The Glutaminase-1 Inhibitor [11C-carbony]BPTES: Synthesis and Positron Emission Tomography Study in Mice

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 known for its potent antitumor activity and plays significant role in senescent cell removal. In this study, we synthesized [11C-carbonyl]BPTES ([11C]BPTES) as positron emission tomography (PET) probe the first time assessed biodistribution mice using PET. [11C]BPTES was by reaction an amine precursor () with [11C-carbonyl]phenylacetyl acid anhydride ([11C]2), which prepared from [11C]CO2 benzyl magnesium chloride, followed situ treatment isobutyl chloroformate. The decay-corrected isolated radiochemical yield 9.5% (based on [11C]CO2) during synthesis 40 min. A PET study showed high uptake levels radioactivity liver, kidney, small intestine mice.