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大鼠反复口服硫丹后其在血浆和脑中的分布情况。

Distribution of endosulfan in plasma and brain after repeated oral administration to rats.

作者信息

Gupta P K

出版信息

Toxicology. 1978 Apr;9(4):371-7. doi: 10.1016/0300-483x(78)90020-3.

DOI:10.1016/0300-483x(78)90020-3
PMID:663945
Abstract

Rats were fed endosulfan (5 or 10 mg/kg) containing alpha- and beta-isomers in the ratio of 2:1, daily for 15 days. The distribution pattern of endosulfan, its isomers and metabolite, endosulfan sulfate, was estimated in the plasma and brain of the rats. On day 16, the alpha-isomer in rats receiving 5 mg/kg was highest in the cerebrum (3.76 microgram/g) followed by the remaining part of the brain (2.66 microgram/g), and the cerebellum (2.04 microgram/g). The concentration of the beta-isomer was 0.06 microgram/g in the cerebrum and 0.02 microgram/g in the cerebellum; no beta-isomer was detected in the remaining part of the brain. The plasma concentration of alpha- and beta-isomers was 2.26 and 0.46 microgram/ml, respectively. No metabolite other than endosulfan sulfate was detected in plasma. No significant changes in brain tissue were observed in any of the groups under treatment. On day 30 (15 days after the last treatment), the concentration in plasma declined more rapidly than that in the brain tissue. At a higher dose (10 mg/kg), the distribution pattern of isomers and its metabolite, endosulfan sulfate, followed almost the same trend except that the concentration was higher than in rats receiving lower doses.

摘要

给大鼠喂食含有比例为2:1的α-异构体和β-异构体的硫丹(5或10毫克/千克),每天一次,持续15天。在大鼠的血浆和大脑中估计硫丹、其异构体和代谢物硫丹硫酸盐的分布模式。在第16天,接受5毫克/千克剂量的大鼠脑中的α-异构体含量最高,在大脑皮层中为3.76微克/克,其次是大脑其余部分(2.66微克/克)和小脑(2.04微克/克)。β-异构体在大脑皮层中的浓度为0.06微克/克,在小脑中为0.02微克/克;在大脑其余部分未检测到β-异构体。α-异构体和β-异构体的血浆浓度分别为2.26和0.46微克/毫升。血浆中未检测到除硫丹硫酸盐以外的其他代谢物。在任何治疗组中均未观察到脑组织有明显变化。在第30天(最后一次治疗后15天),血浆中的浓度下降速度比脑组织中的更快。在较高剂量(10毫克/千克)下,异构体及其代谢物硫丹硫酸盐的分布模式几乎遵循相同趋势,只是浓度高于接受较低剂量的大鼠。

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