Yasuhara Akito, Chaki Shigeyuki
Medicinal Chemistry Laboratories, Taisho Pharmaceutical Co., Ltd.
Open Med Chem J. 2010 May 27;4:20-36. doi: 10.2174/1874104501004020020.
Metabotropic glutamate receptors (mGlu receptors) have emerged as new therapeutic targets for psychiatric disorders, such as schizophrenia, depression and anxiety with their regulatory roles in glutamatergic transmissions. To date, several ligands selective for each mGlu receptor have been synthesized, and pharmacological significances of these ligands have been demonstrated in animal models. Among them, mGlu2/3 receptor agonists have been proven to be effective for treating schizophrenia and anxiety disorders in clinical studies, which may prove utilities of mGlu receptor ligands for the treatment of psychiatric disorders. This article reviews recent advances in development of each mGlu receptor ligands and their therapeutic potential.
代谢型谷氨酸受体（mGlu受体）已成为精神疾病新的治疗靶点，如精神分裂症、抑郁症和焦虑症，因其在谷氨酸能传递中发挥调节作用。迄今为止，已合成了对每种mGlu受体具有选择性的几种配体，并且这些配体的药理学意义已在动物模型中得到证实。其中，mGlu2/3受体激动剂在临床研究中已被证明对治疗精神分裂症和焦虑症有效，这可能证明mGlu受体配体在治疗精神疾病方面的效用。本文综述了每种mGlu受体配体开发的最新进展及其治疗潜力。
