2B or 2B and 2D? - That is the question

摘要

N-methyl-D-aspartate receptors(NMDARs) mediate the slow component of glutamatergic excitatory synaptic currents (EPSCs) and in addition play key roles in both the normal and abnormal functioning of the brain. The development of the central nervous system (CNS) requires NMDAR activity to allow correct synaptic connections to be formed and they are the receptors whose activation can serve as the initial trigger for changes in synaptic strength to occur and for this reason have been implicated in certain forms of learning and memory. However, over-activation of NMDARs can be deleterious to neuronal function - in ischaemic stroke the excessive release of glutamate and the increased activation of NMDARs leads to excitotoxic cell death. In addition, NMDARs have been implicated in neurodegenerative and psychotic diseases. Therefore, not only is the identification of the composition of native NMDARs required to understand better the functioning of the CNS but the development of subtype-selective ligands may beof therapeutic benefit.