The Emergence of Selective 5-HT2B Antagonists Structures, Activities and Potential Therapeutic Applications [General Reviews]
G. Poissonnet, J. G. Parmentier, J. A. Boutin and S. Goldstein
Affiliation: Institut de Recherches SERVIER, 11 rue des Moulineaux 92150 SURESNES - France.
Keywords: receptor, antagonist, serotonin, review
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.
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