The recently gained knowledge in molecular pharmacology has raised interesting ideas to drug design. The progress in understanding transcription factor structure, function and regulation has opened up new strategies for direct and selective pharmacological enhancement or lowering of the expression of a gene by rational targeting of specific transcription factors. In the central nervous system, transcription factor AP-2 family is one of the critical regulatory factors for neural gene expression and neuronal development. A number of genes in the monoaminergic systems, suggested to be involved in psychiatric disorders, have AP-2 binding sites in regulatory regions and several studies have indicated that transcription factor AP-2 is involved in the monoaminergic systems. Transcription factor AP-2β genotype has been studied in relation to personality, platelet monoamine oxidase (MAO) activity, CSF-levels of monoamine metabolites, binge-eating disorder, premenstrual dysphoric disorder, and schizophrenia. In this paper, the involvement of transcription factor AP-2 in monoaminergic functions is discussed. We have also made an effort to elucidate the effect of antidepressant treatment on transcription factor AP-2.