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- Chen, Zhen, et al.
(författare)
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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
- 2019
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Ingår i: Journal of Medicinal Chemistry. - : American Chemical Society (ACS). - 0022-2623 .- 1520-4804. ; 62:7, s. 3336-3353
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Tidskriftsartikel (refereegranskat)abstract
- 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.
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2. |
- Zhang, Ye, et al.
(författare)
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Application of graphdiyne oxide in photoelectrochemical-type photodetectors and ultrafast fiber lasers
- 2022
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Ingår i: Nano Today. - : Elsevier. - 1748-0132 .- 1878-044X. ; 47
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Tidskriftsartikel (refereegranskat)abstract
- Graphdiyne oxide (GDYO), the oxidized form of graphdiyne (GDY), has been widely explored for applica-tions in various technological fields owing to its fascinating properties. However, the research of GDYO for applications in photodetectors (PDs) and mode-locker has been lagging. Herein, we present experimental demonstrations of promising applications of GDYO for narrow-band photoelectrochemical (PEC)-type PDs with tunable performance. Moreover, the measured excellent nonlinear optical absorption of GDYO makes it a suitable material for mode-locking in ultrafast fiber lasers. Ultrastable pulses as short as 1.5 ps could be obtained from an Erbium-doped fiber laser based on GDYO at 1559 nm. These findings have been supported and interpreted by density functional theory (DFT) calculations as well as transient absorption dynamics studies. The presented results provide pathways for the future utilization of GDYO in high-performance optoelectronic devices.
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