Synthesis and receptor binding affinity of new selective GluR5 ligands

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

Standard

Synthesis and receptor binding affinity of new selective GluR5 ligands. / Bunch, L; Johansen, T H; Bräuner-Osborne, Hans; Stensbøl, T B; Johansen, T N; Krogsgaard-Larsen, P; Madsen, U.

In: Bioorganic & Medicinal Chemistry, Vol. 9, No. 4, 04.2001, p. 875-9.

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

Harvard

Bunch, L, Johansen, TH, Bräuner-Osborne, H, Stensbøl, TB, Johansen, TN, Krogsgaard-Larsen, P & Madsen, U 2001, 'Synthesis and receptor binding affinity of new selective GluR5 ligands', Bioorganic & Medicinal Chemistry, vol. 9, no. 4, pp. 875-9. https://doi.org/10.1016/S0968-0896(00)00304-7

APA

Bunch, L., Johansen, T. H., Bräuner-Osborne, H., Stensbøl, T. B., Johansen, T. N., Krogsgaard-Larsen, P., & Madsen, U. (2001). Synthesis and receptor binding affinity of new selective GluR5 ligands. Bioorganic & Medicinal Chemistry, 9(4), 875-9. https://doi.org/10.1016/S0968-0896(00)00304-7

Vancouver

Bunch L, Johansen TH, Bräuner-Osborne H, Stensbøl TB, Johansen TN, Krogsgaard-Larsen P et al. Synthesis and receptor binding affinity of new selective GluR5 ligands. Bioorganic & Medicinal Chemistry. 2001 Apr;9(4):875-9. https://doi.org/10.1016/S0968-0896(00)00304-7

Author

Bunch, L ; Johansen, T H ; Bräuner-Osborne, Hans ; Stensbøl, T B ; Johansen, T N ; Krogsgaard-Larsen, P ; Madsen, U. / Synthesis and receptor binding affinity of new selective GluR5 ligands. In: Bioorganic & Medicinal Chemistry. 2001 ; Vol. 9, No. 4. pp. 875-9.

Bibtex

@article{590238ae3dca4e37bc045265184298a4,
title = "Synthesis and receptor binding affinity of new selective GluR5 ligands",
abstract = "Two hybrid analogues of the kainic acid receptor agonists, 2-amino-3-(5-tert-butyl-3-hydroxy-4-isoxazolyl)propionic acid (ATPA) and (2S,4R)-4-methylglutamic acid ((2S,4R)-4-Me-Glu), were designed, synthesized, and characterized in radioligand binding assays using cloned ionotropic and metabotropic glutamic acid receptors. The (S)-enantiomers of E-4-(2,2-dimethylpropylidene)glutamic acid ((S)-1) and E-4-(3,3-dimethylbutylidene)glutamic acid ((S)-2) were shown to be selective and high affinity GluR5 ligands, with Ki values of 0.024 and 0.39 microM, respectively, compared to Ki values at GluR2 of 3.0 and 2.0 microM. respectively. Their affinities in the [3H]AMPA binding assay on native cortical receptors were shown to correlate with their GluR2 affinity rather than their GluR5 affinity. No affinity for GluR6 was detected (IC50 > 100 microM).",
keywords = "Cell Line, Chromatography, High Pressure Liquid, Glutamates, Humans, Indicators and Reagents, Ligands, Magnetic Resonance Spectroscopy, Receptors, AMPA, Receptors, Kainic Acid, Tumor Cells, Cultured",
author = "L Bunch and Johansen, {T H} and Hans Br{\"a}uner-Osborne and Stensb{\o}l, {T B} and Johansen, {T N} and P Krogsgaard-Larsen and U Madsen",
year = "2001",
month = apr,
doi = "10.1016/S0968-0896(00)00304-7",
language = "English",
volume = "9",
pages = "875--9",
journal = "Bioorganic & Medicinal Chemistry",
issn = "0968-0896",
publisher = "Pergamon Press",
number = "4",

}

RIS

TY - JOUR

T1 - Synthesis and receptor binding affinity of new selective GluR5 ligands

AU - Bunch, L

AU - Johansen, T H

AU - Bräuner-Osborne, Hans

AU - Stensbøl, T B

AU - Johansen, T N

AU - Krogsgaard-Larsen, P

AU - Madsen, U

PY - 2001/4

Y1 - 2001/4

N2 - Two hybrid analogues of the kainic acid receptor agonists, 2-amino-3-(5-tert-butyl-3-hydroxy-4-isoxazolyl)propionic acid (ATPA) and (2S,4R)-4-methylglutamic acid ((2S,4R)-4-Me-Glu), were designed, synthesized, and characterized in radioligand binding assays using cloned ionotropic and metabotropic glutamic acid receptors. The (S)-enantiomers of E-4-(2,2-dimethylpropylidene)glutamic acid ((S)-1) and E-4-(3,3-dimethylbutylidene)glutamic acid ((S)-2) were shown to be selective and high affinity GluR5 ligands, with Ki values of 0.024 and 0.39 microM, respectively, compared to Ki values at GluR2 of 3.0 and 2.0 microM. respectively. Their affinities in the [3H]AMPA binding assay on native cortical receptors were shown to correlate with their GluR2 affinity rather than their GluR5 affinity. No affinity for GluR6 was detected (IC50 > 100 microM).

AB - Two hybrid analogues of the kainic acid receptor agonists, 2-amino-3-(5-tert-butyl-3-hydroxy-4-isoxazolyl)propionic acid (ATPA) and (2S,4R)-4-methylglutamic acid ((2S,4R)-4-Me-Glu), were designed, synthesized, and characterized in radioligand binding assays using cloned ionotropic and metabotropic glutamic acid receptors. The (S)-enantiomers of E-4-(2,2-dimethylpropylidene)glutamic acid ((S)-1) and E-4-(3,3-dimethylbutylidene)glutamic acid ((S)-2) were shown to be selective and high affinity GluR5 ligands, with Ki values of 0.024 and 0.39 microM, respectively, compared to Ki values at GluR2 of 3.0 and 2.0 microM. respectively. Their affinities in the [3H]AMPA binding assay on native cortical receptors were shown to correlate with their GluR2 affinity rather than their GluR5 affinity. No affinity for GluR6 was detected (IC50 > 100 microM).

KW - Cell Line

KW - Chromatography, High Pressure Liquid

KW - Glutamates

KW - Humans

KW - Indicators and Reagents

KW - Ligands

KW - Magnetic Resonance Spectroscopy

KW - Receptors, AMPA

KW - Receptors, Kainic Acid

KW - Tumor Cells, Cultured

U2 - 10.1016/S0968-0896(00)00304-7

DO - 10.1016/S0968-0896(00)00304-7

M3 - Journal article

C2 - 11354670

VL - 9

SP - 875

EP - 879

JO - Bioorganic & Medicinal Chemistry

JF - Bioorganic & Medicinal Chemistry

SN - 0968-0896

IS - 4

ER -

ID: 45613875