Page last updated: 2024-11-05

n-methylaspartate

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Description

N-Methylaspartate: An amino acid that, as the D-isomer, is the defining agonist for the NMDA receptor subtype of glutamate receptors (RECEPTORS, NMDA). [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

N-methyl-D-aspartic acid : An aspartic acid derivative having an N-methyl substituent and D-configuration. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Cross-References

ID SourceID
PubMed CID22880
CHEMBL ID291278
CHEBI ID31882
SCHEMBL ID2220
MeSH IDM0024738

Synonyms (103)

Synonym
n-methylaspartate
methyl aspartic acid
n-methyl aspartic acid
d-aspartic acid, n-methyl-
brn 1724431
aspartic acid, n-methyl-
DIVK1C_000392
KBIO1_000392
EU-0100775
n-methyl-d-aspartic acid, >=98% (tlc), solid
SPECTRUM_001456
SPECTRUM5_001209
BSPBIO_003201
(nmda)
NCGC00015666-01
NCGC00024476-01
lopac-m-3262
tocris-0114
LOPAC0_000775
PDSP2_000767
IDI1_000392
PDSP1_000779
MLS001333165
MLS001333166
n-methyl-d-aspartate
n-methyl-d-aspartic acid
nmda
smr000326806
MLS000859947
NCGC00024476-04
KBIOSS_001936
KBIO2_001936
KBIO3_002421
KBIOGR_000936
KBIO2_004504
KBIO2_007072
NINDS_000392
SPBIO_001520
SPECTRUM3_001601
SPECTRUM2_001580
SPECTRUM4_000318
SPECTRUM1503636
NCGC00024476-02
NCGC00024476-05
NCGC00024476-03
6384-92-5
M 3262
NCGC00024476-06
n-methyl-d-aspartic acid (nmda)
(r)-2-(methylamino)succinic acid
CHEMBL291278 ,
n-methyl-daspartate
(2r)-2-(methylamino)butanedioic acid
HMS501D14
M1360
me-d-asp-oh
HMS1922G08
chebi:31882 ,
2-methylamino-succinic acid
(r)-2-methylamino-succinic acid
bdbm50013876
OEM ,
HMS3262K12
HMS2233F23
CCG-39358
1903b9q6pi ,
3-04-00-01522 (beilstein handbook reference)
unii-1903b9q6pi
LP00775
n-me-d-asp-oh
S7072
gtpl4268
HY-17551
SCHEMBL2220
NCGC00261460-01
tox21_500775
W-203368
nmda (n-methyl-d-aspartic acid)
nmda [mi]
methyl aspartic acid, d-
HB0454
AC-24119
(r)-2-ethylbutannedioic acid
mfcd00004226
DTXSID8041082
SR-01000597701-1
sr-01000597701
n-methyl d-aspartic acid
n-methyl d-aspartate
sr-01000075456
SR-01000075456-1
SW219059-1
(r)-2-(methylamino)succinic acid hydrochloride
Q632856
n-methyl-d-aspartic acid, hydrate - cas 6384-92-5
methyl-d-aspartic acid
AS-15576
AC2467
SDCCGSBI-0050753.P003
NCGC00024476-14
HMS3886P09
AKOS016843186
(r)-2-(methylamino)succinicacid

