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Aineng Peng,1 Jianbo Chai,2 Haiyuan Wu,1 Bing Bai,3 Huihui Yang,1 Weizhi He,1 Yonghou Zhao2 1Heilongjiang University of Chinese Medicine, Harbin, 150040, People’s Republic of China; 2Heilongjiang Mental Hospital, Harbin, 150036, People’s Republic of China; 3Tongde Hospital of Zhejiang Province, Hangzhou, 311100, People’s Republic of ChinaCorrespondence: Yonghou Zhao, Heilongjiang Mental Hospital, 153 Hengdao Street, Harbin, Heilongjiang, 150036, People’s Republic of China, Tel +86 13904638645, Email zyszbx2020@126.comAbstract: Schizophrenia is a disease with a complex pathological mechanism that is influenced by multiple genes. The study of its pathogenesis is dominated by the dopamine hypothesis, as well as other hypotheses such as the 5-hydroxytryptamine hypothesis, glutamate hypothesis, immune-inflammatory hypothesis, gene expression abnormality hypothesis, and neurodevelopmental abnormality hypothesis. The first generation of antipsychotics was developed based on dopaminergic receptor antagonism, which blocks dopamine D2 receptors in the brain to exert antipsychotic effects. The second generation of antipsychotics acts by dual blockade of 5-hydroxytryptamine and dopamine receptors. From the third generation of antipsychotics onwards, the therapeutic targets for antipsychotic schizophrenia expanded beyond D2 receptor blockade to explore D2 receptor partial agonism and the antipsychotic effects of new targets such as D3, 5-HT1A, 5-HT7, and mGlu2/3 receptors. The main advantages of the second and third generation antipsychotics over first-generation antipsychotics are the reduction of side effects and the improvement of negative symptoms, and even though third-generation antipsychotics do not directly block D2 receptors, the modulation of the dopamine transmitter system is still an important part of their antipsychotic process. According to recent research, several receptors, including 5-hydroxytryptamine, glutamate, γ-aminobutyric acid, acetylcholine rece