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[抗胆碱药与胆碱酯酶复活剂的药代动力学相互作用:血浆和脑组织中结合调节的反映]

[The pharmacokinetic interaction of cholinolytics and cholinesterase reactivators as a reflection of the modulation of their binding in blood plasma and in brain tissue].

作者信息

Elaeva N L, Predtechenskiĭ M B, Kul'bitskiĭ G N, Babaina E V, Trefilov V V

出版信息

Eksp Klin Farmakol. 1997 Jul-Aug;60(4):64-7.

PMID:9376763
Abstract

Radioligand assay showed that the cholinesterase (ChE) reactivators dipiroxime and benzyxime, but not carboxime, modulate selective absorption of some cholinolytics (tributam, pediphen, aprophen) in rat brain. Significant suppression of the specific binding of muscarine antagonists was recorded after chlorophos (2.LD50) intoxication. Under such conditions, the ChE reactivators induce increase in the number of binding sites and in the parameters of the constant of cholinolytic absorption on the brain membranes. It was also established by equilibrium dialysis that the binding of cholinolytics in blood plasma under the effect of ChE reactivators is reduced, leading to redistribution of their free and bound fractures, which is most favorable for tissue sorption.

摘要

放射性配体分析表明,胆碱酯酶(ChE)复活剂双吡啶肟和苄肟,而非羧肟,可调节大鼠脑中某些胆碱能抑制剂(曲布他明、哌替芬、阿普芬)的选择性吸收。在毒死蜱(2倍半数致死剂量)中毒后,记录到毒蕈碱拮抗剂的特异性结合受到显著抑制。在这种情况下,ChE复活剂可诱导脑膜上结合位点数量增加以及胆碱能抑制剂吸收常数参数增加。通过平衡透析还发现,在ChE复活剂的作用下,血浆中胆碱能抑制剂的结合减少,导致其游离和结合部分重新分布,这最有利于组织吸附。

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