Laboratory of Molecular Mechanisms of Neural Interactions, Sechenov Institute of Evolutionary Physiology and Biochemistry of RAS, 194223 Saint Petersburg, Russia.
Int J Mol Sci. 2022 Jan 2;23(1):497. doi: 10.3390/ijms23010497.
Metabotropic glutamate receptors (mGluRs) are expressed predominantly on neurons and glial cells and are involved in the modulation of a wide range of signal transduction cascades. Therefore, different subtypes of mGluRs are considered a promising target for the treatment of various brain diseases. Previous studies have demonstrated the seizure-induced upregulation of mGluR5; however, its functional significance is still unclear. In the present study, we aimed to clarify the effect of treatment with the selective mGluR5 antagonist 3-[(2-methyl-1,3-thiazol-4-yl)ethynyl]-pyridine (MTEP) on epileptogenesis and behavioral impairments in rats using the lithium-pilocarpine model. We found that the administration of MTEP during the latent phase of the model did not improve survival, prevent the development of epilepsy, or attenuate its manifestations in rats. However, MTEP treatment completely prevented neuronal loss and partially attenuated astrogliosis in the hippocampus. An increase in excitatory amino acid transporter 2 expression, which has been detected in treated rats, may prevent excitotoxicity and be a potential mechanism of neuroprotection. We also found that MTEP administration did not prevent the behavioral comorbidities such as depressive-like behavior, motor hyperactivity, reduction of exploratory behavior, and cognitive impairments typical in the lithium-pilocarpine model. Thus, despite the distinct neuroprotective effect, the MTEP treatment was ineffective in preventing epilepsy.
代谢型谷氨酸受体(mGluRs)主要表达于神经元和神经胶质细胞,参与广泛的信号转导级联反应的调节。因此,不同亚型的 mGluRs 被认为是治疗各种脑部疾病的有前途的靶点。先前的研究已经证明了癫痫发作诱导的 mGluR5 上调;然而,其功能意义仍不清楚。在本研究中,我们旨在使用锂-匹罗卡品模型阐明选择性 mGluR5 拮抗剂 3-[(2-甲基-1,3-噻唑-4-基)乙炔基]-吡啶(MTEP)治疗对大鼠癫痫发生和行为障碍的影响。我们发现,在模型的潜伏期给予 MTEP 不能提高存活率,不能预防癫痫的发生,也不能减轻其在大鼠中的表现。然而,MTEP 治疗完全防止了海马中的神经元丢失,并部分减轻了星形胶质细胞增生。在接受治疗的大鼠中检测到兴奋性氨基酸转运蛋白 2 表达增加,这可能是一种防止兴奋性毒性的潜在机制,也是神经保护的一种潜在机制。我们还发现,MTEP 给药并不能预防锂-匹罗卡品模型中典型的行为共病,如抑郁样行为、运动过度、探索行为减少和认知障碍。因此,尽管有明显的神经保护作用,但 MTEP 治疗对预防癫痫无效。