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. 2013 Mar 14;56(5):2160-4.
doi: 10.1021/jm301872x. Epub 2013 Feb 27.

Selective mGAT2 (BGT-1) GABA uptake inhibitors: design, synthesis, and pharmacological characterization

Stine B Vogensen  1 , Lars Jørgensen, Karsten K Madsen, Nrupa Borkar, Petrine Wellendorph, Jonas Skovgaard-Petersen, Arne Schousboe, H Steve White, Povl Krogsgaard-Larsen, Rasmus P Clausen
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Selective mGAT2 (BGT-1) GABA uptake inhibitors: design, synthesis, and pharmacological characterization

Stine B Vogensen et al. J Med Chem. .

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.

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