147541-45-5
Chemical Structure
Cilobradine
Synonym(s): Cilo
- CAS No.: 147541-45-5
- Formula:C28H38N2O5
- Molecular Weight:482.61
IUPAC Name: (S)-3-((1-(3,4-dimethoxyphenethyl)piperidin-3-yl)methyl)-7,8-dimethoxy-4,5-dihydro-1H-benzo[d]azepin-2(3H)-one
InChIKey: OBUFMJDDZTXJPY-NRFANRHFSA-N
SMILES: O=C1N(C[C@@H]2CN(CCC3=CC=C(OC)C(OC)=C3)CCC2)CCC4=CC(OC)=C(OC)C=C4C1
Biological Activity: Cilobradine (Cilo) is a HCN channel blocker with heart rate reducing activity. Cilobradine blocks the slow inward current of human HCN1, HCN2, HCN3, and HCN4 channels. Cilobradine has a slightly higher efficiency in blocking endogenous If in mouse sinoatrial node cells (IC50 value is 0.62μM). Cilobradine can dose-dependently reduce the heart rate from 600 to 200 bpm with an ED50 value of 1.2 mg/kg. Cilobradine induces arrhythmias at doses greater than 5 mg/kg, which are characterized by periodic fluctuations between T waves and P waves[1].
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Cilobradine | Cilobradine (Cilo) is a HCN channel blocker with heart rate reducing activity. Cilobradine blocks the slow inward current of human HCN1, HCN2, HCN3, and HCN4 channels. Cilobradine has a slightly higher efficiency in blocking endogenous If in mouse sinoatrial node cells (IC50 value is 0.62μM). Cilobradine can dose-dependently reduce the heart rate from 600 to 200 bpm with an ED50 value of 1.2 mg/kg. Cilobradine induces arrhythmias at doses greater than 5 mg/kg, which are characterized by periodic fluctuations between T waves and P waves. | |||||||||||||||||||||
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