| Publication |
Sentence |
Publish Date |
Extraction Date |
Species |
| Bin Zhu, Peter J Connolly, Yue-Mei Zhang, Mark E McDonnell, Haiyan Bian, Shu-Chen Lin, Li Liu, Sui-Po Zhang, Kristen M Chevalier, Michael R Brandt, Cynthia M Milligan, Christopher M Flores, Mark J Maciela. The discovery of azetidine-piperazine di-amides as potent, selective and reversible monoacylglycerol lipase (MAGL) inhibitors. Bioorganic & medicinal chemistry letters. vol 30. issue 14. 2021-06-01. PMID:32527545. |
monoacylglycerol lipase (magl) is the enzyme that is primarily responsible for hydrolyzing the endocannabinoid 2-arachidononylglycerol (2-ag) to arachidonic acid (aa). |
2021-06-01 |
2023-08-13 |
rat |
| C M Diester, A H Lichtman, S S Negu. Behavioral Battery for Testing Candidate Analgesics in Mice. II. Effects of Endocannabinoid Catabolic Enzyme Inhibitors and ∆9-Tetrahydrocannabinol. The Journal of pharmacology and experimental therapeutics. vol 377. issue 2. 2021-05-13. PMID:33622769. |
enhanced signaling of the endocannabinoid (ecb) system through inhibition of the catabolic enzymes monoacylglycerol lipase (magl) and fatty acid amide hydrolase (faah) has received increasing interest for development of candidate analgesics. |
2021-05-13 |
2023-08-13 |
mouse |
| Bin Zhu, Peter J Connolly, Sui-Po Zhang, Kristen M Chevalier, Cynthia M Milligan, Christopher M Flores, Mark J Maciela. The discovery of diazetidinyl diamides as potent and reversible inhibitors of monoacylglycerol lipase (MAGL). Bioorganic & medicinal chemistry letters. vol 30. issue 12. 2021-05-12. PMID:32334914. |
monoacylglycerol lipase (magl) has emerged as an attractive drug target because of its important role in regulating the endocannabinoid 2-arachidonoylglycerol (2-ag) and its hydrolysis product arachidonic acid (aa) in the brain. |
2021-05-12 |
2023-08-13 |
rat |
| Natasha L Grimsey, Juha R Savinainen, Bala Attili, Muneer Ahame. Regulating membrane lipid levels at the synapse by small-molecule inhibitors of monoacylglycerol lipase: new developments in therapeutic and PET imaging applications. Drug discovery today. vol 25. issue 2. 2021-04-30. PMID:31622747. |
monoacylglycerol lipase (magl) is a major endocannabinoid hydrolyzing enzyme and can be regulated to control endogenous lipid levels in the brain. |
2021-04-30 |
2023-08-13 |
Not clear |
| Carlotta Granchi, Giulia Bononi, Rebecca Ferrisi, Eleonora Gori, Giulia Mantini, Sandra Glasmacher, Giulio Poli, Stefano Palazzolo, Isabella Caligiuri, Flavio Rizzolio, Vincenzo Canzonieri, Tiziana Perin, Jürg Gertsch, Andrea Sodi, Elisa Giovannetti, Marco Macchia, Filippo Minutolo, Tiziano Tuccinardi, Andrea Chicc. Design, synthesis and biological evaluation of second-generation benzoylpiperidine derivatives as reversible monoacylglycerol lipase (MAGL) inhibitors. European journal of medicinal chemistry. vol 209. 2021-04-20. PMID:33045662. |
an interesting enzyme of the endocannabinoid system is monoacylglycerol lipase (magl). |
2021-04-20 |
2023-08-13 |
mouse |
| Giulia Bononi, Giulio Poli, Flavio Rizzolio, Tiziano Tuccinardi, Marco Macchia, Filippo Minutolo, Carlotta Granch. An updated patent review of monoacylglycerol lipase (MAGL) inhibitors (2018-present). Expert opinion on therapeutic patents. vol 31. issue 2. 2021-04-06. PMID:33085920. |
monoacylglycerol lipase (magl) belongs to the endocannabinoid system and is responsible for the inactivation of endocannabinoid 2-arachidonoylglycerol. |
2021-04-06 |
2023-08-13 |
Not clear |
| 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 Lian. Positron Emission Tomography Imaging of the Endocannabinoid System: Opportunities and Challenges in Radiotracer Development. Journal of medicinal chemistry. vol 64. issue 1. 2021-03-08. PMID:33379862. |
herein, we summarized the recent development of pet tracers for imaging cannabinoid receptors 1 (cb1r) and 2 (cb2r) as well as the key enzymes monoacylglycerol lipase (magl) and fatty acid amide hydrolase (faah), particularly focusing on pet neuroimaging applications. |
2021-03-08 |
2023-08-13 |
human |
| Gaurav Bedse, Mathew N Hill, Sachin Pate. 2-Arachidonoylglycerol Modulation of Anxiety and Stress Adaptation: From Grass Roots to Novel Therapeutics. Biological psychiatry. vol 88. issue 7. 2021-03-03. PMID:32197779. |
