Riluzole hydrochloride,850608-87-6

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YZ剂描述：

产品名称：Riluzole hydrochloride

产品别名：PK 26124;

英文别名：PK 26124

靶点：GABA Receptor;Sodium Channel

CAS：850608-87-6

纯度：≥99%

外观：见爱必信官网

保存方法：Room temperature

描述：

Riluzole is a benzothiazole derivative with anti-excitotoxic effects that acts by blocking the presynaptic release of glutamate, indirectly antagonizing glutamate receptors, and inactivating neuronal voltage-gated Na⁺ channels (ED₅₀ = 2.3 μM). Riluzole suppresses glutamate-induced seizures in rats at an ED₅₀ value of 3.2 mg/kg and displays neuroprotective effects in hypoxic animals at an ED₅₀ value of 4 mg/kg.¹ Riluzole has been explored as a therapeutic for slowing disease progression of amyotrophic lateral sclerosis.

溶解性：

体外研究：

Riluzole hydrochloride 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 hydrochloride inhibits peak autaptic IPSCs only slightly but prolongs IPSCs reliably. It is also found that Riluzole hydrochloride causes a strong, concentration-dependent, readily reversible enhancement of responses to 2 μM GABA. At higher concentrations of Riluzole hydrochloride, especially 300 μM, GABA currents exhibit apparent desensitization during prolonged co-exposure to 2 μM GABA and Riluzole hydrochloride. The EC₅₀ of Riluzole hydrochloride potentiation of GABA responses is about 60 μM.

体内研究：

In normal naïve rats, systemic injection of Riluzole hydrochloride (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 hydrochloride (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 hydrochloride 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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