The expression of metabotropic glutamate receptor 5 (mGluR5) is subject to developmental regulation and undergoes significant changes in neuropsychiatric disorders and diseases. Visualizing mGluR5 by fluorescence imaging is a highly desired innovative technology for biomedical applications. Nevertheless, there are substantial problems with the chemical probes that are presently accessible. In this study, we have successfully developed a two-photon fluorogenic probe, , based on the structure of mGluR5 antagonist 6-methyl-2-(phenylethynyl)pyridine (MPEP). Due to this antagonist-based probe selectively recognizes mGluR5, high expression of mGluR5 on living SH-SY5Y human neuroblastoma cells has been detected during intracellular inflammation triggered by lipopolysaccharides (LPS). Of particular significance, the probe can be employed along with two-photon fluorescence microscopy to enable real-time visualization of the mGluR5 in Aβ fiber-treated neuronal cells, thereby establishing a connection to the progression of Alzheimer's disease (AD). These results revealed that the probe can be a valuable imaging tool for studying mGluR5-related diseases in the nervous system.

中文翻译：

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基于拮抗剂的双光子荧光探针，用于神经元细胞中代谢型谷氨酸受体 5 的成像

代谢型谷氨酸受体 5 (mGluR5) 的表达受到发育调节，并在神经精神障碍和疾病中发生显着变化。通过荧光成像可视化 mGluR5 是生物医学应用中非常需要的创新技术。然而，目前可用的化学探针存在重大问题。在本研究中，我们基于mGluR5拮抗剂6-甲基-2-(苯乙炔基)吡啶(MPEP)的结构，成功开发了双光子荧光探针。由于这种基于拮抗剂的探针选择性识别 mGluR5，因此在脂多糖 (LPS) 引发的细胞内炎症过程中，在活体 SH-SY5Y 人神经母细胞瘤细胞上检测到 mGluR5 高表达。特别重要的是，该探针可以与双光子荧光显微镜一起使用，以实现 Aβ 纤维处理的神经元细胞中 mGluR5 的实时可视化，从而建立与阿尔茨海默病 (AD) 进展的联系。这些结果表明，该探针可以成为研究神经系统 mGluR5 相关疾病的有价值的成像工具。