11C 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

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11C 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, Andreas; Leonov, Andrei; Ryazanov, Sergey; Herfert, Kristina; Kuebler, Laura; Buss, Sabrina; Schmidt, Felix; Weckbecker, Daniel; Linder, Ruth; Bender, Dirk; Giese, Armin; Pichler, Bernd J.; Griesinger, Christian.

I: ChemMedChem, Bind 15, Nr. 5, 05.03.2020, s. 411-415.

Publikation: Bidrag til tidsskrift/Konferencebidrag i tidsskrift /Bidrag til avisTidsskriftartikelForskningpeer review

Harvard

Maurer, A, Leonov, A, Ryazanov, S, Herfert, K, Kuebler, L, Buss, S, Schmidt, F, Weckbecker, D, Linder, R, Bender, D, Giese, A, Pichler, BJ & Griesinger, C 2020, '11C 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, bind 15, nr. 5, s. 411-415. https://doi.org/10.1002/cmdc.201900689

APA

Maurer, A., Leonov, A., Ryazanov, S., Herfert, K., Kuebler, L., Buss, S., Schmidt, F., Weckbecker, D., Linder, R., Bender, D., Giese, A., Pichler, B. J., & Griesinger, C. (2020). 11C 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. https://doi.org/10.1002/cmdc.201900689

CBE

Maurer A, Leonov A, Ryazanov S, Herfert K, Kuebler L, Buss S, Schmidt F, Weckbecker D, Linder R, Bender D, Giese A, Pichler BJ, Griesinger C. 2020. 11C 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. https://doi.org/10.1002/cmdc.201900689

MLA

Vancouver

Author

Maurer, Andreas ; Leonov, Andrei ; Ryazanov, Sergey ; Herfert, Kristina ; Kuebler, Laura ; Buss, Sabrina ; Schmidt, Felix ; Weckbecker, Daniel ; Linder, Ruth ; Bender, Dirk ; Giese, Armin ; Pichler, Bernd J. ; Griesinger, Christian. / 11C 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. I: ChemMedChem. 2020 ; Bind 15, Nr. 5. s. 411-415.

Bibtex

@article{d219779e9b374fe3b0e38c9b6b3f6ba5,
title = "11C 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",
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 11C radiolabeling using in-situ generated [11C]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.",
keywords = "diphenylpyrazoles, neurodegenerative diseases, Parkinson's disease, radiotracers, α-synuclein",
author = "Andreas Maurer and Andrei Leonov and Sergey Ryazanov and Kristina Herfert and Laura Kuebler and Sabrina Buss and Felix Schmidt and Daniel Weckbecker and Ruth Linder and Dirk Bender and Armin Giese and Pichler, {Bernd J.} and Christian Griesinger",
year = "2020",
month = mar,
day = "5",
doi = "10.1002/cmdc.201900689",
language = "English",
volume = "15",
pages = "411--415",
journal = "ChemMedChem",
issn = "1860-7179",
publisher = "Wiley - V C H Verlag GmbH & Co. KGaA",
number = "5",

}

RIS

TY - JOUR

T1 - 11C Radiolabeling of anle253b

T2 - a Putative PET Tracer for Parkinson's Disease That Binds to α-Synuclein Fibrils in vitro and Crosses the Blood-Brain Barrier

AU - Maurer, Andreas

AU - Leonov, Andrei

AU - Ryazanov, Sergey

AU - Herfert, Kristina

AU - Kuebler, Laura

AU - Buss, Sabrina

AU - Schmidt, Felix

AU - Weckbecker, Daniel

AU - Linder, Ruth

AU - Bender, Dirk

AU - Giese, Armin

AU - Pichler, Bernd J.

AU - Griesinger, Christian

PY - 2020/3/5

Y1 - 2020/3/5

N2 - 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 11C radiolabeling using in-situ generated [11C]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.

AB - 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 11C radiolabeling using in-situ generated [11C]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.

KW - diphenylpyrazoles

KW - neurodegenerative diseases

KW - Parkinson's disease

KW - radiotracers

KW - α-synuclein

UR - http://www.scopus.com/inward/record.url?scp=85077851158&partnerID=8YFLogxK

U2 - 10.1002/cmdc.201900689

DO - 10.1002/cmdc.201900689

M3 - Journal article

C2 - 31859430

AN - SCOPUS:85077851158

VL - 15

SP - 411

EP - 415

JO - ChemMedChem

JF - ChemMedChem

SN - 1860-7179

IS - 5

ER -