CAS 91940-87-3|Zatebradine hydrochloride

Introduction：Basic information about CAS 91940-87-3|Zatebradine hydrochloride, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.

Table of Contents

1. Names
2. Zatebradine hydrochloride BiologicalActivity
3. Chemical & Physical Properties
4. Safety Information
5. Articles26
6. Synonyms

Common Name	Zatebradine hydrochloride
CAS Number	91940-87-3	Molecular Weight	493.03500
Density	1.115g/cm3	Boiling Point	612.5ºC at 760mmHg
Molecular Formula	C₂₆H₃₇ClN₂O₅	Melting Point	/
MSDS	ChineseUSA	Flash Point	324.3ºC

Names

Name	3-[3-[2-(3,4-dimethoxyphenyl)ethyl-methylamino]propyl]-7,8-dimethoxy-2,5-dihydro-1H-3-benzazepin-4-one,hydrochloride
Synonym	More Synonyms

Zatebradine hydrochloride BiologicalActivity

Description	Zatebradine(UL-FS49) Hcl 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 ChannelResearch 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.

Description

Zatebradine(UL-FS49) Hcl 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 ChannelResearch 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.

Chemical & Physical Properties

Density	1.115g/cm3
Boiling Point	612.5ºC at 760mmHg
Molecular Formula	C₂₆H₃₇ClN₂O₅
Molecular Weight	493.03500
Flash Point	324.3ºC
Exact Mass	492.23900
PSA	60.47000
LogP	3.95270
InChIKey	ZRNKXJHEQKMWCH-UHFFFAOYSA-N
SMILES	COc1ccc(CCN(C)CCCN2CCc3cc(OC)c(OC)cc3CC2=O)cc1OC.Cl

Safety Information

Personal Protective Equipment	Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter
Safety Phrases	22-24/25
RIDADR	NONH for all modes of transport
WGK Germany	3

Articles26

Abnormal diastolic currents in ventricular myocytes from spontaneous hypertensive heart failure rats.

Am. J. Physiol. Heart Circ. Physiol. 291(5) , H2192-8, (2006)

Hypertension is a common cause of heart failure, and ventricular arrhythmias are a major cause of death in heart failure. The spontaneous hypertension heart failure (SHHF) rat model was used to study ...

Effects of tachycardia on regional wall motion in acute ischemic canine heart.

Tohoku J. Exp. Med. 203(2) , 111-21, (2004)

Tachycardia accompanies the preload reduction. Our aim is to assess the effect of the heart rate change on wall motion in ischemic heart. In 8 dogs with occlusion of left anterior descending artery, w...

Validation of a high-sensitivity assay for zatebradine in dried blood spots of human blood at pg/ml concentrations using HILIC-MS/MS.

Bioanalysis 2(11) , 1863-71, (2010)

One of the main reasons for the increased popularity of dried blood spots (DBS) is related to the 3Rs principles (replacement, refinement and reduction) for animal use in drug development. The small b...

Synonyms

Zatebradine dihydrochloride

Zatebradine hydrochloride

UL-FS49

Zatebradine (hydrochloride)

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