第五组代谢型谷氨酸受体：在调节皮层活动中的作用及其与认知的关系。
Group 5 metabotropic glutamate receptors: role in modulating cortical activity and relevance to cognition.
机构信息
Department of Neuroscience, University of Pittsburgh, A210 Langley Hall, Pittsburgh, PA 15260, USA.
出版信息
Eur J Pharmacol. 2010 Aug 10;639(1-3):33-9. doi: 10.1016/j.ejphar.2009.12.042. Epub 2010 Apr 2.
Group 5 metabotropic glutamate (mGlu(5)) receptors are abundant in forebrain and limbic regions and provide a novel pharmacological target for modulation of cognition. Here, we review recent advances in understanding the electrophysiology of these receptors which reveal a role for mGlu(5) receptors in the regulation of tonic and bursting modes of neuronal firing, maintenance of distinct forms of synaptic plasticity, and reversal of detrimental effects of NMDA receptor antagonism on cortical neuronal activity. Furthermore, recordings using recently developed positive allosteric modulators of the mGlu(5) receptor suggest that these agents have an electrophysiological profile comparable to the antipsychotic agent clozapine. These findings, in conjunction with behavioral evidence from preclinical studies of cognition, suggest a potential precognitive profile for the mGlu(5) receptor potentiators.
Group 5 metabotropic glutamate (mGlu(5)) receptors are abundant in forebrain and limbic regions and provide a novel pharmacological target for modulation of cognition. Here, we review recent advances in understanding the electrophysiology of these receptors which reveal a role for mGlu(5) receptors in the regulation of tonic and bursting modes of neuronal firing, maintenance of distinct forms of synaptic plasticity, and reversal of detrimental effects of NMDA receptor antagonism on cortical neuronal activity. Furthermore, recordings using recently developed positive allosteric modulators of the mGlu(5) receptor suggest that these agents have an electrophysiological profile comparable to the antipsychotic agent clozapine. These findings, in conjunction with behavioral evidence from preclinical studies of cognition, suggest a potential precognitive profile for the mGlu(5) receptor potentiators.
5 型代谢型谷氨酸受体（mGlu(5)）在大脑前区和边缘区丰富表达，为认知调节提供了新的药理学靶点。在此，我们综述了近期对这些受体的电生理学理解的进展，这些进展揭示了 mGlu(5)受体在调节神经元放电的紧张和爆发模式、维持不同形式的突触可塑性以及逆转 NMDA 受体拮抗剂对皮质神经元活动的有害影响方面的作用。此外，使用最近开发的 mGlu(5)受体的正变构调节剂进行的记录表明，这些药物具有与抗精神病药物氯氮平相当的电生理特征。这些发现与认知的临床前研究中的行为证据相结合，提示 mGlu(5)受体增强剂可能具有潜在的预测认知能力的特征。
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