کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1369783 | 981789 | 2012 | 6 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Continued optimization of the MLPCN probe ML071 into highly potent agonists of the hM1 muscarinic acetylcholine receptor
دانلود مقاله + سفارش ترجمه
دانلود مقاله ISI انگلیسی
رایگان برای ایرانیان
کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: Continued optimization of the MLPCN probe ML071 into highly potent agonists of the hM1 muscarinic acetylcholine receptor Continued optimization of the MLPCN probe ML071 into highly potent agonists of the hM1 muscarinic acetylcholine receptor](/preview/png/1369783.png)
چکیده انگلیسی
This Letter describes the continued optimization of the MLPCN probe molecule ML071. After introducing numerous cyclic constraints and novel substitutions throughout the parent structure, we produced a number of more highly potent agonists of the M1 mACh receptor. While many novel agonists demonstrated a promising ability to increase soluble APPα release, further characterization indicated they may be functioning as bitopic agonists. These results and the implications of a bitopic mode of action are presented.
Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 22, Issue 10, 15 May 2012, Pages 3467–3472
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 22, Issue 10, 15 May 2012, Pages 3467–3472
نویسندگان
Bruce J. Melancon, Rocco D. Gogliotti, James C. Tarr, Sam A. Saleh, Brian A. Chauder, Evan P. Lebois, Hyekyung P. Cho, Thomas J. Utley, Douglas J. Sheffler, Thomas M. Bridges, Ryan D. Morrison, J. Scott Daniels, Colleen M. Niswender, P. Jeffrey Conn,