[11C]PS13

The drug [11C]PS13 is a PET radioligand developed for imaging cyclooxygenase-1 (COX-1) in the human body, particularly in the brain. It has demonstrated excellent in vivo selectivity for COX-1 over COX-2 in both nonhuman primates and humans. It is chemically known as 11C-labeled 1,5-bis(4-methoxyphenyl)-3-(2,2,2-trifluoroethoxy)-1H-1,2,4-triazole. The radioligand has been successfully used in whole-body PET imaging to visualize organs with high COX-1 density, including the spleen, brain, lungs, kidneys, and gastrointestinal tract. It has also shown promise in oncology research, particularly for imaging ovarian cancer xenografts in preclinical models. When administered intravenously, [11C]PS13 shows high uptake in organs with high COX-1 density, extremely low free fraction in plasma (0.003 ± 0.001), no adverse pharmacological effects at the doses used for imaging, and a mean effective radiation dose of 4.6 ± 0.6 μSv/MBq. [11C]PS13 has been used to measure the in vivo potency of NSAIDs, assess COX-1 distribution in healthy humans, evaluate NSAID selectivity for COX-1 vs. COX-2, and potentially detect early-stage ovarian cancer in preclinical models. It has demonstrated that ketoprofen is a more potent COX-1 inhibitor than celecoxib, and that aspirin's unique mechanism of action does not significantly block [11C]PS13 binding.

Other names

11C-labeled 1,5-bis(4-methoxyphenyl)-3-(2,2,2-trifluoroethoxy)-1H-1,2,4-triazole