Bemesetron 是 5-HT3 的选择性拮抗剂 (IC50 = 0.33 nM),具有神经保护作用。
产品描述
Bemesetron is a selective antagonist of 5-HT3 (IC50 = 0.33 nM) with neuroprotective effects.
体外活性
In primary cortical neuronal cells, Bemesetron (1 μM) significantly blocks the H2O2-induced increase of caspase-3 immunoreactivity. Bemesetron (0.01, 0.1 and 1 μM) and Y25130 (0.05, 0.5 and 5 μM) concentration-dependently reduce the H2O2-induced decrease showing inhibition of 74.9 and 79.0% with 1 μM and 5 μM, respectively[2].
体内活性
In male adult albino mice, Bemesetron (1 mg/kg; i.p.) causes a significant reduction of catalepsy, while Bemesetron (10 mg/kg; i.p.) significantly potentiates the phenomenon. The maximum inhibition of catalepsy (about 75%) occurs at 120 min, and the maximum potentiation (about 4.5-times the control value) occurs at 60 min after Haloperidol[3].
Cas No.
40796-97-2
分子式
C15H17Cl2NO2
分子量
314.21
别名
贝美司琼;3-TROPANYL-3,5-DICHLOROBENZOATE;MDL 72222
储存和溶解度
DMSO:2 mg/mL (6.37 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years