Riluzole

BML-NA138

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Na⁺ channel blocker, K⁺ channel activator

Glutamate release inhibitor. Neuroprotective. Blocks the inactivated state of voltage-gated neuronal Na⁺ channels at very low concentrations (about 0.1µM) and activates the TREK family of two-pore domain potassium channels.

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Product Details

Alternative Name	2-Amino-6-(trifluoromethoxy)-benzothiazole, 6-(Trifluoromethoxy)-2-benzothiazolamine
Appearance	White to off-white solid.
CAS	1744-22-5
Couple Target	Potassium channel, Sodium channel
Couple Type	Activator, Blocker
Formula	C₈H₅F₃N₂OS
MI	14: 8223
MW	234.2
Purity	≥98% (TLC)
Solubility	Soluble in DMSO (>25mg/ml), 100% ethanol (>25mg/ml), methanol (>40mg/ml), 45% (w/v) aq 2-hydroxypropyl-β-cyclodextrin (14mg/ml) or in 0.1N HCl (11mg/ml); insoluble in water.

Handling & Storage

Use/Stability	As indicated on product label or CoA when stored as recommended. Stable for up to 1 year after receipt when stored at +20°C. Stock solutions are stable for up to 3 months at -20°C.
Long Term Storage	Ambient
Shipping	Ambient Temperature

Regulatory Status	RUO – Research Use Only

Therapeutic potential of neuronal two-pore domain potassium-channel modulators: A. Mathie & E.L. Veale; Curr. Opin. Investig. Drugs 8, 555 (2007), Abstract
Do sodium channel blockers have neuroprotective effect after onset of ischemic insult?: O. Ates, et al.; Neurol. Res. 29, 317 (2007), Abstract
Riluzole protects from motor deficits and striatal degeneration produced by systemic 3-nitropropionic acid intoxication in rats: M.C. Guyot, et al.; Neuroscience 81, 141 (1997), Abstract
Differential action of riluzole on tetrodotoxin-sensitive and tetrodotoxin-resistant sodium channels: J.H. Song, et al.; J. Pharmacol. Exp. Ther. 282, 707 (1997), Abstract
Protective effect of riluzole on excitatory amino acid-mediated neurotoxicity in motoneuron-enriched cultures: A.G. Estevez, et al.; Eur. J. Pharmacol. 280, 47 (1995), Abstract
Riluzole prevents MPTP-induced parkinsonism in the rhesus monkey: a pilot study: A. Benazzouz, et al.; Eur. J. Pharmacol. 284, 299 (1995), Abstract
Inhibition by riluzole of glycinergic postsynaptic currents in rat hypoglossal motoneurons: M. Umemiya & A.J. Berger; Br. J. Pharmacol. 116, 3227 (1995), Abstract
Na+ channels as targets for neuroprotective drugs: C.P. Taylor & B.S. Meldrum; TIPS 16, 309 (1995), (Review), Abstract
Anesthetic properties of riluzole (54274 RP), a new inhibitor of glutamate neurotransmission: J. Mantz, et al.; Anesthesiology 76, 844 (1992), Abstract
Effects of riluzole (2-amino-6-trifluoromethoxy benzothiazole) on striatal neurochemical markers in the rat, with special reference to the dopamine, choline, GABA and glutamate synaptosomal high affin: D. Samuel, et al.; Fundam. Clin. Pharmacol. 6, 177 (1992), Abstract

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Riluzole

BML-NA138

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