Ranolazine

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.

Ranolazine is for the treatment of chronic angina. It should be used in combination with amlodipine, beta-blockers or nitrates.

ChEBI: N-(2,6-dimethylphenyl)-2-{4-[2-hydroxy-3-(2-methoxyphenoxy)propyl]piperazin-1-yl}acetamide is an aromatic amide obtained by formal condensation of the carboxy group of 2-{4-[2-hydroxy-3-(2-methoxyphenoxy)propyl]piperazin-1-yl}acetic acid with the amino group of 2,6-dimethylaniline. It is a monocarboxylic acid amide, an aromatic amide, a N-alkylpiperazine, a secondary alcohol and a monomethoxybenzene.

[1] L BELARDINELLI H F J C Shryock. Inhibition of the late sodium current as a potential cardioprotective principle: effects of the late sodium current inhibitor ranolazine.[J]. Heart, 2006, 92 Suppl 4: iv6-iv14. DOI:10.1136/hrt.2005.078790
[2] GING KUO WANG S Y W Joanna Calderon. State- and use-dependent block of muscle Nav1.4 and neuronal Nav1.7 voltage-gated Na+ channel isoforms by ranolazine.[J]. Molecular Pharmacology, 2008, 73 3: 940-948. DOI:10.1124/mol.107.041541
[3] SRIDHARAN RAJAMANI  Luiz B  John C Shryock. Block of tetrodotoxin-sensitive, Na(V)1.7 and tetrodotoxin-resistant, Na(V)1.8, Na+ channels by ranolazine.[J]. Channels (Austin, Tex.), 2008, 2 6: 449-460. DOI:10.4161/chan.2.6.7362