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Chlorophenylpiperazine analogues as high affinity dopamine transporter ligands |
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| Authors: | William C. Motel Jason R. Healy Eddy Viard Buddy Pouw Kelly E. Martin Rae R. Matsumoto Andrew Coop |
| Affiliation: | 1. Department of Pharmaceutical Sciences, University of Maryland, School of Pharmacy, 20 North Pine Street, Baltimore, MD 21201, USA;2. Department of Basic Pharmaceutical Sciences, West Virginia University, School of Pharmacy, One Medical Center Drive, Morgantown, WV 26506, USA;3. Department of Pharmaceutical Sciences, University of Oklahoma Health Sciences Center, College of Pharmacy, Oklahoma City, OK 73190, USA;4. Carolinas Medical Center, Department of Pharmacy, 1000 Blythe Boulevard, Charlotte, NC 28203, USA |
| 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. |
| Keywords: | Sigma receptor Dopamine transporter Structure–activity relationships Neurotransmitter Cocaine Methamphetamine |
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