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" The neurotoxicity induced by carbamazepine may be involved in the teratogenic and adverse effects of overdose associated with the treatment of manic-depressive illness and seizures."( Carbamazepine-induced neurotoxicity and its prevention by NMDA in cultured cerebellar granule cells.
Chuang, DM; Gao, XM, 1992
)
0.28
" Low micromolar concentrations of memantine, levels known to be tolerated by patients receiving the drug for the treatment of Parkinson's disease, prevent NMDA receptor-mediated neurotoxicity in cultures of rat cortical and retinal ganglion cell neurons; memantine also appears to be both safe and effective in a rat stroke model."( Open-channel block of N-methyl-D-aspartate (NMDA) responses by memantine: therapeutic advantage against NMDA receptor-mediated neurotoxicity.
Aggarwal, SK; Chen, HS; Jensen, FE; Lei, SZ; Lipton, SA; Pellegrini, JW; Warach, S, 1992
)
0.28
" In contrast, oxidized DTT did not enhance NMDA toxicity nor was it toxic when added alone."( The action of CGS-19755 on the redox enhancement of NMDA toxicity in rat cortical neurons in vitro.
Aizenman, E; Hartnett, KA, 1992
)
0.28
" Both glutamate and N-methyl-D-aspartate (NMDA) were toxic to cultured cortical cells, as demonstrated by a reduction in their ability to exclude trypan blue dye, and this toxicity was reversed by the NMDA antagonist MK-801."( Ethanol inhibits excitotoxicity in cerebral cortical cultures.
Chan, J; Greenberg, DA; Lustig, HS, 1992
)
0.28
"-) immunoreactivity is colocalized with nicotinamide adenine di-nucleotide phosphate diaphorase in neurons that are uniquely resistant to toxic insults."( Nitric oxide mediates glutamate neurotoxicity in primary cortical cultures.
Bredt, DS; Dawson, TM; Dawson, VL; London, ED; Snyder, SH, 1991
)
0.28
" The antagonistic properties of kynurenate were dose-dependent: equimolar kynurenate had no effect on quinolinate but attenuated the actions of ibotenate, kainate and NMDA; 2 x equimolar kynurenate had no effect on quinolinate or ibotenate but attenuated the toxicity of kainate and NMDA; and 3 x equimolar kynurenate had no effect on the toxicity of kainate or ibotenate, attenuated the actions of NMDA and abolished the toxic action of quinolinate."( A comparison of excitotoxic lesions of the basal forebrain by kainate, quinolinate, ibotenate, N-methyl-D-aspartate or quisqualate, and the effects on toxicity of 2-amino-5-phosphonovaleric acid and kynurenic acid in the rat.
Clark, AJ; Hastings, MH; Latimer, M; Stone, TW; Winn, P, 1991
)
0.28
" In the present study on these neurons, calcium channel antagonists were found at 500-1000 nM concentrations to attenuate the early rise in [Ca2+]i and the subsequent toxic effects of exogenous glutamate, N-methyl-D-aspartate (NMDA), or an endogenous glutamate-related compound present in the retinal cultures."( Calcium channel antagonists attenuate NMDA receptor-mediated neurotoxicity of retinal ganglion cells in culture.
Lei, SZ; Lipton, SA; Sucher, NJ, 1991
)
0.28
" No toxic effect of quisqualate is observed."( Kainate and NMDA toxicity for cultured developing and adult rat spiral ganglion neurons: further evidence for a glutamatergic excitatory neurotransmission at the inner hair cell synapse.
Delrée, P; Lefebvre, PP; Leprince, P; Moonen, G; Rigo, JM; Rogister, B; Weber, T, 1991
)
0.28
" Prior incubation with NMDA (MK-801) or non-NMDA (glutamate diethyl ester, (GDEE] receptor antagonists protected the slices against NAAG-mediated neurotoxicity, indicating the possible involvement of both of these classes of receptors in the toxic action of NAAG."( Toxicity of N-acetylaspartylglutamate and its protection by NMDA and non-NMDA receptor antagonists.
Pai, KS; Ravindranath, V, 1991
)
0.28
" Immature cortical neurons are insensitive to the toxic effects of glutamate receptor stimulation."( Glutamate toxicity in immature cortical neurons precedes development of glutamate receptor currents.
Baraban, JM; Murphy, TH, 1990
)
0.28
" The toxic effects were observed early during the development of the neuronal culture (from 4 days in vitro on) and seemed to be neuron-specific since astrocyte cultures were not affected."( Attenuation of neurotoxicity following anoxia or glutamate receptor activation in EGF- and hippocampal extract-treated neuronal cultures.
Leysen, JE; Pauwels, PJ; van Assouw, HP, 1989
)
0.28
" DX also antagonized morphological and chemical (lactate dehydrogenase efflux) evidence of cortical neuronal cell injury produced by toxic bath exposure to NMDA, quinolinate or glutamate, but did not affect toxic exposure to quisqualate or kainate."( Dextrorphan and levorphanol selectively block N-methyl-D-aspartate receptor-mediated neurotoxicity on cortical neurons.
Choi, DW; Peters, S; Viseskul, V, 1987
)
0.27
"It has long been proposed that the excitatory and toxic properties of acidic amino acid receptor agonists are linked."( Amino acid neurotoxicity: relationship to neuronal depolarization in rat cerebellar slices.
Garthwaite, G; Garthwaite, J; Hajós, F, 1986
)
0.27
"Controversy exists concerning the sensitivity of neurons of the paraventricular nucleus (PVN) of the hypothalamus to the toxic effects of N-methyl aspartic acid (NMA)."( Evidence that neurons of the paraventricular nucleus of the hypothalamus with projections to the spinal cord are sensitive to the toxic effects of N-methyl aspartic acid.
Badura, LL; Brown, MH; Nunez, AA, 1987
)
0.27
" In parallel experiments, the calcium ionophore A23187 was not toxic in the presence of calcium."( The neurotoxicity of excitatory amino acids is produced by passive chloride influx.
Rothman, SM, 1985
)
0.27
"9 LD50 dose of soman reduced the severity of convulsions and increased survival."( Assessment of primary neuronal culture as a model for soman-induced neurotoxicity and effectiveness of memantine as a neuroprotective drug.
Deshpande, SS; Filbert, MG; Smith, CD, 1995
)
0.29
" We have investigated the receptor specificity of endogenous glutamate's toxic effects in organotypic cultures of the hippocampus by acute blockade of these transporters."( Neurotoxicity of acute glutamate transport blockade depends on coactivation of both NMDA and AMPA/Kainate receptors in organotypic hippocampal cultures.
Park, J; Tasker, RC; Vornov, JJ, 1995
)
0.29
" Among various processes that have been thought to mediate the toxic effects of glutamate are activation of the Ca(2+)-dependent proteases calpain I and II and the activation of nitric oxide synthase."( Delayed antagonism of calpain reduces excitotoxicity in cultured neurons.
Brorson, JR; Marcuccilli, CJ; Miller, RJ, 1995
)
0.29
" This inhibitor also limited the toxicity, even when applied at times up to 1 hour after the onset of the toxic exposure."( Delayed antagonism of calpain reduces excitotoxicity in cultured neurons.
Brorson, JR; Marcuccilli, CJ; Miller, RJ, 1995
)
0.29
" MK-801 (a non-competitive antagonist of NMDA receptors; 100 nM) completely inhibited the toxic and trophic actions of glutamate and NMDA, as well as the 45Ca2+ influx induced by NMDA, but only 80% of the 45Ca2+ influx induced by glutamate."( Ethanol inhibits NMDA-induced toxicity and trophism in cultured cerebellar granule cells.
Korpi, ER; Wegelius, K, 1995
)
0.29
" KA and AMPA were found to be more toxic than either N-methyl-D-aspartate (NMDA), quinolinate, or glutamate, both under normal conditions and under states of energy deprivation."( Kainate toxicity in energy-compromised rat hippocampal slices: differences between oxygen and glucose deprivation.
Rigor, BM; Schurr, A, 1993
)
0.29
" Thus, these results show that statin, which is expressed at low levels in embryonic rat cultured hippocampal neurons, is rapidly overexpressed following a toxic insult produced by the activation of the NMDA receptor."( Statin, a marker of cell cycle arrest, is overexpressed during the early phase of delayed NMDA toxicity in hippocampal cell cultures.
Alonso, R; Boksa, P; Buisson, N; Diorio, J; O'Donnell, D; Poirier, J; Quirion, R, 1994
)
0.29
" We have previously shown that although nerve injury at five days does not result in any motoneuron death, it does render these neurons susceptible to the toxic effects of the glutamate agonist N-methyl-D-aspartate."( Transient muscle paralysis in neonatal rats renders motoneurons susceptible to N-methyl-D-aspartate-induced neurotoxicity.
Greensmith, L; Mentis, GZ; Sanusi, J; Vrbová, G, 1995
)
0.29
" Specific activity of GAD but not ChAT was found to be significantly decreased in hippocampi of ethanol-dependent animals following injection of NMDA, suggesting that chronic ethanol administration sensitizes GABAergic neurons to the toxic effects of excitatory amino acid transmitters."( Chronic ethanol administration sensitizes hippocampal neurons to neurotoxicity of N-methyl-D-aspartic acid.
