A new structural class of subtype-selective inhibitor of cloned excitatory amino acid transporter, EAAT2

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

Standard

A new structural class of subtype-selective inhibitor of cloned excitatory amino acid transporter, EAAT2. / Bräuner-Osborne, Hans; Hermit, M B; Nielsen, B; Krogsgaard-Larsen, P; Johansen, T N.

In: European Journal of Pharmacology, Vol. 406, No. 1, 06.10.2000, p. 41-4.

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

Harvard

Bräuner-Osborne, H, Hermit, MB, Nielsen, B, Krogsgaard-Larsen, P & Johansen, TN 2000, 'A new structural class of subtype-selective inhibitor of cloned excitatory amino acid transporter, EAAT2', European Journal of Pharmacology, vol. 406, no. 1, pp. 41-4.

APA

Bräuner-Osborne, H., Hermit, M. B., Nielsen, B., Krogsgaard-Larsen, P., & Johansen, T. N. (2000). A new structural class of subtype-selective inhibitor of cloned excitatory amino acid transporter, EAAT2. European Journal of Pharmacology, 406(1), 41-4.

Vancouver

Bräuner-Osborne H, Hermit MB, Nielsen B, Krogsgaard-Larsen P, Johansen TN. A new structural class of subtype-selective inhibitor of cloned excitatory amino acid transporter, EAAT2. European Journal of Pharmacology. 2000 Oct 6;406(1):41-4.

Author

Bräuner-Osborne, Hans ; Hermit, M B ; Nielsen, B ; Krogsgaard-Larsen, P ; Johansen, T N. / A new structural class of subtype-selective inhibitor of cloned excitatory amino acid transporter, EAAT2. In: European Journal of Pharmacology. 2000 ; Vol. 406, No. 1. pp. 41-4.

Bibtex

@article{7fe00b5e49b54eed9c4d02278a076e3c,
title = "A new structural class of subtype-selective inhibitor of cloned excitatory amino acid transporter, EAAT2",
abstract = "We have studied the pharmacological effects of (RS)-2-amino-3-(3-hydroxy-5-methylisoxazol-4-yl)propionic acid (AMPA) and the enantiomers of (RS)-2-amino-3-(3-hydroxy-1,2, 5-thiadiazol-4-yl)propionic acid (TDPA) on cloned human excitatory amino acid transporter subtypes 1, 2 and 3 (EAAT1-3) expressed in Cos-7 cells. Whereas AMPA and (R)-TDPA were both inactive as inhibitors of [3H]-(R)-aspartic acid uptake on all three EAAT subtypes, (S)-TDPA was shown to selectively inhibit uptake by EAAT2 with a potency equal to that of the endogenous ligand (S)-glutamic acid. (S)-TDPA thus represents a new structural class of EAAT2 inhibitor that will serve as a lead for the design of EAAT selective inhibitors.",
keywords = "ATP-Binding Cassette Transporters, Amino Acid Transport System X-AG, Animals, Aspartic Acid, Biological Transport, COS Cells, Carrier Proteins, DNA, Recombinant, Excitatory Amino Acid Transporter 2, Glutamate Plasma Membrane Transport Proteins, Receptors, Neurotransmitter, Stereoisomerism, Structure-Activity Relationship, Symporters, Tritium, alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid",
author = "Hans Br{\"a}uner-Osborne and Hermit, {M B} and B Nielsen and P Krogsgaard-Larsen and Johansen, {T N}",
year = "2000",
month = oct,
day = "6",
language = "English",
volume = "406",
pages = "41--4",
journal = "European Journal of Pharmacology",
issn = "0014-2999",
publisher = "Elsevier",
number = "1",

}

RIS

TY - JOUR

T1 - A new structural class of subtype-selective inhibitor of cloned excitatory amino acid transporter, EAAT2

AU - Bräuner-Osborne, Hans

AU - Hermit, M B

AU - Nielsen, B

AU - Krogsgaard-Larsen, P

AU - Johansen, T N

PY - 2000/10/6

Y1 - 2000/10/6

N2 - We have studied the pharmacological effects of (RS)-2-amino-3-(3-hydroxy-5-methylisoxazol-4-yl)propionic acid (AMPA) and the enantiomers of (RS)-2-amino-3-(3-hydroxy-1,2, 5-thiadiazol-4-yl)propionic acid (TDPA) on cloned human excitatory amino acid transporter subtypes 1, 2 and 3 (EAAT1-3) expressed in Cos-7 cells. Whereas AMPA and (R)-TDPA were both inactive as inhibitors of [3H]-(R)-aspartic acid uptake on all three EAAT subtypes, (S)-TDPA was shown to selectively inhibit uptake by EAAT2 with a potency equal to that of the endogenous ligand (S)-glutamic acid. (S)-TDPA thus represents a new structural class of EAAT2 inhibitor that will serve as a lead for the design of EAAT selective inhibitors.

AB - We have studied the pharmacological effects of (RS)-2-amino-3-(3-hydroxy-5-methylisoxazol-4-yl)propionic acid (AMPA) and the enantiomers of (RS)-2-amino-3-(3-hydroxy-1,2, 5-thiadiazol-4-yl)propionic acid (TDPA) on cloned human excitatory amino acid transporter subtypes 1, 2 and 3 (EAAT1-3) expressed in Cos-7 cells. Whereas AMPA and (R)-TDPA were both inactive as inhibitors of [3H]-(R)-aspartic acid uptake on all three EAAT subtypes, (S)-TDPA was shown to selectively inhibit uptake by EAAT2 with a potency equal to that of the endogenous ligand (S)-glutamic acid. (S)-TDPA thus represents a new structural class of EAAT2 inhibitor that will serve as a lead for the design of EAAT selective inhibitors.

KW - ATP-Binding Cassette Transporters

KW - Amino Acid Transport System X-AG

KW - Animals

KW - Aspartic Acid

KW - Biological Transport

KW - COS Cells

KW - Carrier Proteins

KW - DNA, Recombinant

KW - Excitatory Amino Acid Transporter 2

KW - Glutamate Plasma Membrane Transport Proteins

KW - Receptors, Neurotransmitter

KW - Stereoisomerism

KW - Structure-Activity Relationship

KW - Symporters

KW - Tritium

KW - alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid

M3 - Journal article

C2 - 11011030

VL - 406

SP - 41

EP - 44

JO - European Journal of Pharmacology

JF - European Journal of Pharmacology

SN - 0014-2999

IS - 1

ER -

ID: 45596078