Japanese
Titleアシアロ糖タンパク - アシアロ糖タンパク受容体系を応用した新しい肝機能検査法の開発 - 第2報 標識ネオ糖タンパクのクリアランス定量性の検討 -
Subtitle《原著》
Authors河相吉*, 羽間弘**, 小島通真*, 西山豊*, 中沢緑*, 長谷川武夫*, 久保田佳嗣**, 鷲野弘明****, 田代裕***, 鮫島美子**, 田中敬正*
Authors(kana)
Organization*関西医科大学放射線科, **第三内科, ***第一生理, ****日本メジフィジックス社
Journal核医学
Volume23
Number7
Page907-916
Year/Month1986/7
Article原著
Publisher日本核医学会
Abstract「要旨」: アシアロ糖タンパク (ASGP) は, 肝細胞膜に存在する受容体に結合し, 特異的に肝に摂取代謝される. このASGPと生理的に等価であるネオ糖タンパクのRI標識製剤を作製し, その肝臓への取り込みの定量性を検討した. 125I-Galactose-Human Serum Albumin (GHSA) とASGP受容体をbinding assayにより, 両者の結合は濃度依存性であることを証明した. 正常家兎門脈内投与における初回循環肝除去率は, 投与GHSAに対し, r=0.95と良好な濃度依存性を示した. 正常およびガラクトサミン急性肝障害ラットに末梢投与99mTc-GHSAの心, 肝計測曲線について, two compartment analysisを用い, クリアランスパラメータKd, Ku, Tmaxを設定した. これらのパラメータは投与濃度依存性を示し, ASGP受容体活性とは0.1%以下の危険率で有意な相関関係が成立した. 以上より標識GHSAは肝ASGP受容体量と定量的結合関係を示し, 肝機能を評価するスキャン製剤として有用であると考えられた.
Practice臨床医学：一般
KeywordsLiver scintigram, Two compartment model, Neoglycoprotein.
English
TitleA New Liver Function Test Using the Asialoglycoprotein-receptor System on the Liver Cell Membrane : II. Quantitative Evaluation of Labeled Neoglycoprotein Clearance
SubtitleOriginal Articles
AuthorsSoukichi KAWA*, Hiroshi HAZAMA**, Michimasa KOJIMA*, Yutaka NSHIYAMA*, Midori NAKAZAWA*, Takeo HASEGAWA*, Yoshitsugu KUBOTA**, Koumei WASHINO****, Yutaka TASHIRO***, Yoshiko SAMESHIMA**, Yoshimasa TANAKA*
Authors(kana)
Organization*Department of Radiology, **The Third Department of Internal Medicine, ***The First Department of Physiology, Kansai Medical University, ****Nihon Medi-Physics Co., Ltd.
JournalThe Japanese Journal of nuclear medicine
Volume23
Number7
Page907-916
Year/Month1986/7
ArticleOriginal article
PublisherTHE JAPANESE SOCIETY OF NUCLEAR MEDICINE
Abstract[Summary] : Asialoglycoprotein (ASGP) binds to the receptors on the liver cell membrane, and is specifically taken up by the liver and metabolized. We produced labeled neoglycoprotein (GHSA) that is physiologically equivalent to ASGP, and quantitatively examined whether its uptake by the liver is dose-related using the following methods in order to evaluate its usefulness as a scanning radiopharmaceutical : 1) binding assay between GHSA and ASGP receptors, 2) measurement of the liver extraction ratio in the initial circulation following administration into the portal vein, and 3) measurement of clearance in normal rats and rats with galacosamine-induced acute liver disorder. The binding assay showed a linear relationship between the concentration of 125I-GHSA and the amount of ASGP receptors obtained from the rat liver. A membrane assay using 125I-GHSA and the liver cell membrane revealed similar results. The liver extraction ratio in the initial circulation following the administration into the portal vein of normal rabbits was highly dose-dependent (r=-0.95 in the range of 5-100μg GHSA) . Serial imaging of 99mTc-GHSA during two-hour period after administration into the peripheral blood showed specific accumulation in the liver beginning immediately after the intravenous injection and subsequent transport mainly via the biliary system into the small intestine in the normal rat and mainly into the urine in the bile duct ligated rat. As a dynamic model of 99mTc-GHSA, its circulation through the heart and liver and inactivated release from the liver was used, and two-compartment analysis was made on measurement curves in the heart and liver to obtain clearance parameters. The concentration of administered 99mTc-GHSA (50-100μg/100 g body weight) showed a positive linear relationship with clearance. Administration of 50μg/100 g body weight of 99mTc-GHSA revealed a significant correlation (p<0.001) between clearance and ASGP receptor activity in normal rats and rats with galactosamine-induced acute liver disorder. These results show that labeled GHSA binds quantitatively to liver ASGP receptors and is useful as a scanning radiopharmaceutical in evaluating liver functions.
PracticeClinical medicine
KeywordsLiver scintigram, Two compartment model, Neoglycoprotein.

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