Literature DB >> 28486208

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

Muneer Ahamed1, Bala Attili1, Daisy van Veghel1, Maarten Ooms1, Philippe Berben1, Sofie Celen1, Michel Koole2, Lieven Declercq1, Juha R Savinainen3, Jarmo T Laitinen3, Alfons Verbruggen1, Guy Bormans4.   

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.
Copyright © 2017 Elsevier Masson SAS. All rights reserved.

Entities:  

Keywords:  Biodistribution; MAGL; MJN110; PET imaging; [(11)C]MA-PB-1

Mesh：

Substances：

Year:  2017        PMID： 28486208     DOI： 10.1016/j.ejmech.2017.04.066

Source DB:  PubMed          Journal:  Eur J Med Chem        ISSN： 0223-5234            Impact factor:   6.514


  10 in total

1.  First demonstration of in vivo mapping for regional brain monoacylglycerol lipase using PET with [11C]SAR127303.

Authors:  Tomoteru Yamasaki; Wakana Mori; Yiding Zhang; Akiko Hatori; Masayuki Fujinaga; Hidekatsu Wakizaka; Yusuke Kurihara; Lu Wang; Nobuki Nengaki; Tomoyuki Ohya; Steven H Liang; Ming-Rong Zhang
Journal:  Neuroimage       Date:  2018-05-05       Impact factor: 6.556

2.  Design, Synthesis, and Evaluation of 18F-Labeled Monoacylglycerol Lipase Inhibitors as Novel Positron Emission Tomography Probes.

Authors:  Zhen Chen; Wakana Mori; Hualong Fu; Michael A Schafroth; Akiko Hatori; Tuo Shao; Genwei Zhang; Richard S Van; Yiding Zhang; Kuan Hu; Masayuki Fujinaga; Lu Wang; Vasily Belov; Daisuke Ogasawara; Pilar Giffenig; Xiaoyun Deng; Jian Rong; Qingzhen Yu; Xiaofei Zhang; Mikhail I Papisov; Yihan Shao; Thomas L Collier; Jun-An Ma; Benjamin F Cravatt; Lee Josephson; Ming-Rong Zhang; Steven H Liang
Journal:  J Med Chem       Date:  2019-09-26       Impact factor: 7.446

3.  Design, Synthesis, and Evaluation of Reversible and Irreversible Monoacylglycerol Lipase Positron Emission Tomography (PET) Tracers Using a "Tail Switching" Strategy on a Piperazinyl Azetidine Skeleton.

Authors:  Zhen Chen; Wakana Mori; Xiaoyun Deng; Ran Cheng; Daisuke Ogasawara; Genwei Zhang; Michael A Schafroth; Kenneth Dahl; Hualong Fu; Akiko Hatori; Tuo Shao; Yiding Zhang; Tomoteru Yamasaki; Xiaofei Zhang; Jian Rong; Qingzhen Yu; Kuan Hu; Masayuki Fujinaga; Lin Xie; Katsushi Kumata; Yuancheng Gou; Jingjin Chen; Shuyin Gu; Liang Bao; Lu Wang; Thomas Lee Collier; Neil Vasdev; Yihan Shao; Jun-An Ma; Benjamin F Cravatt; Christopher Fowler; Lee Josephson; Ming-Rong Zhang; Steven H Liang
Journal:  J Med Chem       Date:  2019-03-21       Impact factor: 7.446

Review 4.  Using molecular imaging to understand early schizophrenia-related psychosis neurochemistry: a review of human studies.

Authors:  Christin Schifani; Sina Hafizi; Tania Da Silva; Jeremy Joseph Watts; M Saad Khan; Romina Mizrahi
Journal:  Int Rev Psychiatry       Date:  2017-12-08

Review 5.  2-Arachidonoylglycerol Modulation of Anxiety and Stress Adaptation: From Grass Roots to Novel Therapeutics.

