Scopolamine, a natural tropane alkaloid, was isolated in 1880 from Scopolia japonica and is considered one of the earliest competitive cholinergic receptor antagonists discovered. Compared to other drugs with similar effects such as atropine, scopolamine exhibits greater permeability across the blood-brain barrier and can remain in the central nervous system longer to exert pharmacological effects. The effects of scopolamine on the central nervous system are widely utilized in the treatment of motion sickness, anesthesia, and pain relief, and may be broadly applied to diseases such as depression. On the other hand, scopolamine can impair central nervous system functions such as cognition, learning and memory, and attention, which limits its clinical use. Additionally, the neurotoxicity of scopolamine has been widely used in animal models of amnesia and delirium and has become an important tool for studying the central cholinergic system. This article outlines the chemical structure and classification of scopolamine, summarizes its clinical use and toxicity in the central nervous system, discusses its application in cholinergic function research and preclinical studies, as well as the controversy surrounding its central nervous system toxicity. We also provided an outlook for the potential use of scopolamine in central nervous system diseases.