Is ZD7288 a selective blocker of hyperpolarization-activated cyclic nucleotide-gated channel currents? |
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| Authors: | Xing Wu Liping Liao Xiangming Liu Fang Luo Tianming Yang Chenhong Li |
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| Institution: | 1.Key Laboratory of Molecular Biophysics of Ministry of Education; College of Life Science and Technology; Wuhan, China;2.The Laboratory of Membrane Ion Channels and Medicine; College of Biomedical Engineering; South-Central University for Nationalities; Wuhan, China;3.Department of Anesthesiology; Tongji Hospital; Huazhong University of Science and Technology; Wuhan, China;4.College of Pharmacy; South-Central University for Nationalities; Wuhan, China |
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| Abstract: | ZD7288 has been widely used as a tool in the study of hyperpolarization-activated cyclic nucleotide-gated channels (HCN channels), and to test the relationships between HCN channels and heart and brain function. ZD7288 is widely considered a selective blocker of HCN currents. Here we show that ZD7288 inhibits not only HCN channel currents, but also Na+ currents in DRG neurons and ZD7288 was confirmed to inhibit Na+ current in HEK293 cells transfected with Nav1.4 plasmids. Thus our findings challenge the view that ZD7288 is a selective blocker of HCN channels. Conclusions about the role of NCN channels in neuronal function should be re-evaluated if based exclusively on the effect of ZD7288. |
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| Keywords: | ZD7288 HCN channel currents Na+ currents neuropathic pain DRG |
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