Chlorophenylpiperazine analogues as high affinity dopamine transporter ligands
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 discovere...
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| Veröffentlicht in: | Bioorganic & medicinal chemistry letters 2013-12, Vol.23 (24), p.6920-6922 |
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| container_end_page | 6922 |
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| container_issue | 24 |
| container_start_page | 6920 |
| container_title | Bioorganic & medicinal chemistry letters |
| container_volume | 23 |
| creator | Motel, William C. Healy, Jason R. Viard, Eddy Pouw, Buddy Martin, Kelly E. Matsumoto, Rae R. Coop, Andrew |
| description | 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. |
| doi_str_mv | 10.1016/j.bmcl.2013.09.038 |
| format | Article |
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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.</description><identifier>ISSN: 0960-894X</identifier><identifier>EISSN: 1464-3405</identifier><identifier>DOI: 10.1016/j.bmcl.2013.09.038</identifier><identifier>PMID: 24211020</identifier><language>eng</language><publisher>England: Elsevier Ltd</publisher><subject>chemistry ; Cocaine ; dopamine ; Dopamine Plasma Membrane Transport Proteins - chemistry ; Dopamine Plasma Membrane Transport Proteins - metabolism ; Dopamine transporter ; Ligands ; Methamphetamine ; Neurotransmitter ; Norepinephrine Plasma Membrane Transport Proteins - chemistry ; Norepinephrine Plasma Membrane Transport Proteins - metabolism ; piperazines ; Piperazines - chemistry ; Piperazines - metabolism ; Protein Binding ; Receptors, sigma - chemistry ; Receptors, sigma - metabolism ; Serotonin Plasma Membrane Transport Proteins - chemistry ; Serotonin Plasma Membrane Transport Proteins - metabolism ; Sigma receptor ; Structure-Activity Relationship ; Structure–activity relationships ; transporters</subject><ispartof>Bioorganic & medicinal chemistry letters, 2013-12, Vol.23 (24), p.6920-6922</ispartof><rights>2013 Elsevier Ltd</rights><rights>Copyright © 2013 Elsevier Ltd. 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| fulltext | fulltext |
| identifier | ISSN: 0960-894X |
| ispartof | Bioorganic & medicinal chemistry letters, 2013-12, Vol.23 (24), p.6920-6922 |
| issn | 0960-894X 1464-3405 |
| language | eng |
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| source | MEDLINE; Elsevier ScienceDirect Journals |
| subjects | chemistry Cocaine dopamine Dopamine Plasma Membrane Transport Proteins - chemistry Dopamine Plasma Membrane Transport Proteins - metabolism Dopamine transporter Ligands Methamphetamine Neurotransmitter Norepinephrine Plasma Membrane Transport Proteins - chemistry Norepinephrine Plasma Membrane Transport Proteins - metabolism piperazines Piperazines - chemistry Piperazines - metabolism Protein Binding Receptors, sigma - chemistry Receptors, sigma - metabolism Serotonin Plasma Membrane Transport Proteins - chemistry Serotonin Plasma Membrane Transport Proteins - metabolism Sigma receptor Structure-Activity Relationship Structure–activity relationships transporters |
| title | Chlorophenylpiperazine analogues as high affinity dopamine transporter ligands |
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