Pastor Catherine M, Planchamp Corinne, Pochon Sibylle, Lorusso Vito, Montet Xavier, Mayer Joachim, Terrier Francois, Vallee Jean-Paul
Department of Radiology, Hôpital Universitaire de Genève, Rue Micheli-du-Crest 24, Bâtiment C, Room 6-795, 1211 Geneva 14, Switzerland.
Radiology. 2003 Oct;229(1):119-25. doi: 10.1148/radiol.2291020726. Epub 2003 Aug 27.
To compare in the entire liver, the hepatic kinetics of gadobenate dimeglumine (Gd-BOPTA) and gadopentetate dimeglumine (Gd-DTPA) and to evaluate the hepatic transport of Gd-BOPTA.
The authors studied both contrast agents in isolated perfused rat livers by measuring the magnetic resonance (MR) signal intensity (SI) in 12 rats, as well as the gadolinium concentrations in hepatic tissues in 42 rats. The intrahepatic transport of Gd-BOPTA was investigated with pharmacologic antagonism by using bromosulfophthalein. MR imaging was performed at 1.5 T with a fast gradient-echo T1-weighted MR sequence.
The hepatic kinetics based on the MR SI measured over time showed a rapid steady state during Gd-DTPA perfusion, while the SI continuously increased during the 30-minute Gd-BOPTA perfusion period. The pharmacokinetic modeling indicated that the half-lives of Gd-DTPA entry and exit were identical (mean, 1.3 minutes +/- 0.9 [standard error of mean]) and shorter than those observed with Gd-BOPTA (P <.001). The uptake of Gd-BOPTA was faster (mean half-life, 4.8 minutes +/- 0.3) than the washout (mean half-life, 17.5 minutes +/- 2.8) (P =.001). The combined perfusion of bromosulfophthalein and Gd-BOPTA decreased the SI enhancement in comparison with the perfusion of Gd-BOPTA alone (mean, 0.56 +/- 0.03 vs 2.54 +/- 0.39, P <.001). The entry and exit kinetic parameters obtained during the perfusion of Gd-BOPTA plus bromosulfophthalein were identical and comparable to those obtained during Gd-DTPA perfusion (P =.95). Acute bile duct ligation did not interfere with the uptake of Gd-BOPTA in hepatocytes, but it slowed down the excretion by approximately 50%. Measurements of gadolinium concentrations in hepatic tissues confirmed these findings.
In the liver, the hepatospecific contrast agent Gd-BOPTA enters into hepatocytes likely through the organic anion transporting peptide 1.
比较钆贝葡胺（Gd - BOPTA）和钆喷酸葡胺（Gd - DTPA）在整个肝脏中的肝脏动力学，并评估Gd - BOPTA的肝脏转运。
作者通过测量12只大鼠的磁共振（MR）信号强度（SI）以及42只大鼠肝脏组织中的钆浓度，在离体灌注大鼠肝脏中研究了这两种造影剂。通过使用溴磺酞钠进行药理拮抗作用来研究Gd - BOPTA的肝内转运。在1.5 T下使用快速梯度回波T1加权MR序列进行MR成像。
基于随时间测量的MR SI得出的肝脏动力学显示，在Gd - DTPA灌注期间呈现快速稳态，而在30分钟的Gd - BOPTA灌注期内SI持续增加。药代动力学模型表明，Gd - DTPA进入和流出的半衰期相同（平均值，1.3分钟±0.9[平均标准误差]），且短于Gd - BOPTA观察到的半衰期（P<.001）。Gd - BOPTA的摄取比洗脱更快（平均半衰期，4.8分钟±0.3）（平均半衰期，17.5分钟±2.8）（P =.001）。与单独灌注Gd - BOPTA相比，溴磺酞钠和Gd - BOPTA联合灌注降低了SI增强（平均值，0.56±0.03对2.54±0.39，P<.001）。在Gd - BOPTA加溴磺酞钠灌注期间获得的进入和流出动力学参数相同，且与Gd - DTPA灌注期间获得的参数相当（P =.95）。急性胆管结扎不干扰Gd - BOPTA在肝细胞中的摄取，但使排泄减慢约50%。肝脏组织中钆浓度的测量证实了这些发现。
在肝脏中，肝特异性造影剂Gd - BOPTA可能通过有机阴离子转运肽1进入肝细胞。
