; O'Malley; Lodge; Ornstein Journal of Medicinal Chemistry, 1992 , vol. 35, # 18 p. 3319 - 3324

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被引用次数: 58

摘要

4d, was found to bind with the greatest affiiity to the AMPA receptor with an ICm of 0.83 pM and antagonized 40 pM AMPA-induced depolarization in the cortical slice preparation with an ICm of 44 pM. 7, 8-Dichloro-1, 2, 4-triazolo [4, 3-a] quinoxalin-4 (5H)-one, 4a, and 7, &dicbloroimidazo [1, 2-a] quinoxalin-4 (5H)-one, 7, pd the beat affiiity for the glycine site with ICso values of 0.63 and 1.26 pM, respectively. It is noteworthy that the SAR for the ...