Weinmann H J, Brasch R C, Press W R, Wesbey G E
AJR Am J Roentgenol. 1984 Mar;142(3):619-24. doi: 10.2214/ajr.142.3.619.
Chelation of the rare-earth element gadolinium (Gd) with diethylenetriaminepentaacetic acid (DTPA) results in a strongly paramagnetic, stable complex that is well tolerated in animals. The strongly paramagnetic gadolinium complex reduces hydrogen-proton relaxation times even in low concentrations (less than 0.01 mmol/L). The pharmacokinetic behavior of intravenously delivered Gd-DTPA is similar to the well known iodinated contrast agents used in urography and angiography; excretion is predominantly through the kidneys with greater than 90% recovery in 24 hr. The intravenous LD50 of the meglumine salt of Gd-DTPA is 10 mmol/kg for the rat; in vivo there is no evidence of dissociation of the gadolinium ion from the DTPA ligand. The combination of strong proton relaxation, in-vivo stability, rapid urinary excretion, and high tolerance favors the further development and the potential clinical application of gadolinium-DTPA as a contrast enhancer in magnetic resonance imaging.
稀土元素钆(Gd)与二乙烯三胺五乙酸(DTPA)螯合会生成一种强顺磁性的稳定络合物,该络合物在动物体内耐受性良好。即使在低浓度(低于0.01 mmol/L)下,强顺磁性钆络合物也会缩短氢质子弛豫时间。静脉注射钆-二乙烯三胺五乙酸(Gd-DTPA)的药代动力学行为与尿路造影和血管造影中使用的著名碘化造影剂相似;排泄主要通过肾脏,24小时内回收率超过90%。Gd-DTPA葡甲胺盐对大鼠的静脉半数致死量为10 mmol/kg;在体内没有证据表明钆离子会从DTPA配体上解离。强质子弛豫、体内稳定性、快速经尿排泄和高耐受性等特性有利于钆-二乙烯三胺五乙酸作为磁共振成像造影增强剂的进一步研发及其潜在的临床应用。