| 名称 | Betaxolol hydrochloride |
| 描述 | Betaxolol hydrochloride (SL 75212 HCl) is a cardioselective beta-blocker used in the treatment of hypertension.Betaxolol hydrochloride has not been linked to instances of clinically apparent drug induced liver injury. |
| 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) |
| 体外活性 | Betaxolol's constituents are capable of partially inhibiting changes induced by NMDA and hypoxia/glucose deficiency. Intraperitoneal injection of Betaxolol in rats during focal ischemia and before reperfusion injury effectively mitigates alterations in calretinin and ChAT immunoreactivity, and also prevents the decline of b-wave amplitude. |
| 体内活性 | At a concentration of 10 µM, Betaxolol significantly inhibits the release of LDH (lactate dehydrogenase) induced by glutamate esters. Additionally, 100 µM Betaxolol effectively prevents the release of LDH in cortical tissue caused by hypoxia. Betaxolol offers protective effects on retinal neurons and attenuates the influx of ^(45)Ca2+ induced by NMDA (N-methyl-D-aspartate) when β-adrenergic receptor agonists are ineffective. |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 50 mg/mL (145.4 mM)
H2O : 29.08 mM
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| 关键字 | Beta Receptor | SL 75212 | Inhibitor | inhibit | Betaxolol Hydrochloride | Betaxolol | SL-75212 | Adrenergic Receptor | Betaxolol hydrochloride |
| 相关产品 | Olanzapine | Mirtazapine | Octopamine hydrochloride | Gemfibrozil | Dexmedetomidine hydrochloride | Phenylephrine hydrochloride | Isoprenaline hydrochloride | Amitriptyline hydrochloride | Trazodone hydrochloride | Mianserin hydrochloride |
| 相关库 | 神经退行性疾病化合物库 | 经典已知活性库 | 膜蛋白靶向化合物库 | 抗癌临床化合物库 | 药物功能重定位化合物库 | 抗癌上市药物库 | FDA 上市药物库 | 已知活性化合物库 | GPCR靶点分子库 | 抗癌药物库 |
United States
