Radiosynthesis and preclinical evaluation of a ⁶⁸Ga-labeled tetrahydroisoquinoline-based ligand for PET imaging of C-X-C chemokine receptor type 4 in an animal model of glioblastoma.

ABSTRACT:

Background

This study aimed to develop a novel positron emission tomography (PET) tracer, [⁶⁸Ga]Ga-TD-01, for CXCR4 imaging. To achieve this goal, the molecular scaffold of TIQ15 was tuned by conjugation with the DOTA chelator to make it suitable for ⁶⁸Ga radiolabeling.

Methods

A bifunctional chelator was prepared by conjugating the amine group of TIQ15 with p-NCS-Bz-DOTA, yielding TD-01, with a high yield (68.92%). TD-01 was then radiolabeled with ⁶⁸Ga using 0.1 M ammonium acetate at 60 °C for 10 min. A 1-h dynamic small animal PET/MRI study of the labeled compound in GL261-luc2 tumor-bearing mice was performed, and brain tumor uptake was assessed. Blocking studies involved pre-administration of TIQ15 (10 mg/kg) 10 min before the PET procedu

SUBMITTER: Suwattananuruk P 

PROVIDER: S-EPMC11335985 | biostudies-literature | 2024 Aug

REPOSITORIES: biostudies-literature