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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
19
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pubmed:dateCreated |
2007-9-13
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pubmed:abstractText |
2Beta-carbo(2-fluoroethoxy)-3beta-(4'-((Z)-2-iodoethenyl)phenyl)nortropane (betaFEpZIENT, 1) was synthesized as a serotonin transporter (SERT) imaging agent for both positron emission tomography (PET) and single photon emission computerized tomography (SPECT). The binding affinity of 1 to human monoamine transporters showed a high affinity for the SERT (Ki = 0.08 nM) with respect to the dopamine transporter (DAT) (Ki = 13 nM) and the norepinephrine transporter (NET) (Ki = 28 nM). In vivo biodistribution and blocking studies performed in male rats demonstrated that [123I]1 was selective and specific for SERT. In vivo microPET brain imaging studies in an anesthetized monkey with [18F]1 showed high uptake in the diencephalon and brainstem with peak uptake achieved at 120 min. A chase study with (R,S)-citalopram.HBr displaced [18F]1 radioactivity from all SERT-rich brain regions. A chase study with the DAT ligand 2beta-carbophenoxy-3beta-(4-chlorophenyl)tropane (9, RTI-113) failed to displace [18F]1, indicating that [18F]1 is specific to the SERT. The in vivo evaluation of [18F]1 indicates that this radiotracer is a good candidate for mapping and quantifying CNS SERT.
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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 |
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pubmed:status |
MEDLINE
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pubmed:month |
Sep
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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 |
20
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pubmed:volume |
50
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
4553-60
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pubmed:dateRevised |
2007-12-3
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pubmed:meshHeading |
pubmed-meshheading:17705359-Animals,
pubmed-meshheading:17705359-Binding, Competitive,
pubmed-meshheading:17705359-Brain,
pubmed-meshheading:17705359-Cell Line,
pubmed-meshheading:17705359-Dopamine Plasma Membrane Transport Proteins,
pubmed-meshheading:17705359-Fluorine Radioisotopes,
pubmed-meshheading:17705359-Humans,
pubmed-meshheading:17705359-Iodine Radioisotopes,
pubmed-meshheading:17705359-Isotope Labeling,
pubmed-meshheading:17705359-Macaca mulatta,
pubmed-meshheading:17705359-Male,
pubmed-meshheading:17705359-Norepinephrine Plasma Membrane Transport Proteins,
pubmed-meshheading:17705359-Nortropanes,
pubmed-meshheading:17705359-Positron-Emission Tomography,
pubmed-meshheading:17705359-Radiopharmaceuticals,
pubmed-meshheading:17705359-Rats,
pubmed-meshheading:17705359-Rats, Sprague-Dawley,
pubmed-meshheading:17705359-Serotonin Plasma Membrane Transport Proteins,
pubmed-meshheading:17705359-Stereoisomerism,
pubmed-meshheading:17705359-Tissue Distribution,
pubmed-meshheading:17705359-Tomography, Emission-Computed, Single-Photon
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pubmed:year |
2007
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pubmed:articleTitle |
Synthesis and in vivo evaluation of fluorine-18 and iodine-123 labeled 2beta-carbo(2-fluoroethoxy)-3beta-(4'-((Z)-2-iodoethenyl)phenyl)nortropane as a candidate serotonin transporter imaging agent.
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pubmed:affiliation |
Department of Radiology, Emory University, Atlanta, Georgia, USA.
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pubmed:publicationType |
Journal Article,
Research Support, U.S. Gov't, Non-P.H.S.,
Research Support, N.I.H., Extramural
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