The invention provides a novel use of benzoic acid with structure of the general formula (I) and its derivatives. The benzoic acid with structure of the general formula (I) and its derivatives have anenhancement/suppression of 5-serotonin transporter (SERT) activity, which can be used in the preparation of neuropsychiatric disorders such as depression, anxiety, schizophrenia, obsessive-compulsivedisorder, neurodegenerative diseases, drug addiction, and digestive system functional disorder diseases such as slow transit constipation, irritable bowel syndrome and functional abdominal distentionand has important drug development value.