English
TitleTc-99m (Sn) Salicylidenephenylalanine Preparation and Evaluation of a Highly Lipophilic Technetium Complex
Subtitle
AuthorsMakoto KATO-AZUMA*
Authors(kana)
Organization*Nihon Medi-Physics Co., Ltd.
JournalThe Japanese Journal of nuclear medicine
Volume17
Number4
Page407-411
Year/Month1980/5
ArticleReport
PublisherTHE JAPANESE SOCIETY OF NUCLEAR MEDICINE
AbstractIn recent years many investigators have been focusing their efforts on the preparation of highly lipophilic technetium complexes from two different viewpoints; some investigators are trying to prepare hepatobiliary imaging agents of low urinary excretion, while others are aiming towards the technetium complexes suitable for the assessment of regional cerebral blood flow. In the course of our investigation on the development of new hepatobiliary imaging agents, we have established stannous preparations of Tc-99m labeled pyridoxylideneaminates, and Tc-99m(Sn) pyridoxylideneisoleucine has been introduced as one of the hydrophobic derivatives. Our interests have also expanded toward the preparation of much more lipohilic complexes in the Tc-99m(Sn) Shiff base system, and we have set up "a Tc-99m complex with a n-octanol/buffer partition coefficient greater than 50" as our first target. This communication describes our preliminary investigation on Tc-99m(Sn) salicylidenephenylalanine, a complex which hit the target.
PracticeClinical medicine
KeywordsTc-99m (Sn) salicylidenephenylalanine, lipophilic technetium complex, hepatobiliary imaging agent
Japanese
TitleTc-99m (Sn)- サリチリデンフェニルアラニン - 高度に脂溶性なテクネチウム錯体の調製とその評価 -
Subtitle《ノート》
Authors東真*
Authors(kana)
Organization*日本メジフィジックス株式会社 技術部
Journal核医学
Volume17
Number4
Page407-411
Year/Month1980/5
Article報告
Publisher日本核医学会
Abstract「要旨」スズ還元法によりTc-99m(Sn)サリチリデンフェニルアラニンを調製し, 諸性質を検討した. 実質標識率100%で錯体が調製されたが, この錯体の分配係数(n-オクタノール/緩衝溶液)はスズ濃度, および標識後の経過時間に依存して変化した. 最高の分配係数はスズ濃度1mM, 標識後2時間で得られ, その値は130であった. 分配係数130の時点でラットに静脈内投与すると放射能は顕著な肝胆道系移行を示し, 予想に一致して尿中への排泄は0.6%(2時間後)と極めて少なかった. 一方, 分配係数130の時点で兎に投与すると放射能は肝臓, および腎臓に強く摂取され, 投与後3時間においても小腸への移行はわずかであった. これらの性質は佐治らによって報告された99mTc-2-mercaptopropionylglycineの性質に類似しており, この錯体の不安定性を示唆した.
Practice臨床医学:一般
KeywordsTc-99m (Sn) salicylidenephenylalanine, lipophilic technetium complex, hepatobiliary imaging agent

【全文PDF】