Koreshonkov O N, Perestenko P V, Dumpis M A, Piotrovskiĭ L B
Biull Eksp Biol Med. 1992 Jun;113(6):563-5.
In the present investigation the interaction of a novel selective NMDA receptors agonist, N-phthalamoyl-L-glutamic acid (PhGA), with the synaptic membranes preparation of human hippocampus was examined against NMDA. It was established that there are two binding sites of 3H-L-Glu, Kd1 = 0.35 +/- 0.11 nM, Bmax1 = 6.5 +/- 2.3 pmol/mg and Kd2 = 51 +/- 12 nM, Bmax2 = 98 +/- 17 pmol/mg. The inhibition constants (Ki) were calculated for NMDA and PhGA and were equal: Ki(NMDA) = 19 microM, Ki (PhGA) = 13 microM, respectively. It was concluded that PhGA is the partial agonist of the NMDA receptors.
在本研究中，针对N-邻苯二甲酰-L-谷氨酸（PhGA）这种新型选择性N-甲基-D-天冬氨酸（NMDA）受体激动剂，研究了其与人脑海马体突触膜制剂的相互作用，并与NMDA进行了对比。已确定存在两个³H-L-谷氨酸的结合位点，解离常数Kd1 = 0.35 ± 0.11 nM，最大结合容量Bmax1 = 6.5 ± 2.3 pmol/mg，以及Kd2 = 51 ± 12 nM，Bmax2 = 98 ± 17 pmol/mg。计算得出NMDA和PhGA的抑制常数（Ki），结果分别为：Ki（NMDA） = 19 μM，Ki（PhGA） = 13 μM。得出的结论是，PhGA是NMDA受体的部分激动剂。
