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Identification and Development of an Irreversible Monoacylglycerol Lipase (MAGL) Positron Emission Tomography (PET) Radioligand With High Specificity

Identification and Development of an Irreversible Monoacylglycerol Lipase (MAGL) Positron Emission Tomography (PET) Radioligand With High Specificity

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, etc.

J Med Chem. 2019 Sep 26;62(18):8532-8543.

PMID: 31483137

Abstract:

Monoacylglycerol lipase (MAGL), a serine hydrolase extensively expressed throughout the brain, serves as a key gatekeeper regulating the tone of endocannabinoid signaling. Preclinically, inhibition of MAGL is known to provide therapeutic benefits for a number of neurological disorders. The availability of a MAGL-specific positron emission tomography (PET) ligand would considerably facilitate the development and clinical characterization of MAGL inhibitors via noninvasive and quantitative PET imaging. Herein, we report the identification of the potent and selective irreversible MAGL inhibitor 7 (PF-06809247) as a suitable radioligand lead, which upon radiolabeling was found to exhibit a high level of MAGL specificity; this enabled cross-species measurement of MAGL brain expression (Bmax), assessment of in vivo binding in the rat, and nonhuman primate PET imaging.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP931086010	Serine Hydrolase Inhibitor-7		931086-01-0	Price

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