Abstract:
: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.
journal_name
Eur J Nucl Med Mol Imagingauthors
Fujita M,Seibyl JP,Vaupel DB,Tamagnan G,Early M,Zoghbi SS,Baldwin RM,Horti AG,KoreN AO,Mukhin AG,Khan S,Bozkurt A,Kimes AS,London ED,Innis RBdoi
10.1007/s00259-001-0695-zsubject
Has Abstractpub_date
2002-02-01 00:00:00pages
183-90issue
2eissn
1619-7070issn
1619-7089journal_volume
29pub_type
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