Literature DB >> 19161278

Discovery of the first selective inhibitor of excitatory amino acid transporter subtype 1.

Anders A Jensen1, Mette N Erichsen, Christina W Nielsen, Tine B Stensbøl, Jan Kehler, Lennart Bunch.   

Abstract

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.

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Year:  2009        PMID： 19161278     DOI： 10.1021/jm8013458

Source DB:  PubMed          Journal:  J Med Chem        ISSN： 0022-2623            Impact factor:   7.446


  19 in total

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