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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
1
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pubmed:dateCreated |
1987-2-24
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pubmed:abstractText |
As part of our program in radiopharmaceutical chemistry we have prepared and evaluated a series of radioiodinated 1-alkyl-4-phenylpiperazines as potential brain-imaging agents. The compounds were chosen on the basis of their synthetic versatility, activation toward electrophilic substitution, and ease of purification. The intermediates 1-6 were readily obtained and converted to the corresponding radioiodinated products 7-12 in 76-91% isolated radiochemical yields. The tissue distribution in rats indicated that the 1-N-butyl derivative 9 possesses the best combination of brain uptake (0.28-0.35% ID X kg/g), retention, and selectivity (brain/blood greater than 20) over the 4-h evaluation period. A subsequent imaging and tissue distribution study in the dog using 131I-labeled 9 supported the results observed in the rat and suggested the potential of this agent as a brain-imaging agent.
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pubmed:grant | |
pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical | |
pubmed:status |
MEDLINE
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pubmed:month |
Jan
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pubmed:issn |
0022-2623
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
30
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
29-34
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pubmed:dateRevised |
2007-11-14
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pubmed:meshHeading |
pubmed-meshheading:3806601-Animals,
pubmed-meshheading:3806601-Blood-Brain Barrier,
pubmed-meshheading:3806601-Brain,
pubmed-meshheading:3806601-Dogs,
pubmed-meshheading:3806601-Female,
pubmed-meshheading:3806601-Indicators and Reagents,
pubmed-meshheading:3806601-Iodine Radioisotopes,
pubmed-meshheading:3806601-Male,
pubmed-meshheading:3806601-Piperazines,
pubmed-meshheading:3806601-Rats,
pubmed-meshheading:3806601-Rats, Inbred Strains,
pubmed-meshheading:3806601-Structure-Activity Relationship,
pubmed-meshheading:3806601-Tissue Distribution
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pubmed:year |
1987
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pubmed:articleTitle |
Phenylpiperazine-based radiopharmaceuticals for brain imaging. 3. Synthesis and evaluation of radioiodinated 1-alkyl-4-phenylpiperazines.
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pubmed:publicationType |
Journal Article,
Comparative Study,
Research Support, U.S. Gov't, P.H.S.,
Research Support, Non-U.S. Gov't
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