Discovery of Dapagliflozin: A Potent, Selective Renal Sodium-Dependent Glucose Cotransporter 2 (SGLT2) Inhibitor for the Treatment of Type 2 Diabetes
Journal of Medicinal Chemistry2008Vol. 51(5), pp. 1145–1149
Citations Over TimeTop 1% of 2008 papers
Wei Meng, Bruce A. Ellsworth, Alexandra A. Nirschl, Peggy J. McCann, Manorama M. Patel, Ravindar N. Girotra, Gang Wu, Philip M. Sher, Eamonn P. Morrison, Scott A. Biller, Robert Zahler, Prashant P. Deshpande, Annie Pullockaran, Deborah Hagan, Nathan Morgan, Joseph R. Taylor, Mary T. Obermeier, W. Griffith Humphreys, Ashish K. Khanna, Lorell Discenza, James G. Robertson, Wang Aiying, Song‐Ping Han, John R. Wetterau, Evan B. Janovitz, Oliver Flint, Jean M. Whaley, William N. Washburn
Abstract
The C-aryl glucoside 6 (dapagliflozin) was identified as a potent and selective hSGLT2 inhibitor which reduced blood glucose levels in a dose-dependent manner by as much as 55% in hyperglycemic streptozotocin (STZ) rats. These findings, combined with a favorable ADME profile, have prompted clinical evaluation of dapagliflozin for the treatment of type 2 diabetes.
Related Papers
- → Role of Thyroid Hormone in Regulation of Renal Phosphate Transport in Young and Aged Rats1(1999)95 cited
- → Characterization of Increased Plasma Dopamine-β-Hydroxylase Activity in Rats with Experimental Diabetes(1981)10 cited
- → Effect of High Sodium Intake on the Response of the Rat Adrenal to Angiotensin II(1969)8 cited
- [Renal SGLT2 inhibitors, new agents for the management of type 2 diabetes].(2011)
- Effects of endogenous and exogenous hyperglycemia on renal glucose transport in the rat.(1991)