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Positive allosteric modulators of metabotropic glutamate 2 receptors in schizophrenia treatment

机译:代谢型谷氨酸2受体的正变构调节剂在精神分裂症治疗中的作用

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摘要

The past two decades have witnessed a rise in the 'NMDA receptor hypofunction' hypothesis for schizophrenia, a devastating disorder that affects around 1% of the population worldwide. A variety of presynaptic, postsynaptic, and regulatory proteins involved in glutamatergic signaling have thus been proposed as potential therapeutic targets. This review focuses on positive allosteric modulation of metabotropic glutamate 2 receptors (mGlu(2)Rs) and discusses how recent preclinical epigenetic data may provide a molecular explanation for the discrepant results of clinical studies, further stimulating the field to exploit the promise of mGlu(2)R as a target for schizophrenia treatment.
机译:在过去的二十年中,精神分裂症的“ NMDA受体功能减退”假说日益增多,精神分裂症是一种破坏性疾病,影响着全球约1%的人口。因此,已经提出了涉及谷氨酸能信号传导的多种突触前,突触后和调节蛋白作为潜在的治疗靶标。这篇综述着重于促代谢型谷氨酸2受体(mGlu(2)Rs)的正变构调节,并讨论了最近的临床前表观遗传学数据如何为临床研究的不同结果提供分子解释,从而进一步刺激了该领域利用mGlu( 2)R作为精神分裂症治疗的靶标。

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