The emergence of selective 5-HT 2B antagonists structures, activities and potential therapeutic applications.
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.
Poissonnet
G
G
Institut de Recherches SERVIER - 11 rue des Moulineaux -92150 Suresnes, France. solo.goldstein@fr.netgrs.com
Parmentier
J G
JG
Boutin
J A
JA
Goldstein
S
S
D000818:Animals; D001667:Binding, Competitive; D015195:Drug Design; D006801:Humans; D043183:Irritable Bowel Syndrome / Q000188:drug therapy / Q000378:metabolism; D008024:Ligands; D008881:Migraine Disorders / Q000188:drug therapy / Q000378:metabolism; D015394:Molecular Structure; D058830:Serotonin 5-HT2 Receptor Antagonists; D012702:Serotonin Antagonists / Q000737:chemistry / Q000627:therapeutic use*
D008024:Ligands; D058830:Serotonin 5-HT2 Receptor Antagonists; D012702:Serotonin Antagonists