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Poissonnet G, Parmentier JG, Boutin JA, Goldstein S: The emergence of selective 5-HT 2B antagonists structures, activities and potential therapeutic applications. Mini Rev Med Chem. 2004 Mar;4(3):325-30.
5-HT (2) receptors mediate a large array of physiological and behavioral functions in humans via three distinct subtypes: 5-HT (2A), 5-HT (2B) and 5-HT (2C). While selective 5-HT (2A) antagonists have been known for some time, knowledge of the precise role played by the 5-HT (2B) receptor was hampered by the existence of solely 5-HT (2B) 5-HT (2C) mixed antagonists. However, selective 5-HT (2B) antagonists began recently to emerge in the literature. Indeed, four structural classes belonging to the piperazine, indole, naphthylpyrimidine and tetrahydro-beta-carboline scaffolds were reported. In this paper, we will briefly review the structural and pharmacological features of selective 5-HT (2B) antagonists, including patent literature of the last five years. |
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