基于萘及类似环系的99mTc标记肝胆显像剂的比较研究。

Comparative study of 99mTc labeled hepatobiliary agents based on naphthalene and similar ring systems.

作者信息

Fritzberg A R, Bloedow D C, Klingensmith W C, Whitney W P

出版信息

Int J Nucl Med Biol. 1982;9(1):1-11. doi: 10.1016/0047-0740(82)90068-7.

Abstract

A series of 99mTc complexes of naphthalene and naphthalene-like ring systems were evaluated pharmacokinetically as hepatobiliary imaging agents and compared to 131I-rose bengal and 99mTc-N-(2,6-diethylacetanilide)-iminodiacetate in rats and dogs. Although all complexes studied exhibited high specificity for biliary excretion, they varied widely in disappearance rate from blood and in biliary excretion. Complexes with 8-hydroxyquinoline-7-carboxylic acid and hydralazine were relatively lipophilic and were eliminated more slowly than 131I-rose bengal; complexes of iminodiacetic derivatives of naphthalene, N-(2-acetylnaphthyl)iminodiacetic acid N-(2-naphthylmethyl)iminodiacetic acid were more polar and were eliminated much faster. Renal excretion of the complexes was 5.6% or less except for that of the latter compound (18%). Plasma binding ranged from 51 to 98%.

摘要

对一系列萘及类萘环系统的99mTc配合物作为肝胆显像剂进行了药代动力学评估，并在大鼠和狗身上与131I-玫瑰红和99mTc-N-(2,6-二乙基乙酰苯胺)-亚氨基二乙酸进行了比较。尽管所研究的所有配合物都表现出对胆汁排泄的高度特异性，但它们在血液中的消失速率和胆汁排泄方面差异很大。含8-羟基喹啉-7-羧酸和肼苯哒嗪的配合物相对亲脂，其消除速度比131I-玫瑰红慢；萘的亚氨基二乙酸衍生物配合物，N-(2-乙酰萘基)亚氨基二乙酸、N-(2-萘基甲基)亚氨基二乙酸极性更强，消除速度快得多。除后一种化合物（18%）外，配合物的肾排泄率为5.6%或更低。血浆结合率在51%至98%之间。