Selective mGAT2 (BGT-1) GABA Uptake Inhibitor: Design, synthesis and pharmacological characterization

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Standard

Selective mGAT2 (BGT-1) GABA Uptake Inhibitor : Design, synthesis and pharmacological characterization. / Vogensen, Stine Byskov; Jørgensen, Lars; Madsen, Karsten Kirkegaard; Borkar, Nrupa Nitin; Wellendorph, Petrine; Skovgaard-Petersen, Jonas; Schousboe, Arne; White, H. Steve; Krogsgaard-Larsen, Povl; Clausen, Rasmus Prætorius.

I: Journal of Medicinal Chemistry, Bind 56, Nr. 5, 11.02.2013, s. 2160-2164.

Publikation: Bidrag til tidsskriftTidsskriftartikelForskningfagfællebedømt

Harvard

Vogensen, SB, Jørgensen, L, Madsen, KK, Borkar, NN, Wellendorph, P, Skovgaard-Petersen, J, Schousboe, A, White, HS, Krogsgaard-Larsen, P & Clausen, RP 2013, 'Selective mGAT2 (BGT-1) GABA Uptake Inhibitor: Design, synthesis and pharmacological characterization', Journal of Medicinal Chemistry, bind 56, nr. 5, s. 2160-2164. https://doi.org/10.1021/jm301872x

APA

Vogensen, S. B., Jørgensen, L., Madsen, K. K., Borkar, N. N., Wellendorph, P., Skovgaard-Petersen, J., ... Clausen, R. P. (2013). Selective mGAT2 (BGT-1) GABA Uptake Inhibitor: Design, synthesis and pharmacological characterization. Journal of Medicinal Chemistry, 56(5), 2160-2164. https://doi.org/10.1021/jm301872x

Vancouver

Vogensen SB, Jørgensen L, Madsen KK, Borkar NN, Wellendorph P, Skovgaard-Petersen J o.a. Selective mGAT2 (BGT-1) GABA Uptake Inhibitor: Design, synthesis and pharmacological characterization. Journal of Medicinal Chemistry. 2013 feb 11;56(5):2160-2164. https://doi.org/10.1021/jm301872x

Author

Vogensen, Stine Byskov ; Jørgensen, Lars ; Madsen, Karsten Kirkegaard ; Borkar, Nrupa Nitin ; Wellendorph, Petrine ; Skovgaard-Petersen, Jonas ; Schousboe, Arne ; White, H. Steve ; Krogsgaard-Larsen, Povl ; Clausen, Rasmus Prætorius. / Selective mGAT2 (BGT-1) GABA Uptake Inhibitor : Design, synthesis and pharmacological characterization. I: Journal of Medicinal Chemistry. 2013 ; Bind 56, Nr. 5. s. 2160-2164.

Bibtex

@article{621bcf24735840a699c479a39c62aa38,
title = "Selective mGAT2 (BGT-1) GABA Uptake Inhibitor: Design, synthesis and pharmacological characterization",
abstract = "β-Amino acids sharing a lipophilic diaromatic side chain were synthesized and characterized pharmacologically on mouse GABA transporter subtypes mGAT1−4. The parent amino acids were also characterized. Compounds 13a, 13b, and 17b displayed more than 6-fold selectivity for mGAT2 over mGAT1. Compound 17b displayed anticonvulsive properties inferring a role of mGAT2 in epileptic disorders. These results provide new neuropharmacological tools and a strategy for designing subtype selective GABA transport inhibitors.",
author = "Vogensen, {Stine Byskov} and Lars J{\o}rgensen and Madsen, {Karsten Kirkegaard} and Borkar, {Nrupa Nitin} and Petrine Wellendorph and Jonas Skovgaard-Petersen and Arne Schousboe and White, {H. Steve} and Povl Krogsgaard-Larsen and Clausen, {Rasmus Pr{\ae}torius}",
year = "2013",
month = "2",
day = "11",
doi = "10.1021/jm301872x",
language = "English",
volume = "56",
pages = "2160--2164",
journal = "Journal of Medicinal Chemistry",
issn = "0022-2623",
publisher = "American Chemical Society",
number = "5",

}

RIS

TY - JOUR

T1 - Selective mGAT2 (BGT-1) GABA Uptake Inhibitor

T2 - Design, synthesis and pharmacological characterization

AU - Vogensen, Stine Byskov

AU - Jørgensen, Lars

AU - Madsen, Karsten Kirkegaard

AU - Borkar, Nrupa Nitin

AU - Wellendorph, Petrine

AU - Skovgaard-Petersen, Jonas

AU - Schousboe, Arne

AU - White, H. Steve

AU - Krogsgaard-Larsen, Povl

AU - Clausen, Rasmus Prætorius

PY - 2013/2/11

Y1 - 2013/2/11

N2 - β-Amino acids sharing a lipophilic diaromatic side chain were synthesized and characterized pharmacologically on mouse GABA transporter subtypes mGAT1−4. The parent amino acids were also characterized. Compounds 13a, 13b, and 17b displayed more than 6-fold selectivity for mGAT2 over mGAT1. Compound 17b displayed anticonvulsive properties inferring a role of mGAT2 in epileptic disorders. These results provide new neuropharmacological tools and a strategy for designing subtype selective GABA transport inhibitors.

AB - β-Amino acids sharing a lipophilic diaromatic side chain were synthesized and characterized pharmacologically on mouse GABA transporter subtypes mGAT1−4. The parent amino acids were also characterized. Compounds 13a, 13b, and 17b displayed more than 6-fold selectivity for mGAT2 over mGAT1. Compound 17b displayed anticonvulsive properties inferring a role of mGAT2 in epileptic disorders. These results provide new neuropharmacological tools and a strategy for designing subtype selective GABA transport inhibitors.

U2 - 10.1021/jm301872x

DO - 10.1021/jm301872x

M3 - Journal article

VL - 56

SP - 2160

EP - 2164

JO - Journal of Medicinal Chemistry

JF - Journal of Medicinal Chemistry

SN - 0022-2623

IS - 5

ER -

ID: 45807862