Blood-brain barrier permeability of ginkgolide: Comparison of the behavior of PET probes 7α-[18F]fluoro- and 10-O-p-[11C]methylbenzyl ginkgolide B in monkey and rat brains

The blood-brain barrier permeability of ginkgolide B was examined using positron emission tomography (PET) probes of a F-18-incorporated ginkgolide B ([F-18]-2) and a C-11-incorporated methylbenzyl-substituted ginkgolide B ([C-11]-3). PET studies in monkeys showed low uptake of [F-18]-2 into the brain, but small amounts of [C-11]-3 were accumulated in the parenchyma. Furthermore, when cyclosporine A was preadministered to rats, the accumulation of [F-18]-2 in the rat brain did not significantly change, however, the accumulation of [C-11]-3 was five times higher than that in the control rat. These results provide effective approaches for investigating the drug potential of ginkgolides. (C) 2016 Elsevier Ltd. All rights reserved.