@article{oai:repo.qst.go.jp:00044506,
 author = {Shinoto, Hitoshi and Inoue, Osamu and Suzuki, Kazutoshi and Tateno, Yukio and Ikehira, Hiroo and et.al and 篠遠 仁 and 井上 修 and 鈴木 和年 and 舘野 之男 and 池平 博夫},
 issue = {10},
 journal = {Journal of Nuclear Medicine},
 month = {Oct},
 note = {Using 11C-labeled Ro15-1788 and positron emission tomography, studies of benzodiazepine binding sites in the human brain were performed on four normal volunteers. Rapid and high accumulation of 11C activity was observed in the brain after i.v. injection of [11C]Ro15-1788, the maximum of which was within 12 min. Initial distribution of 11C activity in the brain was similar to the distribution of the normal cerebral blood flow. Ten minutes after injection, however, a high uptake of 11C activity was observed in the cerebral cortex and moderate uptake was seen in the cerebellar cortex, the basal ganglia, and the thalamus. The accumulation of 11C activity was low in the brain stem. This distribution of 11C activity was approximately parallel to the known distribution of benzodiazepine receptors. Saturation experiments were performed on four volunteers with oral administration of 0.3-1.8 mg/kg of cold Ro15-1788 prior to injection. Initial distribution of 11C activity following injection peaked within 2 min and then the accumulation of 11C activity decreased rapidly and remarkably throughout the brain. The results indicated that [11C] Ro15-1788 associates and dissociates to specific and nonspecific binding sites rapidly and has a high ratio of specific receptor binding to nonspecific binding in vivo. Carbon-11 Ro15-1788 is a suitable radioligand for the study of benzodiazepine receptors in vivo in humans.},
 pages = {1593--1599},
 title = {Visualization of specific binding sites of benzodiazepine in human brain.},
 volume = {27},
 year = {1986}
}