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Synthesis and characterization of a novel 18 F-labeled 2, 5-diarylnicotinamide derivative targeting orexin 2 receptor

Medchemcomm. 2019-11; 
Hiroyuki Watanabe, ORCID logo *a Naoki Matsushita,a Yoichi Shimizu,ab Shimpei Iikuni,a Yuji Nakamoto,b Kaori Togashib and Masahiro Ono
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Biochemicals … 2 R expression cells Chinese hamster ovary (CHO)-K1 cells stably expressing human OX 1 R (CHO-OX 1 R) or OX 2 R (CHO-OX 2 R) were purchased from GenScript (M00224 and M00316, respectively) DAN-1 displayed … Get A Quote

摘要

Orexin 2 receptor (OX2R) is thought to play an important role in the arousal-promoting function, but its distribution and function in the pathophysiology of orexin-mediated disorders remains to be fully elucidated. In the present study, we synthesized and characterized a novel 18F-labeled 2,5-diarylnicotinamide (DAN) derivative as a potential positron emission tomography (PET) probe for in vivo imaging of OX2R. In in vitro binding experiments, [18F]DAN-1 selectively bound to OX2R. In a biodistribution study using normal mice, [18F]DAN-1 displayed moderate brain uptake (2.10% ID per g at 10 min post-injection). In addition, the radioactivity in the mouse brain at 30 min post-injection was significantly decreased... More

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