571108
doi
10.1016/j.ejmech.2017.04.066
oai:zenodo.org:571108
user-inmind
user-eu
Atilli, Bala
Laboratory for Radiopharmacy, Campus Gasthuisberg O&N2, Herestraat 49 Box 821, BE-3000 Leuven, Belgium.
van Veghel, Daisy
Laboratory for Radiopharmacy, Campus Gasthuisberg O&N2, Herestraat 49 Box 821, BE-3000 Leuven, Belgium.
Ooms, Maarten
Laboratory for Radiopharmacy, Campus Gasthuisberg O&N2, Herestraat 49 Box 821, BE-3000 Leuven, Belgium.
Berben, Philippe
Laboratory for Radiopharmacy, Campus Gasthuisberg O&N2, Herestraat 49 Box 821, BE-3000 Leuven, Belgium.
Celen, Sofie
Laboratory for Radiopharmacy, Campus Gasthuisberg O&N2, Herestraat 49 Box 821, BE-3000 Leuven, Belgium.
Koole, Michel
Department of Nuclear Medicine & Molecular Imaging, UZ Herestraat 49, 3000 Leuven, Belgium.
Declerq, Lieven
Laboratory for Radiopharmacy, Campus Gasthuisberg O&N2, Herestraat 49 Box 821, BE-3000 Leuven, Belgium.
Savinainen, Juha R
Institute of Biomedicine, Faculty of Health Sciences, The University of Eastern Finland, Finland.
Laitinen, Jarmo T
Institute of Biomedicine, Faculty of Health Sciences, The University of Eastern Finland, Finland.
Verbruggen, Alfons
Laboratory for Radiopharmacy, Campus Gasthuisberg O&N2, Herestraat 49 Box 821, BE-3000 Leuven, Belgium.
Bormans, Guy
Laboratory for Radiopharmacy, Campus Gasthuisberg O&N2, Herestraat 49 Box 821, BE-3000 Leuven, Belgium.
Synthesis and preclinical evaluation of [11C]MA-PB-1 for in vivo imaging of brain Monoacylglycerol Lipase (MAGL)
Ahamed, Muneer
Laboratory for Radiopharmacy, Campus Gasthuisberg O&N2, Herestraat 49 Box 821, BE-3000 Leuven, Belgium.
info:eu-repo/semantics/openAccess
Creative Commons Attribution 4.0 International
https://creativecommons.org/licenses/by/4.0/legalcode
MAGL
[11C]MA-PB-1
MJN110
biodistribution
PET imaging
<p>MAGL is a potential therapeutic target for oncological and psychiatric diseases. Our objective was to develop a PET tracer for <em>in vivo</em> quantification of MAGL. We report [<sup>11</sup>C]MA-PB-1 as an irreversible MAGL inhibitor PET tracer. The in vitro inhibitory activity, <em>ex vivo</em> distribution, brain kinetics and specificity of [<sup>11</sup>C]MA-PB-1 binding were studied. Ex vivo biodistribution and microPET showed good brain uptake which could be blocked by pretreatment with both MA-PB-1 and a structurally non-related MAGL inhibitor MJN110. These initial results suggest that [<sup>11</sup>C]MA-PB-1 is a suitable tracer for <em>in vivo</em> imaging of MAGL.</p>
Zenodo
2017-04-25
info:eu-repo/semantics/article
799503
user-inmind
user-eu
award_title=Imaging of Neuroinflammation in Neurodegenerative Diseases; award_number=278850; award_identifiers_scheme=url; award_identifiers_identifier=https://cordis.europa.eu/projects/278850; funder_id=00k4n6c32; funder_name=European Commission;
1579540638.880835
1184870
md5:000799b2673d79b30665a15b66e8a946
https://zenodo.org/records/571108/files/Ahamed_EurJMedChem_2016-P13a-AAM.pdf
public
European Journal of Medicinal Chemistry
136
104-113
2017-04-25