A calcium channel inhibitor
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Riluzole

Item No. 35833

Technical Information
Formal Name
6-(trifluoromethoxy)-2-benzothiazolamine
CAS Number
1744-22-5
Synonyms
  • BHV 0223
  • BHV 0233
  • PK26124
  • RP 54274
Molecular Formula
C8H5F3N2OS
Formula Weight
Purity
≥98%
Formulation
A solid
DMF: 10 mg/mlDMSO: 10 mg/mlEthanol: 10 mg/ml
SMILES
FC(F)(OC1=CC2=C(N=C(N)S2)C=C1)F
InChi Code
InChI=1S/C8H5F3N2OS/c9-8(10,11)14-4-1-2-5-6(3-4)15-7(12)13-5/h1-3H,(H2,12,13)
InChi Key
FTALBRSUTCGOEG-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    Riluzole is an inhibitor of calcium channels.1 It is selective for the voltage-gated calcium channels Cav2.2 and Cav2.1 over Cav1.2 at 30 µM. Riluzole (10 µM) inhibits increases in intracellular calcium levels induced by NMDA (Item No. 14581), L-glutamic acid (Item No. 30377), or veratridine in primary rat cerebellar granule cells.2 It reduces glutamate, but not aspartate, release from the left caudate nucleus in cats when used at a concentration of 10 µM.3 Riluzole reduces slow wave activity and increases high frequency neuronal activity induced by carotid artery occlusion (CAO) in gerbils in a dose-dependent manner and decreases the CAO-induced infarcted cortex volume in rats when administered at a dose of 8 mg/kg.4 Dietary administration of riluzole (44 mg/kg per day) increases survival time and the total distance ran in an SOD1-G93A transgenic mouse model of amyotrophic lateral sclerosis (ALS).5 Formulations containing riluzole have been used in the treatment of ALS.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Huang, C.-S., Song, J.-H., Nagata, K., et alEffects of the neuroprotective agent riluzole on the high voltage-activated calcium channels of rat dorsal root ganglion neurons. J. Pharmacol. Exp. Ther. 282(3), 1280-1290 (1997).

    2. Hubert, J.P., Delumeau, J.C., Glowinski, J., et alAntagonism by riluzole of entry of calcium evoked by NMDA and veratridine in rat cultured granule cells: Evidence for a dual mechanism of action. Br. J. Pharmacol. 113(1), 261-267 (1994).

    3. Chéramy, A., Barbeito, L., Godeheu, G., et alRiluzole inhibits the release of glutamate in the caudate nucleus of the cat in vivo. Neurosci. Lett. 147(2), 209-212 (1992).

    4. Pratt, J., Rataud, J., Bardot, F., et alNeuroprotective actions of riluzole in rodent models of global and focal cerebral ischaemia. Neurosci. Lett. 140(2), 225-230 (1992).

    5. Gurney, M.E., Fleck, T.J., Himes, C.S., et alRiluzole preserves motor function in a transgenic model of familial amyotrophic lateral sclerosis. Neurology 50(1), 62-66 (1998).