Cooperative Modulation of [3H]MK‐801 Binding to the N‐Methyl‐d‐Aspartate Receptor‐Ion Channel Complex by l‐Glutamate, Glycine, and Polyamines
Cooperative Modulation of [3H]MK‐801 Binding to the N‐Methyl‐d‐Aspartate Receptor‐Ion Channel Complex by l‐Glutamate, Glycine, and Polyamines
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L-谷氨酸、甘氨酸和多胺协同调节 [3H]MK-801 与 N-甲基-d-天冬氨酸受体-离子通道复合物的结合
DOI：
10.1111/j.1471-4159.1988.tb01818.x
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发表时间：
1988
影响因子：
4.7
通讯作者：
N. Stec
中科院分区：
文献类型：
--
作者：
R. Ransom;N. Stec
摘要：在充分清洗的大鼠皮质膜中，[3 H]（+）-5-甲基-10，11-二氢-5 H-二苯并[a，d]环庚烯-5，10-亚胺（[3 H]MK-801）标记了一组具有相对较低亲和力（KD= 45 nM）的均一位点（Bmax=1.86 pmol/mg蛋白质）。谷氨酸甘氨酸由于放射性配体的Kd降低，亚精胺产生了特异性[3 H]MK-801结合的浓度依赖性增加。在存在高浓度l-谷氨酸、甘氨酸或亚精胺的情况下，[3 H]MK-801的KD值分别降低至11 nM、18 nM和15 nM。三种化合物组合的最大有效浓度进一步增加[3 H]MK-801结合亲和力，如下所示：l-谷氨酸+甘氨酸，KD= 6.2 nM; l-谷氨酸+亚精胺，KD= 2.2 nM：
Abstract: In extensively washed rat cortical membranes [3 H](+)‐ 5 ‐ methyl ‐ 10,11 ‐ dihydro ‐ 5 H‐ dibenzo [a,d]cyclohepten‐5,10‐imine ([3H]MK‐801) labeled a homogeneous set of sites (Bmax=1.86 pmol/mg protein) with relatively low affinity (KD= 45 nM). l‐Glutamate, glycine. and spermidine produced concentration‐dependent increases in specific [3H]MK‐801 binding due to a reduction in the Kd of the radioligand. In the presence of high concentrations of l‐glutamate, glycine, or spermidine, the KD values for [3H]MK‐801 were reduced to 11 nM, 18 nM, and 15 nM, respectively. Maximally effective concentrations of combinations of the three compounds further increased [3H]MK‐801 binding affinity as follows: l‐glutamate + glycine, KD= 6.2 nM; l‐glutamate + spermidine, KD= 2.2 nM:
DOI：
10.1073/pnas.84.21.7744
发表时间：
1987-11-01
影响因子：
11.1
作者：
REYNOLDS, IJ;MURPHY, SN;MILLER, RJ
通讯作者：
MILLER, RJ