Department of Toxicology, Faculty of Pharmacy, Jagiellonian University, Medical College, Medyczna 9, PL 30-688 Kraków, Poland.
Department of Toxicology, Faculty of Pharmacy, Jagiellonian University, Medical College, Medyczna 9, PL 30-688 Kraków, Poland.
Pharmacol Ther. 2014 Jun;142(3):281-305. doi: 10.1016/j.pharmthera.2013.12.012. Epub 2013 Dec 19.
Glutamatergic excitatory transmission is implicated in physiological and pathological conditions like learning, memory, neuronal plasticity and emotions, while glutamatergic abnormalities are reported in numerous neurological and psychiatric disorders, including neurodegenerative diseases, epilepsy, stroke, traumatic brain injury, depression, anxiety, schizophrenia and pain. Also, several lines of evidence have accumulated indicating a pivotal role for glutamatergic neurotransmission in mediating addictive behaviors. Among the proteins regulating glutamatergic transmission, the metabotropic glutamate receptors (mGluR) are being developed as pharmacological targets for treating many neuropsychiatric disorders, including drug addiction. In this review we describe the molecular structure of mGluRs and their distribution, physiology and pharmacology in the central nervous system, as well as their use as targets in preclinical studies of drug addiction.
谷氨酸能兴奋性传递参与学习、记忆、神经元可塑性和情绪等生理和病理状态，而谷氨酸能异常与许多神经和精神疾病有关，包括神经退行性疾病、癫痫、中风、创伤性脑损伤、抑郁、焦虑、精神分裂症和疼痛。此外，有大量证据表明，谷氨酸能神经传递在介导成瘾行为中起着关键作用。在调节谷氨酸能传递的蛋白质中，代谢型谷氨酸受体（mGluR）被开发为治疗许多神经精神疾病（包括药物成瘾）的药物靶点。在这篇综述中，我们描述了 mGluR 的分子结构及其在中枢神经系统中的分布、生理学和药理学，以及它们在药物成瘾的临床前研究中作为靶点的应用。
