Product Introduction
Bioactivity


英文名: Riluzole hydrochloride

描述: Riluzole hydrochloride 是一种抗惊厥药物，属于依赖于使用的钠通道阻滞剂家族，也可以抑制 GABA 摄取，IC50值为 43 μM。

体外活性: 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 IC 50 of 43 μM. At 20 μM, Riluzole hydrochloride inhibits peak autaptic IPSCs only slightly but reliably prolongs IPSCs. 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 EC 50 of Riluzole hydrochloride potentiation of GABA responses is about 60 μM [1].

体内活性: In normal na ve rats, systemic injection of Riluzole hydrochloride (8 mg/kg, i.p.; n=6 rats) reduces 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) [2].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

关键字: Riluzole Hydrochloride | Riluzole hydrochloride