Identification of lead compounds for (99m)Tc and (18)F GPR91 radiotracers.

Identification of lead compounds for (99m)Tc and (18)F GPR91 radiotracers.
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(99m)Tc 和 (18)F GPR91 放射性示踪剂先导化合物的鉴定。

DOI:
10.1016/j.bmcl.2015.04.015
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发表时间:
2015
影响因子:
2.7
通讯作者:
Taylor,AndrewT
Taylor,AndrewT
中科院分区:
医学4区
文献类型:
--
作者:
Klenc,Jeffrey;Lipowska,Malgorzata;Taylor,AndrewT

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为了开发第一个针对GPR91的放射性示踪剂,GPR91是一种细胞膜结合的受体,调节细胞对高血糖和低氧的反应,我们设计并制备了一系列基于已发表的一系列与GPR91高亲和力的1,8-萘啶的化合物。我们的方法提供了一种将放射性原子(99mTc和18F)整合到GPR91药效团中作为最终合成步骤的机制。药理分析证实了该系列中99mTc和18F GPR91放射性示踪剂的先导化合物。
To develop the first radiotracer targeting GPR91, a cell membrane-bound receptor that modulates the cellular response to hyperglycemia and hypoxia, we designed and prepared a small series of compounds based on a published series of 1,8-naphthyridines with high affinity to GPR91. Our approach provides a mechanism to incorporate radioactive atoms (99mTc and18F) into the GPR91 pharmacophore as the final synthetic step. Pharmacological assays confirmed lead compounds for99mTc and18F GPR91 radiotracers within the series.
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