Fluorine-18 isotope labeling for positron emission tomography imaging. Direct evidence for DBPR211 as a peripherally restricted CB1 inverse agonist. Issue 1 (1st January 2019)

• Record Type: Journal Article
• Authors: Chang, Chun-Ping; Huang, Ho-Lien; Huang, Jing-Kai; Hung, Ming-Shiu; Wu, Chien-Huang; Song, Jen-Shin; Lee, Chia-Jui; Yu, Chung-Shan; Shia, Kak-Shan
• Is Part Of: Bioorganic & medicinal chemistry. Volume 27:Issue 1(2019)
• Page Start: 216
• Page End: 223
• Publication Date: 2019-01-01
• Subjects: Cannabinoid-1 antagonist -- Positron emission tomography -- Peripherally restricted CB1 inverse agonist -- Blood-brain barrier; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; Biochemistry -- Periodicals; Chemistry, Clinical -- Periodicals; Chemistry, Organic -- Periodicals; Chimie bio-organique -- Périodiques; Chimie pharmaceutique -- Périodiques; 615.19
• DOI: 10.1016/j.bmc.2018.11.043
• Languages: English
• ISSNs: 0968-0896

Abstract

Graphical abstract: Abstract: The [ 18 F] isotope-labelled CB1 inverse agonist3 was elaborated and synthesized for positron emission tomography scanning studies. After immediate purification and calibration with its unlabeled counterpart, compound3 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.