The efficiency of 18F labelling of a prostate specific membrane antigen ligand via strain-promoted azide–alkyne reaction: reaction speed versus hydrophilicity

Autor: Vladimir V. Popik, Xiaofen Ma, Zhanhong Wu, Zibo Li, Hui Wang, Mengzhe Wang, Christopher D. McNitt, Sarah M. Scarry
Rok vydání: 2018
Předmět:
Zdroj: Chemical Communications. 54:7810-7813
ISSN: 1364-548X
1359-7345
DOI: 10.1039/c8cc03999b
Popis: Here we report the 18F 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 18F-BCN-azide-PSMA demonstrated much higher tumor uptake and a much higher tumor to background contrast.
Databáze: OpenAIRE