| 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
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.
Originator
Approval Year
PubMed
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
ACTIVE MOIETY
SUBSTANCE RECORD
