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

Zhang, Yiding; Kumata, Katsushi; Xie, Lin; Kurihara, Yusuke; Ogawa, Masanao; Kokufuta, Tomomi; Nengaki, Nobuki; Zhang, Ming-Rong

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

POSITRON emission tomography; BENZYL chloride; MAGNESIUM chloride; MICE; SMALL intestine; THIADIAZOLES

Pharmaceuticals (14248247), 2023, Vol 16, Issue 7, p963

1424-8247

Academic Journal

10.3390/ph16070963