2. Academic Validation
  3. Selective mGAT2 (BGT-1) GABA uptake inhibitors: design, synthesis, and pharmacological characterization

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

  • J Med Chem. 2013 Mar 14;56(5):2160-4. doi: 10.1021/jm301872x.
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
Affiliations

Affiliation

  • 1 Department of Drug Design and Pharmacology, Faculty of Health and Medical Sciences, University of Copenhagen, 2100 Copenhagen, Denmark.
PMID: 23398473 DOI: 10.1021/jm301872x
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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