کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1370464 | 981819 | 2011 | 4 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Discovery of a novel potent GABAB receptor agonist
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: Discovery of a novel potent GABAB receptor agonist Discovery of a novel potent GABAB receptor agonist](/preview/png/1370464.png)
چکیده انگلیسی
Structure–activity studies have led to a discovery of 3-(4-pyridyl)methyl ether derivative 9d that has 25- to 50-fold greater functional potency than R-baclofen at human and rodent GABAB receptors in vitro. Mouse hypothermia studies confirm that this compound crosses the blood–brain barrier and is approximately 50-fold more potent after systemic administration.
Novel substituted analogs or R-baclofen was explored and a highly potent agonist was discovered. (9d pEC50 = 8.5). Characterization of 9d showed it to be 25- to 50-fold more potent than R-baclofen in vitro and in vivo.Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 21, Issue 21, 1 November 2011, Pages 6582–6585
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 21, Issue 21, 1 November 2011, Pages 6582–6585
نویسندگان
Feng Xu, Ge Peng, Thu Phan, Usha Dilip, Jian Lu Chen, Tania Chernov-Rogan, Xuexiang Zhang, Kent Grindstaff, Thamil Annamalai, Kerry Koller, Mark A. Gallop, David J. Wustrow,