Projekte

(R)-[F-18]NEBIFQUINIDE: A promising new PET tracer for TSPO imaging

Autor(en)
Neydher Berroteran-Infante, Thomas Kalina, Lukas Fetty, Victoria Janisch, Ramona Velasco, Chrysoula Vraka, Marcus Hacker, Alexander R. Haug, Katharina Pallitsch, Wolfgang Wadsak, Markus Mitterhauser
Abstrakt

Positron emission tomography (PET) imaging of the 18 kDa translocator protein (TSPO), has a high diagnostic potential in neurodegenerative disorders and cancer. However, TSPO is considered a challenge for molecular imaging due to the poor availability of suitable radiotracers with adequate pharmacokinetic properties. Here, we describe the development of a radiofluorinated pyridinyl isoquinoline analogue of the established TSPO PET tracer (R)-[C-11]PK11195 with improved binding properties in all known human TSPO phenotypes. We conducted a complete preclinical evaluation using in vitro, in vivo and ex vivo methods to assess the performance of this novel radiotracer and observed high specific binding of the radiotracer to TSPO, as well as high metabolic stability. Therefore, we propose this radiolabeled compound for further evaluation in animal models as well as in clinical trials. (C) 2019 Elsevier Masson SAS. All rights reserved.

Organisation(en)
Institut für Organische Chemie, Institut für Anorganische Chemie
Externe Organisation(en)
Medizinische Universität Wien, Centre for Biomarker Research in Medicine – CBmed GmbH, Universität Wien
Journal
European Journal of Medicinal Chemistry
Band
176
Seiten
410-418
Anzahl der Seiten
9
ISSN
0223-5234
DOI
https://doi.org/10.1016/j.ejmech.2019.05.008
Publikationsdatum
08-2019
Peer-reviewed
Ja
ÖFOS 2012
Medizinische Chemie, Pharmakologie
Schlagwörter
Link zum Portal
https://ucris.univie.ac.at/portal/de/publications/rf18nebifquinide-a-promising-new-pet-tracer-for-tspo-imaging(5d18ba69-e403-4cf6-a736-76118788b57c).html

Publikationen

(R)-[F-18]NEBIFQUINIDE: A promising new PET tracer for TSPO imaging

Autor(en)
Neydher Berroteran-Infante, Thomas Kalina, Lukas Fetty, Victoria Janisch, Ramona Velasco, Chrysoula Vraka, Marcus Hacker, Alexander R. Haug, Katharina Pallitsch, Wolfgang Wadsak, Markus Mitterhauser
Abstrakt

Positron emission tomography (PET) imaging of the 18 kDa translocator protein (TSPO), has a high diagnostic potential in neurodegenerative disorders and cancer. However, TSPO is considered a challenge for molecular imaging due to the poor availability of suitable radiotracers with adequate pharmacokinetic properties. Here, we describe the development of a radiofluorinated pyridinyl isoquinoline analogue of the established TSPO PET tracer (R)-[C-11]PK11195 with improved binding properties in all known human TSPO phenotypes. We conducted a complete preclinical evaluation using in vitro, in vivo and ex vivo methods to assess the performance of this novel radiotracer and observed high specific binding of the radiotracer to TSPO, as well as high metabolic stability. Therefore, we propose this radiolabeled compound for further evaluation in animal models as well as in clinical trials. (C) 2019 Elsevier Masson SAS. All rights reserved.

Organisation(en)
Institut für Organische Chemie, Institut für Anorganische Chemie
Externe Organisation(en)
Medizinische Universität Wien, Centre for Biomarker Research in Medicine – CBmed GmbH, Universität Wien
Journal
European Journal of Medicinal Chemistry
Band
176
Seiten
410-418
Anzahl der Seiten
9
ISSN
0223-5234
DOI
https://doi.org/10.1016/j.ejmech.2019.05.008
Publikationsdatum
08-2019
Peer-reviewed
Ja
ÖFOS 2012
Medizinische Chemie, Pharmakologie
Schlagwörter
Link zum Portal
https://ucris.univie.ac.at/portal/de/publications/rf18nebifquinide-a-promising-new-pet-tracer-for-tspo-imaging(5d18ba69-e403-4cf6-a736-76118788b57c).html

Vortraege

(R)-[F-18]NEBIFQUINIDE: A promising new PET tracer for TSPO imaging

Autor(en)
Neydher Berroteran-Infante, Thomas Kalina, Lukas Fetty, Victoria Janisch, Ramona Velasco, Chrysoula Vraka, Marcus Hacker, Alexander R. Haug, Katharina Pallitsch, Wolfgang Wadsak, Markus Mitterhauser
Abstrakt

Positron emission tomography (PET) imaging of the 18 kDa translocator protein (TSPO), has a high diagnostic potential in neurodegenerative disorders and cancer. However, TSPO is considered a challenge for molecular imaging due to the poor availability of suitable radiotracers with adequate pharmacokinetic properties. Here, we describe the development of a radiofluorinated pyridinyl isoquinoline analogue of the established TSPO PET tracer (R)-[C-11]PK11195 with improved binding properties in all known human TSPO phenotypes. We conducted a complete preclinical evaluation using in vitro, in vivo and ex vivo methods to assess the performance of this novel radiotracer and observed high specific binding of the radiotracer to TSPO, as well as high metabolic stability. Therefore, we propose this radiolabeled compound for further evaluation in animal models as well as in clinical trials. (C) 2019 Elsevier Masson SAS. All rights reserved.

Organisation(en)
Institut für Organische Chemie, Institut für Anorganische Chemie
Externe Organisation(en)
Medizinische Universität Wien, Centre for Biomarker Research in Medicine – CBmed GmbH, Universität Wien
Journal
European Journal of Medicinal Chemistry
Band
176
Seiten
410-418
Anzahl der Seiten
9
ISSN
0223-5234
DOI
https://doi.org/10.1016/j.ejmech.2019.05.008
Publikationsdatum
08-2019
Peer-reviewed
Ja
ÖFOS 2012
Medizinische Chemie, Pharmakologie
Schlagwörter
Link zum Portal
https://ucris.univie.ac.at/portal/de/publications/rf18nebifquinide-a-promising-new-pet-tracer-for-tspo-imaging(5d18ba69-e403-4cf6-a736-76118788b57c).html