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Brief Report

A New Positron Emission Tomography Probe for Orexin Receptors Neuroimaging

Chengdu Institute of Biology, Chinese Academy of Sciences, Chengdu 610041, China
Athinoula A. Martinos Center for Biomedical Imaging, Department of Radiology, Massachusetts General Hospital, Harvard Medical School, Charlestown, MA 02129, USA
University of Chinese Academy of Sciences, Beijing 100049, China
Author to whom correspondence should be addressed.
Molecules 2020, 25(5), 1018;
Received: 17 December 2019 / Revised: 19 February 2020 / Accepted: 20 February 2020 / Published: 25 February 2020
(This article belongs to the Special Issue Radiolabelled Molecules for Brain Imaging with PET and SPECT)
The orexin receptor (OX) is critically involved in motivation and sleep−wake regulation and holds promising therapeutic potential in various mood disorders. To further investigate the role of orexin receptors (OXRs) in the living human brain and to evaluate the treatment potential of orexin-targeting therapeutics, we herein report a novel PET probe ([11C]CW24) for OXRs in the brain. CW24 has moderate binding affinity for OXRs (IC50 = 0.253 μM and 1.406 μM for OX1R and OX2R, respectively) and shows good selectivity to OXRs over 40 other central nervous system (CNS) targets. [11C]CW24 has high brain uptake in rodents and nonhuman primates, suitable metabolic stability, and appropriate distribution and pharmacokinetics for brain positron emission tomography (PET) imaging. [11C]CW24 warrants further evaluation as a PET imaging probe of OXRs in the brain. View Full-Text
Keywords: orexin receptors; PET; radiotracer; imaging orexin receptors; PET; radiotracer; imaging
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MDPI and ACS Style

Bai, P.; Bai, S.; Placzek, M.S.; Lu, X.; Fiedler, S.A.; Ntaganda, B.; Wey, H.-Y.; Wang, C. A New Positron Emission Tomography Probe for Orexin Receptors Neuroimaging. Molecules 2020, 25, 1018.

AMA Style

Bai P, Bai S, Placzek MS, Lu X, Fiedler SA, Ntaganda B, Wey H-Y, Wang C. A New Positron Emission Tomography Probe for Orexin Receptors Neuroimaging. Molecules. 2020; 25(5):1018.

Chicago/Turabian Style

Bai, Ping, Sha Bai, Michael S. Placzek, Xiaoxia Lu, Stephanie A. Fiedler, Brenda Ntaganda, Hsiao-Ying Wey, and Changning Wang. 2020. "A New Positron Emission Tomography Probe for Orexin Receptors Neuroimaging" Molecules 25, no. 5: 1018.

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