although initial preclinical and clinical development efforts focused on pharmacological inhibition of fatty acid amide hydrolase to elevate levels of the endocannabinoid anandamide, more recent efforts have focused on inhibition of monoacylglycerol lipase (magl) to enhance signaling of the most abundant and efficacious endocannabinoid ligand, 2-arachidonoylglycerol (2-ag). |
2021-03-03 |
2023-08-13 |
Not clear |
| Amal Thomas, Bright N Okine, David P Finn, Willias Masoch. Peripheral deficiency and antiallodynic effects of 2-arachidonoyl glycerol in a mouse model of paclitaxel-induced neuropathic pain. Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie. vol 129. 2021-03-01. PMID:32603895. |
we also evaluated the peripheral antiallodynic activity of the endocannabinoid 2-arachidonoyl glycerol (2-ag) and an inhibitor of monoacylglycerol lipase (magl), an enzyme responsible for 2-ag hydrolysis. |
2021-03-01 |
2023-08-13 |
mouse |
| Alessandra Longaretti, Chiara Forastieri, Marina Gabaglio, Tiziana Rubino, Elena Battaglioli, Francesco Ruscon. Termination of acute stress response by the endocannabinoid system is regulated through lysine-specific demethylase 1-mediated transcriptional repression of 2-AG hydrolases ABHD6 and MAGL. Journal of neurochemistry. vol 155. issue 1. 2021-02-10. PMID:32141088. |
we employ mouse models of stress response coupled to gene expression analyses, unravelling that in response to acute psychosocial stress in the mouse hippocampus, ecs-mediated synaptic modulation is enhanced via transcriptional repression of two enzymes involved in 2-ag degradation: α/β-hydrolase domain containing 6 (abhd6) and monoacylglycerol lipase (magl). |
2021-02-10 |
2023-08-13 |
mouse |
| Jing Wang, Xiaohua Zhang, Chongmei Yang, Shulei Zha. Effect of monoacylglycerol lipase inhibition on intestinal permeability in chronic stress model. Biochemical and biophysical research communications. vol 525. issue 4. 2020-12-28. PMID:32173532. |
the endocannabinoid 2-arachidonoylglycerol (2-ag) is an anti-nociceptive lipid, which is inactivated through cellular uptake and subsequent catabolism by monoacylglycerol lipase (magl). |
2020-12-28 |
2023-08-13 |
rat |
| Emily Kabeiseman, Riley Paulsen, Brian D Burrel. Characterization of a monoacylglycerol lipase in the medicinal leech, Hirudo verbana. Comparative biochemistry and physiology. Part B, Biochemistry & molecular biology. vol 243-244. 2020-11-11. PMID:32205202. |
among the endocannabinoids, 2-arachydonoyl glycerol (2-ag) is the most prevalent endocannabinoid and monoacylglycerol lipase (magl) is a serine hydrolase primarily responsible for metabolizing 2-ag in mammals. |
2020-11-11 |
2023-08-13 |
Not clear |
| Qin Yang, Shunli Sun, Wei Liu, Qingguang Liu, Jibing Wan. Hypoxia training improves hepatic steatosis partly by downregulation of CB1 receptor in obese mice. Biochemical and biophysical research communications. vol 525. issue 3. 2020-11-04. PMID:32122652. |
the present study investigated the effects of ht, a new prospective weight-loss method, on nutritionally obese mice and demonstrated that ht significantly reduced body weight, fat mass, transcriptional expression of liver endocannabinoid receptor 1 (cb1), biosynthetic enzyme diacylglycerol lipase α (daglα) and improved the transcriptional expression of degrading enzyme monoacylglycerol lipase (magl). |
2020-11-04 |
2023-08-13 |
mouse |
| Ren-Shi Li, Ryo Fukumori, Tomoki Takeda, Yingxia Song, Satoshi Morimoto, Ruri Kikura-Hanajiri, Taku Yamaguchi, Kazuhito Watanabe, Kousuke Aritake, Yoshitaka Tanaka, Hideyuki Yamada, Tsuneyuki Yamamoto, Yuji Ishi. Elevation of endocannabinoids in the brain by synthetic cannabinoid JWH-018: mechanism and effect on learning and memory. Scientific reports. vol 9. issue 1. 2020-10-26. PMID:31270353. |
biochemical analyses revealed that this was the result of suppression of two hydrolases involved in endocannabinoid degradation (fatty acid amide hydrolase [faah] and monoacylglycerol lipase [magl]). |
2020-10-26 |
2023-08-13 |
Not clear |
