Abstract: Organic cation transporters (OCTs) are multispecific bidirectional transporters that participate in the transport of organic cation drugs, toxins and endogenous substances. OCTs include OCT1, OCT2 and OCT3, with high expression in peripheral tissues such as liver, intestine and kidney, and low expression in the brain, playing an important role. Evidence indicates that OCTs may play a compensatory role when monamine transmitters with high affinity such as dopamine transporter, norepinephrine transporter and serotonin transporter are blocked. The change of OCTs at blood-brain barrier may affect concentrations of some exogenous drugs and toxic substances in the brain. OCT-mediated drug interactions may increase the risk of side effects with the central nervous system. The distribution of OCTs in the brain, the role of OCTs in homeostasis maintenance in the brain and the significance in pharmacological research are reviewed, aiming to provide reference for the further study of OCTs in drug transport and intracerebral diseases.