Abstract
Bis-2-(5-phenylacetamido-1,3,4-thiadiazol-2-yl)ethyl sulfide (BPTES) is a selective inhibitor of glutaminase-1 (GLS1), consequently inhibiting glutaminolysis. BPTES is known for its potent antitumor activity and plays a significant role in senescent cell removal. In this study, we synthesized [(11)C-carbonyl]BPTES ([(11)C]BPTES) as a positron emission tomography (PET) probe for the first time and assessed its biodistribution in mice using PET. [(11)C]BPTES was synthesized by the reaction of an amine precursor () with [(11)C-carbonyl]phenylacetyl acid anhydride ([(11)C]2), which was prepared from [(11)C]CO(2) and benzyl magnesium chloride, followed by in situ treatment with isobutyl chloroformate. The decay-corrected isolated radiochemical yield of [(11)C]BPTES was 9.5% (based on [(11)C]CO(2)) during a synthesis time of 40 min. A PET study with [(11)C]BPTES showed high uptake levels of radioactivity in the liver, kidney, and small intestine of mice.