Data for: Pharmacokinetics of two Bis-pyridinium Aldoximes

Aims: K117 and K127 are bis-pyridinium aldoximes. Both K117 and K127 are developed as potential antidotes in the case of poisoning both acetylcholinesterase and butyrylcholinesterese in terrorist attacks or intoxication with other organophosphorous compounds. Their distribution has been scouted in the body of rats.
Main methods: White male Wistar rats were intramuscularly injected. The animals were sacrificed, tissue samples were homogenized, and either K117 or K127 concentrartions were determined using reversed-phase high-performance liquid chromatography.
Key findings: Both K117 and K127 were present in all tissues that were analyzed including blood (serum), the brains, cerebrospinal fluid, the eyes, livers, kidneys, lungs and testes. Two novel proper names should be conceptualized in the practice of these antidotes, t1/10 (instead of t1/2) and maximal blood-brain penetration cmaxBBP.(instead of the individual cmax values for blood and also for the brain).
Significance: Either K117 or K127 meets the essential requirements for antidotes. Dose dependence and kinetics of their distribution were compared to that of other pyridinium aldoximes.

目的：K117与K127均为双吡啶鎓醛氧化物。二者均被开发为在恐怖袭击中同时中毒于乙酰胆碱酯酶和丁酰胆碱酯酶，或因其他有机磷化合物中毒时的潜在解毒剂。它们在雄性Wistar大鼠体内的分布已进行过探查。
主要方法：对雄性Wistar大鼠进行肌肉注射。对动物进行处决，组织样本进行均质化处理，并使用反相高效液相色谱法测定K117或K127的浓度。
关键发现：K117和K127均存在于所有分析的组织中，包括血液（血清）、大脑、脑脊液、眼睛、肝脏、肾脏、肺脏和睾丸。在解毒剂的实践中应构思两个新的专有名词，即t1/10（而非t1/2）和最大血脑渗透率cmaxBBP（而非血液和大脑的个别cmax值）。
意义：K117或K127均满足解毒剂的基本要求。它们分布的剂量依赖性和动力学与其它吡啶鎓醛氧化物的分布进行了比较。