β-arrestin is involved in multiple physiological and pathological processes，such as cardiovascular and gastrointestinal diseases，kidney and lung dysfunction，inflammation and metabolic disorders，bone mineral homeostasis maintenance，reproductive and central nervous system diseases. With the in-depth understanding of β-arrestin mediated pathways，G protein-coupled receptors（GPCR）biased signal transduction gives us an insight into the development of selective drugs with higher efficiency and fewer side effects. In recent years，G protein-biased or β-arrestin-biased ligands have continuously emerged. Especially，β-arrestin-biased ligands have shown great application prospects in treating neuropsychiatric diseases.