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首页> 外文期刊>Journal of applied toxicology >Paraoxon has only a minimal effect on pralidoxime brain concentration in rats.
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Paraoxon has only a minimal effect on pralidoxime brain concentration in rats.

机译：对氧磷对大鼠吡咯肟肟的脑部浓度影响很小。

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Clinical experience with oximes, cholinesterase reactivators used in organophosphorus poisoning, has been disappointing. Their major anatomic site of therapeutic action and their ability to pass the blood-brain barrier (BBB) are controversial. Although their physico-chemical properties do not favour BBB penetration, access of oximes to the brain may be facilitated by organophosphates. The effect of the organophosphate paraoxon (POX) on pralidoxime (2-PAM) brain entry was therefore determined. Rats either received 50 micromol 2-PAM only (G(1)) or additionally 1 micromol POX ( approximately LD(75)) (G(2)). Three animals each were killed after 5, 15, 30, 60, 90, 120, 180, 240, 360, 480 min, and 2-PAM concentrations in the brain and plasma were measured using HPLC. Moreover, the effect of brain perfusion with isotonic saline on subsequent 2-PAM measurements was assessed. The maximal 2-PAM concentration (C(max)) in G(1) brain was 6% of plasma C(max), while in G(2) brains it was 8%. Similarly, the ratio of the area under the curve (AUC) brain to plasma was 8% in G(1) and 12% in G(2). Brain t(max) (15 min) was slightly higher than plasma t(max) (5 min). The AUC of plasma 2-PAM did not differ between G(1) and G(2). However, in G(1), AUC brain was significantly lower than in G(2), the differences probably being clinically irrelevant. In perfused brains, 2-PAM concentrations were very close to those of non-perfused brains. The results indicate that brain penetration of 2-PAM is poor and that organophosphates only have a modest effect on 2-PAM BBB penetration. Brain perfusion does not significantly alter 2-PAM measurements and is therefore considered unnecessary.
机译：肟（用于有机磷中毒的胆碱酯酶活化剂）的临床经验令人失望。它们主要的治疗作用解剖部位及其通过血脑屏障（BBB）的能力引起争议。尽管它们的物理化学性质不利于BBB的渗透，但是有机磷酸酯可能会促进肟进入大脑。因此确定了有机磷酸酯对氧磷（POX）对吡咯肟（2-PAM）脑进入的影响。大鼠只接受50微摩尔2-PAM（G（1））或另外接受1微摩尔POX（大约LD（75））（G（2））。在5、15、30、60、90、120、180、240、360、480分钟后分别杀死三只动物，并使用HPLC测量脑和血浆中2-PAM的浓度。此外，评估了等渗盐水对脑灌注对随后的2-PAM测量的影响。 G（1）脑中的最大2-PAM浓度（C（max））为血浆C（max）的6％，而G（2）脑中的最大2-PAM浓度为8％。同样，G（1）中曲线下面积（AUC）的大脑与血浆的比率为8％，而在G（2）中为12％。脑部t（max）（15分钟）略高于血浆t（max）（5分钟）。血浆2-PAM的AUC在G（1）和G（2）之间没有差异。但是，在G（1）中，AUC脑明显低于G（2），差异可能与临床无关。在灌注的大脑中，2-PAM的浓度非常接近非灌注的大脑。结果表明2-PAM的脑渗透性较差，有机磷酸酯对2-PAM BBB的渗透仅具有中等作用。脑灌注不会显着改变2-PAM的测量，因此被认为是不必要的。

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