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 |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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| ASN008
ASN008 is a permanently positively charged sodium channel blocker. |
| Psalmotoxin 1
Psalmotoxin 1 (PcTx1) is a protein toxin that can bind at subunit-subunit interfaces of acid-sensing ion channel 1a (ASIC1a). |
| Jingzhaotoxin-III
Jingzhaotoxin-III is a potent and selective blocker of Nav1.5 channels, with an IC50 of 348 nM, and shows no effect on other sodium channel isoforms. |
| Huwentoxin-IV
Huwentoxin-IV is a potent and selective sodium channel blocker, inhibits neuronal Nav1.7, Nav1.2, Nav1.3 and Nav1.4 with IC50s of 26, 150, 338 and 400 nM, respectively. |
| Phrixotoxin 3
Phrixotoxin 3 is a potent blocker of voltage-gated sodium channels, with IC50s of 0.6, 42, 72, 288, 610 nM for NaV1.2, NaV1.3, NaV1.4, NaV1.1 and NaV1.5, respectively. |
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