Katayama, Seiji; Ae, Nobuyuki; Kodo, Toru; Masumoto, Shuji; Hourai, Shinji; Tamamura, Chika; Tanaka, Hiroyasu; Nagata, Ryu published the artcile< Tricyclic Indole-2-carboxylic Acids: Highly in Vivo Active and Selective Antagonists for the Glycine Binding Site of the NMDA Receptor>, Product Details of C9H9NO4, the main research area is benzindoleacetanilide preparation NMDA receptor antagonist.
A series of tricyclic indole-2-carboxylic acid derivatives were synthesized and evaluated by the radioligand binding assay and the anticonvulsant effects in the mouse NMDA-induced seizure model. Among them, I [R = OCH2CO2H, CH2CO2H, (R)-OCHMeCO2H] showed high affinity to the NMDA-glycine binding site. The absolute configuration of the parent acid was confirmed by X-ray crystallog. anal. In particular, I [R = (R)-CHMeCO2H] was found to be a highly active glycine antagonist for both in vitro and in vivo assays (Ki = 1.0 ± 0.1 nM, ED50 = 2.3 mg/kg, i.v.) and also showed high selectivity for the glycine site. In addition, I [R = (R)-CHMeCO2H] was soluble enough in aqueous media (>10 mg/mL at pH 7.4) to use for medications by i.v. injection.
Journal of Medicinal Chemistry published new progress about NMDA receptors Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 30095-98-8 belongs to class esters-buliding-blocks, and the molecular formula is C9H9NO4, Product Details of C9H9NO4.
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