Cilobradine is an HCN channel blocker primarily targeting the hyperpolarization-activated cyclic nucleotide-gated channels HCN1, HCN2, HCN3, and HCN4. It exhibits significant biological activity by decreasing heart rate, effectively reducing endogenous If current in mouse sinoatrial node cells with an IC50 of 0.62 μM. Cilobradine can lower heart rates from 600 bpm to 200 bpm in a dose-dependent manner, with an ED50 of 1.2 mg/kg. However, at doses exceeding 5 mg/kg, Cilobradine may induce arrhythmias characterized by periodic fluctuations between T waves and P waves, making it a valuable tool for cardiovascular research.
Cilobradine is an HCN channel blocker primarily targeting the hyperpolarization-activated cyclic nucleotide-gated channels HCN1, HCN2, HCN3, and HCN4. It exhibits significant biological activity by decreasing heart rate, effectively reducing endogenous If current in mouse sinoatrial node cells with an IC50 of 0.62 μM. Cilobradine can lower heart rates from 600 bpm to 200 bpm in a dose-dependent manner, with an ED50 of 1.2 mg/kg. However, at doses exceeding 5 mg/kg, Cilobradine may induce arrhythmias characterized by periodic fluctuations between T waves and P waves, making it a valuable tool for cardiovascular research.
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