title: The antagonist properties of S 11978 on 5HT3 receptors in N1E-115 neuroblastoma cells.
abstract: The effects of the novel antagonist S 11978 (Endo-7-[(8-methyl-8-azabicyclo[3,2,1]-3-octyl)oxycarbonyl] benzo[b] thiophene) on 5HT3 receptors were examined in N1E-115 mouse neuroblastoma x rat glioma hybrid cells, with radioligand binding and whole cell patch clamp techniques. The 5HT3 receptor ligand [3H] quipazine was displaced by ICS 205-930, GR 38032F and S 11978 with KI values of 2.25 nM, 36.5 nM and 1.75 nM respectively. Electrophysiological studies showed that S 11978 is a potent 5HT3 antagonist: IC50 values for inhibition of 5HT-induced inward current by ICS 205-930, GR 38032F and S 11978 were 0.22 nM, 0.63 nM and 0.43 nM respectively at a holding potential of -65 mV. It is concluded that S 11978 is a potent, high affinity 5HT3 receptor antagonist.
authors.affiliation: Institut de Recherches Servier, Suresnes, France.
authors.forename: P
authors.initials: P
authors.lastname: Morain
authors.forename: C
authors.initials: C
authors.lastname: Abraham
authors.forename: J M
authors.initials: JM
authors.lastname: Lacoste
authors.forename: C
authors.initials: C
authors.lastname: Malen
authors.forename: M
authors.initials: M
authors.lastname: Laubie
authors.forename: E
authors.initials: E
authors.lastname: Giesen-Crouse
mesh_terms: D000818:Animals; D001667:Binding, Competitive; D004594:Electrophysiology; D007211:Indoles / Q000378:metabolism / Q000494:pharmacology; D007700:Kinetics; D051379:Mice; D009447:Neuroblastoma / Q000188:drug therapy / Q000648:ultrastructure*; D017294:Ondansetron / Q000378:metabolism / Q000494:pharmacology; D011814:Quipazine / Q000378:metabolism; D012702:Serotonin Antagonists; D013876:Thiophenes / Q000494:pharmacology*; D014316:Tritium; D000077526:Tropisetron; D014407:Tumor Cells, Cultured / Q000187:drug effects
chemical_list: D007211:Indoles; C083093:S 11978; D012702:Serotonin Antagonists; D013876:Thiophenes; D014316:Tritium; D017294:Ondansetron; D011814:Quipazine; D000077526:Tropisetron