title: Novel sulfonamides having dual dopamine D2 and D3 receptor affinity show in vivo antipsychotic efficacy with beneficial cognitive and EPS profile.
abstract: A novel series of arylsulfonamides was prepared either by automated parallel or by traditional solution-phase synthesis. Several members of this compound library were identified as high-affinity dopamine D3 and D2 receptor ligands. The most interesting representative, compound 2, showed potent antipsychotic behaviour coupled with a beneficial cognitive and EPS profile.
authors.affiliation: Gedeon Richter Ltd, Budapest, 10. PO Box 27, H-1475, Hungary. e.csongor@richter.hu
authors.forename: Eva
authors.initials: E
authors.lastname: Agai-Csongor
authors.forename: Katalin
authors.initials: K
authors.lastname: Nógrádi
authors.forename: János
authors.initials: J
authors.lastname: Galambos
authors.forename: István
authors.initials: I
authors.lastname: Vágó
authors.forename: Attila
authors.initials: A
authors.lastname: Bielik
authors.forename: Ildikó
authors.initials: I
authors.lastname: Magdó
authors.forename: Györgyi
authors.initials: G
authors.lastname: Ignácz-Szendrei
authors.forename: György Miklós
authors.initials: GM
authors.lastname: Keseru
authors.forename: István
authors.initials: I
authors.lastname: Greiner
authors.forename: István
authors.initials: I
authors.lastname: Laszlovszky
authors.forename: Eva
authors.initials: E
authors.lastname: Schmidt
authors.forename: Béla
authors.initials: B
authors.lastname: Kiss
authors.forename: Katalin
authors.initials: K
authors.lastname: Sághy
authors.forename: Judit
authors.initials: J
authors.lastname: Laszy
authors.forename: István
authors.initials: I
authors.lastname: Gyertyán
authors.forename: Mária
authors.initials: M
authors.lastname: Zájer-Balázs
authors.forename: Larisza
authors.initials: L
authors.lastname: Gémesi
authors.forename: György
authors.initials: G
authors.lastname: Domány
mesh_terms: D000818:Animals; D014150:Antipsychotic Agents / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology*; D001058:Apomorphine / Q000494:pharmacology; D001362:Avoidance Learning / Q000187:drug effects; D001667:Binding, Competitive / Q000187:drug effects; D001682:Biological Availability; D001921:Brain / Q000378:metabolism; D002375:Catalepsy / Q000139:chemically induced; D003071:Cognition / Q000187:drug effects*; D006801:Humans; D007202:Indicators and Reagents; D008297:Male; D018782:Maze Learning / Q000187:drug effects; D008569:Memory Disorders / Q000139:chemically induced; D021281:Quantitative Structure-Activity Relationship; D051381:Rats; D017208:Rats, Wistar; D017448:Receptors, Dopamine D2 / Q000378:metabolism*; D050637:Receptors, Dopamine D3 / Q000378:metabolism*; D013239:Stereotyped Behavior / Q000187:drug effects; D013449:Sulfonamides / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology*
chemical_list: D014150:Antipsychotic Agents; D007202:Indicators and Reagents; D017448:Receptors, Dopamine D2; D050637:Receptors, Dopamine D3; D013449:Sulfonamides; D001058:Apomorphine