Ranolazine is an antianginal and anti-ischemic drug that is used in patients with chronic angina. Ranolazine displays a broad pharmacological profile on a number of targets and has complex electrophysiological effects in myocardium. This drug seems to preferentially reduce the persistent late cardiac NaV1.5 Na+ currents with a 50% inhibitory concentration (IC50) of 15 μM, whereas normal transient Na+ currents are less affected, with an IC50 of 135 μM4. The binding site of ranolazine in human cardiac Na+ channels is probably the same as the local anesthetic (LA) receptor within the inner cavity of the Na+ channel, because a single mutation in this channel (e.g., residue hNav1.5-F1760A) alters the ranolazine binding affinity drastically.
产品描述
A Blocker of Voltage-Gated Na+ Channels
产品形式
Voltage-gated Na+ (NaV) channels are essential for the generation and propagation of action potentials in excitable membranes. The NaV channel protein contains four homologous domains (D1-D4), each with six transmembrane segments (S1-S6). There are 9 isoforms (NaV1.1-1.9) found among mammalian excitable tissues, including central nervous system, peripheral nervous system, skeletal muscle, and heart.