کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
9921154 | 1559204 | 2005 | 5 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Novel parent structures for inhibitors of the murine GABA transporters mGAT3 and mGAT4
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کلمات کلیدی
موضوعات مرتبط
علوم زیستی و بیوفناوری
علم عصب شناسی
علوم اعصاب سلولی و مولکولی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: Novel parent structures for inhibitors of the murine GABA transporters mGAT3 and mGAT4 Novel parent structures for inhibitors of the murine GABA transporters mGAT3 and mGAT4](/preview/png/9921154.png)
چکیده انگلیسی
Searching for potent and subtype selective parent structures of the murine γ-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 μM 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.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: European Journal of Pharmacology - Volume 519, Issues 1â2, 5 September 2005, Pages 43-47
Journal: European Journal of Pharmacology - Volume 519, Issues 1â2, 5 September 2005, Pages 43-47
نویسندگان
Andrea Kragler, Georg Höfner, Klaus T. Wanner,