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Bisoprolol (fumarate)

Names

[ CAS No. ]:
105878-43-1

[ Name ]:
Bisoprolol (fumarate)

[Synonym ]:
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

Biological Activity

[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]:

Research Areas >> Cancer
Research Areas >> Cardiovascular Disease
Signaling Pathways >> GPCR/G Protein >> Adrenergic Receptor
Research Areas >> Inflammation/Immunology

[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]

[1]. Jillian G Baker, et al. The selectivity of beta-adrenoceptor antagonists at the human beta1, beta2 and beta3 adrenoceptors. Br J Pharmacol. 2005 Feb;144(3):317-22.

[2]. Jing Wang, et al. Bisoprolol, a β 1 antagonist, protects myocardial cells from ischemia-reperfusion injury via PI3K/AKT/GSK3β pathway. Fundam Clin Pharmacol. 2020 Dec;34(6):708-720.

[3]. Hong Yang, et al. Bisoprolol reverses epinephrine-mediated inhibition of cell emigration through increases in the expression of β-arrestin 2 and CCR7 and PI3K phosphorylation, in dendritic cells loaded with cholesterol. Thromb Res. 2013 Mar;131(3):230-7.

[4]. Jinhua Liu, et al. Protective Effects of Bisoprolol Against Cadmium-induced Myocardial Toxicity Through Inhibition of Oxidative Stress and NF-κΒ Signalling in Rats. J Vet Res. 2021 Oct 20;65(4):505-511.

[5]. Yajuan Ni, et al. Bisoprolol reversed small conductance calcium-activated potassium channel (SK) remodeling in a volume-overload rat model. Mol Cell Biochem. 2013 Dec;384(1-2):95-103.

Chemical & Physical Properties

[ Molecular Formula ]:
C22H35NO8

Related Compounds