186097-54-1

186097-54-1 structure

Name: DK-AH 269
Chemical Name: Cilobradine hydrochloride
CAS Number: 186097-54-1
Molecular Formula: C₂₈H₃₉ClN₂O₅
Molecular Weight: 519.07300
Catalog: Signaling Pathways Membrane Transporter/Ion Channel HCN Channel
Create Date: 2018-02-24 08:00:00
Modify Date: 2024-01-10 20:18:47
Cilobradine is an HCN Channel blocker; an open channel blocker of neuronal Ih and related cardiac If channels.Target: HCN Channel blockerCilobradine is a HCN channel blocker that is about 3 times more potent than ZD7288. At a concentration of 10 μM, Cilobradine inhibits WT mHCN2 channel current by 86 ± 2% (n = 5). In contrast, I432A and A425G channel currents were only reduced by 14 ± 1% (n = 4) and 19 ± 2% (n = 8), respectively, by this concentration of Cilobradine. The double mutant (I432A/A425G) channel was even less sensitive to 10 μM Cilobradine (8 ± 2% inhibition; n = 4).

Name	Cilobradine hydrochloride
Synonyms	DK-AH 269 (S)-(+)-7,8-Dimethoxy-3-[[1-(2-(3,4-dimethoxyphenyl)ethyl)-3-piperidinyl]methyl]-1,3,4,5-tetrahydro-2H-3-benzazepin-2-one hydrochloride 3-[[(3S)-1-[2-(3,4-dimethoxyphenyl)ethyl]piperidin-3-yl]methyl]-7,8-dimethoxy-2,5-dihydro-1H-3-benzazepin-4-one,hydrochloride DK-AH 269 Cilobradine (hydrochloride)

Description	Cilobradine is an HCN Channel blocker; an open channel blocker of neuronal Ih and related cardiac If channels.Target: HCN Channel blockerCilobradine is a HCN channel blocker that is about 3 times more potent than ZD7288. At a concentration of 10 μM, Cilobradine inhibits WT mHCN2 channel current by 86 ± 2% (n = 5). In contrast, I432A and A425G channel currents were only reduced by 14 ± 1% (n = 4) and 19 ± 2% (n = 8), respectively, by this concentration of Cilobradine. The double mutant (I432A/A425G) channel was even less sensitive to 10 μM Cilobradine (8 ± 2% inhibition; n = 4).
Related Catalog	Signaling Pathways >> Membrane Transporter/Ion Channel >> HCN Channel Research Areas >> Cardiovascular Disease
References	[1]. Cheng L, et al. Molecular mapping of the binding site for a blocker of hyperpolarization-activated, cyclic nucleotide-modulated pacemaker channels. J Pharmacol Exp Ther. 2007 Sep;322(3):931-939.

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