Abstract: Nitric oxide (NO) as a signal transduction species and/or effector molecule plays an extremely important role in the cardiovascular, nervous, and immune systems. Insufficient production or abnormal signal transduction of NO is closely associated with onset and progression of many diseases. Studies on direct or indirect regulation of NO levels in vivo and related metabolic pathways have become a hot spot in biomedical and pharmaceutical fields. This review briefly introduces the generation of NO in vivo and its physiological and pathological functions in cardio-cerebrovascular system, with focus on the authors'' research on NO-donating cardio-cerebrovascular and related drugs, aiming to provide some reference for future development of these drugs.