Identification of a major radiometabolite of [11C]PBB3

Authors: Hashimoto H, Kawamura K, Takei M, Igarashi N, Fujishiro T, Shiomi S, Watanabe R, Muto M, Furutsuka K, Ito T, Yamasaki K, Yui J, Nemoto K, Kimura Y, Higuchi M, Zhang M-R
Publication: Nucl Med Biol
Keywords: cytochrome P450 (CYP), PET, radiometabolite, sulfotransferase, tau probe
Software: ADMET Predictor®

Introduction

[11C]PBB3 is a clinically used positron emission tomography (PET) probe for in vivo imaging of tau pathology in the brain. Our previous study showed that [11C]PBB3 was rapidly decomposed to a polar radiometabolite in the plasma of mice. For the pharmacokinetic evaluation of [11C]PBB3 it is important to elucidate the characteristics of radiometabolites. In this study, we identified the chemical structure of a major radiometabolite of [11C]PBB3 and proposed the metabolic pathway of [11C]PBB3.