Liu Y, Zhang J
National Institute of Mental Health, 36 Convent Dr. MSC 4033, Building 36, Room 1A31, Bethesda, MD 20892, USA.
Chin Med J (Engl). 2000 Oct;113(10):948-56.
To identify the structure and the function of NMDA receptors, to understand the modulatory mechanism of some endogenous and exogenous compounds on NMDA receptors, and to provide theoretical basis for developing new drugs that modulate NMDA receptors.
A total of 24 originally identified articles were selected.
A total of 24 articles were selected from several hundred original articles or reviews. The content of selected articles are in accordance with our purpose and the authors are authorized scientists in the study on NMDA receptors.
After careful review of the selected papers, the meaningful results and conclusions were extracted using scientific criteria and our experience in the research of NMDA receptors.
NMDA receptor contains at least five subunits. They were designated as the NR1 (sigma 1), NR2A (epsilon 1), NR2B (epsilon 2), NR2C (epsilon 3), and NR2D (epsilon 4). A unique feature of NMDA receptor is the requirement for both glutamate and the co-against glycine for the efficient gating. NMDA receptor is modulated by a number of endogenous and exogenous compounds. Mg2+ not only blocks the NMDA channel in a voltage-dependent manner but also potentiates NMDA-induced responses at positive membrane potentials. Na+, K+ and Ca2+ not only pass through the NMDA receptor channel but also modulate the activity of NMDA receptors. Zn2+ blocks the NMDA current in a noncompetitive and a voltage-independent manner. It has been demonstrated that polyamines do not directly activate NMDA receptors, but instead act to potentiate or inhibit glutamate-mediated responses. The activity of NMDA receptors is also strikingly sensitive to the changes in H+ concentration, and partially inhibited by the ambient concentration of H+ under physiological conditions. regulated by ion channels that are permeable to Ca2+, Na+, K+ and are sensitive to voltage-dependent Mg2+ block. This channel complex contributes to excitatory synaptic transmission at sites throughout the brain and the spinal cord, and is modulated by a number of endogenous and exogenous compounds. NMDA receptors play a key role in wide range of physiologic and pathologic processes. Five NMDA receptor subunits have now been characterized in both rat and mouse brain.
确定N-甲基-D-天冬氨酸（NMDA）受体的结构与功能，了解一些内源性和外源性化合物对NMDA受体的调节机制，为研发调节NMDA受体的新药提供理论依据。
共筛选出24篇最初鉴定的文章。
从数百篇原始文章或综述中总共筛选出24篇文章。所选文章的内容符合我们的目的，且作者是NMDA受体研究领域的权威科学家。
在仔细审阅所选论文后，运用科学标准和我们在NMDA受体研究方面的经验提取有意义的结果和结论。
NMDA受体至少包含五个亚基。它们被命名为NR1（σ1）、NR2A（ε1）、NR2B（ε2）、NR2C（ε3）和NR2D（ε4）。NMDA受体的一个独特特征是高效门控需要谷氨酸和共激动剂甘氨酸同时存在。NMDA受体受到多种内源性和外源性化合物的调节。镁离子（Mg2+）不仅以电压依赖性方式阻断NMDA通道，而且在正膜电位时增强NMDA诱导的反应。钠离子（Na+）、钾离子（K+）和钙离子（Ca2+）不仅通过NMDA受体通道，还调节NMDA受体的活性。锌离子（Zn2+）以非竞争性和电压非依赖性方式阻断NMDA电流。已证明多胺并不直接激活NMDA受体，而是增强或抑制谷氨酸介导的反应。NMDA受体的活性对氢离子（H+）浓度的变化也极为敏感，在生理条件下会受到环境中H+浓度的部分抑制。由对Ca2+、Na+、K+通透且对电压依赖性Mg2+阻断敏感的离子通道调节。这种通道复合体在整个脑和脊髓的部位对兴奋性突触传递起作用，并受到多种内源性和外源性化合物的调节。NMDA受体在广泛的生理和病理过程中起关键作用。目前已在大鼠和小鼠脑中鉴定出五种NMDA受体亚基。
