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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
5
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pubmed:dateCreated |
1992-10-26
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pubmed:abstractText |
A new PET radiotracer for in vivo labeling of serotonin (5-HT) uptake sites, cis-N,N-[11C]dimethyl-3-(2',4'-dichlorophenyl)-indanamine, cis-[11C]DDPI, was synthesized and its biological behavior was studied. The radiosynthesis of cis-[11C]DDPI was performed by N-methylation of cis-N-methyl-3-(2',4'-dichlorophenyl)-indanamine with [11C]iodomethane. The average radiochemical yield was approx. 8%, with an average specific activity of 600 mCi/mumol. Following intravenous administration, cis-[11C]DDPI accumulated in mouse brain regions rich in 5-HT uptake sites, such as olfactory tubercles, hypothalamus and frontal cortex. Following pre-injection of 1 mg/kg of paroxetine, a high affinity 5-HT uptake blocker, the binding of cis-[11C]DDPI in the olfactory tubercles, hypothalamus and frontal cortex was decreased by 23, 25 and 16%; this corresponds to 73, 82 and 59% of the specific binding in these regions. These results suggest that the accumulation of cis-[11C]DDPI in the tissues rich in 5-HT sites is a result of specific binding of cis-[11C]DDPI to 5-HT uptake sites. Due to the relatively high non-specific uptake and slow clearance of this compound from non-specific binding sites, the ratio between specific and non-specific binding increased slowly with time, reaching 1.5:1 at 60 min after injection.
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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 |
Jul
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pubmed:issn |
0883-2897
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
19
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
549-53
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pubmed:dateRevised |
2008-2-21
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pubmed:meshHeading |
pubmed-meshheading:1399685-Animals,
pubmed-meshheading:1399685-Binding Sites,
pubmed-meshheading:1399685-Brain,
pubmed-meshheading:1399685-Carbon Radioisotopes,
pubmed-meshheading:1399685-Indans,
pubmed-meshheading:1399685-Isotope Labeling,
pubmed-meshheading:1399685-Mice,
pubmed-meshheading:1399685-Receptors, Serotonin,
pubmed-meshheading:1399685-Serotonin,
pubmed-meshheading:1399685-Tissue Distribution,
pubmed-meshheading:1399685-Tomography, Emission-Computed
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pubmed:year |
1992
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pubmed:articleTitle |
Synthesis and biodistribution of a new radiotracer for in vivo labeling of serotonin uptake sites by PET, cis-N,N-[11C]dimethyl-3-(2',4'-dichlorophenyl)-indanamine (cis-[11C]DDPI).
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pubmed:affiliation |
Division of Nuclear Medicine and Radiation Health Sciences, Johns Hopkins Medical Institutions, Baltimore, MD 21205.
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pubmed:publicationType |
Journal Article,
Research Support, U.S. Gov't, P.H.S.
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