...
  • 主题
高级搜索  >
历史搜索 清空历史
首页> 外文期刊>Journal of Neuroscience Methods >Detection of low level histamine H3 receptor occupancy by autoradiography.
【24h】

Detection of low level histamine H3 receptor occupancy by autoradiography.

机译：通过放射自显影检测低水平的组胺H3受体占有率。

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

Histamine H(3) receptor antagonists have been proposed as a novel approach to the treatment of cognitive, attentional, and sleep disorders. It is apparent that H(3) receptor antagonists produce in vivo effects in preclinical animal models of central diseases across a wide dose range. In order to characterize the relationship between efficacy in the preclinical models and H(3) receptor occupancy, a brain slice receptor autoradiography method was used. Brain slice receptor autoradiography requires less in vitro tissue processing, preserves brain structure, and provides anatomical localization of compound in the brain. Consistent with H(3) receptor distribution, in vitro autoradiography experiments demonstrated specific binding of [(3)H]NAMH (N-alpha-methylhistamine) in rat cortex, and other brain regions, but not in cerebellum. Ex vivo H(3)R brain slice autoradiography was able to detect H(3) receptor occupancy by reference antagonists at doses lower than previously found using a homogenate assay format. The method is relatively quick with image acquisition on a beta-imager and is capable of detecting receptor occupancy in different brain regions simultaneously. Furthermore, the increased sensitivity should be useful in providing dosing guidelines for H(3) antagonists in both preclinical and clinical settings.
机译：组胺H（3）受体拮抗剂已被提出作为一种新的方法来治疗认知，注意和睡眠障碍。显然，H（3）受体拮抗剂在广泛剂量范围内的中枢疾病的临床前动物模型中产生体内效应。为了表征临床前模型中的功效与H（3）受体占有率之间的关系，使用了脑片受体放射自显影方法。脑片受体放射自显影术需要较少的体外组织处理，可以保留脑结构，并提供脑中化合物的解剖定位。与H（3）受体分布一致，体外放射自显影实验显示[（3）H] NAMH（N-α-甲基组胺）在大鼠皮层和其他大脑区域，但在小脑中没有特异性结合。离体H（3）R脑片放射自显影能够检测参考拮抗剂的H（3）受体占有率，其剂量低于以前使用匀浆测定法发现的剂量。该方法在β成像仪上进行图像采集时相对较快，并且能够同时检测不同大脑区域中的受体占有率。此外，增加的敏感性应在临床前和临床环境中为H（3）拮抗剂的剂量指南提供帮助。

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