title: N-arylalkylpiperidines as high-affinity sigma-1 and sigma-2 receptor ligands: phenylpropylamines as potential leads for selective sigma-2 agents.
abstract: To delineate the differences between the structural requirements necessary for recognition at sigma-1 and sigma-2 receptors, a range of phenethyl- and phenylpropylpiperidines were evaluated in binding assays. Phenethylpiperidines were found to favor sigma-1 receptors, whereas phenylpropylpiperidines tend to favor sigma-2 receptors. It appears that phenylpropylamine is a potential pharmacophore for selective sigma-2 ligands.
authors.affiliation: Department of Pharmaceutical Sciences, University of Maryland School of Pharmacy, 20 North Pine Street, Baltimore, MD 21201, USA.
authors.forename: Dean Y
authors.initials: DY
authors.lastname: Maeda
authors.forename: Wanda
authors.initials: W
authors.lastname: Williams
authors.forename: Wes E
authors.initials: WE
authors.lastname: Kim
authors.forename: Linn N
authors.initials: LN
authors.lastname: Thatcher
authors.forename: Wayne D
authors.initials: WD
authors.lastname: Bowen
authors.forename: Andrew
authors.initials: A
authors.lastname: Coop
mesh_terms: D014150:Antipsychotic Agents / Q000138:chemical synthesis; D001667:Binding, Competitive / Q000187:drug effects; D008024:Ligands; D010880:Piperidines / Q000138:chemical synthesis* / Q000494:pharmacology*; D011437:Propylamines / Q000737:chemistry*; D011725:Pyridines / Q000138:chemical synthesis* / Q000494:pharmacology*; D017480:Receptors, sigma / Q000187:drug effects*; D013329:Structure-Activity Relationship; D000097605:Sigma-1 Receptor
chemical_list: D014150:Antipsychotic Agents; D008024:Ligands; D010880:Piperidines; D011437:Propylamines; D011725:Pyridines; D017480:Receptors, sigma; D000097605:Sigma-1 Receptor; C106107:sigma-2 receptor