Discovery of the first selective inhibitor of excitatory amino acid transporter subtype 1
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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.
Originalsprog | Engelsk |
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Tidsskrift | Journal of Medicinal Chemistry |
Vol/bind | 52 |
Udgave nummer | 4 |
Sider (fra-til) | 912-915 |
ISSN | 0022-2623 |
DOI | |
Status | Udgivet - 2009 |
- Det tidligere Farmaceutiske Fakultet
Forskningsområder
ID: 10245107