Davidson, M; Shanley, BC; Wilce, PA, 1993
)
0.29
" Furthermore, adult motoneurons remain resistant to the toxic effects of N-methyl-D-aspartate, even after nerve injury."( Nerve injury increases the susceptibility of motoneurons to N-methyl-D-aspartate-induced neurotoxicity in the developing rat.
Greensmith, L; Hasan, HI; Vrbová, G, 1994
)
0.29
"Membrane-permeating, fluorescent Ca2+ indicators have been used to investigate the role of increased intracellular Ca2+ (Ca2+i) levels in excitotoxic neuronal injury, but their ability to chelate Ca2+i and their own toxic effects in some cells could obscure this relationship."( Calcium indicators and excitotoxicity in cultured cortical neurons.
Ahern, KV; Chan, J; Greenberg, DA; Lustig, HS, 1993
)
0.29
"Recent reports suggest that NMDA receptor antagonists when administered in vivo can protect dopaminergic neurons from the toxic actions of MPP+."( The N-methyl-D-aspartate antagonist MK-801 fails to protect dopaminergic neurons from 1-methyl-4-phenylpyridinium toxicity in vitro.
Finiels-Marlier, F; Marini, AM; Paul, SM; Williams, P, 1993
)
0.29
"We have previously shown that ascorbic acid (AA) protects cortical neurons in culture from the toxic effects of NMDA."( Interaction of ascorbic acid with the neurotoxic effects of NMDA and sodium nitroprusside.
Beglan, CL; Bell, JA; London, ED, 1996
)
0.29
" The neuropeptide vasoactive intestinal peptide and inhibitors of poly(ADP-ribose) polymerase also prevented this injury, but without inhibiting NO synthesis, both acting by inhibiting a toxic action of NO that is critical to tissue injury."( Excitotoxicity in the lung: N-methyl-D-aspartate-induced, nitric oxide-dependent, pulmonary edema is attenuated by vasoactive intestinal peptide and by inhibitors of poly(ADP-ribose) polymerase.
Berisha, HI; Pakbaz, H; Said, SI, 1996
)
0.29
" Persisting stimulation of mGluRs after the toxic exposure did not improve the survival of pyramidal or granular cells."( Activation of multiple metabotropic glutamate receptor subtypes prevents NMDA-induced excitotoxicity in rat hippocampal slices.
Consolandi, O; Memo, M; Pizzi, M; Spano, PF, 1996
)
0.29
" Recently, there have been several reports that A beta has toxic effects on both cultured neurons and in the brain."( A new compound (AZ36041) promotes the survival of the neurons and reduces neurotoxicity of Alzheimer's beta-amyloid protein.
Aratake, H; Endo, T; Hasegawa, Y; Kitaguchi, N; Morikawa, A; Ogawa, K; Sugimoto, E, 1995
)
0.29
" In the present paper, the authors comment on an important role of glutamatergic systems in the behavioral and toxic effects of MA."( The role of glutamate in behavioral and neurotoxic effects of methamphetamine.
Abekawa, T; Koyama, T; Ohmori, T, 1996
)
0.29
"D-myo-Inositol hexakisphosphate (InsP6, phytate), a normal cellular constituent, was found to be toxic to neuronal perikarya when injected into the rat hippocampus."( Neuronal cytotoxicity of inositol hexakisphosphate (phytate) in the rat hippocampus.
Lees, GJ; Leong, W, 1996
)
0.29
"Extracellular levels of endogenous glutamate are relatively high in the developing rabbit retina but nonetheless appear to promote cell survival and developmental processes at concentrations considered toxic in the adult."( N-methyl-D-aspartate-mediated glutamate toxicity in the developing rabbit retina.
Haberecht, MF; Lo, GJ; Mitchell, CK; Redburn, DA, 1997
)
0.3
" Activation of the coagulation system and adverse effects of homocysteine on the endothelium and vessel wall are believed to underlie disease pathogenesis."( Neurotoxicity associated with dual actions of homocysteine at the N-methyl-D-aspartate receptor.
Arnelle, DR; Choi, YB; D'Emilia, DM; Kim, WK; Kumar, S; Lipton, SA; Rayudu, PV; Stamler, JS, 1997
)
0.3
"Dopamine (DA), at concentrations greater than 100 microM, has previously been demonstrated to be toxic to mesencephalic, striatal and dorsal root ganglion cell cultures."( Dopamine neurotoxicity in cortical neurons.
Alagarsamy, S; Johnson, KM; Pappas, T; Phillips, M, 1997
)
0.3
" In particular, the amino acid glutamate has been shown to act as a neurotoxin which exerts its toxic effect on RGCs predominantly through the N-methyl-D-aspartate (NMDA) subtype of glutamate receptor."( Molecular basis of glutamate toxicity in retinal ganglion cells.
Dreyer, EB; Lipton, SA; Sucher, NJ, 1997
)
0.3
" Autonomic motor neurons that were stained for either nicotinamide adenine dinucleotide phosphate reduced diaphorase or choline acetyltransferase only were both able to tolerate 50 microM N-methyl-D-aspartate treatment for over seven days in culture with no apparent adverse effects."( Differential vulnerability of autonomic and somatic motor neurons to N-methyl-D-aspartate-induced excitotoxicity.
Annis, CM; Vaughn, JE, 1998
)
0.3
"Neuronal nitric oxide synthase (nNOS) neurons kill adjacent neurons through the action of NMDA-glutamate receptor activation, although they remain relatively resistant to the toxic effects of NMDA and NO."( Manganese superoxide dismutase protects nNOS neurons from NMDA and nitric oxide-mediated neurotoxicity.
Dawson, TM; Dawson, VL; Engelhardt, JF; Ensz, LM; Gonzalez-Zulueta, M; Lebovitz, RM; Mukhina, G; Oberley, LW; Zwacka, RM, 1998
)
0.3
" Brief exposures to toxic NMDA concentrations induced significant increases in superoxide production which correlated with the degree of neuronal injury."( NMDA-induced superoxide production and neurotoxicity in cultured rat hippocampal neurons: role of mitochondria.
Krieglstein, J; Prehn, JH; Preis, E; Sengpiel, B, 1998
)
0.3
"Microglia have been shown to be immunostimulated by inflammatory cytokines and produce a number of toxic mediators."( Potentiation of N-methyl-D-aspartate-mediated neurotoxicity by immunostimulated murine microglia.
Kim, WK; Ko, KH, 1998
)
0.3
" This previously unrecognized toxic action of glutamate constituted a chief excitotoxic mechanism under conditions producing submaximal Ca2+ loading."( Distinct influx pathways, not calcium load, determine neuronal vulnerability to calcium neurotoxicity.
Charlton, MP; Hafner, M; Sattler, R; Tymianski, M, 1998
)
0.3
" Lowering the IOP may slow down glutamate production, but if nothing is done to block the toxic effects of glutamate as well, visual loss may result despite excellent IOP control."( An experimental basis for implicating excitotoxicity in glaucomatous optic neuropathy.
Dreyer, EB; Gorla, MS; Vorwerk, CK, 1999
)
0.3
" In contrast, neither QA up to 5 mM nor trans-ACPD had a significant toxic effect in either KCl group."( NMDA and non-NMDA receptor-mediated excitotoxicity are potentiated in cultured striatal neurons by prior chronic depolarization.
Chen, Q; Reiner, A; Surmeier, DJ, 1999
)
0.3
" We report that, at high concentrations (300 microM-30 mM), a folic acid hexaglutamate analog is dose-dependently toxic to dissociated rat cortical cultures and that this toxicity is reversed by 2-PMPA, a potent and selective NAALADase inhibitor."( Toxicity induced by a polyglutamated folate analog is attenuated by NAALADase inhibition.
Olkowski, JL; Slusher, BS; Thomas, AG; Vornov, JJ, 1999
)
0.3
" Any evaluation of the efficacy of a putative viral vector should consider the possible protective or toxic effect of the native virus."( Infection with adeno-associated virus may protect against excitotoxicity.
Bennett, J; Dreyer, EB; Simon, PD; Vorwerk, CK; Zurakowski, D, 1999
)
0.3
" In particular, murine amacrine neurons have been known to show marked susceptibility to the toxic effects of kainate."( Involvement of NMDA-receptor in kainate-induced neurotoxicity in cultured fetal retinal neurons.
Akaike, A; Honda, Y; Kashii, S; Sasa, M; Tamura, Y; Ujihara, H; Yasuyoshi, H; Zhang, S, 2000
)
0.31
" Besides adverse effects on the endothelium and vessel wall, Hcy exert a toxic action on neuronal cells trough the stimulation of N-methyl-D-aspartate (NMDA) receptors."( [Hyperhomocysteinemia: atherothrombosis and neurotoxicity].
Fridman, O, 1999
)
0.3
" Mixed or pure neuronal cultures were also exposed for 48 h to a toxic fragment of the beta-amyloid peptide (beta-amyloid peptide-(25-35), 12."( Neuroprotective activity of chemokines against N-methyl-D-aspartate or beta-amyloid-induced toxicity in culture.
Besong, G; Bruno, V; Copani, A; Nicoletti, F; Scoto, G, 2000
)
0.31
" Excitotoxicity is thought to underlie these and other toxic models of neuronal death."( NMDA but not non-NMDA excitotoxicity is mediated by Poly(ADP-ribose) polymerase.
Berliner, AR; Dawson, TM; Dawson, VL; Feldman, A; Guastella, DB; Herring, WJ; Mandir, AS; Poirier, GG; Poitras, MF; Wang, ZQ, 2000
)
0.31
