The emergence of selective 5-HT 2B antagonists structures, activities and potential therapeutic applications
G Poissonnet1, J G Parmentier, J A Boutin
1Institut de Recherches SERVIER - 11 rue des Moulineaux -92150 Suresnes, France. solo.goldstein@fr.netgrs.com
Abstract:
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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