Whole-body biodistribution of [11C]oseltamivir and [11C]Ro 64-0802 was determined in mice using the dissection method and micro-PET. In vitro and in vivo metabolite assay was performed in the plasma and brain of mice.
Between 1 and 60 min after injection of [11C]oseltamivir and [11C]Ro 64-0802, 0.20–0.06 % and 0.39–0.03 % ID/g were detected in the mouse brains, respectively (dissection method). Radioactivity concentrations in the living brains between 0 and 90 min after injection were measured at standardized uptake values of 0.25–0.05 for [11C]oseltamivir and 0.38–0.02 for [11C]Ro 64-0802 (micro-PET). In vivo metabolite assay demonstrated the presence of [11C]oseltamivir and [11C]Ro 64-0802 in the brains after [11C]oseltamivir injection.
This study determined the distribution and metabolism of [11C]oseltamivir and [11C]Ro 64-0802 in mice. PET could be used to measure their amounts in the living brain and to elucidate the relationship between the amounts in the brain and the side effects of Tamiflu in the central nervous system.
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