sodium channel type II Inhibitors
Chemical inhibitors of sodium channel type II include a variety of compounds that interact with the channel in different ways to prevent the flow of sodium ions across neuronal membranes. Tetrodotoxin and saxitoxin, for instance, are known to bind to the extracellular side of sodium channel type II and block sodium ion entry, which stops the initiation and propagation of action potentials. Similarly, μ-conotoxin selectively attaches to these channels, inhibiting sodium ion flow and thus blocking neuronal signaling. Lidocaine, on the other hand, acts as a local anesthetic by binding to these channels on the neuronal cell membrane, inhibiting the necessary ionic fluxes for impulse initiation and conduction, leading to loss of sensation.
Other compounds such as phenytoin, carbamazepine, and lamotrigine modulate sodium channel type II by stabilizing the inactive state of the channel or by blocking the channels, thereby reducing neuronal excitability and synaptic transmission. Riluzole indirectly inhibits these sodium channels by enhancing their inactivation, which suppresses repetitive neuronal firing. Ranolazine is unique in that it selectively inhibits the late phase of the inward sodium current, which is thought to reduce excitability in a similar manner in neuronal cells. Aconitine, batrachotoxin, and veratridine all interact with sodium channel type II but do so by binding and holding the channels open, preventing inactivation, and leading to prolonged depolarization that ultimately inhibits normal action potential generation due to the sustained influx of sodium ions.
SEE ALSO...
| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Lidocaine | 137-58-6 | sc-204056 sc-204056A | 50 mg 1 g | $50.00 $128.00 | ||
Lidocaine acts as a local anesthetic by blocking sodium channels, including sodium channel type II, on the neuronal cell membrane. This action inhibits the ionic fluxes required for the initiation and conduction of impulses, resulting in a loss of sensation. | ||||||
5,5-Diphenyl Hydantoin | 57-41-0 | sc-210385 | 5 g | $70.00 | ||
Phenytoin binds to and modulates voltage-gated sodium channels like sodium channel type II, stabilizing the inactive state of the channel. This reduces the neuronal firing rate by limiting repetitive firing and preventing the generation of sustained high-frequency action potentials. | ||||||
Carbamazepine | 298-46-4 | sc-202518 sc-202518A | 1 g 5 g | $32.00 $70.00 | 5 | |
Carbamazepine works by binding to and inhibiting voltage-gated sodium channels, including sodium channel type II. This action diminishes synaptic transmission by reducing the post-synaptic excitatory effects of glutamate and aspartate to their respective receptors. | ||||||
Riluzole | 1744-22-5 | sc-201081 sc-201081A sc-201081B sc-201081C | 20 mg 100 mg 1 g 25 g | $20.00 $189.00 $209.00 $311.00 | 1 | |
Riluzole indirectly inhibits sodium channels, including sodium channel type II, by enhancing the inactivation of the voltage-dependent sodium channels. This suppresses the repetitive neuronal firing and stabilizes the neuronal membrane. | ||||||
Ranolazine | 95635-55-5 | sc-212769 | 1 g | $107.00 | 3 | |
Ranolazine selectively inhibits the late phase of the inward sodium current in cardiac cells, thereby reducing intracellular calcium overload. As it inhibits persistent or late inward sodium current, it is thought to inhibit sodium channel type II in a similar manner in neuronal cells, which would result in reduced excitability of the cell. | ||||||
Lamotrigine | 84057-84-1 | sc-201079 sc-201079A | 10 mg 50 mg | $118.00 $476.00 | 1 | |
Lamotrigine blocks voltage-sensitive sodium channels, including sodium channel type II, leading to stabilization of the neuronal membrane and inhibition of the release of excitatory neurotransmitters such as glutamate and aspartate. | ||||||
Aconitine | 302-27-2 | sc-202441 sc-202441A sc-202441B sc-202441C sc-202441D | 25 mg 50 mg 100 mg 250 mg 500 mg | $300.00 $450.00 $650.00 $1252.00 $2050.00 | ||
Aconitine binds to the voltage-dependent sodium channels like sodium channel type II on the cell membrane of neurons and muscles, holding the channels open and preventing inactivation. This results in persistent sodium influx, which ultimately inhibits action potential propagation due to prolonged depolarization. | ||||||
Veratridine | 71-62-5 | sc-201075B sc-201075 sc-201075C sc-201075A | 5 mg 10 mg 25 mg 50 mg | $80.00 $102.00 $197.00 $372.00 | 3 | |
Veratridine binds to and activates voltage-gated sodium channels such as sodium channel type II, holding them open and leading to a prolonged sodium influx. This results in continuous depolarization, which eventually inhibits normal action potential generation due to the inactivation of voltage-gated sodium channels. | ||||||