Glycine neurotransmission in the dorsal horn of the spinal cord plays a key role in regulating nociceptive signaling, but in chronic pain states reduced glycine neurotransmission is associated with the development of allodynia and hypersensitivity to painful stimuli. This suggests that restoration of glycine neurotransmission may be therapeutic for the treatment of chronic pain. Glycine transporter 2 inhibitors have been demonstrated to enhance glycine neurotransmission and provide relief from allodynia in rodent models of chronic pain. In recent years, photoswitchable compounds have been developed to provide the possibility of controlling the activity of target proteins using light. In this study we have developed a photoswitchable noncompetitive inhibitor of glycine transporter 2 that has different affinities for the transporter at 365 nm compared to 470 nm light.

中文翻译：

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光可切换 ORG25543 同源物可实现甘氨酸转运蛋白 2 的光学控制。

脊髓背角中的甘氨酸神经传递在调节伤害性信号传导中起关键作用，但在慢性疼痛状态下，甘氨酸神经传递减少与异常性疼痛的发展和对疼痛刺激的超敏反应有关。这表明甘氨酸神经传递的恢复可能对治疗慢性疼痛具有治疗作用。甘氨酸转运蛋白 2 抑制剂已被证明可增强甘氨酸神经传递并缓解啮齿动物慢性疼痛模型中的异常性疼痛。近年来，已开发出光可切换化合物以提供使用光控制靶蛋白活性的可能性。