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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
3
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pubmed:dateCreated |
2003-2-4
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pubmed:abstractText |
A series of optically pure phenyl-and non-phenyl-substituted 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(2-hydroxypropyl)piperazines was synthesized and their binding affinity for dopamine transporter (DAT) was investigated. The analogues with a hydroxyl group in the S configuration were more selective for the DAT over the serotonin transporter (SERT) than the corresponding R enantiomers. Compound (+)-11 showed high affinity and selectivity for DAT over the SERT and, therefore, is a potential candidate for the development of a long-acting cocaine abuse therapeutic agent.
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
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pubmed:status |
MEDLINE
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pubmed:month |
Feb
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pubmed:issn |
0960-894X
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pubmed:author |
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pubmed:issnType |
Print
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pubmed:day |
10
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pubmed:volume |
13
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
553-6
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:12565970-Animals,
pubmed-meshheading:12565970-Cocaine,
pubmed-meshheading:12565970-Cocaine-Related Disorders,
pubmed-meshheading:12565970-Conditioning, Operant,
pubmed-meshheading:12565970-Dopamine Plasma Membrane Transport Proteins,
pubmed-meshheading:12565970-Dopamine Uptake Inhibitors,
pubmed-meshheading:12565970-Ligands,
pubmed-meshheading:12565970-Macaca mulatta,
pubmed-meshheading:12565970-Membrane Glycoproteins,
pubmed-meshheading:12565970-Membrane Transport Proteins,
pubmed-meshheading:12565970-Nerve Tissue Proteins,
pubmed-meshheading:12565970-Piperazines,
pubmed-meshheading:12565970-Protein Binding,
pubmed-meshheading:12565970-Stereoisomerism,
pubmed-meshheading:12565970-Structure-Activity Relationship
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pubmed:year |
2003
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pubmed:articleTitle |
Synthesis and dopamine transporter affinity of chiral 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(2-hydroxypropyl)piperazines as potential cocaine abuse therapeutic agents.
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pubmed:affiliation |
Laboratory of Medicinal Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, MD 20892, USA.
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pubmed:publicationType |
Journal Article,
Research Support, U.S. Gov't, P.H.S.
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