Ligands for in vivo imaging of nicotinic receptor subtypes in Alzheimer brain

@article{Sihver2000LigandsFI,
  title={Ligands for in vivo imaging of nicotinic receptor subtypes in Alzheimer brain},
  author={Wiebke Sihver and Bengt L{\aa}ngstr{\"o}m and Agneta Nordberg},
  journal={Acta Neurologica Scandinavica},
  year={2000},
  volume={102}
}
The neuronal nicotinic acetylcholine receptors (nAChR) are involved in functional processes in brain including cognitive function and memory. A severe loss of the nAChRs has been detected in brain of patients with Alzheimer's disease (AD). There is a great interest to image nAChRs noninvasive for detection of receptor impairments even at a presymptomatic stage of AD as well for monitoring outcome of drug treatment. (S) [11C]Nicotine, has so far been the only nAChR ligand used in positron… 
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This article attempts to summarize the peer-reviewed publications of the most recent development and preclinical studies of novel α4β2-nAChR PET radioligands with improved brain kinetics and first human studies with one of these radiolIGands ([(18) F]AZAN).
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TLDR
18F-AZAN specifically labels nAChRs in baboon brains with a high value of BPND and it requires only 90 min of PET scanning to produce estimates of VT and BPND in the various brain regions.
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References

SHOWING 1-10 OF 82 REFERENCES
Imaging of nicotinic and muscarinic receptors in Alzheimer's disease: effect of tacrine treatment.
TLDR
In this study the cholinergic nicotinic and muscarinic receptors were studied in brain by positron emission tomography and the binding capacity of 11C-benztropine was found to be decreased in the temporal cortex after 3 months of tacrine treatment.
Neuronal nicotinic receptors in the human brain
Attempts to visualize nicotinic receptors in the brain of monkey and man by positron emission tomography.
Imaging central nicotinic acetylcholine receptors in baboons with [18F]fluoro-A-85380.
TLDR
The results demonstrate the feasibility and the safety of imaging nAChRs in vivo using labeled or unlabeled fluoro-A-85380 in baboons and mice.
Epibatidine and ABT 418 reveal selective losses of α4β2 nicotinic receptors in Alzheimer brains
TLDR
The alpha 4 beta 2 nAChR subunit might be the most vulnerable in Alzheimer's disease (AD) and a possible target for therapeutic strategies using the nicotinic agonists epibatidine, ABT 418 and (-)nicotine in competition studies with [3H]nicotine and [3 H]cytisine.
Fluorine-18-FPH for PET imaging of nicotinic acetylcholine receptors.
  • A. Horti, U. Scheffel, R. Dannals
  • Biology, Chemistry
    Journal of nuclear medicine : official publication, Society of Nuclear Medicine
  • 1997
TLDR
Because of its high uptake into the brain and high ratios of specific-to-nonspecific binding, this radioligand appears to be ideally suited for PET imaging of nAChR in the mammalian brain.
In vivo labeling of neuronal nicotinic acetylcholine receptors with radiolabeled isomers of norchloroepibatidine
TLDR
Data indicate that [3H](+) and (-)NCEPB are useful in vivo binding ligands for the cholinergic nicotinic receptor.
Decreased Protein Levels of Nicotinic Receptor Subunits in the Hippocampus and Temporal Cortex of Patients with Alzheimer’s Disease
TLDR
The results reveal brain region‐specific changes in the protein levels of the nAChR, α3, α4, and α7 subunits in AD.
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