Whole-body biodistribution, radiation absorbed dose, and brain SPET imaging with [123I]5-I-A-85380 in healthy human subjects

Masahiro Fujita, John P. Seibyl, Bruce D. Vaupel, Gilles Tamagnan, Michele Early, Sami S. Zoghbi, Ronald M. Baldwin, Andrew G. Horti, Andrei O. Koren, Alexey G. Mukhin, Shaukat Khan, Ali Bozkurt, Alane S. Kimes, Edythe D. London, Robert B. Innis

Research output: Contribution to journalArticle

Abstract

The biodistribution of radioactivity after the administration of a new tracer for α4β2 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 (μGy/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 α4β2 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 α4β2 nAChRs in humans, with acceptable dosimetry and high brain uptake.

Original languageEnglish (US)
Pages (from-to)183-190
Number of pages8
JournalEuropean Journal of Nuclear Medicine
Volume29
Issue number2
DOIs
StatePublished - Feb 23 2002

Keywords

  • Biodistribution
  • Dosimetry
  • Nicotinic acetylcholine receptors
  • SPET
  • [I]5-I-A-85380

ASJC Scopus subject areas

  • Radiology Nuclear Medicine and imaging

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    Fujita, M., Seibyl, J. P., Vaupel, B. D., Tamagnan, G., Early, M., Zoghbi, S. S., Baldwin, R. M., Horti, A. G., Koren, A. O., Mukhin, A. G., Khan, S., Bozkurt, A., Kimes, A. S., London, E. D., & Innis, R. B. (2002). Whole-body biodistribution, radiation absorbed dose, and brain SPET imaging with [123I]5-I-A-85380 in healthy human subjects. European Journal of Nuclear Medicine, 29(2), 183-190. https://doi.org/10.1007/s00259-001-0695-z