180979-18-4Relevant academic research and scientific papers
Selective mGAT2 (BGT-1) GABA uptake inhibitors: Design, synthesis, and pharmacological characterization
Vogensen, Stine B.,J?rgensen, Lars,Madsen, Karsten K.,Borkar, Nrupa,Wellendorph, Petrine,Skovgaard-Petersen, Jonas,Schousboe, Arne,White, H. Steve,Krogsgaard-Larsen, Povl,Clausen, Rasmus P.
supporting information, p. 2160 - 2164 (2013/05/08)
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.
