Riluzole [1744-22-5]

Cat# HY-B0211-500mg

Size : 500mg

Brand : MedChemExpress

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Riluzole is an anticonvulsant agent and belongs to the family of use-dependent Na+ channel blocker which can also inhibit GABA uptake with an IC50 of 43 μM.

For research use only. We do not sell to patients.

Riluzole Chemical Structure

CAS No. : 1744-22-5

*

This product is a controlled substance and not for sale in your territory.

  • Cell Res. 2022 Apr 4.  [Abstract]
  • Nat Commun. 2023 Dec 12;14(1):8255.  [Abstract]
  • Proc Natl Acad Sci U S A. 2023 Oct 10;120(41):e2309773120.  [Abstract]
  • Front Cell Neurosci. 2020 Oct 16;14:575626.  [Abstract]
  • Pharmacol Biochem Behav. 2018 May;168:43-50.  [Abstract]
  • Front Neural Circuits. 2021 Apr 6;15:657445.  [Abstract]
  • Neurosci Lett. 2021 Mar 24;135846.  [Abstract]
  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Riluzole is an anticonvulsant agent and belongs to the family of use-dependent Na+ channel blocker which can also inhibit GABA uptake with an IC50 of 43 μM.

Sodium channel
IC50: 43 μM (GABA receptor)

In Vitro

Riluzole is an anticonvulsant drug and belongs to the family of use-dependent Na+ channel blocker which can also inhibit GABA uptake with an IC50 of 43 μM. At 20 μM, Riluzole inhibits peak autaptic IPSCs only slightly but prolongs IPSCs reliably. It is also found that Riluzole causes a strong, concentration-dependent, readily reversible enhancement of responses to 2 μM GABA. At higher concentrations of Riluzole, especially 300 μM, GABA currents exhibit apparent desensitization during prolonged co-exposure to 2 μM GABA and Riluzole. The EC50 of Riluzole potentiation of GABA responses is about 60 μM.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

In normal na ve rats, systemic injection of Riluzole (8 mg/kg, i.p.; n=6 rats) decreases the duration of ultrasonic but not audible vocalizations evoked by noxious stimulation of the knee joint compare to vehicle tested in the same rats (P<0.05). Systemic application of Riluzole (8 mg/kg, i.p.; n=19 rats) decreases the vocalizations of arthritic rats compare to predrug and vehicle significantly (P<0.05 to 0.001). Riluzole administered into the CeA significantly decreases the duration of audible and ultrasonic vocalizations evoked by noxious stimulation of the knee compare to predrug values (n=8 rats; P<0.05 to 0.01).

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

234.20

C8H5F3N2OS

1744-22-5

Solid

White to yellow

NC1=NC2=CC=C(OC(F)(F)F)C=C2S1

Room temperature in continental US; may vary elsewhere.

In Vitro: 

DMSO : 100 mg/mL (426.99 mM; Need ultrasonic)

H2O : 1 mg/mL (4.27 mM; ultrasonic and adjust pH to 3 with HCl)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.2699 mL 21.3493 mL 42.6985 mL
5 mM 0.8540 mL 4.2699 mL 8.5397 mL
10 mM 0.4270 mL 2.1349 mL 4.2699 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (10.67 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (10.67 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (10.67 mM); Clear solution

*All of the co-solvents are available by MedChemExpress (MCE).
  • [1]. He Y, et al. Neuroprotective agent riluzole potentiates postsynaptic GABA(A) receptor function. Neuropharmacology. 2002 Feb;42(2):199-209.  [Content Brief]

    [2]. Thompson JM, et al. Small-conductance calcium-activated potassium (SK) channels in the amygdala mediate pain-inhibiting effects of clinically available riluzole in a rat model of arthritis pain. Mol Pain. 2015 Aug 28;11:51.  [Content Brief]

Two-electrode voltage clamp of Xenopus oocytes expressing exogenous GABAA receptors is performed with a CA-1B high performance oocyte clamp. The extracellular recording solution is ND-96 medium. Riluzole is applied from a common tip via a gravity-driven multibarrel drug-delivery system. Data acquisition and analysis are performed with pCLAMP 6 software.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Adult male Sprague-Dawley rats (180 to 350 g) are housed in a temperature-controlled room and maintained on a 12-h day/night cycle with unrestricted access to food and water. Pain behaviors are measured before and 5 h after induction of a mono-arthritis in the left knee joint. To test the effects of systemic (intraperitoneal, i.p.) application of Riluzole, pain behaviors are measured 1 h postinjection of Riluzole in normal and arthritic animals. To determine effects of Riluzole into the amygdala, pain behaviors are measured 15 min after starting Riluzole application through a stereotaxically implanted microdialysis probe. To investigate site of action in the amygdala of systemically applied Riluzole, potassium channel blockers are administered into the amygdala 45 min after systemic application of Riluzole and pain behaviors are measured 15 min later, i.e., 1 h postinjection of riluzole (i.p.).

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

  • [1]. He Y, et al. Neuroprotective agent riluzole potentiates postsynaptic GABA(A) receptor function. Neuropharmacology. 2002 Feb;42(2):199-209.  [Content Brief]

    [2]. Thompson JM, et al. Small-conductance calcium-activated potassium (SK) channels in the amygdala mediate pain-inhibiting effects of clinically available riluzole in a rat model of arthritis pain. Mol Pain. 2015 Aug 28;11:51.  [Content Brief]

  • [1]. He Y, et al. Neuroprotective agent riluzole potentiates postsynaptic GABA(A) receptor function. Neuropharmacology. 2002 Feb;42(2):199-209.

    [2]. Thompson JM, et al. Small-conductance calcium-activated potassium (SK) channels in the amygdala mediate pain-inhibiting effects of clinically available riluzole in a rat model of arthritis pain. Mol Pain. 2015 Aug 28;11:51.

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  • Membrane Transporter/Ion Channel Neuronal Signaling
  • Sodium Channel GABA Receptor
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