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In vivo positron em...
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
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Sihver, Wiebke (författare)
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Fasth, Karl-Johan (författare)
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Ögren, Matthias (författare)
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- Lundqvist, Hans (författare)
- Uppsala universitet,Institutionen för onkologi, radiologi och klinisk immunologi,BMS
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Bergström, Mats (författare)
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Watanabe, Yasuyoshi (författare)
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Langström, Bengt (författare)
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- Nordberg, Agneta (författare)
- Uppsala universitet,Institutionen för neurovetenskap
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(creator_code:org_t)
- 1999
- 1999
- Engelska.
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Ingår i: Nuclear Medicine and Biology. - 0969-8051 .- 1872-9614. ; 26:6, s. 633-640
- Relaterad länk:
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https://urn.kb.se/re...
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https://doi.org/10.1...
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Abstract
Ämnesord
Stäng
- 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.
Nyckelord
- Nicotinic ligand
- Positron emission tomography
- [11C]MPA
- [11C]ABT
- (S)(−)[11C]nicotine
- Rhesus monkey
- MEDICINE
- MEDICIN
Publikations- och innehållstyp
- ref (ämneskategori)
- art (ämneskategori)
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