Abstract: Neuroinflammation plays a pivotal regulatory role in the onset and progression of various central nervous system diseases. As a key immune sensor, the NOD-like receptor thermal protein domain associated protein 3 (NLRP3) inflammasome, upon activation, can exacerbate neuroinflammation, leading to neuronal injury and death, thereby accelerating the pathological processes of neurodegenerative diseases such as Alzheimer's disease and Parkinson's disease. Consequently, the NLRP3 inflammasome has emerged as an important therapeutic target for modulating neuroinflammation. In recent years, significant progress has been made in the development of NLRP3 inflammasome inhibitors. Numerous novel inhibitors have been identified that effectively reduce inflammatory responses and protect neurons from damage, demonstrating promising efficacy in animal models, particularly in improving cognitive and motor functions. This review will summarize the canonical activation mechanisms of the NLRP3 inflammasome, explore its pathogenic roles in central nervous system diseases such as Alzheimer's disease, Parkinson's disease, multiple sclerosis, and depression, and provide an overview of recent advances in NLRP3-targeted drug development, aiming to offer new insights and strategies for the treatment of central nervous system diseases.