cyclic nucleotide-gated channel

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.

8-Demethyl Ivabradine, a metabolite of Ivabradine, is an orally bioavailable cyclic nucleotide-gated (HCN) channel blocker with hyperpolarization-activated properties[1].

Ivabradine is a potent, orally active HCN (hyperpolarization-activated cyclic nucleotide-gated) channel blocker that inhibits pacemaker current (If). ivabradine decreases heart rate in a dose-dependent manner and does not alter blood pressure. ivabradine has anticonvulsant, anti-ischaemic and anti-anginal effects.

Ivabradine Impurity 1, identified as an impurity of Ivabradine, is an orally bioavailable compound that functions as a blocker of the hyperpolarization-activated, cyclic nucleotide-gated (HCN) channel [1].

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

Pan-HCN-IN-1 (Compound J&J12e) is an inhibitor of the hyperpolarization-activated and cyclic-nucleotide-gated 1 (HCN1) ion channel, with an IC50 of 58 nM. Pan-HCN-IN-1 reduces the voltage sag response and enhances EPSP summation in ex vivo rat brain slices [1].

Sp-8-Br-PET-cGMPS is a membrane-permeable PKG activator and an inhibitor of the membrane-permeable retinal cGMP-gated ion channels (cGMP-gated ion channel). It also serves as an activator for cGMP-dependent protein kinase I α and β. Resistant to mammalian cyclic nucleotide-dependent phosphodiesterases, Sp-8-Br-PET-cGMPS does not undergo metabolic side effects and exhibits stronger lipophilicity and permeability compared to Sp-8-pCPT-cGMPS. This compound is useful for investigating the role of the cGMP signaling pathway in the nervous system.