| Title : Synthesis and preclinical evaluation of [(11)C]MA-PB-1 for in vivo imaging of brain monoacylglycerol lipase (MAGL) - Ahamed_2017_Eur.J.Med.Chem_136_104 |
| Author(s) : Ahamed M , Attili B , van Veghel D , Ooms M , Berben P , Celen S , Koole M , Declercq L , Savinainen JR , Laitinen JT , Verbruggen A , Bormans G |
| Ref : Eur Journal of Medicinal Chemistry , 136 :104 , 2017 |
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Abstract :
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. |
| PubMedSearch : Ahamed_2017_Eur.J.Med.Chem_136_104 |
| PubMedID: 28486208 |
Ahamed M, Attili B, van Veghel D, Ooms M, Berben P, Celen S, Koole M, Declercq L, Savinainen JR, Laitinen JT, Verbruggen A, Bormans G (2017)
Synthesis and preclinical evaluation of [(11)C]MA-PB-1 for in vivo imaging of brain monoacylglycerol lipase (MAGL)
Eur Journal of Medicinal Chemistry
136 :104
Ahamed M, Attili B, van Veghel D, Ooms M, Berben P, Celen S, Koole M, Declercq L, Savinainen JR, Laitinen JT, Verbruggen A, Bormans G (2017)
Eur Journal of Medicinal Chemistry
136 :104