5-[123I]Iodo-A-85380: assessment of pharmacological safety, radiation dosimetry and SPECT imaging of brain nicotinic receptors in healthy human subjects
Abstract
Recently, 5-[123I]iodo-3-(2(S)-azetidinylmethoxy)pyridine ([123I]5IA) was developed as a ligand for imaging the nicotinic acetylcholine receptor (nAChR) in human brain using single photon emission computed tomography (SPECT). In the present study, the toxicity and radiation absorbed dose of [123I]5IA were investigated. Behavior and physiological parameters were examined in mice and rats after administration of 5IA. There were no changes in these parameters in animals administered 1 microg/kg of 5IA or less, indicating that the no observed effect level (NOEL) of 5IA was 1 microg/kg. [123I]5IA was then administered to healthy human subjects and serial whole-body images were acquired over 24 hr. Initially, high levels of radioactivity were observed in the liver and urinary bladder and moderate levels in the lungs, kidneys, and brain. Whole brain activity at 1 hr was 4.6 +/- 0.4% of the injected dose and this value gradually decreased with time. The majority (-75%) of the radioactivity was excreted in urine within 24 hr, and less than 1% remained in all organs tested. The biological half-life of [1231]51A averaged 7.2 +/- 4.0 hr. Based on the biodistribution data, radiation absorbed doses were estimated using MIRDOSE 3.1 software with the dynamic bladder model and the ICRP gastrointestinal (GI) tract model. Consequently, the effective dose equivalent was estimated to be 30 +/- 1.4 microSv/MBq, which is an acceptable radiation burden. Having determined the safety of this compound,…
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[123I]5-IA demonstrates low nonspecific binding, acceptable dosimetry in human subjects, high brain uptake, and good test-retest reproducibility.
“This ligand demonstrates low nonspecific binding40 and has acceptable dosimetry in human subjects with high brain uptake41, 42 and good test-retest reproducibility43.”
From β2-Nicotinic Acetylcholine Receptor Availability During Acute and Prolonged Abstinence From Tobacco Smoking (2009) · cites this paper as [42]
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Musachio, J. L., Scheffel, U., Finley, P. A., Zhan, Y., Mochizuki, T., Wagner, H. N., & Dannals, R. F. (1998) · Life Sciences · doi:10.1016/s0024-3205(98)00180-5 · Cited by 57 · see citing works
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Cosgrove, K. P., Batis, J., Bois, F., Maciejewski, P. K., Esterlis, I., Kloczynski, T., Stiklus, S., Krishnan-Sarin, S., O’Malley, S., Perry, E., et al. (2009) · Archives of General Psychiatry · doi:10.1001/archgenpsychiatry.2009.41 · Cited by 159 · see citing works
Temporal Change in Human Nicotinic Acetylcholine Receptor After Smoking Cessation: 5IA SPECT Study
Mamede, M., Ishizu, K., Ueda, M., Mukai, T., Iida, Y., Kawashima, H., Fukuyama, H., Togashi, K., & Saji, H. (2007) · Journal of Nuclear Medicine · doi:10.2967/jnumed.107.043471 · Cited by 90 · see citing works
Self-citation
- Authors
- Ueda, M., Iida, Y., Mukai, T., Mamede, M., Ishizu, K., Ogawa, M., Magata, Y., Konishi, J., & Saji, H.
- Affiliations
- Kyoto University (JP)
- Hamamatsu University (JP)
- Corresponding author
- Saji, Hideo
- Venue
- Annals of Nuclear Medicine
- Published
- 2004-06
- Volume
- 18
- Issue
- 4
- Pages
- 337-344
- ISSN
- 0914-7187 (ISSN-L)
- 1864-6433
- OpenAlex
- W2107699817
- Cited by
- 26
- References
- 1
- Citations by year
- 2019: 2 · 2018: 1 · 2017: 1 · 2016: 2 · 2013: 2
- FWCI
- 1.96
- Type
- journal article
- Language
- en
- Open access
- closed
- Licence
- www.springer.com/tdm (tdm)
- Locations
- Annals of Nuclear Medicine (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Health Sciences › Medicine › Radiology, Nuclear Medicine and Imaging › Radiopharmaceutical Chemistry and Applications
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Nicotinic Acetylcholine Receptors Study
- Health Sciences › Medicine › Radiology, Nuclear Medicine and Imaging › Medical Imaging Techniques and Applications
- Keywords
- nicotinic acetylcholine receptors, neuroimaging, SPECT radiotracer, radiation dosimetry, pharmacological safety, tissue distribution, effective dose, no-observed-effect level, radioligands
- MeSH terms
- Adult, Aged, Animals, Azetidines, Body Burden, Brain, Humans, Male, Metabolic Clearance Rate, Mice, Inbred ICR, Organ Specificity, Pyridines, Radiation Dosage, Radiation Injuries, Radiometry, Radionuclide Imaging, Receptors, Nicotinic, Relative Biological Effectiveness, Species Specificity, Tissue Distribution, Whole-Body Counting, Rats, Sprague-Dawley, Radiopharmaceuticals, Mice, Rats
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