Synthesis and Pharmacological Characterization of the Selective GluK1 Radioligand (S)-2-Amino-3-(6-[3H]-2,4-dioxo-3,4-dihydrothieno[3,2-d]pyrimidin-1(2H)-yl)propanoic acid ([3H]-NF608)

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

Standard

Synthesis and Pharmacological Characterization of the Selective GluK1 Radioligand (S)-2-Amino-3-(6-[3H]-2,4-dioxo-3,4-dihydrothieno[3,2-d]pyrimidin-1(2H)-yl)propanoic acid ([3H]-NF608). / Alcaide, Anna; Marconi, Laura; Marek, Ales; Haym, Isabell; Nielsen, Birgitte; Møllerud, Stine; Jensen, Mikael; Conti, Paola; Pickering, Darryl S; Bunch, Lennart.

In: MedChemComm, Vol. 7, 2016, p. 2136-2144.

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

Harvard

Alcaide, A, Marconi, L, Marek, A, Haym, I, Nielsen, B, Møllerud, S, Jensen, M, Conti, P, Pickering, DS & Bunch, L 2016, 'Synthesis and Pharmacological Characterization of the Selective GluK1 Radioligand (S)-2-Amino-3-(6-[3H]-2,4-dioxo-3,4-dihydrothieno[3,2-d]pyrimidin-1(2H)-yl)propanoic acid ([3H]-NF608)', MedChemComm, vol. 7, pp. 2136-2144. https://doi.org/10.1039/c6md00339g

APA

Alcaide, A., Marconi, L., Marek, A., Haym, I., Nielsen, B., Møllerud, S., Jensen, M., Conti, P., Pickering, D. S., & Bunch, L. (2016). Synthesis and Pharmacological Characterization of the Selective GluK1 Radioligand (S)-2-Amino-3-(6-[3H]-2,4-dioxo-3,4-dihydrothieno[3,2-d]pyrimidin-1(2H)-yl)propanoic acid ([3H]-NF608). MedChemComm, 7, 2136-2144. https://doi.org/10.1039/c6md00339g

Vancouver

Alcaide A, Marconi L, Marek A, Haym I, Nielsen B, Møllerud S et al. Synthesis and Pharmacological Characterization of the Selective GluK1 Radioligand (S)-2-Amino-3-(6-[3H]-2,4-dioxo-3,4-dihydrothieno[3,2-d]pyrimidin-1(2H)-yl)propanoic acid ([3H]-NF608). MedChemComm. 2016;7:2136-2144. https://doi.org/10.1039/c6md00339g

Author

Alcaide, Anna ; Marconi, Laura ; Marek, Ales ; Haym, Isabell ; Nielsen, Birgitte ; Møllerud, Stine ; Jensen, Mikael ; Conti, Paola ; Pickering, Darryl S ; Bunch, Lennart. / Synthesis and Pharmacological Characterization of the Selective GluK1 Radioligand (S)-2-Amino-3-(6-[3H]-2,4-dioxo-3,4-dihydrothieno[3,2-d]pyrimidin-1(2H)-yl)propanoic acid ([3H]-NF608). In: MedChemComm. 2016 ; Vol. 7. pp. 2136-2144.

Bibtex

@article{d338c22eda54497b9369456fe99d0224,
title = "Synthesis and Pharmacological Characterization of the Selective GluK1 Radioligand (S)-2-Amino-3-(6-[3H]-2,4-dioxo-3,4-dihydrothieno[3,2-d]pyrimidin-1(2H)-yl)propanoic acid ([3H]-NF608)",
abstract = "The kainic acid receptors belong to the class of ionotropic glutamate receptors and comprise five subunits named GluK1-5. Radioligands are essential tools for use in binding assays aimed at ligand-receptor structure-activity-relationship studies. Previous work has led to the synthesis of GluK1 radioligands [3H]-SYM2081, [3H]-UBP310 and [3H]-ATPA, however all strategies were work-intensive and thus not attractive. Herein, we report the synthesis of [3H]-NF608 and subsequent pharmacological evaluation at homomeric recombinant rat GluK1 receptors. Binding affinities of a series of standard GluK1 ligands were shown to be in line with previously reported affinities obtained by use of already reported radioligands.",
author = "Anna Alcaide and Laura Marconi and Ales Marek and Isabell Haym and Birgitte Nielsen and Stine M{\o}llerud and Mikael Jensen and Paola Conti and Pickering, {Darryl S} and Lennart Bunch",
year = "2016",
doi = "10.1039/c6md00339g",
language = "English",
volume = "7",
pages = "2136--2144",
journal = "MedChemComm",
issn = "2040-2503",
publisher = "Royal Society of Chemistry",

}

RIS

TY - JOUR

T1 - Synthesis and Pharmacological Characterization of the Selective GluK1 Radioligand (S)-2-Amino-3-(6-[3H]-2,4-dioxo-3,4-dihydrothieno[3,2-d]pyrimidin-1(2H)-yl)propanoic acid ([3H]-NF608)

AU - Alcaide, Anna

AU - Marconi, Laura

AU - Marek, Ales

AU - Haym, Isabell

AU - Nielsen, Birgitte

AU - Møllerud, Stine

AU - Jensen, Mikael

AU - Conti, Paola

AU - Pickering, Darryl S

AU - Bunch, Lennart

PY - 2016

Y1 - 2016

N2 - The kainic acid receptors belong to the class of ionotropic glutamate receptors and comprise five subunits named GluK1-5. Radioligands are essential tools for use in binding assays aimed at ligand-receptor structure-activity-relationship studies. Previous work has led to the synthesis of GluK1 radioligands [3H]-SYM2081, [3H]-UBP310 and [3H]-ATPA, however all strategies were work-intensive and thus not attractive. Herein, we report the synthesis of [3H]-NF608 and subsequent pharmacological evaluation at homomeric recombinant rat GluK1 receptors. Binding affinities of a series of standard GluK1 ligands were shown to be in line with previously reported affinities obtained by use of already reported radioligands.

AB - The kainic acid receptors belong to the class of ionotropic glutamate receptors and comprise five subunits named GluK1-5. Radioligands are essential tools for use in binding assays aimed at ligand-receptor structure-activity-relationship studies. Previous work has led to the synthesis of GluK1 radioligands [3H]-SYM2081, [3H]-UBP310 and [3H]-ATPA, however all strategies were work-intensive and thus not attractive. Herein, we report the synthesis of [3H]-NF608 and subsequent pharmacological evaluation at homomeric recombinant rat GluK1 receptors. Binding affinities of a series of standard GluK1 ligands were shown to be in line with previously reported affinities obtained by use of already reported radioligands.

U2 - 10.1039/c6md00339g

DO - 10.1039/c6md00339g

M3 - Journal article

VL - 7

SP - 2136

EP - 2144

JO - MedChemComm

JF - MedChemComm

SN - 2040-2503

ER -

ID: 164572302