Chemical fate of the nicotinic acetylcholinergic radiotracer [123I]5-IA-85380 in baboon brain and plasma
| Autor: | Ronald M. Baldwin, Julie K. Staley, Eric Brenner, Louis Amici, Mohammed S. Al-Tikriti, Robert B. Innis, Sami S. Zoghbi, Masahiro Fujita, Gilles Tamagnan |
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| Rok vydání: | 2006 |
| Předmět: |
Male
Cancer Research Metabolic Clearance Rate Pyridines Metabolite Standardized uptake value Receptors Nicotinic High-performance liquid chromatography chemistry.chemical_compound Pharmacokinetics biology.animal Animals Tissue Distribution Radiology Nuclear Medicine and imaging Radionuclide Imaging Chromatography biology Brain Metabolism Papio anubis Nicotinic acetylcholine receptor Nicotinic agonist Biochemistry chemistry Organ Specificity Injections Intravenous Azetidines Molecular Medicine Radiopharmaceuticals Baboon |
| Zdroj: | Nuclear Medicine and Biology. 33:549-554 |
| ISSN: | 0969-8051 |
| DOI: | 10.1016/j.nucmedbio.2006.03.002 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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