Discovery of the first selective inhibitor of excitatory amino acid transporter subtype 1
The discovery of the first class of subtype-selective inhibitors of the human excitatory amino acid transporter subtype 1 (EAAT1) and its rat orthologue GLAST is reported. An opening structure-activity relationship of 25 analogues is presented that addresses the influence of substitutions at the 4- and 7-positions of the parental skeleton 2-amino-5-oxo-5,6,7,8-tetrahydro-4H- chromene-3-carbonitrile. The most potent analogue 1o displays high nanomolar inhibitory activity at EAAT1 and a >400-fold selectivity over EAAT2 and EAAT3, making it a highly valuable pharmacological tool.
Jensen, Anders A.,Erichsen, Mette N.,Nielsen, Christina W.,Stensb?l, Tine B.,Kehler, Jan,Bunch, Lennart
supporting information; experimental part
p. 912 - 915
(2009/12/25)
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