کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1376368 | 981956 | 2008 | 5 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Use of receptor chimeras to identify small molecules with high affinity for the dynorphin A binding domain of the κ opioid receptor
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
A series of 2-substituted sulfamoyl arylacetamides of general structure 2 were prepared as potent κ opioid receptor agonists and the affinities of these compounds for opioid and chimeric receptors were compared with those of dynorphin A. Compounds 2e and 2i were identified as non-peptide small molecules that bound to chimeras 3 and 4 with high affinities similar to dynorphin A, resulting in Ki values of 1.5 and 1.2 nM and 1.3 and 2.2 nM, respectively.
A series of 2-substituted sulfamoyl arylacetamides of general structure 2 were prepared as potent κ opioid receptor agonists for the dynorphin A binding domain.Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 18, Issue 12, 15 June 2008, Pages 3667–3671
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 18, Issue 12, 15 June 2008, Pages 3667–3671
نویسندگان
Virendra Kumar, Deqi Guo, Michael Marella, Joel A. Cassel, Robert N. DeHaven, Jeffrey D. Daubert, Erik Mansson,