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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
2
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pubmed:dateCreated |
2002-4-2
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pubmed:abstractText |
The biodistribution of radioactivity after the administration of a new tracer for alpha4beta2 nicotinic acetylcholine receptors (nAChRs), [123I]5-iodo-3-[2(S)-2-azetidinylmethoxy]pyridine (5-I-A-85380), was studied in ten healthy human subjects. Following administration of 98+/-6 MBq [123I]5-I-A-85380, serial whole-body images were acquired over 24 h and corrected for attenuation. One to four brain single-photon emission tomography (SPET) images were also acquired between 2.5 and 24 h. Estimates of radiation absorbed dose were calculated using MIRDOSE 3.1 with a dynamic bladder model and a dynamic gastrointestinal tract model. The estimates of the highest absorbed dose (microGy/MBq) were for the urinary bladder wall (71 and 140), lower large intestine wall (70 and 72), and upper large intestine wall (63 and 64), with 2.4-h and 4.8-h urine voiding intervals, respectively. The whole brain activity at the time of the initial whole-body imaging at 14 min was 5.0% of the injected dose. Consistent with the known distribution of alpha4beta2 nAChRs, SPET images showed the highest activity in the thalamus. These results suggest that [123I]5-I-A-85380 is a promising SPET agent to image alpha4beta2 nAChRs in humans, with acceptable dosimetry and high brain uptake.
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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 |
Feb
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pubmed:issn |
1619-7070
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pubmed:author |
pubmed-author:BaldwinRonald MRM,
pubmed-author:BozkurtAliA,
pubmed-author:EarlyMicheleM,
pubmed-author:FujitaMasahiroM,
pubmed-author:HortiAndrew GAG,
pubmed-author:InnisRobert BRB,
pubmed-author:KhanShaukatS,
pubmed-author:KimesAlane SAS,
pubmed-author:KoreNAndrei OAO,
pubmed-author:LondonEdythe DED,
pubmed-author:MukhinAlexey GAG,
pubmed-author:SeibylJohn PJP,
pubmed-author:TamagnanGillesG,
pubmed-author:VaupelD BruceDB,
pubmed-author:ZoghbiSami SSS
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pubmed:issnType |
Print
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pubmed:volume |
29
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
183-90
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pubmed:dateRevised |
2007-11-14
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pubmed:meshHeading |
pubmed-meshheading:11926380-Adult,
pubmed-meshheading:11926380-Azetidines,
pubmed-meshheading:11926380-Brain,
pubmed-meshheading:11926380-Female,
pubmed-meshheading:11926380-Humans,
pubmed-meshheading:11926380-Iodine Radioisotopes,
pubmed-meshheading:11926380-Male,
pubmed-meshheading:11926380-Pyridines,
pubmed-meshheading:11926380-Radiation Dosage,
pubmed-meshheading:11926380-Radiopharmaceuticals,
pubmed-meshheading:11926380-Receptors, Nicotinic,
pubmed-meshheading:11926380-Tissue Distribution,
pubmed-meshheading:11926380-Tomography, Emission-Computed, Single-Photon
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pubmed:year |
2002
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pubmed:articleTitle |
Whole-body biodistribution, radiation absorbed dose, and brain SPET imaging with [123i]5-i-A-85380 in healthy human subjects.
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pubmed:affiliation |
Department of Psychiatry, Yale University School of Medicine and VA Connecticut Healthcare System, VA Connecticut/116A2, West Haven 06516, USA. masahiro.fujita@yale.edu
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pubmed:publicationType |
Journal Article,
Research Support, U.S. Gov't, P.H.S.
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