Discovery of Potent and Selective Agonists for the Free Fatty Acid Receptor 1 (FFA1/GPR40), a Potential Target for the Treatment of Type II Diabetes

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• 作者：Elisabeth Christiansen ; Christian Urban ; Nicole Merten ; Kathrin Liebscher ; Kasper K. Karlsen ; Alexandra Hamacher ; Andreas Spinrath ; Andrew D. Bond ; Christel Drewke ; Susanne Ullrich ; Matthias U. Kassac
• 刊名：Journal of Medicinal Chemistry
• 出版年：2008
• 出版时间：November 27, 2008
• 年：2008
• 卷：51
• 期：22
• 页码：7061-7064
• 全文大小：156K
• 年卷期：v.51,no.22(November 27, 2008)
• ISSN：1520-4804

文摘

A series of 4-phenethynyldihydrocinnamic acid agonists of the free fatty acid receptor 1 (FFA₁) has been discovered and explored. The preferred compound 20 (TUG-424, EC₅₀ = 32 nM) significantly increased glucose-stimulated insulin secretion at 100 nM and may serve to explore the role of FFA₁ in metabolic diseases such as diabetes or obesity.