1206629-06-2Relevant academic research and scientific papers
Identification of a potent and selective free fatty acid receptor 1 (FFA1/GPR40) agonist with favorable physicochemical and in vitro ADME properties
Christiansen, Elisabeth,Urban, Christian,Grundmann, Manuel,Due-Hansen, Maria E.,Hagesaether, Ellen,Schmidt, Johannes,Pardo, Leonardo,Ullrich, Susanne,Kostenis, Evi,Kassack, Matthias,Ulven, Trond
supporting information; experimental part, p. 6691 - 6703 (2011/12/02)
The free fatty acid receptor 1 (FFA1, also known as GPR40) enhances glucose-stimulated insulin secretion from pancreatic β-cells and is recognized as an interesting new target for treatment of type 2 diabetes. Several series of selective FFA1 agonists are already known. Most of these are derived from free fatty acids (FFAs) or glitazones and are relatively lipophilic. Aiming for the development of potent, selective, and less lipophilic FFA1 agonists, the terminal phenyl of a known compound series was replaced by nitrogen containing heterocycles. This resulted in the identification of 37, a selective FFA1 agonist with potent activity on recombinant human FFA1 receptors and on the rat insulinoma cell line INS-1E, optimal lipophilicity, and excellent in vitro permeability and metabolic stability.
COMPOUNDS FOR THE TREATMENT OF METABOLIC DISEASES
-
Page/Page column 68, (2010/04/03)
There is provided novel compounds capable of modulating the G-protein-coupled receptor GPR40, compositions comprising the compounds, and methods for their use for controlling insulin levels in vivo and for the treatment of conditions such as type Il diabetes, hypertension, ketoacidosis, obesity, glucose intolerance, and hypercholesterolemia and related disorders associated with abnormally high or low plasma lipoprotein, triglyceride or glucose levels.
