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

Research output: Contribution to journal › Journal article › Research › peer-review

Standard

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.

In: Journal of Medicinal Chemistry, Vol. 52, No. 4, 2009, p. 912-915.

Research output: Contribution to journal › Journal article › Research › peer-review

Harvard

Jensen, AA, Erichsen, MN, Nielsen, CW, Stensbøl, TB, Kehler, J & Bunch, L 2009, 'Discovery of the first selective inhibitor of excitatory amino acid transporter subtype 1', Journal of Medicinal Chemistry, vol. 52, no. 4, pp. 912-915. https://doi.org/10.1021/jm8013458

APA

Jensen, A. A., Erichsen, M. N., Nielsen, C. W., Stensbøl, T. B., Kehler, J., & Bunch, L. (2009). Discovery of the first selective inhibitor of excitatory amino acid transporter subtype 1. Journal of Medicinal Chemistry, 52(4), 912-915. https://doi.org/10.1021/jm8013458

Vancouver

Jensen AA, Erichsen MN, Nielsen CW, Stensbøl TB, Kehler J, Bunch L. Discovery of the first selective inhibitor of excitatory amino acid transporter subtype 1. Journal of Medicinal Chemistry. 2009;52(4):912-915. https://doi.org/10.1021/jm8013458

Author

Jensen, Anders Asbjørn ; Erichsen, Mette Navy ; Nielsen, Christina Wøhlk ; Stensbøl, Tine Bryan ; Kehler, Jan ; Bunch, Lennart. / Discovery of the first selective inhibitor of excitatory amino acid transporter subtype 1. In: Journal of Medicinal Chemistry. 2009 ; Vol. 52, No. 4. pp. 912-915.

Bibtex

@article{21238ca0f75d11ddbf70000ea68e967b,
title = "Discovery of the first selective inhibitor of excitatory amino acid transporter subtype 1",
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.",
keywords = "Former Faculty of Pharmaceutical Sciences",
author = "Jensen, {Anders Asbj{\o}rn} and Erichsen, {Mette Navy} and Nielsen, {Christina W{\o}hlk} and Stensb{\o}l, {Tine Bryan} and Jan Kehler and Lennart Bunch",
year = "2009",
doi = "10.1021/jm8013458",
language = "English",
volume = "52",
pages = "912--915",
journal = "Journal of Medicinal Chemistry",
issn = "0022-2623",
publisher = "American Chemical Society",
number = "4",

}

RIS

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