title: Dopamine D(3) receptor antagonists: The quest for a potentially selective PET ligand. Part two: Lead optimization.
abstract: The lead optimization process to identify new selective dopamine D(3) receptor antagonists is reported. DMPK parameters and binding data suggest that selective D(3) receptor antagonists as potential PET ligands might have been identified.
authors: GlaxoSmithKline, Neurosciences Centre of Excellence for Drug Discovery, Medicine Research Centre, Verona, Italy. fm20244@gsk.com
authors: Fabrizio
authors: F
authors: Micheli
authors: Ian
authors: I
authors: Holmes
authors: Luca
authors: L
authors: Arista
authors: Giorgio
authors: G
authors: Bonanomi
authors: Simone
authors: S
authors: Braggio
authors: Francesca
authors: F
authors: Cardullo
authors: Romano
authors: R
authors: Di Fabio
authors: Daniele
authors: D
authors: Donati
authors: Gabriella
authors: G
authors: Gentile
authors: Dieter
authors: D
authors: Hamprecht
authors: Silvia
authors: S
authors: Terreni
authors: Christian
authors: C
authors: Heidbreder
authors: Chiara
authors: C
authors: Savoia
authors: Cristiana
authors: C
authors: Griffante
authors: Angela
authors: A
authors: Worby
mesh_terms: D000818:Animals; D001921:Brain / Q000187:drug effects; D002625:Chemistry, Organic / Q000379:methods; D002626:Chemistry, Pharmaceutical / Q000379:methods; D065127:Dopamine D2 Receptor Antagonists; D006801:Humans; D048289:Imidazolidines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D020128:Inhibitory Concentration 50; D008024:Ligands; D008956:Models, Chemical; D049268:Positron-Emission Tomography; D051381:Rats; D017448:Receptors, Dopamine D2 / Q000378:metabolism; D050637:Receptors, Dopamine D3 / Q000037:antagonists & inhibitors* / Q000378:metabolism; D013329:Structure-Activity Relationship; D013552:Swine
chemical_list: D065127:Dopamine D2 Receptor Antagonists; D048289:Imidazolidines; D008024:Ligands; D017448:Receptors, Dopamine D2; D050637:Receptors, Dopamine D3