In vivo imaging of brain nicotinic acetylcholine receptors with 5-[123I]iodo-A-85380 using single photon emission computed tomography
Abstract
The distribution and kinetics of 5-[123I]iodo-A-85380, a novel ligand for brain nicotinic acetylcholine receptors (nAChRs), were evaluated in the Rhesus monkey using single photon emission computed tomography (SPECT). Peak levels of radioactivity were measured in brain at 90 min after injection of the tracer. Accumulation of radioactivity was highest in the thalamus, intermediate in the frontal cortex and basal ganglia, and lowest in the cerebellum. The ratio of specific to nonspecific binding (V3") in the thalamus, estimated from the (thalamic-cerebellar)/cerebellar radioactivity ratio, reached a value of 6 at 4 h post-injection. Specific binding was reduced by subcutaneous injection of 1 mg/kg cytisine at 2.25 h after injection of radiotracer. At 2.5 h after cytisine administration, radioactivity in the thalamus was reduced by 84%, in the frontal cortex, by 76%, and in the basal ganglia, by 57% of the level measured at the time of cytisine administration, demonstrating that the binding was reversible. On the basis of these findings, together with other data indicating high affinity, receptor subtype selectivity, low nonspecific binding and lack of toxicity in animals, 5-[123I]iodo-A-85380 appears to be a promising ligand for SPECT imaging of nAChRs in the human brain.
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Imaging with [123I]5-IA SPECT in nonhuman primate and human subjects results in a binding pattern consistent with the established regional distribution of β2-nAChR and is highest in the thalamus and intermediate throughout the cortex and cerebellum.
“Imaging with [123I]5-IA SPECT in nonhuman primate and human subjects results in a binding pattern that is consistent with the established regional distribution of β2-nAChR and is highest in the thalamus and intermediate throughout the cortex and cerebellum43, 44.”
From β2-Nicotinic Acetylcholine Receptor Availability During Acute and Prolonged Abstinence From Tobacco Smoking (2009) · cites this paper as [44]
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Functional brain imaging of tobacco use and dependence
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5-Iodo-A-85380, an α4β2 Subtype-Selective Ligand for Nicotinic Acetylcholine Receptors
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- Authors
- Chefer, S. I., Horti, A. G., Lee, K. S., Koren, A. O., Jones, D. W., Gorey, J. G., Links, J. M., Mukhin, A. G., Weinberger, D. R., & London, E. D.
- Affiliations
- National Institutes of Health (US)
- Corresponding author
- London, Edythe D.
- Venue
- Life Sciences
- Publisher
- Elsevier BV
- Published
- 1998-11
- Volume
- 63
- Issue
- 25
- Pages
- PL355-PL360
- ISSN
- 0024-3205 (ISSN-L)
- OpenAlex
- W2016131093
- Cited by
- 63
- References
- 1
- Citations by year
- 2020: 1 · 2015: 1 · 2014: 3 · 2012: 3
- FWCI
- 1.63
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Life Sciences (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Nicotinic Acetylcholine Receptors Study
- Health Sciences › Medicine › Radiology, Nuclear Medicine and Imaging › Radiopharmaceutical Chemistry and Applications
- Health Sciences › Medicine › Radiology, Nuclear Medicine and Imaging › Medical Imaging Techniques and Applications
- Keywords
- nicotinic acetylcholine receptors, SPECT imaging, rhesus monkey brain, thalamus, frontal cortex, basal ganglia, cerebellum, cytisine, receptor subtype selectivity
- MeSH terms
- Animals, Azetidines, Brain, Iodine Radioisotopes, Macaca mulatta, Male, Receptors, Nicotinic, Tissue Distribution, Tomography, Emission-Computed, Single-Photon, Radiopharmaceuticals
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