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Fluorine-18 isotope labeling for positron emission tomography imaging. Direct evidence for DBPR211 as a peripherally restricted CB1 inverse agonist
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Fluorine-18 isotope labeling for positron emission tomography imaging. Direct evidence for DBPR211 as a peripherally restricted CB1 inverse agonist

Chun-Ping Chang, Ho-Lien Huang, Jing-Kai Huang, Ming-Shiu Hung, Chien-Huang Wu, Jen-Shin Song, Chia-Jui Lee, Chung-Shan YuKak-Shan Shia
Bioorganic and Medicinal Chemistry
2018

摘要

Blood-brain barrier Cannabinoid-1 antagonist Peripherally restricted CB1 inverse agonist Positron emission tomography Biochemistry Molecular Medicine Molecular Biology Pharmaceutical Science Drug Discovery Clinical Biochemistry Organic Chemistry
The [ 18 F] isotope-labelled CB1 inverse agonist 3 was elaborated and synthesized for positron emission tomography scanning studies. After immediate purification and calibration with its unlabeled counterpart, compound 3 was intravenously injected in mice and revealed that its distribution percentage in brain over 90-min scans among five region of interests, including brain, liver, heart, thigh muscle and kidney was lower than 1%, thus providing direct evidence to justify itself as a peripherally restricted CB1 antagonist.

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