Mützel W, Press W R, Weinmann H J
Fortschr Geb Rontgenstrahlen Nuklearmed Erganzungsbd. 1989;128:28-32.
Iotrolan, a nonionic, hexaiodinated dimer, is an extremely hydrophilic compound (P = 0.005). Due to its larger Stokes' radius compared with monomeric compounds such as metrizamide, the diffusion time through membranes is extended. Iotrolan deforms erythrocytes only minimally. There is practically no binding to plasma proteins. The new contrast agent has been shown to exert a very limited effect on the complement system (in vitro); it does not inhibit lysozyme (a standard enzyme) in concentrations less than 100 mg I/ml. To inhibit activity of the enzyme collagenase, much higher concentrations of iotrolan than of metrizamide or iopamidol are needed and this could offer an advantage when used for diskography preceding diskolysis with collagenase. After a single intravenous injection in rats, iotrolan has an LD50 of 28.3 g I/kg - the best general tolerance known for water-soluble contrast media thus far. The superior tolerance of iotrolan compared with iohexol and iopamidol (p less than or equal to 0.05) in rats is statistically significant. On the basis of preclinical experience, iotrolan is a very promising contrast medium for intrathecal and intravascular use.
碘曲仑是一种非离子型六碘化二聚体，是一种极具亲水性的化合物（P = 0.005）。与诸如甲泛葡胺等单体化合物相比，由于其斯托克斯半径更大，穿过膜的扩散时间延长。碘曲仑对红细胞的变形作用极小。实际上它与血浆蛋白几乎不结合。已表明这种新型造影剂对补体系统（体外）的作用非常有限；在浓度低于100 mg I/ml时它不抑制溶菌酶（一种标准酶）。为抑制胶原酶的活性，所需碘曲仑的浓度比甲泛葡胺或碘帕醇的浓度高得多，而这在胶原酶溶核术前用于椎间盘造影时可能具有优势。在大鼠单次静脉注射后，碘曲仑的半数致死量为28.3 g I/kg——这是迄今为止已知的水溶性造影剂中最好的总体耐受性。碘曲仑在大鼠中与碘海醇和碘帕醇相比具有更高的耐受性（p≤0.05），具有统计学意义。基于临床前经验，碘曲仑是一种非常有前景的用于鞘内和血管内的造影剂。