" The following mechanisms are discussed now: (1) possible increase in extracellular glutamate via release or inhibition of uptake/degradation, (2) generation of cysteine alpha-carbamate, a toxic analog of NMDA, (3) generation of toxic oxidized cysteine derivatives, (4) chelation of Zn2+ which blocks the NMDA receptor-ionophore, (5) direct interaction with the NMDA receptor redox site(s), (6) generation of free radicals, and (7) formation of S-nitrosocysteine."( Mechanisms of L-cysteine neurotoxicity.
Hermann, A; Janáky, R; Oja, SS; Saransaari, P; Varga, V, 2000
)
0.31
" This was likely because of the fact that glutamate, now toxic at much lower concentrations, was able to reach and activate dendritic receptors under these conditions."( NMDA and glutamate evoke excitotoxicity at distinct cellular locations in rat cortical neurons in vitro.
Aizenman, E; Blitzblau, RC; Du, S; Leszkiewicz, DN; Rosenberg, PA; Sinor, JD; Venneti, S, 2000
)
0.31
" Acetaldehyde, on the other hand, is toxic by itself at low concentrations (> or =10 mM)."( A comparison between acute exposures to ethanol and acetaldehyde on neurotoxicity, nitric oxide production and NMDA-induced excitotoxicity in primary cultures of cortical neurons.
Wan, JY; Wang, JY; Wang, Y, 2000
)
0.31
"The potential toxic effects of the metabotropic glutamate receptor agonist (1S,3R)-1-aminocyclopentane-1,3-dicarboxylic acid (ACPD) and its interactions with the N-methyl-D-aspartate (NMDA) receptor were studied in hippocampal brain slice cultures, using densitometric measurements of the cellular uptake of propidium iodide (PI) to quantify neuronal degeneration."( The metabotropic glutamate receptor agonist 1S,3R-ACPD stimulates and modulates NMDA receptor mediated excitotoxicity in organotypic hippocampal slice cultures.
Blaabjerg, M; Bonde, C; Kristensen, BW; Zimmer, J, 2001
)
0.31
" In mixed cultures of cortical cells, the selective mGlu1/5 agonist, 3,5-dihydroxyphenylglycine (DHPG), amplified neurodegeneration induced by a toxic pulse of NMDA."( An activity-dependent switch from facilitation to inhibition in the control of excitotoxicity by group I metabotropic glutamate receptors.
Battaglia, G; Bruno, V; Ceña, V; Cespédes, VM; Copani, A; Flor, PJ; Galindo, MF; Gasparini, F; Kuhn, R; Nicoletti, F; Sánchez-Prieto, J, 2001
)
0.31
" Both protective and toxic effects of IL-1 were fully antagonized by IL-1 receptor antagonist."( Interleukin-1beta exacerbates hypoxia-induced neuronal damage, but attenuates toxicity produced by simulated ischaemia and excitotoxicity in rat organotypic hippocampal slice cultures.
Anthony, DC; Iannotti, F; Johns, P; Niyadurupola, N; Pringle, AK, 2001
)
0.31
"In this study, we have focused our investigation of the facts whether co-administration of a NMDA antagonist dextromethorphan (DM) with morphine during pregnancy and throughout lactation could prevent the adverse effects associated with chronic morphine administration in rat offspring."( Co-administration of dextromethorphan during pregnancy and throughout lactation significantly decreases the adverse effects associated with chronic morphine administration in rat offspring.
Su, CH; Tao, PL; Wu, YH; Yeh, GC, 2001
)
0.31
" We therefore explored whether a glutamate congener was toxic if applied directly within the optic nerve, or if toxicity depended upon an interaction at the cell body level."( Excitotoxicity can be mediated through an interaction within the optic nerve; activation of cell body NMDA receptors is not required.
Dreyer, EB; McDermott, LM; Naskar, R; Quinto, KM; Schuettauf, F; Vorwerk, CK; Zurakowski, D, 2001
)
0.31
" The pathomechanisms involved are still unknown, a contribution of toxic organic acids, in particular MMA, has been suggested."( Neurodegeneration in methylmalonic aciduria involves inhibition of complex II and the tricarboxylic acid cycle, and synergistically acting excitotoxicity.
Farkas, LM; Feyh, P; Hinz, A; Hoffmann, GF; Hörster, F; Kölker, S; Mayatepek, E; Okun, JG; Sauer, S; Unsicker, K, 2002
)
0.31
" Memantine was well tolerated with a frequency of adverse events comparable to placebo."( Efficacy and safety of memantine in patients with mild to moderate vascular dementia: a randomized, placebo-controlled trial (MMM 300).
Forette, F; Möbius, HJ; Orgogozo, JM; Rigaud, AS; Stöffler, A, 2002
)
0.31
" It might suggest that, because of individual differences, the pharmacological use of NMDA-antagonist for neuroprotective purposes might have an adverse effect, even if the affinity is low."( Immune-related mechanisms participating in resistance and susceptibility to glutamate toxicity.
Kimchi, A; Raveh, T; Schori, H; Schwartz, M; Wheeler, LA; Yoles, E, 2002
)
0.31
"Cerebellar granule cells (CGCs) express K+-dependent (NCKX) and K+-independent (NCX) plasmalemmal Na+/Ca2+ exchangers which, under plasma membrane-depolarizing conditions and high cytosolic [Na+], may reverse and mediate potentially toxic Ca2+ influx."( In depolarized and glucose-deprived neurons, Na+ influx reverses plasmalemmal K+-dependent and K+-independent Na+/Ca2+ exchangers and contributes to NMDA excitotoxicity.
Czyz, A; Kiedrowski, L, 2002
)
0.31
" The results showed that NMDA (1 mM) had toxic effect on the rat cortical neurons on 12, but not on 7 day in vitro."( Neuroprotective effects of estrone on NMDA-induced toxicity in primary cultures of rat cortical neurons are independent of estrogen receptors.
Bień, E; Kajta, M; Lasoń, W; Marszał, M,
)
0.13
" Safety and tolerability evaluation included adverse events, physical examination, vital functions, electrocardiogram, laboratory tests, and 24-hour Holter (100-mg and 450-mg dose panels)."( Safety, pharmacokinetics, and pharmacodynamics of CHF 3381, a novel N-methyl-D-aspartate antagonist, after single oral doses in healthy subjects.
Dostert, P; Fabbri, L; Guillevic, Y; Imbimbo, BP; Mariotti, F; Rondelli, I; Tarral, A, 2003
)
0.32
" A better understanding of the mechanism underlying these adverse effects should allow for the safer use of these agents and might clarify mechanisms underlying certain clinical disorders."( Muscimol prevents NMDA antagonist neurotoxicity by activating GABAA receptors in several brain regions.
Dikranian, K; Farber, NB; Jiang, X; Nemmers, B, 2003
)
0.32
" It has been discovered, however, that many of these compounds cause adverse behavioral (psychotomimetic) effects and can produce neurotoxicity characterized by neuronal vacuolization, induction of heat-shock protein, neuronal/axonal degeneration and regional brain cell death in several animal species."( Review of NMDA antagonist-induced neurotoxicity and implications for clinical development.
Low, SJ; Roland, CL, 2004
)
0.32
" Given that cigarette smoking is highly prevalent in some of these patient groups and nicotine has been shown to reduce toxic consequences of NMDA receptor function, it may be suggested that nicotine intake may attenuate the neurotoxic effects of hypercortisolemia."( (-)-nicotine ameliorates corticosterone's potentiation of N-methyl-d-aspartate receptor-mediated cornu ammonis 1 toxicity.
Harris, BR; Littleton, JM; Mulholland, PJ; Prendergast, MA; Self, RL, 2004
)
0.32
" We tested whether the NCX or NCKX family of exchangers contributes most to the toxic NMDA-induced Ca(2+) influx in depolarized neurons."( Differential contribution of plasmalemmal Na/Ca exchange isoforms to sodium-dependent calcium influx and NMDA excitotoxicity in depolarized neurons.
Baranauskas, G; Czyz, A; Kiedrowski, L; Li, XF; Lytton, J, 2004
)
0.32
" However, adverse effects of tPA have been observed in animal models of ischemic brain injuries."( 2,7-Bis-(4-amidinobenzylidene)-cycloheptan-1-one dihydrochloride, tPA stop, prevents tPA-enhanced excitotoxicity both in vitro and in vivo.
Ali, C; Benchenane, K; Buisson, A; Fernández-Monreal, M; Léveillé, F; Liot, G; López-Atalaya, JP; Mackenzie, ET; Ruocco, A; Vivien, D, 2004
)
0.32
" However, many investigators doubt that NMDA antagonists are safe and effective for treating persons with AD because they have failed in stroke and trauma programs."( Why do many NMDA antagonists fail, while others are safe and effective at blocking excitotoxicity associated with dementia and acute injury?
Albensi, BC; Igoechi, C; Ilkanich, E; Janigro, D,
)
0.13
"Minocycline has been shown to exert neuroprotection against a wide variety of toxic insults both in vitro and in vivo."( In vivo studies on the protective role of minocycline against excitotoxicity caused by malonate or N-methyl-d-aspartate.
Aguirre, N; Goñi-Allo, B; Jordán, J; Ramos, M, 2005
)
0.33
" The addition of homocysteinic acid in a nontoxic concentration of 100 microM potentiated the toxic effect of NMDA and led to massive cell death."( Homocysteinic acid causes oxidative stress in lymphocytes by potentiating toxic effect of NMDA.
Boldyrev, AA, 2005
)
0.33
