School of Medicine, Faculty of Health, Deakin University, Australia.
Curr Pharm Biotechnol. 2012 Jun;13(8):1522-34. doi: 10.2174/138920112800784817.
In recent years metabotropic glutamate receptors have emerged as key targets for the design of new antipsychotic medications for schizophrenia, in particular mGluR5 and mGluR2/3. These receptors exhibit diverse interactions with other neurotransmitter receptors and critical elements of intracellular signalling cascades known to be important to the pharmacotherapy of schizophrenia. In addition, mGluR5 and mGluR2/3 are intimately involved in behavioural domains related to the symptoms of this disorder. Both animal and clinical studies using novel drugs targeting these receptors have provided encouraging results. The number of patents registered for drugs targeting metabotropic glutamate receptors has grown dramatically, and positive allosteric modulators for both receptors show particular promise.
近年来，代谢型谷氨酸受体已成为设计新型抗精神分裂症药物的关键靶点，特别是 mGluR5 和 mGluR2/3。这些受体与其他神经递质受体以及已知对精神分裂症药物治疗至关重要的细胞内信号转导级联的关键元件表现出多种相互作用。此外，mGluR5 和 mGluR2/3 与与该疾病症状相关的行为领域密切相关。使用针对这些受体的新型药物进行的动物和临床研究均取得了令人鼓舞的结果。针对代谢型谷氨酸受体的药物专利数量大幅增长，两种受体的正变构调节剂尤其有前景。
