Dong Zhoujun, Xiong Baichen, Sun Tianyu, Jiang Ruijia, Feng Feng, Sun Haopeng
Department of Natural Medicinal Chemistry, China Pharmaceutical University, Nanjing 210009, China.
School of Pharmacy, China Pharmaceutical University, Nanjing 211198, China.
Bioorg Med Chem. 2025 Oct 1;128:118180. doi: 10.1016/j.bmc.2025.118180. Epub 2025 Apr 4.
Na1.7 has been the most studied ion channel among the 9 subtypes of sodium ion, and it is also one of the popular analgesic targets in recent years. Compared with opioid receptors, because of its advantages of targeting a variety of pain types and being unrelated to addiction, many related inhibitors have been excavated for it, including old drugs and new uses, peptides, and new skeleton small molecules. Some of these inhibitors have reached the second phase of clinical research, and some are still in the laboratory research stage. So far, no exclusive Na1.7 inhibitor has successfully passed the third phase of clinical research and entered the field of vision of patients. This article reviews the action sites and mechanisms of different Na1.7 inhibitors in terms of historical background and related analgesic activities, and also summarizes the related inhibitors that are currently under active development, hoping to provide useful information for the research of new Na1.7 inhibitors.