" Increase in age decreased the SOD and MAO enzyme activities; Abeta (25-35) addition further had damaging/toxic effects on the enzymes, whereas NKB alone and in combination with amyloid lowered the toxic effects caused by Abeta (25-35) addition, which was concentration (peptide) and age dependent."( Neuroprotective role of neurokinin B (NKB) on beta-amyloid (25-35) induced toxicity in aging rat brain synaptosomes: involvement in oxidative stress and excitotoxicity.
Baquer, NZ; Cowsik, SM; Mantha, AK; Moorthy, K, 2006
)
0.33
" The aim of the present study was to examine the toxic effects of IL-1 on rat cortical cell cultures."( Interleukin-1-induced neurotoxicity is mediated by glia and requires caspase activation and free radical release.
Allan, SM; Gibson, RM; Pinteaux, E; Rothwell, NJ; Thornton, P, 2006
)
0.33
" Since the metabolic product of PLA(2) signaling, PGE(2), which augments toxic effect of NMDA, is known to stimulate cAMP, the effect of adenyl cyclase activator (forskolin plus IBMX) and inhibitor (MDL12,300) on NMDA-induced DPYSL3 degradation was tested."( PLA(2) signaling is involved in calpain-mediated degradation of synaptic dihydropyrimidinase-like 3 protein in response to NMDA excitotoxicity.
Chakravarthy, B; Kowara, R; Moraleja, KL, 2008
)
0.35
"Intravitreal drug administration leads to high intraocular concentrations with potentially toxic effects on ocular tissues."( Toxicity assessment of intravitreal triamcinolone and bevacizumab in a retinal explant mouse model using two-photon microscopy.
Euler, T; Jonas, JB; Mittmann, W; Rensch, F; Schlichtenbrede, FC; Vom Hagen, F, 2009
)
0.35
"2P microscopy in combination with SR101 staining allows fast morphologic assessment of living retinal explants and can be used to evaluate adverse effects on retinal viability of test substances."( Toxicity assessment of intravitreal triamcinolone and bevacizumab in a retinal explant mouse model using two-photon microscopy.
Euler, T; Jonas, JB; Mittmann, W; Rensch, F; Schlichtenbrede, FC; Vom Hagen, F, 2009
)
0.35
"Even at higher doses, bevacizumab and ranibizumab showed no toxic effects on RGC in vivo in either untreated rats or in the NMDA-induced RGC damage model."( Toxicity testing of the VEGF inhibitors bevacizumab, ranibizumab and pegaptanib in rats both with and without prior retinal ganglion cell damage.
Bartz-Schmidt, KU; Bolz, S; Choragiewicz, TJ; Fiedorowicz, M; Henke-Fahle, S; Schuettauf, F; Thaler, S; Tura, A; Yoeruek, E; Ziemssen, F; Zrenner, E, 2010
)
0.36
" To that aim, SOD1(G93A) or WT cultures were exposed to either NMDA by itself or to Zn²+ prior to a toxic challenge with NMDA, and neuronal loss evaluated 24 h later."( Zinc pre-treatment enhances NMDAR-mediated excitotoxicity in cultured cortical neurons from SOD1(G93A) mouse, a model of amyotrophic lateral sclerosis.
Frazzini, V; Longone, P; Marini, C; Nutini, M; Sensi, SL; Spalloni, A, 2011
)
0.37
"In addition to supporting rapid nerve conduction, myelination nurtures and stabilizes axons and protects them from acute toxic insults."( Myelin-associated glycoprotein protects neurons from excitotoxicity.
Ahmad, AS; Doré, S; Lopez, PH; Mehta, NR; Rowland, EA; Schnaar, RL; Toner, M; Zhang, J, 2011
)
0.37
" Our results suggest that altered activation of p38 MAPK contributes to mhtt enhancement of GluN2B/PSD-95 toxic signaling."( P38 MAPK is involved in enhanced NMDA receptor-dependent excitotoxicity in YAC transgenic mouse model of Huntington disease.
Fan, J; Gladding, CM; Kaufman, AM; Milnerwood, AJ; Raymond, LA; Wang, L; Zhang, LY, 2012
)
0.38
" A similar disruption of safe taste memories formation induced by the inhibition of protein synthesis in the perirhinal cortex (PRh) has been reported."( Basolateral amygdala lesions attenuate safe taste memory-related c-fos expression in the rat perirhinal cortex.
Gallo, M; Gámiz, F; Gómez-Chacón, B, 2012
)
0.38
" The current study shows that D3 mESCs differentiate efficiently into neural cells involving a neurosphere-like state and that this system is suitable to detect adverse effects of neurodevelopmental toxicants."( Neural differentiation of mouse embryonic stem cells as a tool to assess developmental neurotoxicity in vitro.
Gulich, K; Hayess, K; Luch, A; Oelgeschläger, M; Pohl, EE; Riebeling, C; Seiler, AE; Sittner, D; Slawik, B; Visan, A, 2012
)
0.38
" The resulting poly-glutamine expansion in the huntingtin protein imparts a novel toxic gain of function causing selective loss of medium spiny neurons (MSNs) in the striatum."( Decreasing Levels of the cdk5 Activators, p25 and p35, Reduces Excitotoxicity in Striatal Neurons.
Fan, J; Leavitt, BR; Lu, G; Park, KH; Raymond, LA, 2012
)
0.38
" Assessment of neuronal network functions using microelectrode array recordings revealed that hippocampal neurons expressing ATF3 were able to regain their ability for functional synaptic transmission and to participate in coherent neuronal network activity within 48 h after exposure to toxic concentrations of NMDA."( The nuclear calcium signaling target, activating transcription factor 3 (ATF3), protects against dendrotoxicity and facilitates the recovery of synaptic transmission after an excitotoxic insult.
Ahlgren, H; Bading, H; Bas-Orth, C; Freitag, HE; Hellwig, A; Ottersen, OP, 2014
)
0.4
" In the present study, we investigated whether and how EP chelates Zn(2+) in neurons when it is present at toxic levels."( Neuroprotective effect of ethyl pyruvate against Zn(2+) toxicity via NAD replenishment and direct Zn(2+) chelation.
Kim, HJ; Kim, SW; Lee, HK; Lee, JK; Yoon, SH, 2016
)
0.43
" R6W and wt Dyn A peptides were most toxic to primary cerebellar neurons."( Altered secondary structure of Dynorphin A associates with loss of opioid signalling and NMDA-mediated excitotoxicity in SCA23.
Bakalkin, G; Dooley, C; Marrink, SJ; McLaughlin, J; Melo, MN; Reits, E; Sinke, RJ; Smeets, CJ; Stargardt, A; Verbeek, DS; Zmorzyńska, J, 2016
)
0.43
"Diazoxide, a well-known mitochondrial KATP channel opener with neuroprotective effects, has been proposed for the effective and safe treatment of neuroinflammation."( Diazoxide enhances excitotoxicity-induced neurogenesis and attenuates neurodegeneration in the rat non-neurogenic hippocampus.
Andrade, C; Batlle, M; Gimeno-Bayón, J; Mahy, N; Martínez-Moreno, M; Ortega, FJ; Rodríguez, MJ, 2016
)
0.43
" The toxic effects of glutamate on RGCs are mediated by the overstimulation of N-methyl-D-aspartate (NMDA) receptors."( Neuroprotective Effect of Magnesium Acetyltaurate Against NMDA-Induced Excitotoxicity in Rat Retina.
Agarwal, P; Agarwal, R; Arfuzir, NN; Bakar, NS; Iezhitsa, I; Ismail, NM; Jafri, AJ; Krasilnikova, A; Kutty, MK; Lambuk, L; Ozerov, A; Rozali, KN; Spasov, A; Yusof, AP, 2017
)
0.46
"Although propofol is a widely used intravenous general anaesthetic, many studies report its toxic potential, particularly on the developing central nervous system."( Neurotoxicity of propofol on rat hypoglossal motoneurons in vitro.
Corsini, S; Ghezzi, F; Monni, L; Nistri, A, 2017
)
0.46
" One of the major adverse effects of cisplatin is its neurotoxicity."( Effect of memantine hydrochloride on cisplatin-induced neurobehavioral toxicity in mice.
Al-Baggou, BK; Salih, NA, 2020
)
0.56
" Unlike guanabenz, Sephin1 provides neuroprotection without adverse effects on the α2-adrenergic system and therefore it is considered a promising pharmacological therapeutic tool."( Sephin1 Protects Neurons against Excitotoxicity Independently of the Integrated Stress Response.
Alberdi, E; Luchena, C; Matute, C; Ortiz-Sanz, C; Ruiz, A; Zuazo, J, 2020
)
0.56
" Doxycycline has been postulated as the potential ideal candidate for further therapeutic development as it has fewer adverse effects than minocycline."( Minocycline, but not doxycycline attenuates NMDA-induced [Ca2+]i and excitotoxicity.
Chen, W; Du, N; Du, Y; Gu, H; Liu, Q; Lu, Y; Yang, Y, 2021
)
0.62
"Gelsenicine is one of the most toxic compounds in the genus Gelsemium, but the mechanism of toxicity is not clear."( Phosphoproteomics reveals NMDA receptor-mediated excitotoxicity as a key signaling pathway in the toxicity of gelsenicine.
Huang, CY; Huang, SJ; Liu, ZY; Qi, XJ; Zuo, MT, 2021
)
0.62
" In vivo, metformin treatment significantly increased the number of surviving RGCs, the b/NR wave amplitude and the thickness of the inner retina but had no obvious adverse effects on the fundus."( Regulation of mitophagy by metformin improves the structure and function of retinal ganglion cells following excitotoxicity-induced retinal injury.
Hu, FY; Liu, HL; Wu, JH; Xu, P, 2022
)
0.72
" In SH-SY5Y neuroblastoma cell lines they exhibited a neuroprotective effect against rotenone- and NMDA-mediated toxic insults."( Novel S1R agonists counteracting NMDA excitotoxicity and oxidative stress: A step forward in the discovery of neuroprotective agents.
Bedeschi, M; Collina, S; Denora, N; Dondio, G; Franchini, S; Linciano, P; Marino, N; Marsala, A; Miserocchi, G; Peviani, M; Rossi, D; Rossino, G; Sorbi, C; Tesei, A, 2023
)
0.91

