Ranolazine (142387-99-3) is an FDA-approved drug used for the treatment of chronic angina. It inhibits the late inward sodium current in heart muscle leading to decreased intracellular calcium levels.1 Ranolazine blocks Nav 1.4, 1.5, 1.7 and 1.8 (IC50's = 2.42, 6.22, 1.72(10.33), 21.53 μM respectively.
1) Belardinelli et al., (2006), Inhibition of the late sodium current as a potential cardioprotective principle: effects of the late sodium current inhibitor ranolazine; Heart, 92 iv6
2) Wang et al. (2008), State- and Use-Dependent Block of Muscle Nav1.4 and Neuronal Nav1.7 Voltage-Gated Na+-Channel Isoforms by Ranolazine; Mol. Pharmacol. 73 940
3) Rajamani et al., (2008), Block of tetrodotoxin-sensitive, Na(V)1.7 and tetrodotoxin-resistant, Na(V)1.8, Na+ channels by ranolazine; Channels(Austin) 2 449