简介：Riluzole 是一种抗惊厥药物，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
物理性状及指标：
外观：…………………… White crystalline powder
M.P：……………………117~119.5℃
溶解性：…………………H2O : 100mg/ml
含量：……………………≥99%
储存温度：常温，避光防潮密闭干燥
生物活性（仅来自于公开文献）：
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描述
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Riluzole is an anticonvulsant drug and belongs to the family of use-dependentNa+channelblocker which can also inhibitGABAuptake with anIC50of 43 μM. |
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IC50& Target |
Sodium channel IC50: 43 μM (GABA receptor) |
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体外 |
Riluzole is an anticonvulsant drug and belongs to the family of use-dependent Na+channel blocker which can also inhibit GABA uptake with an IC50of 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 EC50of Riluzole potentiation of GABA responses is about 60 μM. |
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体内 |
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). |
储液配置及储存：按表中溶解性配置；如溶解困难，可以通过快速搅拌，超声或温和加热（在45-60°C下水浴）。液体稳定性报道的很少，建议现配现用，如需储存，建议：-20℃1-3月；-80℃ 3-6月。
| 浓度/体积/质量 |
1 mg |
5 mg |
10 mg |
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1 mM |
4.2699 mL |
21.3493 mL |
42.6985 mL |
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5 mM |
0.8540 mL |
4.2699 mL |
8.5397 mL |
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10 mM |
0.4270 mL |
2.1349 mL |
4.2699 mL |
【注意】
●我司产品为非无菌包装，若用于细胞培养，请提前做预处理，除去热原细菌，否则会导致染菌。
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