首页> 外国专利> RADIOACTIVE LIGANDS FOR CARDIAC BETA1 ADRENORECEPTOR FOR IMAGING CONGESTIVE HEART FAILURE

RADIOACTIVE LIGANDS FOR CARDIAC BETA1 ADRENORECEPTOR FOR IMAGING CONGESTIVE HEART FAILURE

机译:心脏BETA1肾上腺受体的放射性配体对影像性心力衰竭的影像

摘要

Novel β1 adrenoreceptor ligands that find use as imaging agents within nuclear medicine applications (e.g., PET imaging and SPECT imaging) are provided. Methods of imaging, including methods of imaging congestive heart failure, are also provided. The novel compounds may exhibit high affinity and selectivity, minimal metabolism, minimal non-specific binding and have a favorable log P value ( 0). In some instances, β1-AR selective ligands are conjugated to an imaging moiety in such a way that it does not impact the antagonist affinity and their use. In other instances, the conjugation may be directly to the antagonist at several sites that will not impact affinity. In further instances, the conjugation may be by means of a linking group, which can be used to alter the pharmacokinetics and clearance of the complex.
机译:提供了在核医学应用(例如,PET成像和SPECT成像)中用作成像剂的新型β1肾上腺素受体配体。还提供了成像方法,包括对充血性心力衰竭进行成像的方法。所述新型化合物可以表现出高亲和力和选择性,最小的代谢,最小的非特异性结合并且具有有利的log P值(<0)。在一些情况下,β1-AR选择性配体以不影响拮抗剂亲和力及其使用的方式缀合至成像部分。在其他情况下,缀合可以在不影响亲和力的几个位点直接与拮抗剂结合。在其他情况下,可以通过连接基团进行缀合,该连接基团可用于改变复合物的药代动力学和清除率。

著录项

相似文献

  • 专利
  • 外文文献
  • 中文文献
获取专利

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