Abstract
Hyperpolarization-activated cyclic nucleotide-gated (HCN) channels play important roles both in the control of heart rate and neuronal excitability. HCN channels open on hyperpolarization voltage, permeate to potassium and sodium, and generate an inward current, which is modulated by intracellular cAMP. HCN channels have been reported to involve in various human diseases, including heart failure, pain and epilepsy with datas from mutagenesis, transgenic mice and pharmacological studies. As a result, HCN channels may offer excellent drug development opportunities for novel analgestic, bradycardic and anticonvulsant drugs. Ivabradine is the first HCN channel inhibitor being clinically approved in 2005 for the treatment of chronic stable angina pectoris and heart failure. This review will summarize the structure and function of HCN channels. Further, we will discuss recent advances concerning the identification and action mechanism of reported HCN channel inhibitors.
Keywords: Arrhythmia, channel inhibitors, epilepsy, HCN channels, heart failure, ivabradine, pain
Graphical Abstract
Current Topics in Medicinal Chemistry
Title:HCN Channel as Therapeutic Targets for Heart Failure and Pain
Volume: 16 Issue: 16
Author(s): Ying Cao, Jianxin Pang and Pingzheng Zhou
Affiliation:
Keywords: Arrhythmia, channel inhibitors, epilepsy, HCN channels, heart failure, ivabradine, pain
Abstract: Hyperpolarization-activated cyclic nucleotide-gated (HCN) channels play important roles both in the control of heart rate and neuronal excitability. HCN channels open on hyperpolarization voltage, permeate to potassium and sodium, and generate an inward current, which is modulated by intracellular cAMP. HCN channels have been reported to involve in various human diseases, including heart failure, pain and epilepsy with datas from mutagenesis, transgenic mice and pharmacological studies. As a result, HCN channels may offer excellent drug development opportunities for novel analgestic, bradycardic and anticonvulsant drugs. Ivabradine is the first HCN channel inhibitor being clinically approved in 2005 for the treatment of chronic stable angina pectoris and heart failure. This review will summarize the structure and function of HCN channels. Further, we will discuss recent advances concerning the identification and action mechanism of reported HCN channel inhibitors.
Export Options
About this article
Cite this article as:
Cao Ying, Pang Jianxin and Zhou Pingzheng, HCN Channel as Therapeutic Targets for Heart Failure and Pain, Current Topics in Medicinal Chemistry 2016; 16 (16) . https://dx.doi.org/10.2174/1568026616666151215104058
DOI https://dx.doi.org/10.2174/1568026616666151215104058 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
- Announcements
Related Articles
-
Recent Progress in Transition-Metal-Catalyzed C-N Cross-Couplings: Emerging Approaches Towards Sustainability
Current Organic Synthesis α7-Nicotinic Acetylcholine Receptors: An Old Actor for New Different Roles
Current Drug Targets Considerations in the Development of Reversibly Binding PET Radioligands for Brain Imaging
Current Medicinal Chemistry Targeting Ionotropic Glutamate Receptors in the Treatment of Epilepsy
Current Neuropharmacology Development of Radioligands for the Imaging of α7 Nicotinic Acetylcholine Receptors with Positron Emission Tomography
Current Drug Targets 3D QSAR Studies on 1, 3, 4-Thiadiazole Derivatives: An Approach to Design Novel Anticonvulsants
Medicinal Chemistry Random Walks on Biomedical Networks
Current Proteomics The Ubiquitous Choline Transporter SLC44A1
Central Nervous System Agents in Medicinal Chemistry Hormone Replacement Therapy and Stroke
Current Vascular Pharmacology Metabotropic Glutamate Receptors in the Control of Mood Disorders
CNS & Neurological Disorders - Drug Targets Nano-Neurotherapeutics (NNTs): An Emergent and Multifaceted Tool for CNS Disorders
Current Drug Metabolism Curcumin: Not So Spicy After All
Mini-Reviews in Medicinal Chemistry Synthesis, Neurotoxicity and Anticonvulsant Study of Some Benzothiazole Analogs
Letters in Drug Design & Discovery Meet the Editorial Board Member
CNS & Neurological Disorders - Drug Targets Environment, Physical Activity, and Neurogenesis: Implications for Prevention and Treatment of Alzhemiers Disease
Current Alzheimer Research Application of Human Placental Villous Tissue Explants to Study ABC Transporter Mediated Efflux of 2,4-Dinitrophenyl-S-Glutathione
Current Pharmaceutical Biotechnology Revolutionary Impact of Nanodrug Delivery on Neuroscience
Current Neuropharmacology Systematic Comparison of the Performance of Different 2D and 3D Ligand-Based Virtual Screening Methodologies to Discover Anticonvulsant Drugs
Combinatorial Chemistry & High Throughput Screening α7-Nicotinic Receptors and Cognition
Current Drug Targets Heterotrimeric G Proteins Control Diverse Pathways of Transmembrane Signaling, a Base for Drug Discovery
Mini-Reviews in Medicinal Chemistry