The serotonin 2B receptor (5-HT2BR) is the most recent addition to the 5-HT2R family. During the last decade, a growing number of studies have shown that the central 5-HT2BR participates in the control of serotonin (5-HT) and dopamine (DA) neuron activity and have underlined its potential for new therapeutic strategies for several neuropsychiatric disorders such as drug addiction, depression and schizophrenia. After reviewing the major advances in the identification and characterization of this receptor within the central nervous system, this chapter focuses on its functional role in the control of ascending DA pathway activity and on the mechanisms underlying this interaction, by covering electrophysiological, neurochemical and behavioral data mainly from in vivo studies in rats. Afterwards, the therapeutic relevance of 5-HT2BR antagonists for treating DA-dependent neuropsychiatric disorders is discussed by focusing on schizophrenia