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 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 - 2002
Externally publishedYes

Fingerprint

Whole-Body Irradiation
Photons
Healthy Volunteers
Nicotinic Receptors
Tomography
Large Intestine
Brain
Urinary Bladder
Whole Body Imaging
Body Image
Thalamus
Radioactivity
Gastrointestinal Tract
Urine
Radiation
5-iodo-3-(2-azetidinylmethoxy)pyridine

Keywords

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

ASJC Scopus subject areas

  • Radiology Nuclear Medicine and imaging
  • Radiological and Ultrasound Technology

Cite this

Whole-body biodistribution, radiation absorbed dose, and brain SPET imaging with [123I]5-I-A-85380 in healthy human subjects. / Fujita, Masahiro; Seibyl, John P.; Vaupel, Bruce D.; Tamagnan, Gilles; Early, Michele; Zoghbi, Sami S.; Baldwin, Ronald M.; Horti, Andrew; Koren, Andrei O.; Mukhin, Alexey G.; Khan, Shaukat; Bozkurt, Ali; Kimes, Alane S.; London, Edythe D.; Innis, Robert B.

In: European Journal Of Nuclear Medicine, Vol. 29, No. 2, 2002, p. 183-190.

Research output: Contribution to journalArticle

Fujita, M, Seibyl, JP, Vaupel, BD, Tamagnan, G, Early, M, Zoghbi, SS, Baldwin, RM, Horti, A, Koren, AO, Mukhin, AG, Khan, S, Bozkurt, A, Kimes, AS, London, ED & Innis, RB 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, vol. 29, no. 2, pp. 183-190. https://doi.org/10.1007/s00259-001-0695-z
Fujita, Masahiro ; Seibyl, John P. ; Vaupel, Bruce D. ; Tamagnan, Gilles ; Early, Michele ; Zoghbi, Sami S. ; Baldwin, Ronald M. ; Horti, Andrew ; Koren, Andrei O. ; Mukhin, Alexey G. ; Khan, Shaukat ; Bozkurt, Ali ; Kimes, Alane S. ; London, Edythe D. ; Innis, Robert B. / Whole-body biodistribution, radiation absorbed dose, and brain SPET imaging with [123I]5-I-A-85380 in healthy human subjects. In: European Journal Of Nuclear Medicine. 2002 ; Vol. 29, No. 2. pp. 183-190.
@article{8dec73ee5c834c3faf249c3bb80f76c5,
title = "Whole-body biodistribution, radiation absorbed dose, and brain SPET imaging with [123I]5-I-A-85380 in healthy human subjects",
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.",
keywords = "[I]5-I-A-85380, Biodistribution, Dosimetry, Nicotinic acetylcholine receptors, SPET",
author = "Masahiro Fujita and Seibyl, {John P.} and Vaupel, {Bruce D.} and Gilles Tamagnan and Michele Early and Zoghbi, {Sami S.} and Baldwin, {Ronald M.} and Andrew Horti and Koren, {Andrei O.} and Mukhin, {Alexey G.} and Shaukat Khan and Ali Bozkurt and Kimes, {Alane S.} and London, {Edythe D.} and Innis, {Robert B.}",
year = "2002",
doi = "10.1007/s00259-001-0695-z",
language = "English (US)",
volume = "29",
pages = "183--190",
journal = "European Journal of Nuclear Medicine and Molecular Imaging",
issn = "1619-7070",
publisher = "Springer Verlag",
number = "2",

}

TY - JOUR

T1 - Whole-body biodistribution, radiation absorbed dose, and brain SPET imaging with [123I]5-I-A-85380 in healthy human subjects

AU - Fujita, Masahiro

AU - Seibyl, John P.

AU - Vaupel, Bruce D.

AU - Tamagnan, Gilles

AU - Early, Michele

AU - Zoghbi, Sami S.

AU - Baldwin, Ronald M.

AU - Horti, Andrew

AU - Koren, Andrei O.

AU - Mukhin, Alexey G.

AU - Khan, Shaukat

AU - Bozkurt, Ali

AU - Kimes, Alane S.

AU - London, Edythe D.

AU - Innis, Robert B.

PY - 2002

Y1 - 2002

N2 - 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.

AB - 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.

KW - [I]5-I-A-85380

KW - Biodistribution

KW - Dosimetry

KW - Nicotinic acetylcholine receptors

KW - SPET

UR - http://www.scopus.com/inward/record.url?scp=0036169966&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=0036169966&partnerID=8YFLogxK

U2 - 10.1007/s00259-001-0695-z

DO - 10.1007/s00259-001-0695-z

M3 - Article

C2 - 11926380

AN - SCOPUS:0036169966

VL - 29

SP - 183

EP - 190

JO - European Journal of Nuclear Medicine and Molecular Imaging

JF - European Journal of Nuclear Medicine and Molecular Imaging

SN - 1619-7070

IS - 2

ER -