Discovery of the first selective inhibitor of excitatory amino acid transporter subtype 1
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Discovery of the first selective inhibitor of excitatory amino acid transporter subtype 1. / Jensen, Anders Asbjørn; Erichsen, Mette Navy; Nielsen, Christina Wøhlk; Stensbøl, Tine Bryan; Kehler, Jan; Bunch, Lennart.
I: Journal of Medicinal Chemistry, Bind 52, Nr. 4, 2009, s. 912-915.Publikation: Bidrag til tidsskrift › Tidsskriftartikel › Forskning › fagfællebedømt
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TY - JOUR
T1 - Discovery of the first selective inhibitor of excitatory amino acid transporter subtype 1
AU - Jensen, Anders Asbjørn
AU - Erichsen, Mette Navy
AU - Nielsen, Christina Wøhlk
AU - Stensbøl, Tine Bryan
AU - Kehler, Jan
AU - Bunch, Lennart
PY - 2009
Y1 - 2009
N2 - 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.
AB - 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.
KW - Former Faculty of Pharmaceutical Sciences
U2 - 10.1021/jm8013458
DO - 10.1021/jm8013458
M3 - Journal article
C2 - 19161278
VL - 52
SP - 912
EP - 915
JO - Journal of Medicinal Chemistry
JF - Journal of Medicinal Chemistry
SN - 0022-2623
IS - 4
ER -
ID: 10245107