Evaluation of [76Br]FBAU 3′,5′-dibenzoate as a lipophilic prodrug for brain imaging

Add time:07/23/2019    Source:sciencedirect.com

[76Br]FBAU is a potential PET tracer for assessing proliferation. This study proposes that [76Br]FBAU 3′,5′-dibenzoate has higher blood-brain-barrier permeability than [76Br]FBAU itself and thus might be better suited for applications in the brain. The brain uptake indexes of the two compounds measured after carotid injection (29.6 ± 13.9 for [76Br]FBAU 3′,5′-dibenzoate, versus 10.0 ± 8.7 for [76Br]FBAU) support this claim. Biodistribution study also showed that the brain accumulation of activity was higher in rats injected with [76Br]FBAU 3′,5′-dibenzoate than with [76Br]FBAU (0.119±0.023 DUR at 1 h, versus 0.061 ± 0.006). [76Br]FBAU 3′,5′-dibenzoate was relatively stable in rat plasma, gradually being hydrolyzed to [76Br]FBAU exponentially with a calculated half-life of 0.8 h. DNA incorporation of [76Br]FBAU was also confirmed. The results presented support the hypothesis that the 3′,5′-dibenzoate can act as a prodrug for FBAU and deliver more radiolabeled nucleoside to the brain.

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