• 主题
高级搜索  >
历史搜索 清空历史
首页> 外文期刊>Life sciences >Distribution of [C-14]suramin in tissues of male rats following a single intravenous dose
【24h】

Distribution of [C-14]suramin in tissues of male rats following a single intravenous dose

机译：单次静脉注射后[C-14]苏拉明在雄性大鼠组织中的分布

获取原文
获取原文并翻译 | 示例
           
页面导航
  • 摘要
  • 著录项
  • 相似文献
  • 相关主题

摘要

Purpose: Suramin has been shown to have efficacy in treatment of prostate cancer. In the present study we evaluated distribution of [C-14]suramin in tissues over time following a single intravenous dose. Methods: Male rats were given a single IV dose of 300 mg/kg [C-14]suramin and sacrificed at 1 or 6 hours, or at 1, 7, 14, 28, 56, or 84 days postdose. Radioactivity remaining in tissues was measured by quantitative whole body autoradiography. Results: At one hour highest tissue activity was found in blood vessel walls and caecum, followed by lung, blood, skin, preputial, thyroid, brown fat, heart, kidney, lymph nodes, liver, salivary, adrenal, Harder's and lacrimal glands, prostate, and spleen. Considerable activity was present in membranes surrounding muscle groups, bone and other organs. Relatively low activity was found in brain tissue although persistent concentration was evident in choroid plexus. High levels were present in bladder and caecum contents. Activity declined in blood but continued to increase in many tissues at later time points. Kidney reached maximum levels at 7 days postdose and retained concentration considerably higher than other tissues over the course of the study. Concentrations in tissues were persistent and considerable activity remained at 84 days postdose. Terminal elimination half life in tissues was prolonged, approximately 39 days in blood and 91 and 102 days in kidney and spleen, respectively. Uptake in prostate was highest in membranous structures separating secretory lobules. Conclusion: Suramin is widely distributed to tissues and appears to have particular affinity for boundary membranes surrounding organs and other structural tissue elements, possibly due to uptake by glycosaminoglycans. Antitumor activity may be related to inhibition of growth factors associated with these elements. (C) 2000 Elsevier Science Inc. All rights reserved. [References: 23]
机译：目的：苏拉明已被证明具有治疗前列腺癌的功效。在本研究中，我们评估了单次静脉注射剂量后[C-14]苏拉明在组织中的分布。方法：给雄性大鼠单次静脉内注射300 mg / kg [C-14]苏拉明的剂量，并在给药后1或6小时或给药后1、7、14、28、56或84天处死。通过定量全身放射自显影术测量残留在组织中的放射性。结果：一小时后，在血管壁和盲肠中发现最高的组织活性，其次是肺，血液，皮肤，口腔，甲状腺，褐色脂肪，心脏，肾脏，淋巴结，肝脏，唾液，肾上腺，哈德氏和泪腺，前列腺和脾脏。肌肉群，骨骼和其他器官周围的膜中存在相当大的活​​性。在脑组织中发现相对较低的活性，尽管脉络丛中的持续浓度很明显。膀胱和盲肠中含量很高。血液中的活性下降，但随后的许多组织中的活性继续增加。在研究过程中，肾脏在给药后7天达到最高水平，并且保留的浓度明显高于其他组织。在给药后84天，组织中的浓度持续存在并且相当大的活​​性保持。最终消除组织中的半衰期延长，血液中约39天，肾脏和脾中分别约91天和102天。前列腺的吸收在分离分泌小叶的膜结构中最高。结论：苏拉明广泛分布于组织中，并且似乎对糖胺聚糖的摄取对器官和其他结构组织元素周围的边界膜具有特殊的亲和力。抗肿瘤活性可能与抑制与这些元素相关的生长因子有关。 （C）2000 Elsevier Science Inc.保留所有权利。 [参考：23]

著录项

相似文献

  • 外文文献
  • 中文文献
  • 专利
获取原文

客服邮箱：kefu@zhangqiaokeyan.com

京公网安备：11010802029741号 ICP备案号：京ICP备15016152号-6 六维联合信息科技 (北京) 有限公司©版权所有

  • 客服微信

  • 服务号