The efficiency of 18F labelling of a prostate specific membrane antigen ligand via strain-promoted azide–alkyne reaction: reaction speed versus hydrophilicity. Issue 56 (27th June 2018)

• Record Type: Journal Article
• Authors: Wang, Mengzhe; McNitt, Christopher D.; Wang, Hui; Ma, Xiaofen; Scarry, Sarah M.; Wu, Zhanhong; Popik, Vladimir V.; Li, Zibo
• Is Part Of: Chemical communications. Volume 54:Issue 56(2018)
• Page Start: 7810
• Page End: 7813
• Publication Date: 2018-06-27
• Subjects: Chemistry -- Periodicals; 540
• DOI: 10.1039/c8cc03999b
• Languages: English
• ISSNs: 1359-7345

Abstract

Abstract : Here we report the 18 F labeling of a prostate specific membrane antigen ligand via a strain promoted oxa-dibenzocyclooctyne- or bicyclo[6.1.0]nonyne-azide reaction. Abstract : Here we report the 18 F labeling of a prostate specific membrane antigen (PSMA) ligand via a strain promoted oxa-dibenzocyclooctyne (ODIBO)- or bicyclo[6.1.0]nonyne (BCN)-azide reaction. Although ODIBO reacts with azide 20 fold faster than BCN, in vivo PET imaging suggests that 18 F-BCN-azide-PSMA demonstrated much higher tumor uptake and a much higher tumor to background contrast.