PET imaging of brain aromatase in humans and rhesus monkeys by ¹¹C-labeled cetrozole analogs.

ABSTRACT: Aromatase is an estrogen synthetic enzyme that plays important roles in brain functions. To quantify aromatase expression in the brain by positron emission tomography (PET), we had previously developed [¹¹C]cetrozole, which showed high specificity and affinity. To develop more efficient PET tracer(s) for aromatase imaging, we synthesized three analogs of cetrozole. We synthesized meta-cetrozole, nitro-cetrozole, and iso-cetrozole, and prepared the corresponding ¹¹C-labeled tracers. The inhibitory activities of these three analogs toward aromatase were evaluated using marmoset placenta, and PET imaging of brain aromatase was performed using the ¹¹C-labeled tracers in monkeys. The most promising analog in the monkey study, iso-cetrozole, was evaluated in the

SUBMITTER: Takahashi K 

PROVIDER: S-EPMC8654920 | biostudies-literature | 2021 Dec

REPOSITORIES: biostudies-literature