Objective To review the biologic characteristics and biologic effect of cholecystokinine (CCK) on the central nervous system. Methods The literatures of recent years on research advancement of cholecystokinine as neurotransmitters/peptides in signal transduction, neuron protection and pain management in the central nervous system are reviewed. Results CCK possesses the ability to suppress the convulsant effects of convulsants. CCK8 is able to reduce the neural damage caused and delay the neural aging. CCK antagonists play an important role in human pain transduction. Conclusion CCK has been proven to be one of the richest neurotransmitters/neuropeptides as well as an important signal factor in the brain, and its important biologic effect is being confirmed.