⁶⁸Ga-Labeled Maleimide for Blood Pool and Lymph PET Imaging through Covalent Bonding to Serum Albumin In Vivo.

ABSTRACT: This study aims to develop a novel ⁶⁸Ga-labeled tracer, which can covalently bind to albumin in vivo based on the maleimide-thiol strategy, and to evaluate its potential applications using positron emission tomography (PET). ⁶⁸Ga-labeled maleimide-monoamide-DOTA (denoted as [⁶⁸Ga]Ga-DM) was prepared conveniently with a high radiochemical yield (>90%) and radiochemical purity (>99%). Its molar activity was calculated as 249.60 ± 68.50 GBq/μmol, and the octanol-water partition coefficient (LogP) was -3.15 ± 0.08 with good stabilities. In vitro experiments showed that [⁶⁸Ga]Ga-DM can bind to albumin efficiently and rapidly, with a binding fraction of over 70%. High uptake and excellent retention in blood were observed with a long half-life (<

SUBMITTER: Feng L 

PROVIDER: S-EPMC9386703 | biostudies-literature | 2022 Aug

REPOSITORIES: biostudies-literature