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重复口服利尿剂依托唑啉后孕鼠体内放射性的分布情况。

The distribution of radioactivity in pregnant rats after repeated oral doses of the diuretic agent Etozolin.

作者信息

Franklin E R, Chasseaud L F, Taylor T

出版信息

Arzneimittelforschung. 1977;27(9a):1800-3.

PMID:578769
Abstract
  1. The distribution of radioactivity has been studied by whole-body autoradiography after administration of daily oral doses of (2-14C)-ethyl (Z)-(3-methyl-4-oxo-5-piperidino-thiazolidin-2-ylidene)acetate (etozolin, Gö 687, Elkapin) at a dose level of 100mg/kg to pregnant rats during the 10th to the 17th day of gestation. 2. After the last dose, most of the radioactivity was excreted rapidly and was mainly assoicated with the gastrointestinal and urinary tracts and kidneys of the mothers. 3. Maximal distribution in the mothers occurred at 3--6 h after the last dose, and radioactivity at these times was detectable also in the lungs, muscle mass, fat, mammary and uterine tissue, the reticuloendothelial system, placentae, some ducted and endocrine glands, and in blood, but not in brain or spinal cord. At 4 days, traces of radioactivity had persisted in kidneys, liver, lungs, thyroid and placentae. 4. Radioactivity was present in low and uniform concentrations in most foetal tissues such as the heart, lungs and lens and in even lower concentrations in the brains of the foetuses during 3--6 h after dosing, but was not detected in foetal tissues at 2 days. Concentrations of radioactivity in maternal tissues were at all times much higher compared with those in foetal tissues at corresponding times after dosing.
摘要
  1. 在妊娠第10至17天,给怀孕大鼠每日口服剂量为100mg/kg的(2-¹⁴C)-乙基(Z)-(3-甲基-4-氧代-5-哌啶基-噻唑烷-2-亚基)乙酸酯(依托唑啉,Gö 687,Elkapin)后,通过全身放射自显影研究了放射性分布。2. 最后一次给药后,大部分放射性迅速排出,主要与母体的胃肠道、泌尿道和肾脏相关。3. 母体中的最大分布在最后一次给药后3至6小时出现,此时在肺、肌肉、脂肪、乳腺和子宫组织、网状内皮系统、胎盘、一些导管和内分泌腺以及血液中也可检测到放射性,但在脑或脊髓中未检测到。在第4天,肾脏、肝脏、肺、甲状腺和胎盘中仍有微量放射性。4. 给药后3至6小时,大多数胎儿组织如心脏、肺和晶状体中放射性浓度较低且均匀,胎儿大脑中的浓度甚至更低,但在第2天未在胎儿组织中检测到。与给药后相应时间胎儿组织中的放射性浓度相比,母体组织中的放射性浓度始终要高得多。

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