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. 2008 Nov 27;51(22):7061-4.
doi: 10.1021/jm8010178.

Discovery of potent and selective agonists for the free fatty acid receptor 1 (FFA(1)/GPR40), a potential target for the treatment of type II diabetes

Elisabeth Christiansen  1 , Christian Urban, Nicole Merten, Kathrin Liebscher, Kasper K Karlsen, Alexandra Hamacher, Andreas Spinrath, Andrew D Bond, Christel Drewke, Susanne Ullrich, Matthias U Kassack, Evi Kostenis, Trond Ulven
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Discovery of potent and selective agonists for the free fatty acid receptor 1 (FFA(1)/GPR40), a potential target for the treatment of type II diabetes

Elisabeth Christiansen et al. J Med Chem. .

Abstract

A series of 4-phenethynyldihydrocinnamic acid agonists of the free fatty acid receptor 1 (FFA(1)) has been discovered and explored. The preferred compound 20 (TUG-424, EC(50) = 32 nM) significantly increased glucose-stimulated insulin secretion at 100 nM and may serve to explore the role of FFA(1) in metabolic diseases such as diabetes or obesity.

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