| Novel parent structures for inhibitors of the murine GABA transporters mGAT3 and mGAT4. | |
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MedLine Citation:
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PMID: 16111674 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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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 [3H]GABA uptake test system based on transiently expressed mGAT1-4. From several potent inhibitors showing IC50 values at mGAT3 and mGAT4 in the low microM 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. |
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Authors:
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Andrea Kragler; Georg Höfner; Klaus T Wanner |
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Publication Detail:
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Type: Comparative Study; Journal Article; Research Support, Non-U.S. Gov't |
Journal Detail:
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Title: European journal of pharmacology Volume: 519 ISSN: 0014-2999 ISO Abbreviation: Eur. J. Pharmacol. Publication Date: 2005 Sep |
Date Detail:
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Created Date: 2005-09-05 Completed Date: 2005-11-07 Revised Date: 2006-11-15 |
Medline Journal Info:
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Nlm Unique ID: 1254354 Medline TA: Eur J Pharmacol Country: Netherlands |
Other Details:
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Languages: eng Pagination: 43-7 Citation Subset: IM |
Affiliation:
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Department Pharmazie-Zentrum für Pharmaforschung-Ludwig-Maximilians-Universität München, Butenandtstr. 5-13, D-81377 München, Germany. |
Export Citation:
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| MeSH Terms | |
Descriptor/Qualifier:
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Acetic Acids
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chemistry,
pharmacology Animals COS Cells Cell Line Cercopithecus aethiops Dose-Response Relationship, Drug GABA Plasma Membrane Transport Proteins Guanidines / chemistry, pharmacology Humans Membrane Transport Modulators* Membrane Transport Proteins / antagonists & inhibitors*, genetics, metabolism Mice Molecular Structure Neurotransmitter Uptake Inhibitors / chemistry, pharmacology* Plasmids / genetics Propionic Acids / chemistry, pharmacology Serine / analogs & derivatives, chemistry, pharmacology Structure-Activity Relationship Thiazoles / chemistry, pharmacology Transfection Tritium beta-Alanine / analogs & derivatives, chemistry, pharmacology gamma-Aminobutyric Acid / metabolism |
| Chemical | |
Reg. No./Substance:
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0/(2-amino-1,3-thiazol-4-yl)acetic acid; 0/Acetic Acids; 0/GABA Plasma Membrane Transport Proteins; 0/Gabt4 protein, mouse; 0/Guanidines; 0/Membrane Transport Modulators; 0/Membrane Transport Proteins; 0/Neurotransmitter Uptake Inhibitors; 0/Propionic Acids; 0/Slc6a12 protein, mouse; 0/Slc6a13 protein, mouse; 0/Thiazoles; 10028-17-8/Tritium; 107-95-9/beta-Alanine; 353-09-3/guanidinopropionic acid; 515-94-6/2,3-diaminopropionic acid; 56-12-2/gamma-Aminobutyric Acid; 56-45-1/Serine; 565-71-9/isoserine |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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