Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C26H36N2O5.ClH |
| Molecular Weight | 493.035 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
Cl.COC1=CC=C(CCN(C)CCCN2CCC3=C(CC2=O)C=C(OC)C(OC)=C3)C=C1OC
InChI
InChIKey=ZRNKXJHEQKMWCH-UHFFFAOYSA-N
InChI=1S/C26H36N2O5.ClH/c1-27(13-9-19-7-8-22(30-2)23(15-19)31-3)11-6-12-28-14-10-20-16-24(32-4)25(33-5)17-21(20)18-26(28)29;/h7-8,15-17H,6,9-14,18H2,1-5H3;1H
DescriptionCurator's Comment: The description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/15648302 | https://www.ncbi.nlm.nih.gov/pubmed/14561092 |
https://www.ncbi.nlm.nih.gov/pubmed/19093365
Curator's Comment: The description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/15648302 | https://www.ncbi.nlm.nih.gov/pubmed/14561092 |
https://www.ncbi.nlm.nih.gov/pubmed/19093365
Zatebradine is a bradycardic compound that blocks hyperpolarization-activated inward current (If) through cyclic nucleotide-gated cation (HCN) channels in sinoatrial node cells. Additionally, it can block voltage-gated outward K+ (IK) currents and related neuronal hyperpolarization-activated inward current (Ih) channels but exhibits little or no activity for L-type Ca2+ (ICa) currents. When assessed through telemetric ECG recording in mice, zatebradine reduced heart rate from 600 to 200 beats per minute with an ED50 value of 1.8 mg/kg and induced increasing arrhythmia at concentrations >10 mg/kg.
Approval Year
PubMed
| Title | Date | PubMed |
|---|---|---|
| Cardiovascular characterization of UL-FS 49, 1,3,4,5-tetrahydro-7,8-dimethoxy-3-[3-][2-(3,4-dimethoxyphenyl)ethyl] methylimino]propyl]-2H-3-benzazepin-2-on hydrochloride, a new "specific bradycardic agent". | 1984 Sep 3 |
|
| Specific bradycardic agents, a new therapeutic modality for anesthesiology: hemodynamic effects of UL-FS 49 and propranolol in conscious and isoflurane-anesthetized dogs. | 1987 Nov |
|
| Effect of zatebradine on contractility, relaxation and coronary blood flow. | 1993 Feb |
|
| Zatebradine, a specific bradycardic agent, enhances the positive inotropic actions of dobutamine in ischemic myocardium. | 1994 Jan |
|
| Zatebradine attenuates cyclic AMP-related positive chronotropic but not inotropic responses in isolated, perfused right atria of the dog. | 1995 Jan |
|
| Increases in inotropic state without change in heart rate: combined use of dobutamine and zatebradine in conscious dogs. | 1996 Dec 5 |
|
| Bradycardic and proarrhythmic properties of sinus node inhibitors. | 2006 Apr |
Sample Use Guides
Rats were treated with Zatebradine at dose 3 mg/kg i.v
Route of Administration:
Intravenous
Sinoatrial node pacemaker cells were isolated enzymatically from rabbit hearts. The inward currents, elicited by hyperpolarizing pulses of 2000 ms from a holding potential of −40 mV to −140 mV in 10 mV increments and then clamp back to 0 mV for 1000 ms, were recorded first in the absence and then in the presence of zatebradine or CsCl. The established If blockers zatebradine (1 mkM) and CsCl (2 mM) inhibited If by 63.7 ± 8.4% and 91.8 ± 5.6%, respectively
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3045335
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WJB7DYV16A
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DTXSID6045745
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m11583
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91940-87-3
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ACTIVE MOIETY
SUBSTANCE RECORD
