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  11 C radiolabeling of anle253b: A putative PET tracer for Parkinson's disease that binds to α-synuclein fibrils in vitro and crosses the blood-brain barrier.

Maurer, A., Leonov, A., Ryazanov, S., Herfert, K., Kuebler, L., Buss, S., et al. (2020). 11 C radiolabeling of anle253b: A putative PET tracer for Parkinson's disease that binds to α-synuclein fibrils in vitro and crosses the blood-brain barrier. ChemMedChem, 15(5), 411-415. doi:10.1002/cmdc.201900689.

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Item Permalink: http://hdl.handle.net/21.11116/0000-0005-7A00-2 Version Permalink: http://hdl.handle.net/21.11116/0000-0005-C882-6
Genre: Journal Article

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 Creators:
Maurer, A., Author
Leonov, A.1, Author              
Ryazanov, S.1, Author              
Herfert, K., Author
Kuebler, L., Author
Buss, S., Author
Schmidt, F., Author
Weckbecker, D., Author
Linder, R., Author
Bender, D., Author
Giese, A., Author
Pichler, B. J., Author
Griesinger, C.1, Author              
Affiliations:
1Department of NMR Based Structural Biology, MPI for biophysical chemistry, Max Planck Society, ou_578567              

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Free keywords: Parkinson's disease; diphenylpyrazoles; neurodegenerative diseases; radiotracers; α-synuclein
 Abstract: There is an urgent clinical need for imaging of α-synuclein (αSyn) fibrils, the hallmark biomarker for Parkinson's disease, in neurodegenerative disorders. Despite immense efforts, promising tracer candidates for nuclear imaging of αSyn are rare. Diphenyl pyrazoles are known modulators of αSyn aggregation and thus bear potential for non-invasive detection of this biomarker in vivo. Here we demonstrate high-affinity binding of the family member anle253b to fibrillar αSyn and present a high-yielding site-selective radiosynthesis route for 11 C radiolabeling using in-situ generated [11 C]formaldehyde and reductive methylation. Radio-HPLC of the tracer after incubation with rat serum in vitro shows excellent stability of the molecule. Positron emission tomography in healthy animals is used to assess the pharmacokinetics and biodistribution of the tracer, showing good penetration of the blood-brain barrier and low background binding to the non-pathological brain.

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Language(s): eng - English
 Dates: 2019-12-202020-03-05
 Publication Status: Published in print
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 Table of Contents: -
 Rev. Method: Peer
 Identifiers: DOI: 10.1002/cmdc.201900689
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Title: ChemMedChem
Source Genre: Journal
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Pages: - Volume / Issue: 15 (5) Sequence Number: - Start / End Page: 411 - 415 Identifier: -