title: New spiro-piperidines as 5-HT2B receptor antagonists.
abstract: A functional screening highlighted a series of spiro-piperidines as 5-HT2B receptor antagonists. Preliminary structure-activity relationship has been explored driving to potent antagonists (IC50 = 1 nM) and indicating directions for further explorations.
authors.affiliation: Urogene, Hopital Saint-Louis, 1 Avenue Claude Vellefaux, 75010 Paris, France.
authors.forename: Hugues
authors.initials: H
authors.lastname: Bienaymé
authors.forename: Laurent
authors.initials: L
authors.lastname: Chêne
authors.forename: Serge
authors.initials: S
authors.lastname: Grisoni
authors.forename: Antonio
authors.initials: A
authors.lastname: Grondin
authors.forename: El-Bachir
authors.initials: el-B
authors.lastname: Kaloun
authors.forename: Stéphane
authors.initials: S
authors.lastname: Poigny
authors.forename: Houcine
authors.initials: H
authors.lastname: Rahali
authors.forename: Eric
authors.initials: E
authors.lastname: Tam
mesh_terms: D020128:Inhibitory Concentration 50; D008024:Ligands; D015394:Molecular Structure; D010880:Piperidines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D044403:Receptor, Serotonin, 5-HT2B / Q000378:metabolism; D058830:Serotonin 5-HT2 Receptor Antagonists; D013329:Structure-Activity Relationship
chemical_list: D008024:Ligands; D010880:Piperidines; D044403:Receptor, Serotonin, 5-HT2B; D058830:Serotonin 5-HT2 Receptor Antagonists