Sökning: onr:"swepub:oai:DiVA.org:umu-158574" > Design, Synthesis, ...
Fältnamn | Indikatorer | Metadata |
---|---|---|
000 | 03755naa a2200697 4500 | |
001 | oai:DiVA.org:umu-158574 | |
003 | SwePub | |
008 | 190527s2019 | |||||||||||000 ||eng| | |
024 | 7 | a https://urn.kb.se/resolve?urn=urn:nbn:se:umu:diva-1585742 URI |
024 | 7 | a https://doi.org/10.1021/acs.jmedchem.8b017782 DOI |
040 | a (SwePub)umu | |
041 | a engb eng | |
042 | 9 SwePub | |
072 | 7 | a ref2 swepub-contenttype |
072 | 7 | a art2 swepub-publicationtype |
100 | 1 | a Chen, Zhen4 aut |
245 | 1 0 | a 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 |
264 | c 2019-03-04 | |
264 | 1 | b American Chemical Society (ACS),c 2019 |
338 | a print2 rdacarrier | |
520 | a Monoacylglycerol lipase (MAGL) is a senile hydrolase that degrades 2-arachidonoylglycerol (2-AG) in the endocannabinoid system (eCB). Selective inhibition of MAGL has emerged as a potential therapeutic approach for the treatment of diverse pathological conditions, including chronic pain, inflammation, cancer, and neurodegeneration. Herein, we disclose a novel array of reversible and irreversible MAGL inhibitors by means of "tail switching" on a piperazinyl azetidine scaffold. We developed a lead irreversible-binding MAGL inhibitor 8 and reversible-binding compounds 17 and 37, which are amenable for radiolabeling with C-11 or F-18. [C-11]8 ([C-11]MAGL-2-11) exhibited high brain uptake and excellent binding specificity in the brain toward MAGL. Reversible radioligands [C-11]17 ([C-11]PAD) and [F-18]37 ([F-18]MAGL-4-11) also demonstrated excellent in vivo binding specificity toward MAGL in peripheral organs. This work may pave the way for the development of MAGL-targeted positron emission tomography tracers with tunability in reversible and irreversible binding mechanisms. | |
650 | 7 | a MEDICIN OCH HÄLSOVETENSKAPx Medicinsk bioteknologix Medicinsk bioteknologi0 (SwePub)304012 hsv//swe |
650 | 7 | a MEDICAL AND HEALTH SCIENCESx Medical Biotechnologyx Medical Biotechnology0 (SwePub)304012 hsv//eng |
700 | 1 | a Mori, Wakana4 aut |
700 | 1 | a Deng, Xiaoyun4 aut |
700 | 1 | a Cheng, Ran4 aut |
700 | 1 | a Ogasawara, Daisuke4 aut |
700 | 1 | a Zhang, Genwei4 aut |
700 | 1 | a Schafroth, Michael A.4 aut |
700 | 1 | a Dahl, Kenneth4 aut |
700 | 1 | a Fu, Hualong4 aut |
700 | 1 | a Hatori, Akiko4 aut |
700 | 1 | a Shao, Tuo4 aut |
700 | 1 | a Zhang, Yiding4 aut |
700 | 1 | a Yamasaki, Tomoteru4 aut |
700 | 1 | a Zhang, Xiaofei4 aut |
700 | 1 | a Rong, Jian4 aut |
700 | 1 | a Yu, Qngzhen4 aut |
700 | 1 | a Hu, Kuan4 aut |
700 | 1 | a Fujinaga, Masayuki4 aut |
700 | 1 | a Xie, Lin4 aut |
700 | 1 | a Kumata, Katsushi4 aut |
700 | 1 | a Gou, Yuancheng4 aut |
700 | 1 | a Chen, Jingjin4 aut |
700 | 1 | a Gu, Shuyin4 aut |
700 | 1 | a Bao, Liang4 aut |
700 | 1 | a Wang, Lu4 aut |
700 | 1 | a Collier, Thomas Lee4 aut |
700 | 1 | a Vasdev, Neil4 aut |
700 | 1 | a Shao, Yihan4 aut |
700 | 1 | a Ma, Jun-An4 aut |
700 | 1 | a Cravatt, Benjamin F.4 aut |
700 | 1 | a Fowler, Christopheru Umeå universitet,Farmakologi4 aut0 (Swepub:umu)chfo0001 |
700 | 1 | a Josephson, Lee4 aut |
700 | 1 | a Zhang, Ming-Rong4 aut |
700 | 1 | a Liang, Steven H.4 aut |
710 | 2 | a Umeå universitetb Farmakologi4 org |
773 | 0 | t Journal of Medicinal Chemistryd : American Chemical Society (ACS)g 62:7, s. 3336-3353q 62:7<3336-3353x 0022-2623x 1520-4804 |
856 | 4 | u https://europepmc.org/articles/pmc6581563?pdf=render |
856 | 4 8 | u https://urn.kb.se/resolve?urn=urn:nbn:se:umu:diva-158574 |
856 | 4 8 | u https://doi.org/10.1021/acs.jmedchem.8b01778 |
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