Pharmacokinetics

ExcerptReferenceRelevance
" UK-240,455 has a short elimination half-life in rats, dogs and man (0."( Pharmacokinetics and disposition of a novel NMDA glycine site antagonist (UK-240,455) in rats, dogs and man.
Cole, S; Gedge, J; Roffey, S; Walker, D; Webster, R; Wild, W, 2003
)
0.32
"5-2 h) and cleared from plasma with a half-life of 3 to 4 hours."( Safety, pharmacokinetics, and pharmacodynamics of CHF 3381, a novel N-methyl-D-aspartate antagonist, after single oral doses in healthy subjects.
Dostert, P; Fabbri, L; Guillevic, Y; Imbimbo, BP; Mariotti, F; Rondelli, I; Tarral, A, 2003
)
0.32
" The discovery of 4,4-disubstituted piperidine inhibitors of GlyT1 which exhibit improved pharmacokinetic properties, including oral bioavailability, is discussed."( Discovery of GlyT1 inhibitors with improved pharmacokinetic properties.
Gibson, C; Hartman, GD; Jacobson, MA; Kinney, GG; Leister, WH; Lemaire, W; Lindsley, CW; Ma, BK; O'Brien, J; Pettibone, DJ; Polsky-Fisher, SL; Smith, S; Sur, C; Tiller, PR; Williams, DL; Wisnoski, DD; Wolkenberg, SE; Zhao, Z, 2009
)
0.35

Compound-Compound Interactions

ExcerptReferenceRelevance
" Here, using intracellular recording in vitro, we investigated the effects of topiramate on glutamatergic neurotransmission in the rat mPFC, both when given alone and in combination with raclopride or clozapine."( Differential effects of topiramate on prefrontal glutamatergic transmission when combined with raclopride or clozapine.
Jardemark, KE; Konradsson, A; Marcus, MM; Schilström, B; Svensson, TH, 2009
)
0.35

