Journal
EUROPEAN JOURNAL OF PHARMACOLOGY
Volume 519, Issue 1-2, Pages 43-47Publisher
ELSEVIER
DOI: 10.1016/j.ejphar.2005.06.053
Keywords
murine GABA transporter (mGAT1-4); GABA (gamma-aminobutyric acid) uptake; structure activity relationship; subtype selectivity
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Searching for potent and subtype selective parent structures of the murine gamma-aminobutyric acid (GABA) transporter subtypes mGAT3 and mGAT4 a series of amino acids was characterised in a uniform [H-3]GABA uptake test system based on transiently expressed mGAT1-4. From several potent inhibitors showing IC50 values at mGAT3 and mGAT4 in the low mu M range cis-4-aminocrotonic acid and (RS)-2,3-diaminopropionic acid turned out to be most subtype selective for these transporters. With (RS)-isoserine - a compound unknown as GAT inhibitor until now - one of the most potent amino acids selectively inhibiting mGAT3 and mGAT4 was found. Furthermore, (2-amino-1,3-thiazol-4-yl)acetic acid was identified as the first parent structure exhibiting a clear, though still moderate, selective inhibition of GABA uptake at mGAT3. (c) 2005 Elsevier B.V. All rights reserved.
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