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己烯雌酚在大鼠和人体中的生物处置研究。

Studies on the biological disposition of diethylstilbestrol in rats and humans.

作者信息

Fischer L J, Weissinger J L, Rickert D E, Hintze K L

出版信息

J Toxicol Environ Health. 1976 Mar;1(4):587-605. doi: 10.1080/15287397609529360.

DOI:10.1080/15287397609529360
PMID:1263279
Abstract

Studies were conducted to elucidate the processes involved in the biological disposition of diethylstilbestrol (DES). The apparent biological half-life of [14C] DES decreased with increasing age in immature rats. The half-life of DES in adult rats (14 min) was reached between the 15th and 25th day after birth. Comparison of the intestinal absorption of [14C] DES and [14C]DES monoglucuronide showed the unconjugated drug to be absorbed much more rapidly. Hydrolysis of the conjugate took place in the lower intestine, and this permitted the drug to undergo enterohepatic cycling.

摘要

开展了多项研究以阐明己烯雌酚(DES)的生物处置过程。在未成熟大鼠中,[14C]DES的表观生物半衰期随年龄增长而缩短。DES在成年大鼠体内的半衰期(14分钟)在出生后第15天至第25天之间达到。对[14C]DES和[14C]DES单葡萄糖醛酸苷的肠道吸收情况进行比较,结果显示未结合的药物吸收速度要快得多。结合物在小肠下段发生水解,这使得药物能够进行肠肝循环。

相似文献

1
Studies on the biological disposition of diethylstilbestrol in rats and humans.己烯雌酚在大鼠和人体中的生物处置研究。
J Toxicol Environ Health. 1976 Mar;1(4):587-605. doi: 10.1080/15287397609529360.
2
The fate of diethylstilbestrol in the pregnant mouse.己烯雌酚在怀孕小鼠体内的代谢情况
J Pharmacol Exp Ther. 1976 Jun;197(3):687-96.
3
Absorption of diethylstilbestrol and its glucuronide conjugate from the intestines of five- and twenty-five-day-old rats.
J Pharmacol Exp Ther. 1973 Apr;185(1):163-70.
4
Hepatic presystemic elimination of diethylstilbestrol by rats and effect of pretreatment with inducers of UDP-glucuronosyltransferase.
J Toxicol Environ Health. 1985;16(3-4):615-29. doi: 10.1080/15287398509530768.
5
Absorption and glucuronylation of diethylstilbestrol by the rat small intestine.大鼠小肠对己烯雌酚的吸收及葡萄糖醛酸化作用。
Xenobiotica. 1978 Nov;8(11):665-72. doi: 10.3109/00498257809069578.
6
Development in the newborn rat of the conjugation and de-conjugation processes involved in the enterohepatic circulation of diethylstilboestrol.新生大鼠体内己烯雌酚肝肠循环中结合与去结合过程的发育情况。
Xenobiotica. 1972 Jul;2(4):399-412. doi: 10.3109/00498257209111067.
7
Dose-dependent kinetics of diethylstilbestrol in the rat.己烯雌酚在大鼠体内的剂量依赖性动力学
J Toxicol Environ Health Suppl. 1976;1:61-76.
8
Transplacental effects of diethylstilbestrol in mice.
Natl Cancer Inst Monogr. 1979 May(51):67-72.
9
The disposition of radioactivity after administration of the anthelminthic methyl-14C-5-cyclopropylcarbonyl-2-benzimidazole carbamate (ciclobendazole) to rats and dogs.抗蠕虫药甲基-14C-5-环丙基羰基-2-苯并咪唑氨基甲酸酯(环苯达唑)对大鼠和犬给药后的放射性分布情况。
Arzneimittelforschung. 1977;27(3):593-8.
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Role of metabolic activation in the transplacental carcinogenicity of diethylstilbestrol.
Int J Biol Res Pregnancy. 1982;3(3):103-7.

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Int J Environ Res Public Health. 2021 Sep 22;18(19):9965. doi: 10.3390/ijerph18199965.
2
Multigenerational endometriosis : consequence of fetal exposure to diethylstilbestrol ?多代子宫内膜异位症:胎儿暴露于己烯雌酚的后果?
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Disposition of orally administered 2,2-Bis(4-hydroxyphenyl)propane (Bisphenol A) in pregnant rats and the placental transfer to fetuses.
口服2,2-双(4-羟苯基)丙烷(双酚A)在妊娠大鼠体内的处置及胎盘向胎儿的转运。
Environ Health Perspect. 2000 Oct;108(10):931-5. doi: 10.1289/ehp.00108931.
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beta-Glucuronidase levels in patients with fibrocystic breast disease.纤维囊性乳腺病患者的β-葡萄糖醛酸酶水平。
Breast Cancer Res Treat. 1986;8(3):217-22. doi: 10.1007/BF01807334.