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.
In:
Journal of Medicinal Chemistry, Vol. 56, No. 5, 11.02.2013, p. 2160-2164.
Research output: Contribution to journal › Journal article › Research › peer-review
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, vol. 56, no. 5, pp. 2160-2164.
https://doi.org/10.1021/jm301872xAPA
Vogensen, S. B., Jørgensen, L., Madsen, K. K., Borkar, N. N.
, Wellendorph, P., Skovgaard-Petersen, J.
, Schousboe, A., White, H. S.
, Krogsgaard-Larsen, P., & 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/jm301872xVancouver
Vogensen SB, Jørgensen L, Madsen KK, Borkar NN
, Wellendorph P, Skovgaard-Petersen J et al.
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/jm301872xAuthor
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. In: Journal of Medicinal Chemistry. 2013 ; Vol. 56, No. 5. pp. 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 = feb,
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 -
