扩展P2X7R工具箱：发现一种新的碘-125放射性配体。

IF 3 4区医学 Q2 NEUROSCIENCES

Purinergic Signalling Pub Date : 2025-05-09 DOI:10.1007/s11302-025-10094-7

Giorgia Tempra, Carlo Matera

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引用次数: 0

摘要

这篇Journal Club文章回顾了Qiu等人在2025年的一项研究，该研究报告了一种新的碘-125放射性配体的发展，靶向嘌呤能P2X7受体（P2X7R）。研究人员创建了一个结构修饰的P2X7R拮抗剂的小文库，并因其高亲和力和选择性而将化合物1c确定为先导物。用碘-125进行放射性标记，得到收率高、纯度高的[125I]1c。结合研究证实了其强大的纳米摩尔亲和力，支持其在放射配体筛选中的应用以及在炎症和神经退行性疾病中P2X7R成像的潜在应用。该研究证明了放射性标记探针在药物发现和嘌呤能信号研究中的价值。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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Expanding the P2X7R toolbox: discovery of a novel Iodine-125 radioligand.

This Journal Club article reviews a 2025 study by Qiu et al. that reports the development of a novel iodine-125 radioligand targeting the purinergic P2X7 receptor (P2X7R). The researchers created a small library of structurally modified P2X7R antagonists and identified compound 1c as a lead due to its high affinity and selectivity. Radiolabeling with iodine-125 produced [¹²⁵I]1c with high yield and purity. Binding studies confirmed its strong nanomolar affinity, supporting its use in radioligand screening and potential applications in imaging P2X7R in inflammatory and neurodegenerative diseases. The study demonstrates the value of radiolabeled probes in drug discovery and purinergic signaling research.

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来源期刊

Purinergic Signalling 医学-神经科学

CiteScore

6.60

自引率

17.10%

发文量

审稿时长

6-12 weeks

期刊介绍： Nucleotides and nucleosides are primitive biological molecules that were utilized early in evolution both as intracellular energy sources and as extracellular signalling molecules. ATP was first identified as a neurotransmitter and later as a co-transmitter with all the established neurotransmitters in both peripheral and central nervous systems. Four subtypes of P1 (adenosine) receptors, 7 subtypes of P2X ion channel receptors and 8 subtypes of P2Y G protein-coupled receptors have currently been identified. Since P2 receptors were first cloned in the early 1990’s, there is clear evidence for the widespread distribution of both P1 and P2 receptor subtypes in neuronal and non-neuronal cells, including glial, immune, bone, muscle, endothelial, epithelial and endocrine cells.