کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
2022969 1542426 2010 9 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Novel, non-peptidic somatostatin receptor subtype 5 antagonists improve glucose tolerance in rodents
موضوعات مرتبط
علوم زیستی و بیوفناوری بیوشیمی، ژنتیک و زیست شناسی مولکولی زیست شیمی
پیش نمایش صفحه اول مقاله
Novel, non-peptidic somatostatin receptor subtype 5 antagonists improve glucose tolerance in rodents
چکیده انگلیسی

BackgroundSomatostatin regulates numerous endocrine processes, including glucose homeostasis. The contribution and effects of the 5 somatostatin receptors are still unclear, in part due to the lack of suitable subtype specific receptor antagonists. We explored the effects of two novel, non-peptidic, orally bioavailable somatostatin receptor subtype 5 antagonists named Compound A and Compound B on glycemia in animal models of type 2 diabetes after an initial in vitro characterization.Methods and resultsCompound A led to a dose-dependent decrease in glucose and insulin excursions during an OGTT in Zucker (fa/fa) rats after single treatment by up to 17% and 49%, respectively. Diet-induced obese mice showed after three weeks treatment with compounds A and B a dose-dependent decrease of the glucose excursion of up to 45% and 37%, respectively. In contrast to the acute effect observed in Zucker rats, Compound A showed a dose-dependent insulin increase by up to 72%, whereas body weight, liver triglycerides, ALT and AST were dose-dependently decreased.ConclusionsSSTR5 antagonists have the potential for short- and long-term improvements of the glucose homeostasis in rodent models of type 2 diabetes.Further work on the mechanism and the relevance for human disease is warranted.

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Regulatory Peptides - Volume 159, Issues 1–3, 8 January 2010, Pages 19–27
نویسندگان
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