title: The potent 5-HT3 receptor antagonist (R)-zacopride labels an additional high affinity site in the central nervous system.
abstract: The binding characteristics of [3H](R)- and [3H](S)-zacopride were investigated in membranes from the rat entorhinal cortex and NG 108-15 clonal cells. In contrast to [3H](S)-zacopride which bound solely to 5-HT3 receptors, [3H](R)-zacopride recognized another class of binding sites, called the (R)-sites, in both membrane preparations. In addition to (R)-zacopride (Ki = 3-11 nM), only (R)-iodo-zacopride, (R)-dechloro-zacopride, prazosin and mianserin exhibited high to moderate affinity for the (R)-sites, whose possible functions remain to be established.
authors.affiliation: INSERM U288, Neurobiologie Cellulaire et Fonctionnelle, Faculté de Médecine Pitié-Salpêtrière, Paris, France.
authors.forename: E
authors.initials: E
authors.lastname: Kidd
authors.forename: I
authors.initials: I
authors.lastname: Bouchelet de Vendegies
authors.forename: J C
authors.initials: JC
authors.lastname: Levy
authors.forename: M
authors.initials: M
authors.lastname: Hamon
authors.forename: H
authors.initials: H
authors.lastname: Gozlan
mesh_terms: D000818:Animals; D001549:Benzamides / Q000494:pharmacology*; D001665:Binding Sites; D001921:Brain / Q000378:metabolism*; D001643:Bridged Bicyclo Compounds / Q000494:pharmacology*; D019086:Bridged Bicyclo Compounds, Heterocyclic; D002462:Cell Membrane / Q000378:metabolism; D002999:Clone Cells; D066298:In Vitro Techniques; D051381:Rats; D012702:Serotonin Antagonists; D014316:Tritium
chemical_list: D001549:Benzamides; D001643:Bridged Bicyclo Compounds; D019086:Bridged Bicyclo Compounds, Heterocyclic; D012702:Serotonin Antagonists; D014316:Tritium; C055971:zacopride