title: Chlorophenylpiperazine analogues as high affinity dopamine transporter ligands.
abstract: Selective σ2 ligands continue to be an active target for medications to attenuate the effects of psychostimulants. In the course of our studies to determine the optimal substituents in the σ2-selective phenyl piperazines analogues with reduced activity at other neurotransmitter systems, we discovered that 1-(3-chlorophenyl)-4-phenethylpiperazine actually had preferentially increased affinity for dopamine transporters (DAT), yielding a highly selective DAT ligand.
authors.affiliation: Department of Pharmaceutical Sciences, University of Maryland, School of Pharmacy, 20 North Pine Street, Baltimore, MD, 21201, USA.
authors.forename: William C
authors.initials: WC
authors.lastname: Motel
authors.affiliation: Department of Basic Pharmaceutical Sciences, West Virginia University, School of Pharmacy, One Medical Center Drive, Morgantown, WV, 26506, USA.
authors.forename: Jason R
authors.initials: JR
authors.lastname: Healy
authors.affiliation: Department of Basic Pharmaceutical Sciences, West Virginia University, School of Pharmacy, One Medical Center Drive, Morgantown, WV, 26506, USA.
authors.forename: Eddy
authors.initials: E
authors.lastname: Viard
authors.affiliation: Department of Pharmaceutical Sciences, University of Oklahoma Health Sciences Center, College of Pharmacy, Oklahoma City, OK, 73190, USA.
authors.forename: Buddy
authors.initials: B
authors.lastname: Pouw
authors.affiliation: Department of Pharmaceutical Sciences, University of Maryland, School of Pharmacy, 20 North Pine Street, Baltimore, MD, 21201, USA.
authors.forename: Kelly
authors.initials: K
authors.lastname: Martin
authors.affiliation: Department of Basic Pharmaceutical Sciences, West Virginia University, School of Pharmacy, One Medical Center Drive, Morgantown, WV, 26506, USA.|Department of Pharmaceutical Sciences, University of Oklahoma Health Sciences Center, College of Pharmacy, Oklahoma City, OK, 73190, USA.
authors.forename: Rae R
authors.initials: RR
authors.lastname: Matsumoto
authors.affiliation: Department of Pharmaceutical Sciences, University of Maryland, School of Pharmacy, 20 North Pine Street, Baltimore, MD, 21201, USA.
authors.forename: Andrew
authors.initials: A
authors.lastname: Coop
mesh_terms: D050483:Dopamine Plasma Membrane Transport Proteins / Q000737:chemistry* / Q000378:metabolism; D008024:Ligands; D050484:Norepinephrine Plasma Membrane Transport Proteins / Q000737:chemistry / Q000378:metabolism; D010879:Piperazines / Q000737:chemistry* / Q000378:metabolism; D011485:Protein Binding; D017480:Receptors, sigma / Q000737:chemistry / Q000378:metabolism; D050486:Serotonin Plasma Membrane Transport Proteins / Q000737:chemistry / Q000378:metabolism; D013329:Structure-Activity Relationship
chemical_list: D050483:Dopamine Plasma Membrane Transport Proteins; D008024:Ligands; D050484:Norepinephrine Plasma Membrane Transport Proteins; D010879:Piperazines; D017480:Receptors, sigma; D050486:Serotonin Plasma Membrane Transport Proteins; C031503:phenylpiperazine
keywords: Cocaine; Dopamine transporter; Methamphetamine; Neurotransmitter; Sigma receptor; Structure–activity relationships