Tolperisone hydrochloride. A Non-Selective Nav Channel Blocker.
Voltage-gated Na+ channels (VGSC, Nav) are critically important for electrogenesis and nerve impulse conduction. Certain Na+ channel isoforms are predominantly expressed in peripheral sensory neurons associated with pain sensation, and the expression and functional properties of Nav in peripheral sensory neurons can be dynamically regulated following axonal injury or peripheral inflammation.
Tolperisone is a centrally acting muscle relaxant (muscle relaxant acting on spasticity by interaction with upper motor neurons), which is also used for the treatment of chronic pain. It is mainly used for treating muscle spasticities of neurological origin and painful muscle spasms due to rheumatologic conditions. Besides being an effective antispastic agent, tolperisone also has analgesic activity in rodents and in humans. It possesses relatively few side effects in humans.
Tolperisone is an ion channel blocker that acts, at micromolar concentrations, as an acute blocker of seven different isoforms of Nav, expressed in Xenopus oocytes. The drug concentrations needed to exert 50% block differ between the different isoforms and are 116, 802, 96, 131, 326, 394 and 49 μM for Nav1.2, Nav1.3, Nav1.4, Nav1.5, Nav1.6, Nav1.7 and Nav1.8 channel, respectively. Nav1.8, which is the most prominently affected channel, is known to be upregulated in an animal model of neuropathic pain.
The inhibitory effect is reversible and develops rapidly, with an IC50 value of 198 μM in dorsal root ganglion (DRG) cells.
Ion Channel Modulators; Voltage - Gated Na+ Channel Blockers
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