Synthesis and preclinical evaluation of [11C]MA-PB-1 for in vivo imaging of brain monoacylglycerol lipase (MAGL)

Muneer Ahamed; Bala Attili; Daisy van Veghel; Maarten Ooms; Philippe Berben; Sophie Celen; Michel Koole; Lieven Declercq; Juha Savinainen; Jarmo Laitinen; Alfons Verbruggen; Guy Bormans

doi:10.1016/j.ejmech.2017.04.066

Synthesis and preclinical evaluation of [11C]MA-PB-1 for in vivo imaging of brain monoacylglycerol lipase (MAGL)

Muneer Ahamed, Bala Attili, Daisy van Veghel, Maarten Ooms, Philippe Berben, Sophie Celen, Michel Koole, Lieven Declercq, Juha Savinainen, Jarmo Laitinen, Alfons Verbruggen, Guy Bormans

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25 Citations (Scopus)

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 [¹¹C]MA-PB-1 as an irreversible MAGL inhibitor PET tracer. The in vitro inhibitory activity, ex vivo distribution, brain kinetics and specificity of [¹¹C]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 [¹¹C]MA-PB-1 is a suitable tracer for in vivo imaging of MAGL.

Original language	English
Pages (from-to)	104-113
Number of pages	10
Journal	European Journal of Medicinal Chemistry
Volume	136
Issue number	18 August 2017
Early online date	2017
DOIs	https://doi.org/10.1016/j.ejmech.2017.04.066
Publication status	Published - 2017

Keywords

Biodistribution
MAGL
MJN110
PET imaging
[ C]MA-PB-1

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This output contributes to the following UN Sustainable Development Goals (SDGs)

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10.1016/j.ejmech.2017.04.066

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Ahamed, M., Attili, B., van Veghel, D., Ooms, M., Berben, P., Celen, S., Koole, M., Declercq, L., Savinainen, J., Laitinen, J., Verbruggen, A., & Bormans, G. (2017). Synthesis and preclinical evaluation of [11C]MA-PB-1 for in vivo imaging of brain monoacylglycerol lipase (MAGL). European Journal of Medicinal Chemistry, 136(18 August 2017), 104-113. https://doi.org/10.1016/j.ejmech.2017.04.066

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title = "Synthesis and preclinical evaluation of [11C]MA-PB-1 for in vivo imaging of brain monoacylglycerol lipase (MAGL)",

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 [11C]MA-PB-1 as an irreversible MAGL inhibitor PET tracer. The in vitro inhibitory activity, ex vivo distribution, brain kinetics and specificity of [11C]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 [11C]MA-PB-1 is a suitable tracer for in vivo imaging of MAGL.",

keywords = "Biodistribution, MAGL, MJN110, PET imaging, [ C]MA-PB-1",

author = "Muneer Ahamed and Bala Attili and {van Veghel}, Daisy and Maarten Ooms and Philippe Berben and Sophie Celen and Michel Koole and Lieven Declercq and Juha Savinainen and Jarmo Laitinen and Alfons Verbruggen and Guy Bormans",

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Ahamed, M, Attili, B, van Veghel, D, Ooms, M, Berben, P, Celen, S, Koole, M, Declercq, L, Savinainen, J, Laitinen, J, Verbruggen, A & Bormans, G 2017, 'Synthesis and preclinical evaluation of [11C]MA-PB-1 for in vivo imaging of brain monoacylglycerol lipase (MAGL)', European Journal of Medicinal Chemistry, vol. 136, no. 18 August 2017, pp. 104-113. https://doi.org/10.1016/j.ejmech.2017.04.066

TY - JOUR

T1 - Synthesis and preclinical evaluation of [11C]MA-PB-1 for in vivo imaging of brain monoacylglycerol lipase (MAGL)

AU - Ahamed, Muneer

AU - Attili, Bala

AU - van Veghel, Daisy

AU - Ooms, Maarten

AU - Berben, Philippe

AU - Celen, Sophie

AU - Koole, Michel

AU - Declercq, Lieven

AU - Savinainen, Juha

AU - Laitinen, Jarmo

AU - Verbruggen, Alfons

AU - Bormans, Guy

PY - 2017

Y1 - 2017

N2 - 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 [11C]MA-PB-1 as an irreversible MAGL inhibitor PET tracer. The in vitro inhibitory activity, ex vivo distribution, brain kinetics and specificity of [11C]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 [11C]MA-PB-1 is a suitable tracer for in vivo imaging of MAGL.

AB - 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 [11C]MA-PB-1 as an irreversible MAGL inhibitor PET tracer. The in vitro inhibitory activity, ex vivo distribution, brain kinetics and specificity of [11C]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 [11C]MA-PB-1 is a suitable tracer for in vivo imaging of MAGL.

KW - Biodistribution

KW - MAGL

KW - MJN110

KW - PET imaging

KW - [ C]MA-PB-1

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U2 - 10.1016/j.ejmech.2017.04.066

DO - 10.1016/j.ejmech.2017.04.066

M3 - Article

SN - 0223-5234

VL - 136

SP - 104

EP - 113

JO - European Journal of Medicinal Chemistry

JF - European Journal of Medicinal Chemistry

IS - 18 August 2017

ER -

Synthesis and preclinical evaluation of [11C]MA-PB-1 for in vivo imaging of brain monoacylglycerol lipase (MAGL)

Abstract

Keywords

UN SDGs

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