کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1366715 981600 2007 5 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
PDE-10A inhibitors as insulin secretagogues
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
PDE-10A inhibitors as insulin secretagogues
چکیده انگلیسی

Modulation of cAMP levels has been linked to insulin secretion in preclinical animal models and in humans. The high expression of PDE-10A in pancreatic islets suggested that inhibition of this enzyme may provide the necessary modulation to elicit increased insulin secretion. Using an HTS approach, we have identified quinoline-based PDE-10A inhibitors as insulin secretagogues in vitro. Optimized compounds were evaluated in vivo where improvements in glucose tolerance and increases in insulin secretion were measured.

A series of quinoline-based PDE-10A inhibitors was determined to cause insulin secretion in vitro. Optimized compounds were evaluated in vivo where improvements in glucose tolerance and increases in insulin secretion were measured.Figure optionsDownload as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 17, Issue 10, 15 May 2007, Pages 2869–2873
نویسندگان
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