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Riluzole

CAS No. : 1744-22-5

MCE 国际站：Riluzole

产品活性：Riluzole 是一种抗惊厥活性分子，属于依赖于使用的钠通道阻滞剂家族，它也可以抑制 GABA 摄取，其 IC₅₀ 值为 43 μM。

研究领域：Membrane Transporter/Ion Channel  |  Neuronal Signaling

作用靶点：Sodium Channel  |  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.

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).

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