Osteoarthritis (OA) is a highly prevalent joint disease that causes substantial disability, yet effective approaches to disease prevention or to the delay of OA progression are lacking. Emerging evidence has pinpointed ion channels as pivotal mediators in OA pathogenesis and as promising targets for disease-modifying treatments. Preclinical studies have assessed the potential of a variety of ion channel modulators to modify disease pathways involved in cartilage degeneration, synovial inflammation, bone hyperplasia and pain, and to provide symptomatic relief in models of OA. Some of these modulators are currently being evaluated in clinical trials. This review explores the structures and functions of ion channels, including transient receptor potential channels, Piezo channels, voltage-gated sodium channels, voltage-dependent calcium channels, potassium channels, acid-sensing ion channels, chloride channels and the ATP-dependent P2XR channels in the osteoarthritic joint. The discussion spans channel-targeting drug discovery and potential clinical applications, emphasizing opportunities for further research, and underscoring the growing clinical impact of ion channel biology in OA.

骨关节炎 (OA) 是一种非常普遍的关节疾病，可导致严重残疾，但缺乏有效的疾病预防或延迟 OA 进展的方法。新的证据表明离子通道是 OA 发病机制的关键介质，也是缓解疾病治疗的有希望的靶标。临床前研究评估了多种离子通道调节剂改变与软骨变性、滑膜炎症、骨质增生和疼痛有关的疾病途径的潜力，并在 OA 模型中缓解症状。其中一些调节剂目前正在临床试验中进行评估。本文探讨了离子通道的结构和功能，包括瞬时受体电位通道、压电通道、电压门控钠通道、电压依赖性钙通道、钾通道、酸敏感离子通道、氯离子通道和ATP依赖性P2XR通道在骨关节炎关节中。讨论涵盖了通道靶向药物的发现和潜在的临床应用，强调了进一步研究的机会，并强调了离子通道生物学在 OA 中日益增长的临床影响。