title: The 5-HT3 antagonist tropisetron (ICS 205-930) is a potent and selective alpha7 nicotinic receptor partial agonist.
abstract: The 5-HT3 receptor antagonist tropisetron (ICS 205-930) was found to be a potent and selective partial agonist at alpha7 nicotinic receptors. Two other 5-HT3 receptor antagonists, ondansetron and LY-278,584, were found to lack high affinity at the alpha7 nicotinic receptor. Quinuclidine analogues (1 and 2) of tropisetron were also found to be potent and selective partial agonists at alpha7 nicotinic receptors.
authors.affiliation: AstraZeneca, Three Biotech, Worcester, MA 01605, USA. john.macor@bms.com
authors.forename: J E
authors.initials: JE
authors.lastname: Macor
authors.forename: D
authors.initials: D
authors.lastname: Gurley
authors.forename: T
authors.initials: T
authors.lastname: Lanthorn
authors.forename: J
authors.initials: J
authors.lastname: Loch
authors.forename: R A
authors.initials: RA
authors.lastname: Mack
authors.forename: G
authors.initials: G
authors.lastname: Mullen
authors.forename: O
authors.initials: O
authors.lastname: Tran
authors.forename: N
authors.initials: N
authors.lastname: Wright
authors.forename: J C
authors.initials: JC
authors.lastname: Gordon
mesh_terms: D000818:Animals; D002462:Cell Membrane / Q000737:chemistry; D006624:Hippocampus / Q000648:ultrastructure; D007211:Indoles / Q000494:pharmacology*; D020128:Inhibitory Concentration 50; D007421:Intestine, Small / Q000648:ultrastructure; D008024:Ligands; D008564:Membrane Potentials / Q000187:drug effects; D051379:Mice; D018722:Nicotinic Agonists / Q000494:pharmacology*; D009865:Oocytes / Q000187:drug effects / Q000502:physiology; D011485:Protein Binding; D051381:Rats; D011978:Receptors, Nicotinic / Q000187:drug effects* / Q000378:metabolism; D012702:Serotonin Antagonists / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D000077526:Tropisetron; D014981:Xenopus; D064569:alpha7 Nicotinic Acetylcholine Receptor
chemical_list: C579166:Chrna7 protein, mouse; C579165:Chrna7 protein, rat; D007211:Indoles; D008024:Ligands; D018722:Nicotinic Agonists; D011978:Receptors, Nicotinic; D012702:Serotonin Antagonists; D064569:alpha7 Nicotinic Acetylcholine Receptor; D000077526:Tropisetron