[Effects of N-phthalamoyl-L-glutaminic acid, a selective agonist of NMDA receptor, on binding of 3H-L-glutamate with synaptic membranes of the hippocampus].
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.
Koreshonkov
O N
ON
Perestenko
P V
PV
Dumpis
M A
MA
Piotrovskiĭ
L B
LB
D001665:Binding Sites; D005971:Glutamates / Q000378:metabolism* / Q000494:pharmacology*; D006624:Hippocampus / Q000378:metabolism*; D006801:Humans; D066298:In Vitro Techniques; D016202:N-Methylaspartate / Q000378:metabolism; D016194:Receptors, N-Methyl-D-Aspartate / Q000187:drug effects* / Q000378:metabolism / Q000502:physiology; D013570:Synaptic Membranes / Q000378:metabolism*
D005971:Glutamates; D016194:Receptors, N-Methyl-D-Aspartate; C034741:N-phthaloylglutamic acid; D016202:N-Methylaspartate
Vliianie N-ftalamoil-L-glutaminovoĭ kisloty, selektivnogo agonista retseptorov NMDA, na sviazyvanie 3H-L-glutamata s sinapticheskimi membranami gippokampa.