Inhibition of NMDA NR 1 - NR 2 A Receptors

The N - terminal domains of both NR 1 and NR 2 subunits determine allosteric Zn 2 + inhibition and glycine affinity of NMDA receptors

N-methyl-D-aspartic acid receptor expression in the dorsolateral prefrontal cortex of elderly patients with schizophrenia.

OBJECTIVE The N-methyl-D-aspartic acid (NMDA) class of glutamate receptors has received attention in the pathophysiology of schizophrenia because of the similarity between some schizophrenic symptoms and symptoms caused by NMDA antagonists. To determine if NMDA receptor abnormalities were present at the mRNA level, expression of NMDA receptor (NR) subunits NR(1), NR(2A), and NR(2B) was measured...

Polyamine regulation of the NMDA receptor complex as a target in drug development

 The NMDA receptor complex (NR) is one of the main targets of the excitatory neurotransmitter glutamic acid. A partial block of the NR by protons even at physiological pH can by removed by the natural polyamines (PAs) spermidine and spermine. Several unbranched diamines as arcaine and 1,12-dodecanediamine (N12N) seem to block the NR (at least to some extent) via the same mechanism (polyamine i...

Pentamidine analogs as inhibitors of [(3)H]MK-801 and [(3)H]ifenprodil binding to rat brain NMDA receptors.

The anti-protozoal drug pentamidine is active against opportunistic Pneumocystis pneumonia, but in addition has several other biological targets, including the NMDA receptor (NR). Here we describe the inhibitory potencies of 76 pentamidine analogs at 2 binding sites of the NR, the channel binding site labeled with [(3)H]MK-801 and the [(3)H]ifenprodil binding site. Most analogs acted weaker at ...

Prenatal exposure of testosterone prevents SDN-POA neurons of postnatal male rats from apoptosis through NMDA receptor.

The role of N-methyl-D-aspartate (NMDA) receptor in mediating the effect of testosterone exposure prenatally on neuronal apoptosis in the sexual dimorphic nucleus of the preoptic area (SDN-POA) of rats was studied. The endogenous testosterone was diminished by prenatal stress (PNS) or simulated by testosterone exposure (TE) to understand the effect of testosterone on NR(1) (a functional subunit...