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Formula | C8H5F3N2OS |
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Molecular Weight | 234.2 | CAS No. | 1744-22-5 | |
Solubility (25°C)* | In vitro | DMSO | 47 mg/mL (200.68 mM) | |
Ethanol | 47 mg/mL (200.68 mM) | |||
Water | Insoluble | |||
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
Description | Riluzole is a glutamate release inhibitor with neuroprotective, anticonvulsant, anxiolytic and anesthetic qualities. | |||
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In vitro | Riluzole inhibits the release of glutamic acid from cultured neurons, and from brain slices. These effects may be partly due to inactivation of voltage-dependent sodium channels on glutamatergic nerve terminals, as well as activation of a G-protein-dependent signal transduction process. Electrophysiologic experiments performed on isolated excitatory amino acid receptors expressed in the Xenopus oocyte have revealed that Riluzole inhibits currents evoked by N-methyl-D-aspartate (NMDA) (IC50 = 18 μM) and kainic acid (IC50 = 167 μM). Riluzole has been shown to stabilize inactivated sodium channels in frog sciatic nerve, in rat cerebellar granule cells, and on recombinant rat sodium channels expressed in Xenopus oocytes (Ki = 0.2 μM). Riluzole also blocks some of the postsynaptic effects of glutamic acid by noncompetitive blockade of NMDA receptors. Tiluzole protects cultured neurons from anoxic damage, from the toxic effects of glutamic-acid-uptake inhibitors, and from the toxic factor in the CSF of patients with amyotrophic lateral sclerosis. [1] | |||
In vivo | Riluzole can easily cross the blood-brain barrier. Riluzole has neuroprotective, anticonvulsant, and sedative properties in vivo. In a rodent model of transient global cerebral ischemia, a complete suppression of the ischemia-evoked surge in glutamic acid release has been observed by Riluzole treatment (8 mg/kg i.p.). [1] |
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Data from [Data independently produced by , , J Neuroimmune Pharmacol, 2013, 8(5):1098-105.]
Data from [Data independently produced by , , Int J Mol Sci, 2016, 17(3):357]
BDNF Augmentation Using Riluzole Reverses Doxorubicin-Induced Decline in Cognitive Function and Neurogenesis [ Neurotherapeutics, 2023, none] | PubMed: 36720792 |
Riluzole Suppresses Growth and Enhances Response to Endocrine Therapy in ER+ Breast Cancer [ J Endocr Soc, 2023, 7(10):bvad117] | PubMed: 37766843 |
Intratarget Microdosing for Deep Phenotyping of Multiple Drug Effects in the Live Brain [ Front Bioeng Biotechnol, 2022, 10:855755] | PubMed: 35372313 |
Small-Molecule-Driven Direct Reprogramming of Fibroblasts into Functional Sertoli-Like Cells as a Model for Male Reproductive Toxicology [ Adv Biol (Weinh), 2022, e2101184] | PubMed: 35212192 |
Targeting Mitochondrial Metabolism in Clear Cell Carcinoma of the Ovaries [ Int J Mol Sci, 2021, 22(9)4750] | PubMed: 33947138 |
Reduction of glutamate neurotoxicity: A novel therapeutic approach for Niemann-Pick disease, type C1 [ Mol Genet Metab, 2021, S1096-7192(21)00826-X] | PubMed: 34802899 |
Concurrent Targeting of Glutaminolysis and Metabotropic Glutamate Receptor 1 (GRM1) Reduces Glutamate Bioavailability in GRM1+ Melanoma [ Cancer Res, 2019, 79(8):1799-1809] | PubMed: 30987979 |
Treatment with the glutamate modulator riluzole prevents early life stress-induced cognitive deficits and impairments in synaptic plasticity in APPswe/PS1dE9 mice [ Neuropharmacology, 2019, 150:175-183] | PubMed: 30794835 |
The new role of riluzole in the treatment of pancreatic cancer through the apoptosis and autophagy pathways [ J Cell Biochem, 2019, 10.1002/jcb.29533] | PubMed: 31709624 |
Targetable Clinical Nanoparticles for Precision Cancer Therapy Based on Disease-Specific Molecular Inflection Points. [ Nano Lett, 2017, 17(11):7160-7168] | PubMed: 29035540 |
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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
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