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Discovery of Dihydrobenzoxazepinone (GS-6615) Late Sodium Current Inhibitor (Late INai), a Phase II Agent with Demonstrated Preclinical Anti-Ischemic and Antiarrhythmic Properties.
Zablocki JA, Elzein E, Li X, Koltun DO, Parkhill EQ, Kobayashi T, Martinez R, Corkey B, Jiang H, Perry T, Kalla R, Notte GT, Saunders O, Graupe M, Lu Y, Venkataramani C, Guerrero J, Perry J, Osier M, Strickley R, Liu G, Wang WQ, Hu L, Li XJ, El-Bizri N, Hirakawa R, Kahlig K, Xie C, Li CH, Dhalla AK, Rajamani S, Mollova N, Soohoo D, Lepist EI, Murray B, Rhodes G, Belardinelli L, Desai MC. Zablocki JA, et al. Among authors: hirakawa r. J Med Chem. 2016 Oct 13;59(19):9005-9017. doi: 10.1021/acs.jmedchem.6b00939. Epub 2016 Oct 3. J Med Chem. 2016. PMID: 27690427
Discovery of triazolopyridinone GS-462808, a late sodium current inhibitor (Late INai) of the cardiac Nav1.5 channel with improved efficacy and potency relative to ranolazine.
Koltun DO, Parkhill EQ, Elzein E, Kobayashi T, Jiang RH, Li X, Perry TD, Avila B, Wang WQ, Hirakawa R, Smith-Maxwell C, Wu L, Dhalla AK, Rajamani S, Mollova N, Stafford B, Tang J, Belardinelli L, Zablocki JA. Koltun DO, et al. Among authors: hirakawa r. Bioorg Med Chem Lett. 2016 Jul 1;26(13):3207-3211. doi: 10.1016/j.bmcl.2016.03.096. Epub 2016 Mar 26. Bioorg Med Chem Lett. 2016. PMID: 27038498
A novel, potent, and selective inhibitor of cardiac late sodium current suppresses experimental arrhythmias.
Belardinelli L, Liu G, Smith-Maxwell C, Wang WQ, El-Bizri N, Hirakawa R, Karpinski S, Li CH, Hu L, Li XJ, Crumb W, Wu L, Koltun D, Zablocki J, Yao L, Dhalla AK, Rajamani S, Shryock JC. Belardinelli L, et al. Among authors: hirakawa r. J Pharmacol Exp Ther. 2013 Jan;344(1):23-32. doi: 10.1124/jpet.112.198887. Epub 2012 Sep 25. J Pharmacol Exp Ther. 2013. PMID: 23010360
Contribution of the late sodium current to intracellular sodium and calcium overload in rabbit ventricular myocytes treated by anemone toxin.
Kornyeyev D, El-Bizri N, Hirakawa R, Nguyen S, Viatchenko-Karpinski S, Yao L, Rajamani S, Belardinelli L. Kornyeyev D, et al. Among authors: hirakawa r. Am J Physiol Heart Circ Physiol. 2016 Feb 1;310(3):H426-35. doi: 10.1152/ajpheart.00520.2015. Epub 2015 Dec 4. Am J Physiol Heart Circ Physiol. 2016. PMID: 26637557 Free article.
37 results