Bioavailability

ExcerptReferenceRelevance
") also decreased basal cGMP levels in mouse cerebellum for up to 3 h, a result suggesting brain bioavailability and a long duration of NMDA receptor antagonism in vivo."( Neurochemical interactions of competitive N-methyl-D-aspartate antagonists with dopaminergic neurotransmission and the cerebellar cyclic GMP system: functional evidence for a phasic glutamatergic control of the nigrostriatal dopaminergic pathway.
Cler, JA; Contreras, PC; Emmett, MR; Farah, JM; Iyengar, S; Mick, SJ; Rao, TS; Wood, PL, 1991
)
0.28
") injections of HA-966, demonstrating the bioavailability of this glycine receptor antagonist."( In vivo antagonism of agonist actions at N-methyl-D-aspartate and N-methyl-D-aspartate-associated glycine receptors in mouse cerebellum: studies of 1-hydroxy-3-aminopyrrolidone-2.
Cler, J; Emmett, MR; Iyengar, S; Mick, S; Oei, E; Rao, TS; Wood, PL, 1990
)
0.28
") did not affect cGMP responses, suggesting poor bioavailability in brain."( Indole-2-carboxylates, novel antagonists of the N-methyl-D-aspartate (NMDA)-associated glycine recognition sites: in vivo characterization.
Cler, JA; Cordi, AA; Dappen, MS; Emmett, MR; Gray, NM; Iyengar, S; Mick, SJ; Monahan, JB; Rao, TS; Wood, PL, 1993
)
0.29
" Impairment of glucose bioavailability reduced Rh 123 fluorescence."( Mitochondrial membrane potential measurement in rat cerebellar neurons by flow cytometry.
Camarasa, J; Camins, A; Comas, J; Escubedo, E; Gabriel, C; Sureda, FX, 1997
)
0.3
" Ingestion of food did not affect the extent of absorption of the drug, while the rate of absorption was considerably reduced (tmax = 4 h)."( Safety, pharmacokinetics, and pharmacodynamics of CHF 3381, a novel N-methyl-D-aspartate antagonist, after single oral doses in healthy subjects.
Dostert, P; Fabbri, L; Guillevic, Y; Imbimbo, BP; Mariotti, F; Rondelli, I; Tarral, A, 2003
)
0.32
" Although it has to be mentioned that the conclusion which can be drawn is limited, the bioavailability of the compounds could be different as well."( Glutamate agonists activate the hypothalamic-pituitary-adrenal axis through hypothalamic paraventricular nucleus but not through vasopressinerg neurons.
Makara, GB; Mergl, Z; Zelena, D, 2005
)
0.33
" Together, these data support the idea that the synthesis of estrogen can be rapidly regulated in the brain, thus producing rapid changes in local estrogen bioavailability that could rapidly modify brain function with a time course similar to what has previously been described for neurotransmitters and neuromodulators."( Rapid control of brain aromatase activity by glutamatergic inputs.
Baillien, M; Ball, GF; Balthazart, J, 2006
)
0.33
"These results suggest that ExT may have beneficial effects on the erectile dysfunction in diabetes through improvement of NO bioavailability within the PVN."( Exercise training improves the defective centrally mediated erectile responses in rats with type I diabetes.
Mayhan, WG; Patel, KP; Zheng, H, 2011
)
0.37
" Therefore, the pathological impairment of eNOS and nNOS functions contribute importantly to cerebrovascular dysfunction in ECM and the recovery of intrinsic functionality of NOS to increase NO bioavailability and restore vascular health represents a target for ECM treatment."( Nitric oxide synthase dysfunction contributes to impaired cerebroarteriolar reactivity in experimental cerebral malaria.
Cabrales, P; Carvalho, LJ; Frangos, JA; Hofer, A; Martins, YC; Melchior, B; Ong, PK; Orjuela-Sánchez, P; Zanini, GM, 2013
)
0.39
"To assess the role of intestinal lymphatic transport in the oral bioavailability and brain deposition of a highly lipophilic, centrally acting drug candidate (Org 49209) in comparison to cholesterol, a close structural analogue."( The influence of intestinal lymphatic transport on the systemic exposure and brain deposition of a novel highly lipophilic compound with structural similarity to cholesterol.
Caliph, SM; Faassen, FW; Porter, CJ, 2014
)
0.4
"The intestinal lymphatic transport of Org 49209 and cholesterol was assessed in lymph-cannulated anaesthetised rats and total bioavailability evaluated in non-lymph-cannulated animals."( The influence of intestinal lymphatic transport on the systemic exposure and brain deposition of a novel highly lipophilic compound with structural similarity to cholesterol.
Caliph, SM; Faassen, FW; Porter, CJ, 2014
)
0.4
"The contribution of intestinal lymphatic transport to total bioavailability was similar for Org 49209 and cholesterol (approximately 40% of the absorbed dose)."( The influence of intestinal lymphatic transport on the systemic exposure and brain deposition of a novel highly lipophilic compound with structural similarity to cholesterol.
Caliph, SM; Faassen, FW; Porter, CJ, 2014
)
0.4
"The oral bioavailability of Org 49209 was significantly lower than that of its structural analogue cholesterol; however, intestinal lymphatic transport played a similar role in oral bioavailability for both compounds."( The influence of intestinal lymphatic transport on the systemic exposure and brain deposition of a novel highly lipophilic compound with structural similarity to cholesterol.
Caliph, SM; Faassen, FW; Porter, CJ, 2014
)
0.4
" The bioavailability and pharmacological properties of the ligands were determined using OSIRIS server."( Bioavailability and Neuroprotectivity of 3-(3, 4-dimethoxy phenyl)-1-4 (methoxy phenyl) prop-2-en-1-one against Schizophrenia: an
Chintha, V; Wudayagiri, R,
)
0.13

