title: Haloperidol: towards further understanding of the structural contributions of its pharmacophoric elements at D2-like receptors.
abstract: An attempt to understand the pharmacophore-relevant position of the alcoholic moiety in haloperidol and the contributions of other pharmacophoric elements led to the re-synthesis of its tropane analogue (compound 2). An analysis of the binding data suggests that haloperidol binds to the DA receptors with the OH group in the axial position and the OH group, while not essential for binding, enhances binding especially at the D2 receptor. It also became clear that shortening the butyrophenone chain not only reduces binding affinity at the DA receptors but eliminates subtype selectivity.
authors.affiliation: College of Pharmacy and Pharmaceutical Sciences, Florida A & M University, Tallahassee, FL 32307, USA.
authors.forename: Donald M N
authors.initials: DM
authors.lastname: Sikazwe
authors.forename: Shouming
authors.initials: S
authors.lastname: Li
authors.forename: Leroy
authors.initials: L
authors.lastname: Mardenborough
authors.forename: Vivian
authors.initials: V
authors.lastname: Cody
authors.forename: Brian L
authors.initials: BL
authors.lastname: Roth
authors.forename: Seth Y
authors.initials: SY
authors.lastname: Ablordeppey
mesh_terms: D006220:Haloperidol / Q000737:chemistry* / Q000378:metabolism*; D015394:Molecular Structure; D011485:Protein Binding / Q000502:physiology; D017448:Receptors, Dopamine D2 / Q000378:metabolism*; D013329:Structure-Activity Relationship
chemical_list: D017448:Receptors, Dopamine D2; D006220:Haloperidol