| Sally Miller, Shashank Kulkarni, Alex Ciesielski, Spyros P Nikas, Ken Mackie, Alexandros Makriyannis, Alex Straike. Controlled-Deactivation CB1 Receptor Ligands as a Novel Strategy to Lower Intraocular Pressure. Pharmaceuticals (Basel, Switzerland). vol 11. issue 2. 2020-09-30. PMID:29786643. |
we have recently shown that blocking monoacylglycerol lipase (magl), an enzyme that breaks the endocannabinoid 2-arachidonoyl glycerol (2-ag), substantially lowers iop. |
2020-09-30 |
2023-08-13 |
mouse |
| 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 Lian. 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. Journal of medicinal chemistry. vol 62. issue 7. 2020-09-14. PMID:30829483. |
monoacylglycerol lipase (magl) is a serine hydrolase that degrades 2-arachidonoylglycerol (2-ag) in the endocannabinoid system (ecb). |
2020-09-14 |
2023-08-13 |
Not clear |
| Sara Martínez-Torres, Laura Cutando, Antoni Pastor, Ako Kato, Kenji Sakimura, Rafael de la Torre, Emmanuel Valjent, Rafael Maldonado, Masanobu Kano, Andrés Ozait. Monoacylglycerol lipase blockade impairs fine motor coordination and triggers cerebellar neuroinflammation through cyclooxygenase-2. Brain, behavior, and immunity. vol 81. 2020-08-14. PMID:31251974. |
monoacylglycerol lipase (magl) is the main enzyme implicated in the degradation of the most abundant endocannabinoid in the brain, 2-arachidonoylglycerol (2-ag), producing arachidonic acid (aa) and glycerol. |
2020-08-14 |
2023-08-13 |
mouse |
| Ryan M Wyatt, Ian Fraser, Natalie Welty, Brian Lord, Michelle Wennerholm, Steven Sutton, Michael K Ameriks, Christine Dugovic, Sujin Yun, Allison White, Leslie Nguyen, Tatiana Koudriakova, Gaochao Tian, Javier Suarez, Lawrence Szewczuk, William Bonnette, Kay Ahn, Brahma Ghosh, Christopher M Flores, Peter J Connolly, Bin Zhu, Mark J Macielag, Michael R Brandt, Kristen Chevalier, Sui-Po Zhang, Timothy Lovenberg, Pascal Bonaventur. Pharmacologic Characterization of JNJ-42226314, [1-(4-Fluorophenyl)indol-5-yl]-[3-[4-(thiazole-2-carbonyl)piperazin-1-yl]azetidin-1-yl]methanone, a Reversible, Selective, and Potent Monoacylglycerol Lipase Inhibitor. The Journal of pharmacology and experimental therapeutics. vol 372. issue 3. 2020-07-06. PMID:31818916. |
the serine hydrolase monoacylglycerol lipase (magl) is the rate-limiting enzyme responsible for the degradation of the endocannabinoid 2-arachidonoylglycerol (2-ag) into arachidonic acid and glycerol. |
2020-07-06 |
2023-08-13 |
human |
| Ryan M Wyatt, Ian Fraser, Natalie Welty, Brian Lord, Michelle Wennerholm, Steven Sutton, Michael K Ameriks, Christine Dugovic, Sujin Yun, Allison White, Leslie Nguyen, Tatiana Koudriakova, Gaochao Tian, Javier Suarez, Lawrence Szewczuk, William Bonnette, Kay Ahn, Brahma Ghosh, Christopher M Flores, Peter J Connolly, Bin Zhu, Mark J Macielag, Michael R Brandt, Kristen Chevalier, Sui-Po Zhang, Timothy Lovenberg, Pascal Bonaventur. Pharmacologic Characterization of JNJ-42226314, [1-(4-Fluorophenyl)indol-5-yl]-[3-[4-(thiazole-2-carbonyl)piperazin-1-yl]azetidin-1-yl]methanone, a Reversible, Selective, and Potent Monoacylglycerol Lipase Inhibitor. The Journal of pharmacology and experimental therapeutics. vol 372. issue 3. 2020-07-06. PMID:31818916. |
significance statement: potentiation of endocannabinoid signaling activity via inhibition of the serine hydrolase monoacylglycerol lipase (magl) is an appealing strategy in the development of treatments for several disorders, including ones related to mood, pain, and inflammation. |
2020-07-06 |
2023-08-13 |
human |
| Lei Zhang, Christopher R Butler, Kevin P Maresca, Akihiro Takano, Sangram Nag, Zhisheng Jia, Ryosuke Arakawa, Justin R Piro, Tarek Samad, Deborah L Smith, Deane M Nason, Steven O'Neil, Laura McAllister, Klaas Schildknegt, Patrick Trapa, Timothy J McCarthy, Anabella Villalobos, Christer Halldi. Identification and Development of an Irreversible Monoacylglycerol Lipase (MAGL) Positron Emission Tomography (PET) Radioligand with High Specificity. Journal of medicinal chemistry. vol 62. issue 18. 2020-06-22. PMID:31483137. |
monoacylglycerol lipase (magl), a serine hydrolase extensively expressed throughout the brain, serves as a key gatekeeper regulating the tone of endocannabinoid signaling. |
2020-06-22 |
2023-08-13 |
Not clear |