Oskarsson A, Tjälve H
Acta Pharmacol Toxicol (Copenh). 1976;39(5):481-99. doi: 10.1111/j.1600-0773.1976.tb03199.x.
Intravenous injections of the quaternary dipyridlium salt paraquat (14C-labelled) dissolved in solutions of low tonicity result in a high uptake in the erythrocytes and concomitantly also in the spleen (red pulp), the latter being probably due to phagocytosis of paraquat-containing erythrocytes by the reticuloendothelial system. Higher tonicities of the injected solutions result in a low uptake and the same applies to oral, intraperitoneal and subcutaneous injections. Paraquat was present in the erythrocytes in a non-metabolized form without being bound to membranes or proteins. The uptake in the erythrocytes was not influenced by alterations of the pH or by the preparation of a charge-transfer complex with serotonin in the injection solutions. Chemical alterations of the paraquat in the injection solutions could not be detected. In vitro the uptake of paraquat in the erythrocytes was higher in the haemolysed (and then reconstituted by adding sodium chloride) erythrocyte-ghosts than in the non-haemolysed erythrocytes, as shown by incubations at various tonicities. It is proposed that the intravenous injections of paraquat in hypotonic solutions temporarily alter the membranes of the erythrocytes in the blood-stream and make them permeable to paraquat, possibly, as judged from the in vitro experiments, only during a short period of partial haemolysis. The distribution studies also showed a retention of paraquat in the lungs. In addition paraquat was accumulated in the melanin of the tissues.
静脉注射溶解于低渗溶液中的季铵盐百草枯（14C标记）会导致红细胞以及脾脏（红髓）对其摄取量很高，后者可能是由于含百草枯的红细胞被网状内皮系统吞噬所致。注射溶液的渗透压较高时摄取量较低，口服、腹腔注射和皮下注射的情况也是如此。百草枯以未代谢的形式存在于红细胞中，未与细胞膜或蛋白质结合。红细胞的摄取不受pH值变化的影响，也不受注射溶液中与血清素形成电荷转移复合物的影响。未检测到注射溶液中百草枯的化学变化。体外实验表明，在不同渗透压下孵育时，溶血（然后通过添加氯化钠重新构建）的红细胞空壳对百草枯的摄取量高于未溶血的红细胞。有人提出，静脉注射低渗溶液中的百草枯会暂时改变血流中红细胞的膜，使其对百草枯具有通透性，从体外实验判断，可能仅在短时间的部分溶血期间如此。分布研究还表明百草枯在肺部有潴留。此外，百草枯在组织的黑色素中也有蓄积。
