Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Riluzole hydrochloride, a use-dependent Na+ channel blocker with anticonvulsant properties, belongs to a category of drugs that also inhibit GABA uptake, exhibiting an inhibitory concentration 50 (IC50) of 43 μM.
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Description | Riluzole hydrochloride, a use-dependent Na+ channel blocker with anticonvulsant properties, belongs to a category of drugs that also inhibit GABA uptake, exhibiting an inhibitory concentration 50 (IC50) of 43 μM. |
In vitro | Riluzole hydrochloride, an anticonvulsant and use-dependent Na+ channel blocker, also obstructs GABA uptake effectively with an IC50 of 43 μM. It marginally inhibits peak autaptic IPSCs at 20 μM, while notably extending their duration. The compound significantly enhances responses to 2 μM GABA in a concentration-dependent and reversible manner. However, at elevated concentrations, particularly 300 μM, it induces apparent desensitization of GABA currents during extended exposure to both 2 μM GABA and Riluzole hydrochloride, with an EC50 for GABA response potentiation at approximately 60 μM [1]. |
In vivo | In naive rats, an intraperitoneal injection of Riluzole hydrochloride (8 mg/kg; n=6) significantly shortens the duration of ultrasonic, but not audible, vocalizations triggered by painful knee joint stimulation compared to a vehicle control (P<0.05). Similarly, Riluzole hydrochloride (8 mg/kg, i.p.; n=19) markedly reduces vocalizations in arthritic rats, compared to both predrug conditions and vehicle control, with a high level of statistical significance (P<0.05 to 0.001). Additionally, when Riluzole hydrochloride is administered directly into the CeA, it substantially decreases the duration of both audible and ultrasonic vocalizations caused by painful knee stimulation, compared to predrug levels (n=8; P<0.05 to 0.01) [2]. |
Molecular Weight | 270.66 |
Formula | C8H6ClF3N2OS |
CAS No. | 850608-87-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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Riluzole hydrochloride 850608-87-6 Riluzole Hydrochloride inhibitor inhibit