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吡啶斯的明和胆碱能阻断剂对梭曼中毒大鼠胆碱酯酶和乙酰胆碱的影响。

Effects of pyridostigmine and cholinolytics on cholinesterase and acetylcholine in Soman poisoned rats.

作者信息

Stitcher D L, Harris L W, Heyl W C, Alter S C

出版信息

Drug Chem Toxicol. 1978;1(4):355-62. doi: 10.3109/01480547809016047.

Abstract

Soman reduced blood and brain cholinesterase (ChE) activity to less than 15% and increased cerebral acetylcholine (ACh) levels to 137.4% of control. When pyridostigmine (P) was used as a prophylactic adjunct, it reduced blood ChE activity to 31.6% of control, failed to significantly alter brain ChE activity, and protected more than 70% of the blood (but not brain enzyme) from phosphonylation by soman. Benactyzine (B) was more effective than atropine (A) in reducing cerebral ACh concentrations, while a combination of the two was more effective than either alone. A prophylaxis of P + A + B was effective in controlling ACh levels in rats poisoned with one LD50 dose of Soman. Since P did not diminish the effects of the cholinolytics on cerebral ACh, this (together with the enzyme data) suggests that the two cholinolytics alone provided the central protection.

摘要

梭曼可使血液和脑胆碱酯酶(ChE)活性降至15%以下,并使脑乙酰胆碱(ACh)水平增至对照值的137.4%。当将吡啶斯的明(P)用作预防性辅助药物时,它可使血液ChE活性降至对照值的31.6%,未能显著改变脑ChE活性,并保护超过70%的血液(而非脑酶)免受梭曼的磷酰化作用。苯那辛(B)在降低脑ACh浓度方面比阿托品(A)更有效,而两者联合使用比单独使用任何一种都更有效。P + A + B联合预防对控制经一个半数致死剂量梭曼中毒的大鼠的ACh水平有效。由于P并未减弱胆碱解抗剂对脑ACh的作用,这一点(连同酶数据)表明仅这两种胆碱解抗剂就提供了中枢保护作用。

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