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In vivo positron emission tomography studies on the novel nicotinic receptor agonist [11C]MPA compared with [11C]ABT-418 and (S)(-)[11C]nicotine in rhesus monkeys
Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Medicine, Department of Oncology, Radiology and Clinical Immunology. (BMS)
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1999 (English)In: Nuclear Medicine and Biology, ISSN 0969-8051, Vol. 26, no 6, 633-640 p.Article in journal (Refereed) Published
Abstract [en]

The novel 11C-labeled nicotinic agonist (R,S)-1-[11C]methyl-2(3-pyridyl)azetidine ([11C]MPA) was evaluated as a positron emission tomography (PET) ligand for in vivo characterization of nicotinic acetylcholine receptors in the brain of Rhesus monkeys in comparison with the nicotinic ligands (S)-3-methyl-5-(1-[11C]methyl-2-pyrrolidinyl)isoxazol ([11C]ABT-418) and (S)(-)[11C]nicotine. The nicotinic receptor agonist [11C]MPA demonstrated rapid uptake into the brain to a similar extent as (S)(-) [11C]nicotine and [11C]ABT-418. When unlabeled (S)(-)nicotine (0.02 mg/kg) was administered 5 min before the radioactive tracers, the uptake of [11C]MPA was decreased by 25% in the thalamus, 19% in the temporal cortex, and 11% in the cerebellum, whereas an increase was found for the uptake of (S)(-)[11C]nicotine and [11C]ABT-418. This finding indicates specific binding of [11C]MPA to nicotinic receptors in the brain in a simple classical displacement study. [11C]MPA seems to be a more promising radiotracer than (S)(-)[11C]nicotine or [11C]ABT-418 for PET studies to characterize nicotinic receptors in the brain.

Place, publisher, year, edition, pages
1999. Vol. 26, no 6, 633-640 p.
Keyword [en]
Nicotinic ligand, Positron emission tomography, [11C]MPA, [11C]ABT, (S)(−)[11C]nicotine, Rhesus monkey
National Category
Medical and Health Sciences
URN: urn:nbn:se:uu:diva-57121DOI: 10.1016/S0969-8051(99)00034-7PubMedID: 10587101OAI: oai:DiVA.org:uu-57121DiVA: diva2:85030
Available from: 2008-10-17 Created: 2008-10-17 Last updated: 2009-11-20Bibliographically approved

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