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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
23
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pubmed:dateCreated |
1994-1-6
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pubmed:abstractText |
Two series of (N-benzylpiperidin-4-yl)- and (9-azabicyclo[3.3.1]nonan- 3 beta-yl)benzamides were prepared, and in vitro binding assays were used to measure the affinity of these compounds for dopamine D2, dopamine D3, serotonin 5-HT2, and alpha 2-adrenergic receptors. The results of these studies indicated compounds 23, 26b, and 34 have the selectivity needed for in vivo studies of the D2 (and possibly D3) receptors. 18F-Labeled analogues of 23, 26b and 34 were prepared by N-alkylation of the corresponding desbenzyl precursors with [18F]-4-fluorobenzyl iodide. Preliminary in vivo studies demonstrated that [18F]-23 and [18F]-26b are suitable candidates for further evaluation in positron emission tomography imaging studies. The slow rate of washout of [18F]-34 from nondopaminergic regions and its comparatively high lipophilicity indicates that this compound may not be suitable for imaging studies because of a high level of nonspecific binding.
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pubmed:grant |
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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 |
http://linkedlifedata.com/resource/pubmed/chemical/Benzamides,
http://linkedlifedata.com/resource/pubmed/chemical/Bicyclo Compounds,
http://linkedlifedata.com/resource/pubmed/chemical/Bicyclo Compounds, Heterocyclic,
http://linkedlifedata.com/resource/pubmed/chemical/Drd3 protein, rat,
http://linkedlifedata.com/resource/pubmed/chemical/Fluorine Radioisotopes,
http://linkedlifedata.com/resource/pubmed/chemical/Piperidines,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Adrenergic, alpha,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Dopamine,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Dopamine D2,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Dopamine D3,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Serotonin,
http://linkedlifedata.com/resource/pubmed/chemical/Recombinant Proteins
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pubmed:status |
MEDLINE
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pubmed:month |
Nov
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pubmed:issn |
0022-2623
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pubmed:author |
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pubmed:issnType |
Print
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pubmed:day |
12
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pubmed:volume |
36
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pubmed:owner |
NLM
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pubmed:authorsComplete |
N
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pubmed:pagination |
3707-20
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pubmed:dateRevised |
2007-11-14
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pubmed:meshHeading |
pubmed-meshheading:8246241-Animals,
pubmed-meshheading:8246241-Baculoviridae,
pubmed-meshheading:8246241-Benzamides,
pubmed-meshheading:8246241-Bicyclo Compounds,
pubmed-meshheading:8246241-Bicyclo Compounds, Heterocyclic,
pubmed-meshheading:8246241-Fluorine Radioisotopes,
pubmed-meshheading:8246241-Molecular Structure,
pubmed-meshheading:8246241-Moths,
pubmed-meshheading:8246241-Piperidines,
pubmed-meshheading:8246241-Pituitary Neoplasms,
pubmed-meshheading:8246241-Rats,
pubmed-meshheading:8246241-Rats, Sprague-Dawley,
pubmed-meshheading:8246241-Receptors, Adrenergic, alpha,
pubmed-meshheading:8246241-Receptors, Dopamine,
pubmed-meshheading:8246241-Receptors, Dopamine D2,
pubmed-meshheading:8246241-Receptors, Dopamine D3,
pubmed-meshheading:8246241-Receptors, Serotonin,
pubmed-meshheading:8246241-Recombinant Proteins,
pubmed-meshheading:8246241-Structure-Activity Relationship,
pubmed-meshheading:8246241-Tomography, Emission-Computed,
pubmed-meshheading:8246241-Tumor Cells, Cultured
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pubmed:year |
1993
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pubmed:articleTitle |
18F-labeled benzamides for studying the dopamine D2 receptor with positron emission tomography.
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pubmed:affiliation |
Cerebrovascular Research Center, University of Pennsylvania, Philadelphia 19104.
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pubmed:publicationType |
Journal Article,
Research Support, U.S. Gov't, P.H.S.
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