105878-43-1
105878-43-1 structure
- Name: Bisoprolol (fumarate)
- Chemical Name: Bisoprolol (fumarate)
- CAS Number: 105878-43-1
- Molecular Formula: C22H35NO8
- Molecular Weight:
- Catalog: Signaling Pathways GPCR/G Protein Adrenergic Receptor
- Create Date: 2021-05-27 07:16:23
- Modify Date: 2024-01-09 12:03:48
-
Bisoprolol fumarate is a potent, selective and orally active β1-adrenergic receptor blocker with little activity on β2-receptor. Bisoprolol fumarate has the potential for hypertension, coronary artery disease and stable ventricular dysfunction research[1][2].
| Name | Bisoprolol (fumarate) |
|---|---|
| Synonyms |
Bisoprolol fumarate
1-(propan-2-ylamino)-3-(4-{[2-(propan-2-yloxy)ethoxy]methyl}phenoxy)propan-2-ol (2E)-but-2-enedioate (1:1) BISOPROLOL MONOFUMARATE, (S)- MFCD00673957 BISOPROLOL MONOFUMARATE, (R)- Bisoprolol (fumarate) Bisoprolol fumarate (1:x) MFCD00792743 1-{4-[(2-Isopropoxyethoxy)methyl]phenoxy}-3-(isopropylamino)-2-propanol (2E)-2-butenedioate (1:1) 2-Propanol, 1-[4-[[2-(1-methylethoxy)ethoxy]methyl]phenoxy]-3-[(1-methylethyl)amino]-, (2E)-2-butenedioate (1:1) (salt) Bisoprolol hemifumarate 1-{4-[(2-Isopropoxyethoxy)methyl]phenoxy}-3-(isopropylamino)propan-2-ol (2E)-but-2-enedioate (1:1) BISOPROLOL MONOFUMARATE |
| Description | Bisoprolol fumarate is a potent, selective and orally active β1-adrenergic receptor blocker with little activity on β2-receptor. Bisoprolol fumarate has the potential for hypertension, coronary artery disease and stable ventricular dysfunction research[1][2]. |
|---|---|
| Related Catalog | |
| Target |
Beta-1 adrenergic receptor |
| In Vitro | Bisoprolol fumarate (2 μM, 1 h) protects myocardial cells (H9c2) from ischemia/reperfusion (I/R) injury[2]. Bisoprolol fumarate (2 μM, 1 h) reduces the H/R-induced ROS production and apoptosis in H9c2 cells[2]. Bisoprolol fumarate (2 μM, 1 h) increases AKT and GSK3β phosphorylation in H9c2 cells[2]. Bisoprolol fumarate (100 μM, 24 h) reverses Epinephrine-inhibited emigration in cholesterol-loaded DCs (dendritic cell) through increasing in β-arrestin 2, CCR7 and PI3K phosphorylation[3]. Cell Viability Assay[2] Cell Line: H9c2 cells Concentration: 0.2, 2, 20 μM Incubation Time: 1 h Result: Elevated the survival rates of cardiomyocytes subjected to H/R (hypoxia/reoxygenation) to 73.20%, 90.38%, 81.25% respectively. Cell Migration Assay [3] Cell Line: DCs Concentration: 100 μM Incubation Time: 6, 12, 24 h Result: Increased the amount of migrating cells by 46.00% (6 h), 64.25% (12 h) and 55.74% (24 h). |
| In Vivo | Bisoprolol fumarate (oral administration, 5 mg/kg, for 1 week) increases left ventricular ejection fraction (LVEF) and decreases the heart rate value[2]. Bisoprolol fumarate (oral gavage, 8 mg/kg, daily for four weeks) shows protective effects against Cadmium-induced myocardial toxicity in rats[4]. Bisoprolol fumarate (oral gavage, 1 mg/kg, daily for 6 weeks) reversessmall conductance calcium-activated potassium channel (SK) remodeling in a volume-overload rat model[5]. Animal Model: Ischemia/reperfusion (I/R) injury rats[2] Dosage: 0.5, 5, 10 mg/kg Administration: Oral administration, for 1 week, prior to 0.5 h ischemia/4 h reperfusion. Result: Reduced infarct size from 44% in I/R group to 31% in treated group. Animal Model: Cadmium-induced rats[4] Dosage: 2, 8 mg/kg Administration: Oral gavage, daily for four weeks. Result: Decreased mean arterial pressure (MAP) at 8 mg/kg. Decreased serum biomarkers (ALT, AST) and NF-kB p65 expression and TNF-α levels (cardiac tissue samples) at 8 mg/kg. |
| References |
| Molecular Formula | C22H35NO8 |
|---|