title: Analogues of the dopamine D2 receptor antagonist L741,626: Binding, function, and SAR.
abstract: A series of analogues of the dopamine D2 receptor antagonist L741,626 were synthesized and evaluated for binding and function at D2 family receptor subtypes. Several analogues showed comparable binding profiles to the parent ligand, however, in general, chemical modification served to reduce D2 binding affinity and selectivity.
authors.affiliation: Medicinal Chemistry, National Institute on Drug Abuse-Intramural Research Program, National Institutes of Health, 5500 Nathan Shock Drive, Baltimore, MD 21224, USA.
authors.forename: Peter
authors.initials: P
authors.lastname: Grundt
authors.forename: Sarah Little Jane
authors.initials: SL
authors.lastname: Husband
authors.forename: Robert R
authors.initials: RR
authors.lastname: Luedtke
authors.forename: Michelle
authors.initials: M
authors.lastname: Taylor
authors.forename: Amy Hauck
authors.initials: AH
authors.lastname: Newman
mesh_terms: D002460:Cell Line; D018492:Dopamine Antagonists / Q000138:chemical synthesis* / Q000494:pharmacology*; D006801:Humans; D007211:Indoles / Q000138:chemical synthesis* / Q000494:pharmacology*; D008024:Ligands; D010880:Piperidines / Q000138:chemical synthesis* / Q000494:pharmacology*; D011485:Protein Binding; D017448:Receptors, Dopamine D2 / Q000187:drug effects* / Q000235:genetics; D013329:Structure-Activity Relationship; D014162:Transfection
chemical_list: D018492:Dopamine Antagonists; D007211:Indoles; D008024:Ligands; D010880:Piperidines; D017448:Receptors, Dopamine D2; C104750:3-(4-(4-chlorophenyl-4-hydroxypiperidino)methyl)indole