CBR– GPR-40 CANNABINOID RECEPTOR – activated by GW1100, TAK-875

 

The Ffa Receptor Gpr40 Links Hyperinsulinemia, Hepatic Steatosis, and Impaired Glucose Homeostasis in Mouse.                                                                       (abst – 2005)  http://www.ncbi.nlm.nih.gov/pubmed/16054069

 

Gpr40 Gene Expression in Human Pancreas and Insulinoma.                   (abst – 2005)

http://www.ncbi.nlm.nih.gov/pubmed/16289108

 

Pharmacological regulation of insulin secretion in MIN6 cells through the fatty acid receptor GPR40: identification of agonist and antagonist small molecules.                                                                     (full – 2006)  http://www.ncbi.nlm.nih.gov/pmc/articles/PMC1751878/?tool=pubmed

 

Expression of the Gene for a Membrane-bound Fatty Acid Receptor in the Pancreas and Islet Cell Tumours in Humans: Evidence for Gpr40 Expression in Pancreatic Beta Cells and Implications for Insulin Secretion.                                                                                    (abst – 2006)  http://www.ncbi.nlm.nih.gov/pubmed/16525841

 

Selective small-molecule agonists of G protein-coupled receptor 40 promote glucose- dependent insulin secretion and reduce blood glucose in mice.                                                                  (full – 2008)  http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2494688/?tool=pubmed

 

Overexpression of GPR40 in pancreatic beta-cells augments glucose-stimulated insulin secretion and improves glucose tolerance in normal and diabetic mice. (full – 2009)  http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2671040/?tool=pubmed

 

Acute administration of GPR40 receptor agonist potentiates glucose-stimulated insulin secretion in vivo in the rat.                                                                (abst – 2009)    http://www.ncbi.nlm.nih.gov/pubmed/19217448

 

International Union of Basic and Clinical Pharmacology. LXXIX. Cannabinoid Receptors and Their Ligands: Beyond CB1 and CB2                                                                   (full – 2010)  http://pharmrev.aspetjournals.org/content/62/4/588.full.pdf+html

 

TAK-875, an orally available G protein-coupled receptor 40/free fatty acid receptor 1 agonist, enhances glucose-dependent insulin secretion and improves both postprandial and fasting hyperglycemia in type 2 diabetic rats.                                                                                                      (abst – 2011)  http://www.ncbi.nlm.nih.gov/pubmed/21752941

 

A Multiple-Ascending-Dose Study to Evaluate Safety, Pharmacokinetics, and Pharmacodynamics of a Novel GPR40 Agonist, TAK-875, in Subjects With Type 2 Diabetes.       (abst – 2012)                                     http://www.ncbi.nlm.nih.gov/pubmed/22669289

 

Optimization of (2,3-dihydro-1-benzofuran-3-yl)acetic acids: discovery of a non-free fatty acid-like, highly bioavailable G protein-coupled receptor 40/free fatty acid receptor 1 agonist as a glucose-dependent insulinotropic agent.                                                                                                   (abst – 2012)  http://www.ncbi.nlm.nih.gov/pubmed/22490067

 

 

 

 

 

 

 

 

TAK-875 versus placebo or glimepiride in type 2 diabetes mellitus: a phase 2, randomised, double-blind, placebo-controlled trial.                                                                                (abst – 2012)  http://www.ncbi.nlm.nih.gov/pubmed/22374408

 

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