Riluzole hydrochloride

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Cat.No. 0768 - Riluzole hydrochloride | C8H5F3N2OS.HCl | CAS No. 850608-87-6
Description: GABA uptake inhibitor; also inhibits glutamate release and blocks NaV channels
Chemical Name: 2-Amino-6-trifluoromethoxybenzothiazole hydrochloride
Purity: ≥98% (HPLC)
Datasheet
Citations (15)
Reviews
Literature

Biological Activity

Inhibits glutamate release from presynaptic terminals and increases Na+-dependent glutamate uptake in rat cortical synaptosomes. Blocks voltage-dependent Na+ channels and inhibits GABA uptake by striatal synaptosomes. Also activates TRPC5 channels. Psychotropic agent with anticonvulsant, hypnotic, anxiolytic, anti-ischemic, anesthetic and neuroprotective properties.

Technical Data

M. Wt 270.66
Formula C8H5F3N2OS.HCl
Storage Store at RT
Purity ≥98% (HPLC)
CAS Number 850608-87-6
PubChem ID 6419992
InChI Key QEAOELIJQRYJJS-UHFFFAOYSA-N
Smiles Cl.NC1=NC2=CC=C(OC(F)(F)F)C=C2S1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 27.07 100
water 2.71 10 with gentle warming

Preparing Stock Solutions

The following data is based on the product molecular weight 270.66. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 3.69 mL 18.47 mL 36.95 mL
5 mM 0.74 mL 3.69 mL 7.39 mL
10 mM 0.37 mL 1.85 mL 3.69 mL
50 mM 0.07 mL 0.37 mL 0.74 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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References

References are publications that support the biological activity of the product.

Fumagalli et al (2008) Riluzole enhances the activity of glutamate transporters GLAST, GLT1 and EAAC1. Eur.J.Pharmacol. 578 171 PMID: 18036519

Song et al (1997) Differential action of Riluzole on tetrodotoxin-sensitive and tetrodotoxin-resistant sodium channels. J.Pharmacol.Exp.Ther. 282 707 PMID: 9262334

Taylor and Meldrum (1995) Na+ channels as targets for neuroprotective drugs. TiPS 16 309 PMID: 7482996

Umeniya and Berger (1995) Inhibition by Riluzole of glycinergic postsynaptic currents in rat hypoglossal motoneurones. Br.J.Pharmacol. 116 3227 PMID: 8719800

Richter et al (2014) Riluzole activates TRPC5 channels independently of PLC activity. Br.J.Pharmacol. 171 158 PMID: 24117252


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View Related Products by Product Action

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Keywords: Riluzole hydrochloride, Riluzole hydrochloride supplier, Glutamate, release, inhibitors, inhibits, GABA, uptake, Na+, channel, blockers, glutamate, mGlur, Receptors, Metabotropic, Sodium, NaV, Channels, voltage-gated, voltage-dependent, iGlu, Ionotropic, BGT-1, GAT, Transporters, Monoamine, Neurotransmitter, neuroprotective, TRPC5, canon, Miscellaneous, Voltage-gated, TRPC, 0768, Tocris Bioscience

15 Citations for Riluzole hydrochloride

Citations are publications that use Tocris products. Selected citations for Riluzole hydrochloride include:

Viemari et al (2013) β-Noradrenergic receptor activation specifically modulates the generation of sighs in vivo and in vitro. Neurochem Int 7 179 PMID: 24273495

Carbone et al (2012) R.zole elevates GLT-1 activity and levels in striatal astrocytes. BMC Neurosci 60 42613 PMID: 22080156

Carbone et al (2012) R.zole neuroprotection in a Parkinson's disease model involves suppression of reactive astrocytosis but not GLT-1 regulation. Cells 13 38 PMID: 22480308

Sperling et al (2017) Riluzole: a potential therapeutic intervention in human brain tumor stem-like cells. Oncotarget 8 96697 PMID: 29228563

Du et al (2015) Generation and expansion of highly pure motor neuron progenitors from human pluripotent stem cells. Nat.Commun. 6 6626 PMID: 25806427

Morgado-Valle et al (2010) Glycinergic pacemaker neurons in preBötzinger complex of neonatal mouse. J Neurosci 30 3634 PMID: 20219997

Le et al (2010) The glutamate release inhibitor R.zole decreases migration, invasion, and proliferation of melanoma cells. J Invest Dermatol 130 2240 PMID: 20505744

Park et al (2013) Slowly inactivating component of Na+ current in peri-somatic region of hippocampal CA1 pyramidal neurons. J Neurophysiol 109 1378 PMID: 23236005

Du et al (2015) Generation and expansion of highly pure motor neuron progenitors from human pluripotent stem cells. Nat Commun 6 6626 PMID: 25806427

Zhang et al (2018) Pauses in Cholinergic Interneuron Activity Are Driven by Excitatory Input and Delayed Rectification, with DA Modulation. Neuron 98 918 PMID: 29754751

Shin et al (2018) Participation of xCT in melanoma cell proliferation in vitro and tumorigenesis in vivo. Oncogenesis 7 86 PMID: 30425240

Sexton et al (2018) Metabotropic glutamate receptor-1 regulates inflammation in triple negative breast cancer. Sci Rep 8 16008 PMID: 30375476

Rosenberg et al (2015) Targeting Glutamatergic Signaling and the PI3 Kinase Pathway to Halt Melanoma Progression. Front Neural Circuits 8 42614 PMID: 25749171

Veettil et al (2014) Glutamate secretion and metabotropic glutamate receptor 1 expression during Kaposi's sarcoma-associated herpesvirus infection promotes cell proliferation. PLoS Pathog 10 e1004389 PMID: 25299066

Dolfi et al (2017) R.zole exerts distinct antitumor effects from a metabotropic glutamate receptor 1-specific inhibitor on breast cancer cells. Oncotarget 8 44639 PMID: 28591718


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*Please note that Tocris will only send literature to established scientific business / institute addresses.


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