5-HT2 receptors mediate a large array of physiological and behavioral functions in humans via three distinct subtypes: 5-HT2A, 5-HT2B and 5-HT2C. While selective 5-HT2A antagonists have been known for some time, knowledge of the precise role played by the 5-HT2B receptor was hampered by the existence of solely 5- HT2B / 5-HT2C mixed antagonists. However, selective 5-HT2B antagonists began recently to emerge in the literature. Indeed, four structural classes belonging to the piperazine, indole, naphthylpyrimidine and tetrahydro-β-carboline scaffolds were reported. In this paper, we will briefly review the structural and pharmacological features of selective 5-HT2B antagonists, including patent literature of the last five years.