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In recent years, there has been a significant increase in research on the structure and function of ion channels, thereby promoting the study of drug targeting mechanisms involving these channels. The ocean serves as a rich reservoir of lead compounds for drug development, undeniably providing a valuable source for ion channel\u2010targeting drugs. However, various factors contribute to the superficial nature of many studies on drug action mechanisms and there is ongoing confusion surrounding related concepts. This review systematically reviews the mechanisms of action of marine natural products and synthetic derivatives studied from 2000 to 2025, with the goal to establish reference standards relevant to this field of study. Additionally, we systematically review the structure\u2010activity relationship studies and summarize drug optimization strategies in subsequent sections. 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