Metabotropic glutamate receptors (mGlu) are a family of class C G protein-coupled receptors (GPCRs) with important biological functions and widespread expression. The mechanisms of mGlu activation and the development of allosteric modulators for these dimeric proteins have attracted singular attention including the use of light regulated ligands. Photopharmacology involves the integration of a photoactive moiety into the ligand structure that following specific illumination undergoes a structural rearrangement and changes its biological activity. The use of light-regulated allosteric ligands offers the opportunity to manipulate mGlu signalling with spatiotemporal precision, unattainable with classical pharmacological approaches. In this review, we will discuss some of the innovations that have been made in the allosteric photopharmacology of mGlu receptors to date. We discuss the prospects of these molecular tools in the control of mGluRs and the new perspectives in understanding mGlu mechanisms, pharmacology and (patho)physiology that can ultimately result in innovative drug discovery concepts.

代谢型谷氨酸受体 (mGlu) 是一类具有重要生物学功能和广泛表达的 CG 蛋白偶联受体 (GPCR)。mGlu 激活的机制和这些二聚体蛋白的变构调节剂的开发已经引起了广泛的关注，包括光调节配体的使用。光药理学涉及将光活性部分整合到配体结构中，在特定光照后经历结构重排并改变其生物活性。光调节变构配体的使用提供了以时空精度操纵 mGlu 信号的机会，这是经典药理学方法无法实现的。在本次审查中，我们将讨论迄今为止在 mGlu 受体的变构光药理学方面取得的一些创新。我们讨论了这些分子工具在控制 mGluR 方面的前景，以及了解 mGlu 机制、药理学和（病理）生理学的新观点，最终可能导致创新的药物发现概念。