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10.1021/ml300133f http://scihub22266oqcxt.onion/10.1021/ml300133f C4025659!4025659!24900539     free     free     free Deprecated: Implicit conversion from float 233.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 233.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 233.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 233.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534       ACS+Med+Chem+Lett 2012 ; 3 (9): 726-30 Nephropedia Template TP {{tp|p=24900539|t=2012. Discovery of AM-1638: A Potent and Orally Bioavailable GPR40/FFA1 Full Agonist |pdf=|usr=}}{{24900539}} gab.com Text Discovery of AM-1638: A Potent and Orally Bioavailable GPR40/FFA1 Full Agonist JO: ACS Med Chem Lett http://www.kidney.de/pget.php?&tw=1&pmid=24900539 #FOAvip GPR40 (FFA1) is a G-protein-coupled receptor, primarily expressed in pancreatic islets, the activation of which elicits increased insulin secretion only in the presence of elevated glucose levels. A potent, orally bioavailable small molecule GPR40 agonist is hypothesized to be an effective antidiabetic posing little or no risk of hypoglycemia. We recently reported the discovery of AMG 837 (1), a potent partial agonist of GPR40. Herein, we present the optimization from the GPR40 partial agonist 1 to the structurally and pharmacologically distinct GPR40 full agonist AM-1638 (21). Moreover, we demonstrate the improved in vivo efficacy that GPR40 full agonist 21 exhibits in BDF/DIO mice as compared to partial agonist 1. Twit Text FOAVip Discovery of AM-1638: A Potent and Orally Bioavailable GPR40/FFA1 Full Agonist ????ACS Med Chem Lett http://www.kidney.de/pget.php?&tw=1&pmid=24900539 #FOAvip Twit Text # Free Paper on # # # # # LINK http://www.kidney.de/pget.php?&tw=1&pmid=24900539 #FOAvip English Wikipedia <ref>{{Cite pmid|24900539}}</ref> Discovery of AM-1638: A Potent and Orally Bioavailable GPR40/FFA1 Full Agonist #MMPMID24900539 Brown SP; Dransfield PJ; Vimolratana M; Jiao X; Zhu L; Pattaropong V; Sun Y; Liu J; Luo J; Zhang J; Wong S; Zhuang R; Guo Q; Li F; Medina JC; Swaminath G; Lin DCH; Houze J ACS Med Chem Lett 2012[Sep]; 3 (9): 726-30 PMID24900539show ga GPR40 (FFA1) is a G-protein-coupled receptor, primarily expressed in pancreatic islets, the activation of which elicits increased insulin secretion only in the presence of elevated glucose levels. A potent, orally bioavailable small molecule GPR40 agonist is hypothesized to be an effective antidiabetic posing little or no risk of hypoglycemia. We recently reported the discovery of AMG 837 (1), a potent partial agonist of GPR40. Herein, we present the optimization from the GPR40 partial agonist 1 to the structurally and pharmacologically distinct GPR40 full agonist AM-1638 (21). Moreover, we demonstrate the improved in vivo efficacy that GPR40 full agonist 21 exhibits in BDF/DIO mice as compared to partial agonist 1. äDiscovery of AM-1638: A Potent and Orally Bioavailable GPR40/FFA1 Full(epmc).pdf DeepDyve Pubget Overpricing