Betaxolol hydrochloride 是一种 β1 肾上腺素受体阻断剂,可用于研究高血压和青光眼。
产品描述
Betaxolol is a cardioselective beta-blocker used in the treatment of hypertension. Betaxolol has not been linked to instances of clinically apparent drug induced liver injury.
体外活性
Betaxolol 的内含物可以部分阻止NMDA 和缺氧/ 葡萄糖引起的改变.在大鼠局部贫血前和再灌注损伤的时候腹腔注射Betaxolol可以有效减少钙网膜蛋白和ChAT免疫反应性的改变,并且可以阻止b波下降.
体内活性
10 μM Betaxolol基本可以完全阻断谷氨酸酯诱导的LDH的释放。 100 μM Betaxolol能有效防止皮质组织中由缺氧引起的LDH的释放。Betaxolol能保护视网膜神经元。Betaxolol在β-肾上腺素受体激动剂无效时,会减弱NMDA诱导的45Ca2+流入。
细胞实验
Dissociated cortical cells from 16–18-day-old fetal rats are grown, in 35 mm dishes, in DMEM supplemented with L-glutamine (4 mM), glucose (6 g/L), penicillin (100 U/mL), streptomycin (100 μg/mL) and 10% hormonal supplemented medium consisting of transferrin (1 mg/mL), insulin (250 μg/mL) putrescine (600 μM), sodium selenite (0.3 μM), progesterone (0.2 μM) and estradiol (0.1 pM) for 7 days in an atmosphere of 5% CO2/95% O2 at 37 °C. The cultures are then transferred to a culture medium which lacks the hormonal supplemented medium. L-glutamate is added to the medium and incubated for a further 4 hours under normoxic conditions. Betaxolol are added to the cultures at the same time as L-glutamate. In other experiments the cultures are subjected to anoxic conditions, 95% N2/5% CO2, for 5 hours at 37 °C. Betaxolol is added prior to anoxia. Reoxygenation is then achieved by replacing the cells in normoxic conditions (95% O2/5% CO2) for 3 hours. Cellular injury is assessed by measuring lactate dehydrogenase (LDH) release into the cell culture supernatant after hypoxia/reoxygenation or glutamate exposure. LDH activity is assayed spectrophotometrically by following NADH metabolism for 2 minutes at 340 nm.(Only for Reference)
Cas No.
63659-19-8
分子式
C18H30ClNO3
分子量
343.89
别名
盐酸倍他洛尔;SL 75212 HCl;SL75212;Betaxolol HCl;Betaxolol hydrochloride
储存和溶解度
H2O:29.08mM
DMSO:200.6 mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years