Characterization of the effects of polyamines on the modulation of the N-methyl-D-aspartate receptor by glycine.
Characterization of the effects of polyamines on the modulation of the N-methyl-D-aspartate receptor by glycine.
复制标题
表征多胺对甘氨酸调节 N-甲基-D-天冬氨酸受体的影响。
DOI：
10.1016/0028-3908(95)00086-l
复制
发表时间：
1995
影响因子：
4.7
通讯作者：
Rothermund,KD
中科院分区：
文献类型：
--
作者：
Reynolds,IJ;Rothermund,KD
We have investigated the effects of polyamine agonists and antagonists on the modulation of the N-Methyl-d-aspartate receptor by glycine using a [3H]dizocilpine ([3H]MK801) binding assay. We monitored the non-equilibrium binding of [3H]dizocilpine in the presence of 5,7-dichlorokynurenate to preclude occupation of the glycine site by endogenous glycine. Using this assay, spermine and spermidine increased both the affinity arid the maximum effect of glycine. Similar effects are produced by other polyamine agonists including 1,5-diethylaminopiperidine, neomycin and Ca2+. These actions are reversed by the polyamine antagonists arcaine and 1,10-diaminodecane in a competitive manner. The increase in the maximum effect of glycine produced by polyamine agonists appears to be due to an increase in the equilibrium affinity of [3H]dizocilpine, and cannot therefore be attributed solely to modulation of glycine binding. Interestingly, 1,5-diethylaminopiperidine increases the maximum effect of glycine to a greater extent than it alters glycine affinity, suggesting that the two effects may be mediated by different sites or mechanisms. These studies will help to define the role of the glycine site in the modulation of the N-Methyl-d-aspartate receptor by polyamines.
