Chemical fate of the nicotinic acetylcholinergic radiotracer [123I]5-IA-85380 in baboon brain and plasma
Abstract
The fate of the nicotinic acetylcholinergic receptor radiotracer [123I]5-IA-85380 ([123I]5-IA) was studied in baboon by analyzing the chemical composition of brain tissue and plasma after intravenous administration of the tracer. Acetonitrile denaturation and high-performance liquid chromatography (HPLC) analysis showed predominantly unchanged (91-98%) parent tracer in all brain tissues examined, compared to significant metabolism (23% parent) in the plasma at 90 min postinjection, and control tissue recovery of 95-98%. [123I]5-IA was distributed to the thalamus with a standardized uptake value of 9.2 (0.04% dose/g) or a concentration 5.8 times higher than that of the cerebellum. The HPLC behavior of a synthesized sample of one hypothesized metabolite, 5-iodo-3-pyridinol (5-IP), was consistent with plasma radiometabolite fraction. Since only parent radiotracer compound was found in brain tissue, these results add confidence that information derived from single photon emission computed tomography images of 123I activity in the brain after [123I]5-IA administration can be interpreted as distribution of an intact radiotracer.
Integrity signals
Registry
Cites
Statistics
Claims the paper makes
Claims other papers make about this one
Each is checked against this paper’s own text: does it say what the citing paper says it does?
[123I]5-IA is metabolized in the liver by enzymes in the cytochrome P450 family, such as CYP2A6, CYP2B6, and CYP2D6.
“Consistently, we expect that [123I]5-IA is metabolized in the liver by enzymes in the cytochrome P450 family, such as CYP2A6, which acts on nicotine, and CYP2B6 and CYP2D6, which catalyze the dealkylation of aromatic ethers56, 57.”
From β2-Nicotinic Acetylcholine Receptor Availability During Acute and Prolonged Abstinence From Tobacco Smoking (2009) · cites this paper as [56]
Cites
5-Iodo-A-85380, an α4β2 Subtype-Selective Ligand for Nicotinic Acetylcholine Receptors
Mukhin, A. G., Gündisch, D., Horti, A. G., Koren, A. O., Tamagnan, G., Kimes, A. S., Chambers, J., Vaupel, D. B., King, S. L., Picciotto, M. R., et al. (2000) · Molecular Pharmacology · doi:10.1124/mol.57.3.642 · Cited by 173 · see citing works
Self-citationMusachio, 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
Flagged first, then by citations
Cited by
Sorted by citations
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
Self-citation
- Authors
- Baldwin, R. M., Zoghbi, S. S., Staley, J. K., Brenner, E., Al-Tikriti, M. S., Amici, L., Fujita, M., Innis, R. B., & Tamagnan, G.
- Affiliations
- Yale University (US)
- Corresponding author
- Baldwin, Ronald M.
- Venue
- Nuclear Medicine and Biology
- Publisher
- Elsevier BV
- Published
- 2006-05
- Volume
- 33
- Issue
- 4
- Pages
- 549-554
- ISSN
- 0969-8051 (ISSN-L)
- OpenAlex
- W2038518848
- Cited by
- 6
- References
- 2
- FWCI
- 0.81
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Nuclear Medicine and Biology (publishedVersion)
- PubMed (publishedVersion)
- Funders
- U.S. Department of Veterans Affairs
- National Institute on Drug Abuse (P50-DA84733)
- National Cancer Institute
- National Center for Research Resources (M01RR000125, MO-1 RR00125)
- 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
- radiotracer metabolism, thalamus, cerebellum, baboon brain, radiotracer stability
- MeSH terms
- Animals, Azetidines, Brain, Injections, Intravenous, Male, Metabolic Clearance Rate, Organ Specificity, Pyridines, Radionuclide Imaging, Receptors, Nicotinic, Tissue Distribution, Radiopharmaceuticals, Papio anubis
About these checks
Registry, retraction, Cites and statistics results are computed, not judged, with one exception: a printed reference that no index lists is read once by a model before it counts as a citation error. Claims are extracted by a model and kept only when their quote appears verbatim in the text; each cited source is then checked, with a model’s help, for whether it says what the claim relies on. Those verdicts can be wrong — read the claim’s quote and the cited source before relying on one.
Statistics and arithmetic are recomputed, not judged.
Confidence bands are shown only for fields calibrated on our annotated test set. None is calibrated yet, so no band is shown.
What counts as a claim ›How we measure confidence ›How we check this ›
Are you an author, or do you see a problem with this page? Request a review
