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

作者：Doi Hisashi; Sato Kengo; Shindou Hideo; Sumi Kengo; Koyama Hiroko; Hosoya Takamitsu; Watanabe Yasuyoshi; Ishii Satoshi; Tsukada Hideo^*; Nakanishi Koji; Suzuki Masaaki^*

来源：Bioorganic & Medicinal Chemistry, 2016, 24(21): 5148-5157.

DOI：10.1016/j.bmc.2016.08.032

• Ginkgolide B
• Platelet-activating factor
• Blood-brain barrier
• PET
• C-[C-11]methylation

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.

• 出版日期2016-11-1
• 单位RIKEN