Authors:  Gaurav Bedse; Mathew N Hill; Sachin Patel
Journal:  Biol Psychiatry       Date:  2020-03-17       Impact factor: 13.382

6.  In Vitro and in Vivo Evaluation of 11C-Labeled Azetidinecarboxylates for Imaging Monoacylglycerol Lipase by PET Imaging Studies.

Authors:  Ran Cheng; Wakana Mori; Longle Ma; Mireille Alhouayek; Akiko Hatori; Yiding Zhang; Daisuke Ogasawara; Gengyang Yuan; Zhen Chen; Xiaofei Zhang; Hang Shi; Tomoteru Yamasaki; Lin Xie; Katsushi Kumata; Masayuki Fujinaga; Yuji Nagai; Takafumi Minamimoto; Mona Svensson; Lu Wang; Yunfei Du; Mary Jo Ondrechen; Neil Vasdev; Benjamin F Cravatt; Christopher Fowler; Ming-Rong Zhang; Steven H Liang
Journal:  J Med Chem       Date:  2018-03-09       Impact factor: 7.446

Review 7.  Positron Emission Tomography Imaging of the Endocannabinoid System: Opportunities and Challenges in Radiotracer Development.

Authors:  Lu Hou; Jian Rong; Ahmed Haider; Daisuke Ogasawara; Cassis Varlow; Michael A Schafroth; Linjing Mu; Jiefeng Gan; Hao Xu; Christopher J Fowler; Ming-Rong Zhang; Neil Vasdev; Simon Ametamey; Benjamin F Cravatt; Lu Wang; Steven H Liang
Journal:  J Med Chem       Date:  2020-12-30       Impact factor: 7.446

8.  Novel Reversible-Binding PET Ligands for Imaging Monoacylglycerol Lipase Based on the Piperazinyl Azetidine Scaffold.

Authors:  Jian Rong; Wakana Mori; Xiaotian Xia; Michael A Schafroth; Chunyu Zhao; Richard S Van; Tomoteru Yamasaki; Jiahui Chen; Zhiwei Xiao; Ahmed Haider; Daisuke Ogasawara; Atsuto Hiraishi; Tuo Shao; Yiding Zhang; Zhen Chen; Fuwen Pang; Kuan Hu; Lin Xie; Masayuki Fujinaga; Katsushi Kumata; Yuancheng Gou; Yang Fang; Shuyin Gu; Huiyi Wei; Liang Bao; Hao Xu; Thomas L Collier; Yihan Shao; Richard E Carson; Benjamin F Cravatt; Lu Wang; Ming-Rong Zhang; Steven H Liang
Journal:  J Med Chem       Date:  2021-09-27       Impact factor: 8.039

9.  Target occupancy study and whole-body dosimetry with a MAGL PET ligand [11C]PF-06809247 in non-human primates.

Authors:  Ryosuke Arakawa; Akihiro Takano; Sangram Nag; Zhisheng Jia; Nahid Amini; Kevin P Maresca; Lei Zhang; Edmund J Keliher; Christopher R Butler; Justin R Piro; Tarek A Samad; Deborah Smith; Deane Nason; Steve O'Neil; Patrick Trapa; Kari R Fonseca; John Litchfield; Timothy McCarthy; Richard E Carson; Christer Halldin
Journal:  EJNMMI Res       Date:  2022-03-04       Impact factor: 3.138

10.  Development of a highly-specific 18F-labeled irreversible positron emission tomography tracer for monoacylglycerol lipase mapping.

Authors:  Zhen Chen; Wakana Mori; Jian Rong; Michael A Schafroth; Tuo Shao; Richard S Van; Daisuke Ogasawara; Tomoteru Yamasaki; Atsuto Hiraishi; Akiko Hatori; Jiahui Chen; Yiding Zhang; Kuan Hu; Masayuki Fujinaga; Jiyun Sun; Qingzhen Yu; Thomas L Collier; Yihan Shao; Benjamin F Cravatt; Lee Josephson; Ming-Rong Zhang; Steven H Liang
Journal:  Acta Pharm Sin B       Date:  2021-04-01       Impact factor: 11.413
  10 in total

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