| Japanese |
|---|
| Title | イオマゼニル (123I) の薬物動態に関する検討 |
|---|
| Subtitle | 技術報告 |
|---|
| Authors | 吉村弘一*, 柳井明良*, 松本博樹*, 井田圭子*, 倉見美規*, 米倉義晴**, 鳥塚莞爾*** |
|---|
| Authors(kana) | |
|---|
| Organization | *日本メジフィジックス株式会社中央研究所, **京都大学医学部脳病態生理学講座(現;福井医科大学高エネルギー研究センター), ***福井医科大学 |
|---|
| Journal | 核医学 |
|---|
| Volume | 32 |
|---|
| Number | 9 |
|---|
| Page | 1037-1043 |
|---|
| Year/Month | 1995/9 |
|---|
| Article | 報告 |
|---|
| Publisher | 日本核医学会 |
|---|
| Abstract | 「要旨」123I-イオマゼニル(123I-IMZ)のラット, ウサギおよびヒトにおける体内分布, 代謝ならびに排泄の様相を検討し, 薬物動態を明らかにした. 静脈内に投与された123I-IMZは, いずれの動物種においても速やかに代謝され, 24時間で90%以上の放射能が体外に排泄された. 主な代謝物は, ラットおよびヒトでは脱エステル体(R-COOH), そのグルクロン酸抱合体(R-COOH-Glc)および遊離のヨウ素イオン(I-), ウサギではR-COOH, 酸化型の代謝物(R'-CH2COOH)およびI-であった. すなわち, IMZの代謝は側鎖の脱エステル化ならびに酸化, 抱合および脱ヨウ素化が主であると考えられた. 主排泄経路はラットでは腎尿路系および肝胆道系の両者であったのに対し, ウサギおよびヒトでは腎尿路系であった. また, ラットの脳に集積した放射能の化学形は, 未変化体のみであったことより, これら代謝物は脳へ移行しないことが示唆された. |
|---|
| Practice | 臨床医学：一般 |
|---|
| Keywords | 123I-iomazenil, Metabolism, Animal, Human. |
|---|
| English |
|---|
| Title | Pharmacokinetics of 123I-Iomazenil, a Benzodiazepine Receptor Seeker |
|---|
| Subtitle | |
|---|
| Authors | Hirokatsu YOSHIMURA*, Akiyoshi YANAI*, Hiroki MATSUMOTO*, Keiko IDA*, Miki KURAMI*, Yoshiharu YONEKURA**, Kanji TORIZUKA*** |
|---|
| Authors(kana) | |
|---|
| Organization | *Central Research Laboratory, Nihon Medi-Physics CO., Ltd., **Department of Brain Pathophysiology, School of Medicine, Kyoto University(Biomedical Imaging Research Center, Fukui Medical School), ***Fukui Medical School |
|---|
| Journal | The Japanese Journal of nuclear medicine |
|---|
| Volume | 32 |
|---|
| Number | 9 |
|---|
| Page | 1037-1043 |
|---|
| Year/Month | 1995/9 |
|---|
| Article | Report |
|---|
| Publisher | THE JAPANESE SOCIETY OF NUCLEAR MEDICINE |
|---|
| Abstract | The biodistribution, metabolism and excretion of 123I-iomazenil have been studied in rats, rabbits and humans following i. v. administration. In all the species, 123I-iomazenil was rapidly metabolized and more than 90% of the administrated radioactivity was excreted within the first 24 hr. Dominant metabolites were acid metabolite (R-COOH), glucuronide of the acid (R-COOH-Glc) and free iodide (I-) in rats and humans. On the other hand, R-COOH, oxidative metabolite (R'-CH2COOH) and I- were found in rabbits. Thus, the possible metabolic pathways of iomazenil were hydrolysis, oxidation, conjugation and deiodination. The radioactivity was excreted into both urine and feces in rats, while primary route of excretion in rabbits and humans was from the kidneys. At 3 hr after injection, more than 97% of the radioactivity in rat brain was found in the form of the parent compound. This result indicates that metabolites of 123I-iomazenil do not cross the blood-brain barrier. |
|---|
| Practice | Clinical medicine |
|---|
| Keywords | 123I-iomazenil, Metabolism, Animal, Human. |
|---|