Takahashi H, Miyaoka T, Tsuda S, Shirasu Y
Fundam Appl Toxicol. 1984 Oct;4(5):718-23. doi: 10.1016/0272-0590(84)90092-7.
Fenitrothion of oral subtoxic dose (100 mg/kg; 4 hr pretreatment) decreased acute oral LD50 of BPMC from 360 to 66 mg/kg in male mice. The treatment prolonged the hexobarbital sleeping time and increased the plasma BPMC concentrations. The BPMC toxicity and its plasma concentrations were significantly reduced by phenobarbital treatment (80 mg/kg/day, 2 days, ip). This treatment diminished the effects of fenitrothion on BPMC toxicity and plasma BPMC concentrations. BPMC was metabolized by mixed-function oxidases of the liver in vitro. The metabolism of BPMC was competitively inhibited by the addition of fenitrothion (5 micrograms/ml). Fenitrothion remained in the liver (7 micrograms/g liver). These results suggest that competitive inhibition of BPMC metabolism by fenitrothion may, at least in part, play a role in inhibition of BPMC detoxication, resulting in potentiation of its toxicity.
口服亚中毒剂量的杀螟硫磷(100毫克/千克;预处理4小时)可使雄性小鼠体内的BPMC急性经口半数致死剂量从360毫克/千克降至66毫克/千克。该处理延长了己巴比妥睡眠时间,并提高了血浆中BPMC的浓度。苯巴比妥处理(80毫克/千克/天,腹腔注射,共2天)可显著降低BPMC的毒性及其血浆浓度。该处理减弱了杀螟硫磷对BPMC毒性和血浆BPMC浓度的影响。在体外,BPMC可被肝脏的混合功能氧化酶代谢。加入杀螟硫磷(5微克/毫升)后,BPMC的代谢受到竞争性抑制。杀螟硫磷残留在肝脏中(7微克/克肝脏)。这些结果表明,杀螟硫磷对BPMC代谢的竞争性抑制可能至少部分地在抑制BPMC解毒过程中起作用,从而增强其毒性。