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GPR119 is expressed predominantly in the pancreas and gastrointestinal tract in rodents and humans, as well as in the brain in rodents.[5] Activation of the receptor has been shown to cause a reduction in food intake and body weight gain in rats.[5] GPR119 has also been shown to regulate incretin and insulinhormone secretion.[6][7][8] As a result, new drugs acting on the receptor have been suggested as novel treatments for obesity and diabetes.[5][7][9]
↑Izzo AA, Sharkey KA (Apr 2010). "Cannabinoids and the gut: new developments and emerging concepts". Pharmacology & Therapeutics. 126 (1): 21–38. doi:10.1016/j.pharmthera.2009.12.005. PMID20117132.
↑ 5.05.15.25.35.45.5Overton HA, Babbs AJ, Doel SM, Fyfe MC, Gardner LS, Griffin G, Jackson HC, Procter MJ, Rasamison CM, Tang-Christensen M, Widdowson PS, Williams GM, Reynet C (Mar 2006). "Deorphanization of a G protein-coupled receptor for oleoylethanolamide and its use in the discovery of small-molecule hypophagic agents". Cell Metabolism. 3 (3): 167–75. doi:10.1016/j.cmet.2006.02.004. PMID16517404.
↑ 7.07.1Swaminath G (Dec 2008). "Fatty acid binding receptors and their physiological role in type 2 diabetes". Archiv der Pharmazie. 341 (12): 753–61. doi:10.1002/ardp.200800096. PMID19009545.
↑Lan H, Vassileva G, Corona A, Liu L, Baker H, Golovko A, Abbondanzo SJ, Hu W, Yang S, Ning Y, Del Vecchio RA, Poulet F, Laverty M, Gustafson EL, Hedrick JA, Kowalski TJ (May 2009). "GPR119 is required for physiological regulation of glucagon-like peptide-1 secretion but not for metabolic homeostasis". The Journal of Endocrinology. 201 (2): 219–30. doi:10.1677/JOE-08-0453. PMID19282326.
↑Shah U (Jul 2009). "GPR119 agonists: a promising new approach for the treatment of type 2 diabetes and related metabolic disorders". Current Opinion in Drug Discovery & Development. 12 (4): 519–32. PMID19562648.
↑Wu Y, Kuntz JD, Carpenter AJ, Fang J, Sauls HR, Gomez DJ, Ammala C, Xu Y, Hart S, Tadepalli S (Apr 2010). "2,5-Disubstituted pyridines as potent GPR119 agonists". Bioorganic & Medicinal Chemistry Letters. 20 (8): 2577–81. doi:10.1016/j.bmcl.2010.02.083. PMID20227877.
↑Hansen KB, Rosenkilde MM, Knop FK, Wellner N, Diep TA, Rehfeld JF, Andersen UB, Holst JJ, Hansen HS (Sep 2011). "2-Oleoyl glycerol is a GPR119 agonist and signals GLP-1 release in humans". The Journal of Clinical Endocrinology and Metabolism. 96 (9): E1409–E1417. doi:10.1210/jc.2011-0647. PMID21778222.
↑Semple G, Fioravanti B, Pereira G, Calderon I, Uy J, Choi K, Xiong Y, Ren A, Morgan M, Dave V, Thomsen W, Unett DJ, Xing C, Bossie S, Carroll C, Chu ZL, Grottick AJ, Hauser EK, Leonard J, Jones RM (Sep 2008). "Discovery of the first potent and orally efficacious agonist of the orphan G-protein coupled receptor 119". Journal of Medicinal Chemistry. 51 (17): 5172–5. doi:10.1021/jm8006867. PMID18698756.
↑Jones RM, Leonard JN, Buzard DJ, Lehmann J (Oct 2009). "GPR119 agonists for the treatment of type 2 diabetes". Expert Opinion on Therapeutic Patents. 19 (10): 1339–59. doi:10.1517/13543770903153878. PMID19780700.
Further reading
Takeda S, Kadowaki S, Haga T, Takaesu H, Mitaku S (Jun 2002). "Identification of G protein-coupled receptor genes from the human genome sequence". FEBS Letters. 520 (1–3): 97–101. doi:10.1016/S0014-5793(02)02775-8. PMID12044878.
Fredriksson R, Höglund PJ, Gloriam DE, Lagerström MC, Schiöth HB (Nov 2003). "Seven evolutionarily conserved human rhodopsin G protein-coupled receptors lacking close relatives". FEBS Letters. 554 (3): 381–8. doi:10.1016/S0014-5793(03)01196-7. PMID14623098.