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

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Abstract

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 by co-injection with nonradioactive DAN-1, but high nonspecific binding was observed. These results suggested that further structural modifications of [18F]DAN-1 are needed to use it for imaging OX2R in the brain.

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

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Publication details

The article was received on 10 Aug 2019, accepted on 25 Oct 2019 and first published on 18 Nov 2019


Article type: Research Article
DOI: 10.1039/C9MD00397E
Med. Chem. Commun., 2019, Advance Article

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

    H. Watanabe, N. Matsushita, Y. Shimizu, S. Iikuni, Y. Nakamoto, K. Togashi and M. Ono, Med. Chem. Commun., 2019, Advance Article , DOI: 10.1039/C9MD00397E

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