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Ivabradine

Names

[ CAS No. ]:
155974-00-8

[ Name ]:
Ivabradine

[Synonym ]:
Ivabradine [INN]
3-[3-({[(7S)-3,4-dimethoxybicyclo[4.2.0]octa-1,3,5-trien-7-yl]methyl}(methyl)amino)propyl]-7,8-dimethoxy-2,3,4,5-tetrahydro-1H-3-benzazepin-2-one
[14C]-Ivabradine
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
UNII-3H48L0LPZQ
Ivabradine
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
Procoralan
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-
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
Corlanor
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

Biological Activity

[Description]:

Ivabradine is a potent and orally active HCN (hyperpolarization-activated cyclic nucleotide-gated) channel blocker that inhibits the cardiac pacemaker current (If). Ivabradine reduces dose-dependently heart rate without modification of blood pressure. Ivabradine shows anticonvulsant, anti-ischaemic and anti-anginal activity[1][2][3][4].

[Related Catalog]:

Research Areas >> Cardiovascular Disease
Signaling Pathways >> Membrane Transporter/Ion Channel >> HCN Channel

[In Vivo]

Ivabradine (1, 10, 20 mg/kg; i.p.) shows anticonvulsant and neuroprotective action in mice[3]. Ivabradine (5, 10, 20 mg/kg;p.o.; daily for 1 weeks) lowers heart rate in mice with enhanced sympathoadrenergic activities[4]. Animal Model: 25-30 g, 6 weeks male Swiss mice[3] Dosage: 1, 10, 20 mg/kg Administration: I.p.; for 3 days Result: Attenuated PTZ- and PICRO-induced seizures while presented an antioxidant effect in allbrain areas studied, and reduced cleaved caspase-3 expression in the CA1 and DG region of PICRO- and PTZ-treated mice, respectively. Animal Model: 3-4 months transgenic (TG) mice with cardiac-restricted overexpression of b2AR[4] Dosage: 5, 10, 20 mg/kg Administration: P.o; daily for 1 weeks Result: Reduced the maximal HR increase in response to the b-agonist isoproterenol, without modifying the response of contractile parameters at 10 mg/kg.

[References]

[1]. Tardif JC, et al. Efficacy of ivabradine, a new selective I(f) inhibitor, compared with atenolol in patients with chronic stable angina. Eur Heart J. 2005 Dec;26(23):2529-36.

[2]. Mulder P, et al. Heart rate slowing for myocardial dysfunction/heart failure. Adv Cardiol. 2006;43:97-105.

[3]. Cavalcante TMB, et al. Ivabradine possesses anticonvulsant and neuroprotective action in mice. Biomed Pharmacother. 2019 Jan;109:2499-2512.

[4]. Du XJ, et al. I(f) channel inhibitor ivabradine lowers heart rate in mice with enhanced sympathoadrenergic activities. Br J Pharmacol. 2004 May;142(1):107-12.

Chemical & Physical Properties

[ Density]:
1.1±0.1 g/cm3

[ Boiling Point ]:
626.9±55.0 °C at 760 mmHg

[ Molecular Formula ]:
C27H36N2O5

[ Molecular Weight ]:
468.585

[ Flash Point ]:
332.9±31.5 °C

[ Exact Mass ]:
468.262421

[ PSA ]:
60.47000

[ LogP ]:
3.69

[ Vapour Pressure ]:
0.0±1.8 mmHg at 25°C

[ Index of Refraction ]:
1.560

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

DownStream

Related Compounds