Bruno Valeria, Caraci Filippo, Copani Agata, Matrisciano Francesco, Nicoletti Ferdinando, Battaglia Giuseppe
Department of Physiology and Pharmacology, University Sapienza, 00185 Rome, Italy; I.R.C.C.S. Neuromed, 86077 Pozzilli, Italy.
Department of Drug Sciences, University of Catania, 95125 Catania, Italy; I.R.C.C.S. Associazione Oasi Maria S.S., Institute for Research on Mental Retardation and Brain Aging, 94018 Troina, Italy.
Neuropharmacology. 2017 Mar 15;115:180-192. doi: 10.1016/j.neuropharm.2016.04.044. Epub 2016 Apr 30.
Metabotropic glutamate (mGlu) receptor ligands are under clinical development for the treatment of CNS disorders with high social and economic burden, such as schizophrenia, major depressive disorder (MDD), and Parkinson's disease (PD), and are promising drug candidates for the treatment of Alzheimer's disease (AD). So far, clinical studies have shown symptomatic effects of mGlu receptor ligands, but it is unknown whether these drugs act as disease modifiers or, at the opposite end, they accelerate disease progression by enhancing neurodegeneration. This is a fundamental issue in the treatment of PD and AD, and is also an emerging theme in the treatment of schizophrenia and MDD, in which neurodegeneration is also present and contribute to disease progression. Moving from in vitro data and preclinical studies, we discuss the potential impact of drugs targeting mGlu2, mGlu3, mGlu4 and mGlu5 receptor ligands on active neurodegeneration associated with AD, PD, schizophrenia, and MDD. We wish to highlight that our final comments on the best drug candidates are not influenced by commercial interests or by previous or ongoing collaborations with drug companies. This article is part of the Special Issue entitled 'Metabotropic Glutamate Receptors, 5 years on'.
代谢型谷氨酸(mGlu)受体配体正在进行临床开发,用于治疗具有高社会和经济负担的中枢神经系统疾病,如精神分裂症、重度抑郁症(MDD)和帕金森病(PD),并且是治疗阿尔茨海默病(AD)的有前景的候选药物。到目前为止,临床研究已经显示出mGlu受体配体的症状性疗效,但尚不清楚这些药物是作为疾病修饰剂起作用,还是相反,它们通过增强神经退行性变来加速疾病进展。这是PD和AD治疗中的一个基本问题,也是精神分裂症和MDD治疗中一个新出现的主题,在这些疾病中也存在神经退行性变并促进疾病进展。基于体外数据和临床前研究,我们讨论了靶向mGlu2、mGlu3、mGlu4和mGlu5受体配体的药物对与AD、PD、精神分裂症和MDD相关的活动性神经退行性变的潜在影响。我们希望强调的是,我们对最佳候选药物的最终评论不受商业利益或与制药公司先前或正在进行的合作的影响。本文是名为“代谢型谷氨酸受体,五年之后”特刊的一部分。