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.
Products | Products > Disease Areas > Blood or Cardio-cerebrovascular Disease | Products > Signaling Pathways > Metabolic Enzyme/Protease | Products > Research Areas > Cardiovascular Disease | Products > Signaling Pathways > Endogenous Metabolite
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