The novel water-soluble N-methyl-D-aspartate (NMDA) receptor antagonists, N-{4-[4-(4-Guanidinobutylamino)butylamino]butyl}-p-toluenesulfonamide trihydrochloride (1a, TsHSPMG), N-{4-[4-(4-Guanidinobutylamino)butylamino]butyl}butane-1-sulfonamide trihydrochloride (1b, BsHSPMG), N-{3-[4-(3-Guanidinopropylamino)butylamino]propyl}-p-toluenesulfonamide trihydrochroride (2a, TsSPMG) and N-{3-[4-(3-Gua...

The effect of glutamate receptor agonists on the intracellular free calcium concentration ([Ca2+]i), measured with Indo-1, was studied in populations of cultured chick embryonic retina cells. The agonists of the ionotropic glutamate receptors, N-methyl-D-aspartate (NMDA), kainate, and alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) increased the [Ca2+]i through a composite effec...

The aim of this study was to investigate the effects of magnesium as a N-Methyl–D-Aspartate (NMDA) receptor Antagnist and bromocriptine as a dopamine receptor agonist on morphine dependence and withdrawal symptoms. In the present study different groups of mice were received morphine (50 mg/kg, i.p.) for four days and on fourth day 1.5 hour after the last morphine administration they received di...

A number of studies have indicated an important role for N-methyl-D-aspartate (NMDA) receptors in cell survival versus cell death decisions during neuronal development, trauma, and ischemia. Coupling of neurons by electrical synapses (gap junctions) is high or increases in neuronal networks during all three of these conditions. However, whether neuronal gap junctions contribute to NMDA receptor...

N-methyl-D-aspartate (NMDA) glutamate receptor-mediated increases in intracellular calcium are thought to play a critical role in synaptic plasticity. The mechanisms by which changes in cytoplasmic calcium transmit the glutamate signal to the nucleus, which is ultimately important for long-lasting neuronal responses, are poorly understood. We show that NMDA receptor stimulation leads to activat...

Peripheral N-methyl-d-aspartate (NMDA) receptors are found in deep tissues and may play a role in deep tissue pain. Injection of the endogenous NMDA receptor agonist glutamate into the masseter muscle excites deep craniofacial afferent fibers in rats and evokes pain in human subjects. It is not clear whether peripheral NMDA receptors play a role in these effects of glutamate. Accordingly, the e...

Cerebellar granule cells are susceptible to the excitotoxin glutamate, which acts at N-methyl-D-aspartate (NMDA) receptors, as well as the neurotoxin 1-methyl-4-phenylpyridinium ion (MPP+), the active cytotoxic metabolite of 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP). Paradoxically, preincubation of cultured cerebellar granule cells with low concentrations of NMDA or glutamate markedly...

The effect of H+ on the N-methyl-D-aspartate-induced (NMDA) membrane current in enzymatically isolated catfish cone horizontal cells was investigated. Extracellular acidification to pH 5.5 blocked nearly completely the NMDA-induced current and reduced desensitization. The pK for the H+ effect was 6.5, near that for the free amino acid histidine. Protons did not alter the receptor affinity for N...

The noble gas xenon is an antagonist of the NMDA (N-methyl-D-aspartate)-type glutamate receptor which may account for the ideal anesthetic profile and potent neuroprotective properties demonstrated even at subanesthetic concentrations. Because lipid emulsions also promote NMDA antagonistic effects they may serve as ideal carriers for xenon. In this in vitro study, we investigated the efficacy o...

Multiple lines of evidence indicate that hypofunction of glutamatergic neurotransmission via N-methyl-D-aspartate (NMDA) receptors might be implicated in the pathophysiology of schizophrenia, suggesting that increasing NMDA receptor function via pharmacological manipulation could provide a new strategy for the management of schizophrenia. Currently, the glycine modulatory sites on NMDA receptor...