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Riluzole is a compound used to study ALS. Riluzole preferentially blocks TTX-sensitive sodium channels, which are associated with impaired neurons. This reduces the influx of calcium ions and indirectly blocks the stimulation of glutamate receptors. Rilutek inhibits glutamate release from the presynaptic terminal and increases Na+ dependent glutamate uptake from synaptosomes in the rat cortex. It blocks voltage-dependent Na+ channels and inhibits GABA uptake by the synaptosomes of the striatum. Neuroprotection. Riluzole protects cultured neurons from hypoxia damage, toxic effects of glutamate uptake inhibitors, and toxic factors in the cerebrospinal fluid of isolated ALS patients. In vivo, riluzole has neuroprotective, anticonvulsant and sedative effects. Complete inhibition of ischemia-induced surges in glutamate release has been observed in a rodent model of transient global cerebral ischemia. Studies have shown that Riluzole (Rilutek) activates the Potassium ion channel TREK family, directly affecting the glutamate energy system.
| Molecular Weight | 234.2 |
| Formula | C8H5F3N2OS |
| CAS Number | 1744-22-5 |
| Solubility (25°C) | DMSO 60 mg/mL Ethanol 40 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Sodium Channel Products |
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5-(N,N-Hexamethylene)-amiloride (Hexamethylene amiloride) is a potent Na+/H+ exchanger inhibitor, which decreases the intracellular pH (pHi) and induces apoptosis in leukemic cells. 5-(N,N-Hexamethylene)-amiloride (Hexamethylene amiloride) is also an inhibitor of the HIV-1 Vpu virus ion channel and inhibits mouse hepatitis virus (MHV) replication and human coronavirus 229E (HCoV229E) replication in cultured L929 cells with EC50s of 3.91 μM and 1.34 μM, respectively. |
| HwTx-IV
Huwentoxin-IV (HwTx-IV) is a 35-residue neurotoxin peptide with potential application as a novel analgesic. Huwentoxin-IV, a component of tarantula venom, potently blocks sodium channels and is an attractive scaffold for engineering a Nav1.7-selective molecule. |
| ST-2560
ST-2560 is a selective inhibitor of the NaV1.7 sodium channel with IC50 value of 39 nM in primates with ≥1000-fold selectivity over other isoforms of the human NaV1.x family. |
| A-317567
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| XPC-6444
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