Ivabradine hydrochloride

Names

[ Name ]:
Ivabradine hydrochloride

[Synonym ]:
Ivabradine hydrochloride
AMG 998
Coralan
Procoralan
Corlentor
3-[3-[[(7S)-3,4-dimethoxy-7-bicyclo[4.2.0]octa-1,3,5-trienyl]methyl-methylamino]propyl]-7,8-dimethoxy-2,5-dihydro-1H-3-benzazepin-4-one,hydrochloride
ivabradine monohydrochloride
2H-3-Benzazepin-2-one, 3-(3-((((7S)-3,4-dimethoxybicyclo(4.2.0)octa-1,3,5-trien-7-yl)methyl)methylamino)propyl)-1,3,4,5-tetrahydro-7,8-dimethoxy-, monohydrochloride
Ivabradine hcl
2H-3-Benzazepin-2-one, 3-[3-[[[(7S)-3,4-dimethoxybicyclo[4.2.0]octa-1,3,5-trien-7-yl]methyl]methylamino]propyl]-1,3,4,5-tetrahydro-7,8-dimethoxy-, hydrochloride (1:1)
MFCD00929899
3-{3-[{[(7S)-3,4-Dimethoxybicyclo[4.2.0]octa-1,3,5-trien-7-yl]methyl}(methyl)amino]propyl}-7,8-dimethoxy-1,3,4,5-tetrahydro-2H-3-benzazepin-2-one hydrochloride (1:1)
UNII-TP19837BZK
Corlanor

Biological Activity

[Description]:

Ivabradine (hydrochloride) is a new If inhibitor with IC50 of 2.9 μM, and used as a pure heart rate lowering agent.

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> Adrenergic Receptor

Research Areas >> Cardiovascular Disease

[In Vivo]

Ivabradine treatment (10 mg/kg/d) induces long-term HRR, and that improves diastolic LV function probably involving attenuated hypoxia, reduced remodeling, and/or preserved nitric oxide bioavailability, resulting from processes triggered early after HRR initiation: angiogenesis and/or preservation of endothelial nitric oxide synthase expression[1]. Ivabradine leads to a sustained 15-20% heart rate reduction, but has no effect on blood pressure. While ivabradine has no effect on endothelial function and vascular reactive oxygen species production in angiotensin II-treated rats, it improves both parameters in ApoE knockout mice. Ivabradine treatment leads to an attenuation of angiotensin II signaling and increased the expression of telomere-stabilizing proteins in ApoE knockout mice, which may explain its beneficial effects on the vasculature. The absence of these protective ivabradine effects in angiotensin II-infused rats may relate to the treatment duration or the presence of arterial hypertension[2].

[References]

[1]. Fang, Y., et al. Heart rate reduction induced by the if current inhibitor ivabradine improves diastolic function and attenuates cardiac tissue hypoxia. J Cardiovasc Pharmacol, 2012. 59(3): p. 260-7.

[2]. Kroller-Schon, S., et al. Differential effects of heart rate reduction with ivabradine in two models of endothelial dysfunction and oxidative stress. Basic Res Cardiol, 2011. 106(6): p. 1147-58.

[Related Small Molecules]

Chemical & Physical Properties

[ Boiling Point ]:
626.9ºC at 760mmHg

[ Melting Point ]:
193-196?C

[ Molecular Formula ]:
C₂₇H₃₇ClN₂O₅

[ Molecular Weight ]:
505.046

[ Flash Point ]:
332.9ºC

[ Exact Mass ]:
504.239105

[ PSA ]:
60.47000

[ LogP ]:
4.04990

[ Vapour Pressure ]:
1.24E-15mmHg at 25°C

[ Storage condition ]:
-20°C Freezer

MSDS

Click to get detail MSDS

Safety Information

[ Symbol ]:

GHS09

[ Signal Word ]:
Warning

[ Hazard Statements ]:
H400

[ Precautionary Statements ]:
P273

[ Hazard Codes ]:
N

[ Risk Phrases ]:
50/53

[ Safety Phrases ]:
60-61

[ RIDADR ]:
UN 3077 9 / PGIII

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

DownStream

Articles

Beat Rate Variability in Murine Embryonic Stem Cell-Derived Cardiomyocytes: Effect of Antiarrhythmic Drugs.

Cell Physiol. Biochem. 38 , 646-58, (2016)

Heart rate variability (HRV) refers to the fluctuation of the time interval between consecutive heartbeats in humans. It has recently been discovered that cardiomyocytes derived from human embryonic a...

Related Compounds

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