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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
3
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pubmed:dateCreated |
1989-4-6
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pubmed:abstractText |
The iodinated analogue of 1-[2-(4-aminophenyl)ethyl]-4-[3-(trifluoromethyl)phenyl]piperazine (PAPP), IPAPP (4), and the corresponding azido compound azido-IPAPP (5) were synthesized. The corresponding no-carrier-added 125I (T1/2 = 60 days, 35-60 keV) labeled compounds were also prepared. High specific binding was observed from in vitro binding studies using rat brain tissue preparation; Ki = 20 and 17.5 nM against [3H]-5-HT. In vivo biodistribution studies in rats showed that azido-[125I]IPAPP passed through intact blood-brain barrier and localized in the brain. Ex vivo autoradiography of rat brain sections exhibited a diffuse uptake pattern, which may be due to specific and nonspecific binding. The results indicate that IPAPP and azido-IPAPP may not be suitable to image the serotonin receptor in the brain.
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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 |
Mar
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pubmed:issn |
0022-2623
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
32
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
543-7
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:2918500-Animals,
pubmed-meshheading:2918500-Autoradiography,
pubmed-meshheading:2918500-Azides,
pubmed-meshheading:2918500-Binding, Competitive,
pubmed-meshheading:2918500-Brain,
pubmed-meshheading:2918500-Cattle,
pubmed-meshheading:2918500-Iodine Radioisotopes,
pubmed-meshheading:2918500-Isotope Labeling,
pubmed-meshheading:2918500-Male,
pubmed-meshheading:2918500-Piperazines,
pubmed-meshheading:2918500-Rats,
pubmed-meshheading:2918500-Rats, Inbred Strains,
pubmed-meshheading:2918500-Receptors, Serotonin,
pubmed-meshheading:2918500-Tissue Distribution
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pubmed:year |
1989
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pubmed:articleTitle |
Preparation and biodistribution of 1-[2-(3-[125I]iodo-4-aminophenyl)ethyl]-4-[3-(trifluoromethyl) phenyl]piperazine and 1-[2-(3-[125I]iodo-4-azidophenyl)ethyl]-4-[3-(trifluoromethyl)phenyl] piperazine.
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pubmed:affiliation |
Department of Radiology, University of Pennsylvania, Philadelphia 19104.
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pubmed:publicationType |
Journal Article,
In Vitro
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