1. Membrane Transporter/Ion Channel
    Neuronal Signaling
  2. Sodium Channel
    GABA Receptor
  3. Riluzole

Riluzole (Synonyms: PK 26124)

Cat. No.: HY-B0211 Purity: 99.83%
Handling Instructions

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.

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

Riluzole Chemical Structure

Riluzole Chemical Structure

CAS No. : 1744-22-5

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Based on 1 publication(s) in Google Scholar

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Description

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.

IC50 & Target

Sodium channel[1]
IC50: 43 μM (GABA receptor)[1]

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[1].

In Vivo

In normal naïve 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)[2].

Clinical Trial
Molecular Weight

234.20

Formula

C₈H₅F₃N₂OS

CAS No.

1744-22-5

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
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 provided by MCE.
References
Cell Assay
[1]

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[1].

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

Animal Administration
[2]

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.)[2].

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

References
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