کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1378947 982014 2005 6 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Arylacetamide κ opioid receptor agonists with reduced cytochrome P450 2D6 inhibitory activity
کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Arylacetamide κ opioid receptor agonists with reduced cytochrome P450 2D6 inhibitory activity
چکیده انگلیسی

Some κ opioid receptor agonists of the arylacetamide class, for example, ICI 199441 (1), were found to strongly inhibit the activity of cytochrome P450 2D6 (CYP2D6) (1: CYP2D6 IC50 = 26 nM). Certain analogs bearing a substituted sulfonylamino group, for example, 13, were discovered to have significantly reduced CYP2D6 inhibitory activity (13: CYP2D6 IC50 > 10 μM) while displaying high affinity toward the cloned human κ opioid receptor, good κ/δ and κ/μ selectivity, and potent in vitro and in vivo agonist activity.

Synthetic strategies to improve the selectivity of the arylacetamide class of κ opioid agonists toward CYP2D6 is reported.Figure optionsDownload as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 15, Issue 10, 16 May 2005, Pages 2647–2652
نویسندگان
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