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

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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.
Original languageEnglish
JournalJournal of Medicinal Chemistry
Issue number5
Pages (from-to)2160-2164
Number of pages5
Publication statusPublished - 11 Feb 2013

ID: 45807862