Selective mGAT2 (BGT-1) GABA Uptake Inhibitors: Design, Synthesis, and Pharmacological Characterization
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- 作者：Stine B. Vogensen ; Lars J酶rgensen ; Karsten K. Madsen ; Nrupa Borkar ; Petrine Wellendorph ; Jonas Skovgaard-Petersen ; Arne Schousboe ; H. Steve White ; Povl Krogsgaard-Larsen ; Rasmus P. Clausen
- 刊名：Journal of Medicinal Chemistry
- 出版年：2013
- 出版时间：March 14, 2013
- 年：2013
- 卷：56
- 期：5
- 页码：2160-2164
- 全文大小：235K
- 年卷期：v.56,no.5(March 14, 2013)
- ISSN：1520-4804
文摘
尾-Amino acids sharing a lipophilic diaromatic side chain were synthesized and characterized pharmacologically on mouse GABA transporter subtypes mGAT1鈥?. 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.