HCN Channel Inhibitor

ZD7288 (ICI D7288) is a selective hyperpolarization-activated cyclic nucleotide-gated (HCN) channel blocker.

Ivabradine hydrochloride is a potent and orally active HCN (hyperpolarization-activated cyclic nucleotide-gated) channel blocker that inhibits the cardiac pacemaker current (If). Ivabradine hydrochloride reduces dose-dependently heart rate without modification of blood pressure. Ivabradine hydrochloride shows anticonvulsant, anti-ischaemic and anti-anginal activity.

RO-275 (compound 29) is a potent, selective and orally active HCN1 inhibitor with IC₅₀ values of 0.046, 14.3, 4.6, 13.9 µM for HCN1, HCN2, HCN3, HCN4, respectively. RO-275 rescues decremented working memory. RO-275 has the potential for the research of cognitive dysfunction in brain disorder.

Cilobradine hydrochloride is a HCN channel blocker. Cilobradine hydrochloride induces cardiac pacemaker currents and produces antidepressant effects.

Ivabradine is a potent and orally active HCN (hyperpolarization-activated cyclic nucleotide-gated) channel blocker that inhibits the cardiac pacemaker current (If). Ivabradine reduces dose-dependently heart rate without modification of blood pressure. Ivabradine shows anticonvulsant, anti-ischaemic and anti-anginal activity.

HCN2-IN-3 is an orally active HCN2 inhibitor. HCN2-IN-3 inhibits the activity of HCN2 ion channels. HCN2-IN-3 is applicable to research related to pain, tinnitus, central nervous system diseases, mental illnesses and mood disorders.

HCN2-IN-6 is a HCN2 ion channel inhibitor with an IC₅₀ of 7 nM. HCN2-IN-6 shows weak inhibitory activity for HCN4. HCN2-IN-6 can be used for the research of inflammatory disease and neurological disorders.

Norquetiapine ( N-Desalkylauetiapine), a metabolite of Quetiapine (HY-14544), is a selective HCN1 channel inhibitor, with an IC₅₀ of 13.9 μM. Norquetiapine selectively inhibits noradrenaline reuptake, is a partial 5-HT_1A (K_i = 45 nM) receptor agonist, and acts as an antagonist at presynapticα2 (K_i = 237 nM), 5-HT_2C(K_i = 107 nM), and 5-HT₇ (K_i = 76 nM) receptors. Norquetiapine blocks the human cardiac sodium channel Nav1.5 in a state-dependent manner. Norquetiapine shows partial anti-inflammatory effects in LPS (HY-D1056) injected C57BL/6 mice. Norquetiapine can be used for the study of depression and inflammation.

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

MS7710 is a hyperpolarization-activated cyclic nucleotide-gated (HCN) channel inhibitor with blood-brain barrier permeability and an excellent brain/plasma concentration ratio. MS7710 inhibits HCN channel-mediated I_h current, and reduces the firing frequency and burst activity of dopaminergic neurons in the ventral tegmental area. MS7710 ameliorates chronic social defeat stress-induced deficits in social interaction and impairments in reward-related cognitive flexibility in mice. MS7710 exerts only limited effects on ventral tegmental area dopaminergic neuron activity, social interaction, exploratory behavior, locomotor activity or sucrose preference in control mice. MS7710 is applicable to the research of major depressive disorder.

CP 339818 hydrochloride is a non-peptide Kv1.3 channel (IC₅₀ = 200 nM) and Kv1.4 channel blocker. CP 339818 hydrochloride inhibits HCN channel with IC₅₀s of 18.9 μM and 43.4 μM against HCN1 and HCN4 (high Cl^-). CP 339818 hydrochloride has significantly weaker blocking effects on Kv1.1, Kv1.2, Kv1.5, Kv1.6, Kv3.1-4, and Kv4.2 channels. CP 339818 hydrochloride selectively blocked Kv1.3, thereby inhibiting the activation process of human T cells. CP 339818 hydrochloride can be used to study the physiological functions of HCN and Kv channels.

Ivabradine-d₆ hydrochloride is the deuterium labeled Ivabradine hydrochloride. Ivabradine hydrochloride is a new If inhibitor with IC50 of 2.9 μM, and used as a pure heart rate lowering agent.

KIO-301 chloride hydrochloride is an azobenzene photoswitchable compound that blocks voltage-gated ion channels, including hyperpolarization-activated cyclic nucleotide gating (HCN, during exposure to visible light) ) and voltage-gated potassium channels (voltage-gated potassium channels).

YM758 is a "funny" I_f current channel (I_f channel) inhibitor.

Norquetiapine ( N-Desalkylauetiapine) dihydrochloride, a metabolite of Quetiapine (HY-14544), is a selective HCN1 channel inhibitor, with an IC₅₀ of 13.9 μM. Norquetiapine dihydrochloride selectively inhibits noradrenaline reuptake, is a partial 5-HT_1A (K_i = 45 nM) receptor agonist, and acts as an antagonist at presynapticα2 (K_i = 237 nM), 5-HT_2C(K_i = 107 nM), and 5-HT₇ (K_i = 76 nM) receptors. Norquetiapine dihydrochloride blocks the human cardiac sodium channel Nav1.5 in a state-dependent manner. Norquetiapine dihydrochloride shows partial anti-inflammatory effects in LPS (HY-D1056) injected C57BL/6 mice. Norquetiapine dihydrochloride can be used for the study of depression and inflammation.

Ivabradine-d₃ (hydrochloride) is the deuterium labeled Ivabradine hydrochloride. Ivabradine hydrochloride is a new If inhibitor with IC50 of 2.9 μM, and used as a pure heart rate lowering agent.

KIO-301 chloride is an azobenzene photoswitch compound that can block voltage-gated ion channels, including hyperpolarisation-activated cyclic nucleotide-gated (HCN) and voltage-gated potassium channels during exposure to visible light.

HCN2-IN-4 is an orally active HCN2 ion channel inhibitor, with an IC₅₀ of 3 nM. HCN2-IN-4 inhibits the activity of HCN2 ion channels. HCN2-IN-4 can be used in the research of pain, tinnitus and central nervous system diseases.

HCN2-IN-2 (Compound 35), azaindazole derivative, is a selective HCN2 inhibitor with an IC₅₀ of 145 nM. HCN2-IN-2 inhibits HCN2 channel activity blocks abnormal firing of peripheral nociceptive neurons. HCN2-IN-2 can be used for the research of pain.

Ivabradine sulfate is a potent and orally active HCN (hyperpolarization-activated cyclic nucleotide-gated) channel blocker that inhibits the cardiac pacemaker current (If). Ivabradine sulfate reduces dose-dependently heart rate without modification of blood pressure. Ivabradine sulfate shows anticonvulsant, anti-ischaemic and anti-anginal activity.