Selective mGAT2 (BGT-1) GABA Uptake Inhibitor: Design, synthesis and pharmacological characterization
Publikation: Bidrag til tidsskrift › Tidsskriftartikel › Forskning › fagfællebedømt
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.
Originalsprog | Engelsk |
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Tidsskrift | Journal of Medicinal Chemistry |
Vol/bind | 56 |
Udgave nummer | 5 |
Sider (fra-til) | 2160-2164 |
Antal sider | 5 |
DOI | |
Status | Udgivet - 11 feb. 2013 |
ID: 45807862