التفاصيل البيبلوغرافية
| العنوان: |
Synthesis and preclinical evaluation of [11C]MA-PB-1 for in vivo imaging of brain Monoacylglycerol Lipase (MAGL) |
| المؤلفون: |
Ahamed, Muneer, Atilli, Bala, van Veghel, Daisy, Ooms, Maarten, Berben, Philippe, Celen, Sofie, Koole, Michel, Declerq, Lieven, Savinainen, Juha R, Laitinen, Jarmo T, Verbruggen, Alfons, Bormans, Guy |
| المصدر: |
European Journal of Medicinal Chemistry, 136, 104-113, (2017-04-25) |
| بيانات النشر: |
Zenodo |
| سنة النشر: |
2017 |
| المجموعة: |
Zenodo |
| مصطلحات موضوعية: |
MAGL, [11C]MA-PB-1, MJN110, biodistribution, PET imaging |
| الوصف: |
MAGL is a potential therapeutic target for oncological and psychiatric diseases. Our objective was to develop a PET tracer for in vivo quantification of MAGL. We report [ 11 C]MA-PB-1 as an irreversible MAGL inhibitor PET tracer. The in vitro inhibitory activity, ex vivo distribution, brain kinetics and specificity of [ 11 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 [ 11 C]MA-PB-1 is a suitable tracer for in vivo imaging of MAGL. |
| نوع الوثيقة: |
article in journal/newspaper |
| اللغة: |
unknown |
| Relation: |
https://zenodo.org/communities/inmind; https://zenodo.org/communities/eu; https://doi.org/10.1016/j.ejmech.2017.04.066; oai:zenodo.org:571108 |
| DOI: |
10.1016/j.ejmech.2017.04.066 |
| الاتاحة: |
https://doi.org/10.1016/j.ejmech.2017.04.066 |
| Rights: |
info:eu-repo/semantics/openAccess ; Creative Commons Attribution 4.0 International ; https://creativecommons.org/licenses/by/4.0/legalcode |
| رقم الانضمام: |
edsbas.84D622D0 |
| قاعدة البيانات: |
BASE |