Hyperpolarization activated cyclic nucleotide gated channels

Ivabradine hydrochloride (S 16257-2) is a new If inhibitor (IC50: 2.9 μM). Ivabradine Hydrochloride is the hydrochloride salt form of ivabradine, an orally bioavailable, hyperpolarization-activated, cyclic nucleotide-gated (HCN) channel blocker, with negative chronotropic activity. Upon administration, ivabradine selectively binds to the intracellular portion of the HCN channel pore and blocks HCN channels in the pacemaker cells within the sinoatrial (SA) node. This inhibits the If (funny) pacemaker ion current, prevents the inward flow and intracellular accumulation of positively charged ions, reduces pacemaker activity and slows diastolic depolarization.

ZD7288 (ICI D7288), a selective hyperpolarization-activated cyclic nucleotide-gated channel blocker, inhibits hippocampal synaptic plasticity.

Zatebradine is a potent hyperpolarization-activated cyclic nucleotide-gated (HCN) channels inhibitor(IC50 of 1.96 µM).

Ivabradine Impurity 2, an impurity of Ivabradine, is a compound known for its oral bioavailability and mechanism as a blocker of hyperpolarization-activated, cyclic nucleotide-gated (HCN) channels [1].