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
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.
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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 |
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