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二氟甲基膦酸的阴离子水解产物对大鼠和豚鼠胆碱酯酶的抑制作用

The inhibition of rat and guinea pig cholinesterases by anionic hydrolysis products of methylphosphonic difluoride (difluoro).

作者信息

Dahl A R, Hobbs C H, Marshall T C

出版信息

Toxicol Appl Pharmacol. 1986 Jul;84(3):561-6. doi: 10.1016/0041-008x(86)90261-9.

DOI:10.1016/0041-008x(86)90261-9
PMID:3726876
Abstract

Methylphosphonic difluoride (difluoro) and its hydrolysis products, methylphosphonofluoridate (MF) and fluoride, were examined for cholinesterase-inhibiting ability in rats and guinea pigs by both inhalation and intraperitoneal exposure routes. In vivo inhibition was compared to in vitro inhibition. In the whole animal, MF was the active chemical, but in vitro under special conditions, difluoro was more potent than MF and fluoride. Rat and guinea pig blood cholinesterase were equally sensitive to inhibition by MF, but only the guinea pig displayed cholinergic signs leading to death from MF toxicity. Data imply that MF is responsible for the cholinesterase inhibition resulting from exposure to DF vapor. MF may be the first example of a moderately strong acid shown to inhibit cholinesterase and cause death from cholinergic effects.

摘要

通过吸入和腹腔注射暴露途径,对大鼠和豚鼠体内的甲基膦酸二氟化物(二氟化物)及其水解产物甲基膦酸氟化物(MF)和氟化物的胆碱酯酶抑制能力进行了研究。将体内抑制作用与体外抑制作用进行了比较。在整个动物体内,MF是活性化学物质,但在特殊条件下的体外实验中,二氟化物比MF和氟化物更具效力。大鼠和豚鼠血液中的胆碱酯酶对MF抑制作用的敏感性相同,但只有豚鼠表现出胆碱能体征并因MF毒性而死亡。数据表明,MF是导致接触DF蒸气后胆碱酯酶抑制的原因。MF可能是首个被证明能抑制胆碱酯酶并因胆碱能效应导致死亡的中等强度酸的实例。

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