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Zatebradine

Names

[ CAS No. ]:
85175-67-3

[ Name ]:
Zatebradine

[Synonym ]:
Zatebradinum [INN-Latin]
UL-FS-49
3-[3-[(3,4-Dimethoxy phenethyl)methylamino]-propyl]-1,3,4,5-tetrahydro-7,8-dimethoxy-2H-3-benzazepin-2-one
Zatebradina
Zatebradine
Zatebradine [INN]
7,8-dimethoxy-3-<3-<<2-(3,4-dimethoxyphenyl)ethyl>-methylamino>propyl>-1,3,4,5-tetrahydro-2H-benzazepin-2-one
Zatebradina [INN-Spanish]
Zatebradinum
[14C]-Zatebradine
1-[7,8-dimethoxy-1,3,4,5-tetrahydro-2H-3-benzazepin-2-on-3-yl]-3-[N-methyl-N-(2-{3,4-dimethoxy-phenyl}ethyl)-amino]-propane

Biological Activity

[Description]:

Zatebradine(UL-FS49) is a potent HCN channels antagonist, which decreased the heartbeat in a reversible manner; 92% inhibition of the hHCN1-mediated current at 10 uM.IC50 value: 10 uM(92% 92% inhibition of the hHCN1) [1]Target: hHCN channel antagonistThe pharmacological properties of hHCN1-mediated currents resembled those of native hyperpolarization-activated currents (I(h)), that is, blockade by Cs(+) (99% at 5 mm), ZD 7288 (98% at 100 microm) and zatebradine (92% at 10 microm) [1]. When voltage-clamp pulse trains were applied, cilobradine induced a use-dependent blockade of If that was stronger and faster than that with zatebradine. Recovery from blockade during prolonged hyperpolarization was significantly faster with zatebradine [2]. The selective HCN blocker zatebradine reduced the activity of oriens-lacunosum moleculare interneurons in wild-type but not HCN2(-/-) mice and decreased the frequency of spontaneous inhibitory currents in postsynaptic CA1 pyramidal cells [3].

[Related Catalog]:

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

[References]

[1]. Gill CH, et al. Characterization of the human HCN1 channel and its inhibition by capsazepine. Br J Pharmacol. 2004 Oct;143(3):411-21.

[2]. Van Bogaert PP, et al. Use-dependent blockade of cardiac pacemaker current (If) by cilobradine and zatebradine. Eur J Pharmacol. 2003 Oct 8;478(2-3):161-71.

[3]. Matt L, et al. HCN2 channels in local inhibitory interneurons constrain LTP in the hippocampal direct perforant path. Cell Mol Life Sci. 2011 Jan;68(1):125-37.


[Related Small Molecules]

ZD7288 | Zatebradine hydrochloride | DK-AH 269

Chemical & Physical Properties

[ Density]:
1.115g/cm3

[ Boiling Point ]:
612.5ºC at 760 mmHg

[ Molecular Formula ]:
C26H36N2O5

[ Molecular Weight ]:
456.57400

[ Flash Point ]:
324.3ºC

[ Exact Mass ]:
456.26200

[ PSA ]:
60.47000

[ LogP ]:
3.15070

[ Index of Refraction ]:
1.545

[ Storage condition ]:
2-8℃

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

DownStream

Related Compounds