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Details on Person The potassium/sodium hyperpolarization-activated cyclic nucl...

Class:IdSummation:9726919
_displayNameThe potassium/sodium hyperpolarization-activated cyclic nucl...
_timestamp2021-04-13 09:42:29
created[InstanceEdit:9726912] Jassal, Bijay, 2021-04-13
literatureReference[LiteratureReference:9726906] Ivabradine: a new frontier in the treatment of stable coronary artery disease and chronic heart failure
[LiteratureReference:9726898] The Role of Ivabradine in the Management of Angina Pectoris
[LiteratureReference:9726900] Joint population pharmacokinetic/pharmacodynamic model for the heart rate effects at rest and at the end of exercise for cilobradine
[LiteratureReference:9726887] Novel blockers of hyperpolarization-activated current with isoform selectivity in recombinant cells and native tissue
[LiteratureReference:9726909] EC18 as a Tool To Understand the Role of HCN4 Channels in Mediating Hyperpolarization-Activated Current in Tissues
[LiteratureReference:9726929] Inhibitory Effective Perturbations of Cilobradine (DK-AH269), A Blocker of HCN Channels, on the Amplitude and Gating of Both Hyperpolarization-Activated Cation and Delayed-Rectifier Potassium Currents
textThe potassium/sodium hyperpolarization-activated cyclic nucleotide-gated channels (HCNs) are hyperpolarization-activated ion channels exhibiting weak selectivity for potassium over sodium ions which contribute to the native pacemaker currents in the heart (If) and in neurons (Ih). The If current is an important ionic current for regulating pacemaker activity in the sinoatrial (SA) node. The sinus node inhibitors (SNIs) cilobradine, ivabradine, and zatebradine all blocked the slow inward current through human HCN1, HCN2, HCN3, and HCN4 channels (Stieber et al. 2006). Ivabradine is indicated for the symptomatic management of stable heart-related chest pain and heart failure not fully managed by beta blockers (Giavarini & de Silva 2016, Gammone et al. 2020). Even as the close structural analogues of ivabradine cilobradine and zatebradine entered clinical trials (de Mendizábal et al. 2013), their development has been discontinued. They may be useful as starting points for novel compound optimization (Del Lungo et al. 2012) or further research (Romanelli et al. 2019, Lu et al. 2020).
(summation)[Reaction:9726875] HCNs:cAMP bind SNIs [Homo sapiens]
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