Japanese
Title2-Amino-2-methyl-butanoic acid (2-AMB) - 腫瘍集積性および体内挙動からみた腫瘍診断薬としての可能性 -
Subtitle原著
Authors柴和弘*, 森厚文*, 久田欣一**
Authors(kana)
Organization*金沢大学アイソトープ総合センター, **医学部核医学教室
Journal核医学
Volume25
Number6
Page505-511
Year/Month1988/6
Article原著
Publisher日本核医学会
Abstract「要旨」 α-Aminoisobutyric acid (α-AIB) の類似体である2-Amino-2-methyl-butanoic acid (2-AMB) の腫瘍診断薬としての可能性を検討した. 2-AMBとα-AIBをBucherer変法によりC-14標識合成し, エールリッヒ担がんマウスを用いて経時的体内分布, 全身マクロオートラジオグラフィおよび代謝実験を行い, 2-AMBとのα-AIBを比較した. その結果, 2-AMBは, α-AIBに比べ腫瘍集積率がやや低いものの, 十分悪性腫瘍に対する特異的親和性を保持しており, さらにα-AIBで低値を示す腫瘍 - 肝臓, 胃, 腸比も改善され, ほとんどの臓器 (腎臓, 膵臓を除く) における腫瘍 - 臓器比が高値を示した. 両者の代謝を比較してみると, 2-AMB, α-AIBともほとんど尿から未代謝物のまま排泄され, 投与後24時間で, 2-AMBは, 92.3%, α-AIBは48.6%と2-AMBの方が約2倍ほど速く体外へ排泄された. 以上のことから, 2-AMBは, 病巣部不明の場合の検索に優れた腫瘍診断薬と考えられた.
Practice臨床医学:一般
Keywords2-amino-2-methyl-butanoic acid, α-aminoisobutyric acid, Tumor-seeking agent, Tissue distribution, Whole-body autoradiogram
English
Title2-Amino-2-Methyl-Butanoic Acid (2-AMB) - A Potential Tumor-Seeking Agent -
SubtitleOriginal Articles
AuthorsKazuhiro SHIBA*, Hirofumi MORI*, Kinichi HISADA**
Authors(kana)
Organization*Radioisotope Center, **Depatment of Nuclear Medicine, School of Medicine, Kanazawa University
JournalThe Japanese Journal of nuclear medicine
Volume25
Number6
Page505-511
Year/Month1988/6
ArticleOriginal article
PublisherTHE JAPANESE SOCIETY OF NUCLEAR MEDICINE
Abstract[Summary] α-aminoisobutyric acid (α-AIB) has been shown to be potentially useful as a tumor-seeking agent. However, tumor imaging with α-AIB is limited by its low tumor to tissue ratios. We synthesized C-14-labeled 2-amino-2-methyl-butanoic acid (2-AMB) , analog of α-AIB with 2-methyl group using modified Bucherer method in order to seek better tumor-seeking agent than α-AIB. Comparative tissue distribution, whole-body autoradiographic and metabolic studies of these two agents in Ehrlich tumor bearing mice were carried out. 2-AMB was found to have significantly higher tumor to tissue ratios, especially in liver, lung, stomach, heart and small intestine than α-AIB, although 2-AMB had slightly less tumor uptake than α-AIB. Autoradiograms showed that 2-AMB has better tumor localization than α-AIB. 24 hours after injection, the rate of excretion of 2-AMB was 92.3% and 2-AMB was excreted twice as fast as α-AIB. Most of these two agents was excreted with urine, and thin-layer chromatograms showed that these two agents are not metabolized in tissues. These results suggest that 2-AMB may be promising as a suitable tumor-seeking agent.
PracticeClinical medicine
Keywords2-amino-2-methyl-butanoic acid, α-aminoisobutyric acid, Tumor-seeking agent, Tissue distribution, Whole-body autoradiogram

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