Ritzén Andreas, Mathiesen Jesper Mosolff, Thomsen Christian
H. Lundbeck A/S, Research, Department of Medicinal Chemistry, Valby, Denmark.
Basic Clin Pharmacol Toxicol. 2005 Oct;97(4):202-13. doi: 10.1111/j.1742-7843.2005.pto_156.x.
The metabotropic glutamate receptors (mGluR) consist of a family of eight G-protein-coupled receptors that differ in their function, distribution and physiological roles within the central nervous system. In recent years substantial efforts have been made towards developing selective agonists and antagonists which have proven useful for elucidating their potential as novel targets for the treatment of psychiatric and neurological diseases. In the present review we will provide an update of the recent developments of functional allosteric modulators of the mGluR family and explore their therapeutic potential for anxiety/depression, schizophrenia, epilepsy/stroke, pain and Alzheimer's, Parkinson's and Huntington's diseases.
代谢型谷氨酸受体(mGluR)由一个包含八个G蛋白偶联受体的家族组成,这些受体在中枢神经系统中的功能、分布和生理作用各不相同。近年来,人们在开发选择性激动剂和拮抗剂方面付出了巨大努力,这些激动剂和拮抗剂已被证明有助于阐明它们作为治疗精神疾病和神经疾病新靶点的潜力。在本综述中,我们将提供mGluR家族功能性变构调节剂的最新进展,并探讨它们在焦虑/抑郁、精神分裂症、癫痫/中风、疼痛以及阿尔茨海默病、帕金森病和亨廷顿病治疗中的潜在应用。