Japanese
Title11C-Ro 15-1788ポジトロンCTによるin vivoベンゾジアゼピン・レセプターの研究
Subtitle原著
Authors篠遠仁*, 山崎統四郎*, 井上修*, 伊藤高司*, 橋本謙二*, 舘野之男*, 池平博夫*, 鈴木和年**, 樫田義彦***
Authors(kana)
Organization*放射線医学総合研究所臨床研究部, **サイクロトン管理課, ***特別研究員
Journal核医学
Volume22
Number12
Page1789-1797
Year/Month1985/12
Article原著
Publisher日本核医学会
Abstract「要旨」 正常ボランティア15名を対象として11C-Ro 15-1788の臨床治験を行い, 有効性および安全性を評価した. 11C-Ro 15-1788の脳内移行性は良好であり, 大脳皮質にてもっとも高い取り込みが見られた. トレーサー投与初期にはトレーサーの分布は大脳皮質, 基底核, 視床, 小脳で高く正常脳血流の分布と相似していたが, 時間経過とともに大脳皮質でのトレーサーの集積が目立つようになり, 小脳, 基底核, 視床での集積は中等度で, 脳幹部では低いなどin vitroの検索によるベンゾジアゼピン・レセプターの分布 (Bmax) と相似するものとなった. 飽和実験ではコントロール実験と比較しトレーサー投与後20分の時点の大脳皮質の放射能は20〜30%にまで減少した. 一時間にて投与されたトレーサーの約半分が尿中に排泄された.
Practice臨床医学:一般
KeywordsPositron emission tomography, Benzodiazepine, Receptor, Ro 15-1788
English
TitleA Study of Benzodiazepine Receptor in Human Brain Using 11C-Ro 15-1788 and Positron Emission Tomography
SubtitleOriginal Articles
AuthorsHitoshi SHINOTOH*, Toshirou YAMASAKI*, Osamu INOUE*, Takashi ITOH*, Kenji HASHIMOTO*, Yukio TATENO*, Hiroo IKEHIRA*, Kazutoshi SUZUKI**, Yoshihiko KASHIDA***
Authors(kana)
Organization*Division of Clinical Research, **Section of Cyclotron, ***Senior Research Counselor, National Institute of Radiological Sciences
JournalThe Japanese Journal of nuclear medicine
Volume22
Number12
Page1789-1797
Year/Month1985/12
ArticleOriginal article
PublisherTHE JAPANESE SOCIETY OF NUCLEAR MEDICINE
Abstract[Summary] A study of benzodiazepine receptor was performed in 15 healthy normal volunteers using carbon-11 labeled Ro 15-1788 and positron emission tomography. The brain kinetics of 11C-Ro 15-1788 showed a high uptake of the tracer by the brain, the maximum of which was within 20 minutes. The early distribution of the tracer after injection showed a regional distribution similar to that of any perfusion tracer with high activity in the cerebral cortex, the basal ganglia, the thalamus and the cerebellum. The peak of the radioactivity was reached earlier in the basal ganglia, the thalamus and the cerebellum than in the cerebral cortex. The accumulation of 11C was highest in the cerebral cortex, moderate in the thalamus, the basal ganglia and the cerebellum and low in the brain stem at 20 minutes post-injection. The distribution of the tracer at 20 minutes post-injection was approximately parallel to the known distribution of benzodiazepine receptors (Bmax) in human in vitro. Cold Ro 15-1788 was administered with the dose of 0.3mg/kg, 0.5mg/kg and 1.1mg/kg in three volunteers 30 minutes prior to injection. The radioactivity in the cerebral cortex were reduced to 48%, 22%, and 31% of those in the control experiments respectively. About half of the injected tracer was excreted in the urine at 1 hour after injection. 11C-Ro 15-1788 is a potent radioligand to study benzodiazepine receptors in vivo in human.
PracticeClinical medicine
KeywordsPositron emission tomography, Benzodiazepine, Receptor, Ro 15-1788

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