Related Experiment Video

Updated: Mar 28, 2026

Method for Identifying Small Molecule Inhibitors of the Protein-protein Interaction Between HCN1 and TRIP8b
10:20

Method for Identifying Small Molecule Inhibitors of the Protein-protein Interaction Between HCN1 and TRIP8b

Published on: November 11, 2016

9.1K

HCN Channel as Therapeutic Targets for Heart Failure and Pain

Ying Cao, Jianxin Pang, Pingzheng Zhou1

  • 1Department of Guangdong Provincial Key Laboratory of New Drug Screening, School of Pharmaceutical Sciences, Southern Medical University; P.O. Box: No.1023, South Shatai Road, Guangzhou 510515, China. zhoupingzheng@126.com.

Current Topics in Medicinal Chemistry
|December 16, 2015
PubMed

Insights

Hyperpolarization-activated cyclic nucleotide-gated (HCN) channels are crucial for heart rate and neuronal activity. This review covers HCN channel function, disease relevance, and drug development opportunities for conditions like heart failure and epilepsy.

Area of Science:

  • Molecular and Cellular Biology
  • Pharmacology
  • Cardiology
  • Neuroscience

Background:

  • Hyperpolarization-activated cyclic nucleotide-gated (HCN) channels are critical ion channels involved in regulating heart rate and neuronal excitability.
  • These channels conduct both potassium (K+) and sodium (Na+) ions, generating an inward current that is modulated by intracellular cyclic adenosine monophosphate (cAMP).

Purpose of the Study:

  • To review the structure and function of HCN channels.
  • To discuss the involvement of HCN channels in various human diseases, including heart failure, pain, and epilepsy.
  • To explore the therapeutic potential of targeting HCN channels for drug development.

Main Methods:

  • Review of existing scientific literature, including mutagenesis studies, transgenic mouse models, and pharmacological investigations.
  • Analysis of the mechanisms of action for identified HCN channel inhibitors.

Main Results:

  • HCN channels are implicated in significant human diseases, highlighting their physiological and pathological importance.
  • Mutagenesis, transgenic, and pharmacological data support the role of HCN channels in disease pathogenesis.
  • The therapeutic potential for developing novel analgesic, bradycardic, and anticonvulsant drugs targeting HCN channels is substantial.

Conclusions:

  • HCN channels represent promising targets for novel therapeutic interventions in cardiovascular and neurological disorders.
  • Ivabradine, the first approved HCN channel inhibitor, demonstrates the clinical viability of targeting these channels for conditions like angina and heart failure.
  • Further research into HCN channel inhibitors and their mechanisms of action is warranted for advancing drug development.

More Related Videos

Exploring Arterial Smooth Muscle Kv7 Potassium Channel Function using Patch Clamp Electrophysiology and Pressure Myography11:02

Exploring Arterial Smooth Muscle Kv7 Potassium Channel Function using Patch Clamp Electrophysiology and Pressure Myography

Published on: September 14, 2012

16.4K
Mesenteric Artery Contraction and Relaxation Studies Using Automated Wire Myography07:51

Mesenteric Artery Contraction and Relaxation Studies Using Automated Wire Myography

Published on: September 22, 2011

29.7K

Related Concept Videos

Heart Failure Drugs: Inhibitors of Renin-Angiotensin System01:26

Heart Failure Drugs: Inhibitors of Renin-Angiotensin System

The activation of the sympathetic nervous system and the renin-angiotensin-aldosterone system (RAAS) contributes to cardiac remodeling, and inhibiting the RAAS is a pharmacological target in heart failure management. As a result, neurohumoral modulation is a crucial treatment principle for managing heart failure. This approach involves using medications like ACE inhibitors (ACEIs), angiotensin receptor blockers (ARBs), β-blockers, mineralocorticoid receptor antagonists (MRAs), and neutral...
1.4K
Antianginal Drugs: Calcium Channel Blockers and Ranolazine01:25

Antianginal Drugs: Calcium Channel Blockers and Ranolazine

Angina pectoris, a primary symptom of ischemic heart disease, requires careful pharmacological interventions. In this context, calcium channel blockers (CCBs) and ranolazine have emerged as crucial pharmacotherapeutic agents, providing deep insights into the complexities of angina management.
CCBs, a diverse class that includes dihydropyridines (nifedipine) and diphenylalkylamines (verapamil and diltiazem), exert their effect by blocking calcium channels in cardiac and smooth muscle cells. This...
1.8K
Ligand-gated Ion Channels01:19

Ligand-gated Ion Channels

Ligand-gated ion channels are transmembrane proteins with a channel for ions to pass through and a binding site for a ligand. The channel opens only when a ligand attaches to the binding site.
Three Subfamilies of Ligand-gated Ion Channels
Ligand-gated ion channels fall into three subfamilies. The 'Cys-loop' includes the nicotinic acetylcholine receptors, γ-aminobutyric acid (GABA), glycine, and 5-hydroxytryptamine receptors. The second one is the 'Pore-loop' channels that...
15.4K
Heart Failure V: Medical Management01:30

Heart Failure V: Medical Management

Medical Management of Acute Decompensated Heart Failure (ADHF)The primary goals of therapy for patients hospitalized with acute decompensated heart failure (ADHF) include:Relieving symptomsOptimizing volume statusSupporting oxygenation and ventilationMaintaining cardiac output (CO) and end-organ perfusionIdentifying and addressing the cause of ADHFPreventing complicationsProviding patient education on factors precipitating HF exacerbationPlanning for dischargeOngoing monitoring and assessment...
520
Non-gated Ion Channels01:24

Non-gated Ion Channels

Ion channels are specialized proteins on the plasma membrane that allow charged ions to pass down their electrochemical gradient. Their main function is to maintain the membrane potential which is critical for cell viability. These channels are either gated or non-gated and can transport more than a thousand ions within milliseconds for the cellular event to occur.
Compared to the gated ion channels, the non-gated channels, also known as leakage or passive channels, have no gating mechanism....
9.0K
Ligand-Gated Ion Channel Receptor: Gating Mechanism01:30

Ligand-Gated Ion Channel Receptor: Gating Mechanism

Ligand-gated ion channels are transmembrane proteins that play a vital role in intercellular communication and functions of the nervous system. They allow the influx of ions across the membrane once the neurotransmitter binds, allowing the subsequent transmission of electrical excitation across the neurons. Other ligand-gated ion channels, like the γ-aminobutyric acid (GABA) receptor, permit anions like chloride into the cells on the binding of the GABA molecule. Their entry into the cell...
4.7K