Synthesis of [¹⁸F]PS13 and Evaluation as a PET Radioligand for Cyclooxygenase-1 in Monkey.

ABSTRACT: Cyclooxygenase-1 (COX-1) and its isozyme COX-2 are key enzymes in the syntheses of prostanoids. Imaging of COX-1 and COX-2 selective radioligands with positron emission tomography (PET) may clarify how these enzymes are involved in inflammatory conditions and assist in the discovery of improved anti-inflammatory drugs. We have previously labeled the selective high-affinity COX-1 ligand, 1,5-bis(4-methoxyphenyl)-3-(2,2,2-trifluoroethoxy)-1H-1,2,4-triazole (PS13), with carbon-11 (t_1/2 = 20.4 min). This radioligand ([¹¹C]PS13) has been successful for PET imaging of COX-1 in monkey and human brain and in periphery. [¹¹C]PS13 is being used in clinical investigations. Alternative labeling of PS13 with fluorine-18 (t_1/2 = 109.8 min)

SUBMITTER: Taddei C 

PROVIDER: S-EPMC9021884 | biostudies-literature | 2021 Feb

REPOSITORIES: biostudies-literature