Dosage Studied

ExcerptRelevanceReference
" A dose of 300 mg/kg of NMDA significantly shifted the dose-response curve of ketamine for loss of righting reflex to the right."( Ketamine-induced anesthesia involves the N-methyl-D-aspartate receptor-channel complex in mice.
Fukuda, T; Irifune, M; Nomoto, M; Shimizu, T, 1992
)
0.28
" AMOA (150 microM) produced a nearly parallel shift to the right of the dose-response curve for kainate-induced currents."( Stereoselective effects of AMOA on non-NMDA receptors expressed in Xenopus oocytes.
Hansen, JJ; Krogsgaard-Larsen, P; Miledi, R; Nielsen, B; Schousboe, A; Wahl, P, 1992
)
0.28
" delta PWL did not vary with morphine, indicating that the dose-response curves were parallel but shifted to the right for the hyperesthetic paw."( Studies on the spinal interaction of morphine and the NMDA antagonist MK-801 on the hyperesthesia observed in a rat model of sciatic mononeuropathy.
Yaksh, TL; Yamamoto, T, 1992
)
0.28
" In dose-response studies, ifenprodil attenuated the NMDA-induced increase in medium GABA at all ages tested with an Imax of 10 microM."( Developmental differences in antagonism of NMDA toxicity by the polyamine site antagonist ifenprodil.
Nicklas, WJ; Zeevalk, GD, 1992
)
0.28
" Dose-response measurements revealed a rank order of sensitivity to the Glu analogues in the presence of 1 microM glycine and zero extracellular Mg2+; QA greater than AMPA greater than NMDA greater than KA."( Excitatory amino acid receptors on isolated retinal ganglion cells from the goldfish.
Fain, GL; Yazejian, B, 1992
)
0.28
" To test this, the dose-response characteristics for NMDA, glutamate, and kainate in the presence or absence of extracellular Mg2+ and the effects of Mg2+ on metabolic inhibition were examined."( Evidence that the loss of the voltage-dependent Mg2+ block at the N-methyl-D-aspartate receptor underlies receptor activation during inhibition of neuronal metabolism.
Nicklas, WJ; Zeevalk, GD, 1992
)
0.28
" Morphologically, no dose-response effect on the extent of tissue necrosis was found, but a significant difference between groups with severe neurological deficit versus mildly affected groups was observed."( Protective effect of the NMDA antagonist MK-801 on photochemically induced spinal lesions in the rat.
Hao, JX; Seiger, A; Sundström, E; Watson, BD; Wiesenfeld-Hallin, Z; Xu, XJ, 1992
)
0.28
" The brown adipose tissue enzyme T4 5'-deiodinase demonstrated an increased activity in the presence of NMDA, with the lowest dosage eliciting the most significant effect."( N-methyl-D-aspartate does not prevent effects of melatonin on the reproductive and thyroid axes of male Syrian hamsters.
Hoover, PA; Little, JC; Reiter, RJ; Vaughan, MK, 1992
)
0.28
" An enhancing dose of La3+ shifted the dose-response curve for kainate to lower concentrations of agonist without changing the maximum evoked current, and a similar leftward shift of the quisqualate dose-response curve occurred at non-saturating concentrations of quisqualate."( Lanthanum actions on excitatory amino acid-gated currents and voltage-gated calcium currents in rat dorsal horn neurons.
MacDermott, AB; Reichling, DB, 1991
)
0.28
" L-Aspartate (L-Asp) produced a similar dose-response relationship."( Electrogenic uptake contributes a major component of the depolarizing action of L-glutamate in rat hippocampal slices.
Blake, JF; Brown, MW; Collingridge, GL; Frenguelli, BG, 1991
)
0.28
" This is observed as a shift to the right in the NMDA dose-response curves for both the positive and negative postsynaptic components of the evoked tectal response."( Chronic application of NMDA decreases the NMDA sensitivity of the evoked tectal potential in the frog.
Cline, HT; Constantine-Paton, M; Debski, EA; McDonald, JW, 1991
)
0.28
" 200 microM guanosine triphosphate (GTP) produced a decrease of 50% in L-[3H]glutamate binding activity and competition experiments produced an affinity shift to the right of the glutamate dose-response curve."( Characterization of L-[3H]glutamate binding sites in bovine brain coated vesicles.
Cubero, A; González-Calero, G; Martín, M, 1991
)
0.28
" In the presence of 10 microM KA, the dose-response curve of QU became biphasic, whereas with 50 microM KA, a reduction of the response was seen around 1-100 microM QU."( Interactions of glutamate receptor agonists coupled to changes in intracellular Ca2+ in rat cerebellar granule cells in primary culture.
Akerman, KE; Holopainen, I; Louve, M, 1991
)
0.28
" DTT treatment also markedly shifted the dose-response curve of NMDA to the left."( Redox modulation of N-methyl-D-aspartate-stimulated neurotransmitter release from rat brain slices.
Blair, R; Woodward, JJ, 1991
)
0.28
" The dose-response relation for low concentrations of glycine indicated that the measured level of glycine contamination accounted for these responses."( Glycine decreases desensitization of N-methyl-D-aspartate (NMDA) receptors expressed in Xenopus oocytes and is required for NMDA responses.
Bennett, MV; Lerma, J; Zukin, RS, 1990
)
0.28
" Activity-dependent plasticity was also blocked if spontaneous activity was suppressed with dilute tetrodotoxin (TTX; 5-10 nM), a dosage that reduces excitability of neurons but is insufficient to block sodium-dependent action potentials."( Calcium, network activity, and the role of NMDA channels in synaptic plasticity in vitro.
Fields, RD; Nelson, PG; Yu, C, 1991
)
0.28
" A half-maximum dose of 55 microM was calculated from the sigmoid NMDA dose-response curve in the presence of 10 microM Gly."( Proteolytic enzymes do not destroy the N-methyl-D-aspartate (NMDA) sensitivity of acutely isolated hippocampal CA1 and CA3 neurons from postnatal rats.
Gündel, J; Matthies, H; Steinhäuser, C, 1990
)
0.28
" Analyses of dose-response curves of these inward currents indicate that both the QA and KA currents were competitively blocked by 6-cyano-7-nitroquinoxaline-2,3-dione (CNQX), while the NMDA current was blocked non-competitively."( Glutamate receptor agonist-induced inward currents in spinal dorsal horn neurons dissociated from the adult rats.
Arancio, O; MacDermott, AB; Murase, K; Yoshimura, M, 1991
)
0.28
" Animals treated with U-50488H on a similar dosing schedule showed significant neuroprotection at all doses tested, with peak protection observed at 30 mg/kg (51."( The kappa opioid-related anticonvulsants U-50488H and U-54494A attenuate N-methyl-D-aspartate induced brain injury in the neonatal rat.
Althaus, JS; Hudson, CJ; Means, ED; Scherch, HM; Von Voigtlander, PF, 1991
)
0.28
", allowing for better dosage control."( 4-(Tetrazolylalkyl)piperidine-2-carboxylic acids. Potent and selective N-methyl-D-aspartic acid receptor antagonists with a short duration of action.
Arnold, MB; Elzey, T; Leander, JD; Lodge, D; Ornstein, PL; Paschal, JW; Schoepp, DD, 1991
)
0.28
"03-3 mg/kg did not produce changes in the midazolam dose-response curve for either unpunished or punished responding."( NMDA antagonists: lack of antipunishment effect in squirrel monkeys.
Balster, RL; Jortani, SA; Mansbach, RS; Willetts, J, 1991
)
0.28
" However, following intracerebroventricular administration (100-500 micrograms/rat), tiletamine increased pyriform cortical DA metabolism with a bell-shaped dose-response curve."( Contrasting neurochemical interactions of tiletamine, a potent phencyclidine (PCP) receptor ligand, with the N-methyl-D-aspartate-coupled and -uncoupled PCP recognition sites.
Cler, JA; Contreras, PC; Dilworth, VM; Iyengar, S; Mick, SJ; Monahan, JB; Rao, TS; Wood, PL, 1991
)
0.28
" Dose-response curves of motoneurons to L-glutamate, NMDA, and kainate demonstrated that motoneurons are sensitive to these agonists prior to the formation of synapses between afferents and motoneurons."( NMDA receptors mediate poly- and monosynaptic potentials in motoneurons of rat embryos.
Ziskind-Conhaim, L, 1990
)
0.28
" The dose-response relationship of quisqualate acting at the N-methyl-D-aspartate (NMDA) receptor was measured as that portion of the whole-cell current activated by quisqualate that could be blocked by the addition of two NMDA antagonists, 5-fluoroindole-2-carboxylic acid, a competitive antagonist of the NMDA receptor-associated glycine site, and D-2-amino-5-phosphonovalerate, a competitive NMDA binding site antagonist."( Quisqualate activates N-methyl-D-aspartate receptor channels in hippocampal neurons maintained in culture.
Grudt, TJ; Jahr, CE, 1990
)
0.28
" Ethanol shifted the N-methyl-D-aspartate (NMDA) dose-response curves to the right in a non-parallel manner."( Ethanol inhibition of NMDA mediated depolarizations is increased in the presence of Mg2+.
Bian, XP; Martin, D; Morrisett, RA; Swartzwelder, HS; Wilson, WA, 1991
)
0.28
"25 and 200 mumol/kg as revealed by the dose-response curves obtained in both experiments."( NMDA antagonist properties of gamma-L-glutamyl-L-aspartate demonstrated on chemically induced seizures in mice.
De Barry, J; Mathis, C; Ungerer, A, 1990
)
0.28
" Dose-response curves were well fit by the logistic equation, or by a model with 2 independent agonist binding sites."( Structure-activity relationships for amino acid transmitter candidates acting at N-methyl-D-aspartate and quisqualate receptors.
Mayer, ML; Patneau, DK, 1990
)
0.28
" An evaluation of the parenteral dose-response curve for HA-966, revealed no effect on basal activity within the cerebellum."( In vivo antagonism of agonist actions at N-methyl-D-aspartate and N-methyl-D-aspartate-associated glycine receptors in mouse cerebellum: studies of 1-hydroxy-3-aminopyrrolidone-2.
Cler, J; Emmett, MR; Iyengar, S; Mick, S; Oei, E; Rao, TS; Wood, PL, 1990
)
0.28
" As in the in vitro experiments, the dose-response curve for the antagonist was shifted rightward in a parallel fashion when D-serine was coinjected."( Activity of 5,7-dichlorokynurenic acid, a potent antagonist at the N-methyl-D-aspartate receptor-associated glycine binding site.
Baron, BM; Harrison, BL; McDonald, IA; Miller, FP; Palfreyman, MG; Salituro, FG; Schmidt, CJ; Sorensen, SM; White, HS, 1990
)
0.28
" Dose-response comparisons revealed that MK-801 was 3, 6, 19 and 119 times more potent at activating A10 neurons than PCP, (+)-SKF-10,047, ketamine and (+)-pentazocine, respectively."( Non-competitive N-methyl-D-aspartate antagonists are potent activators of ventral tegmental A10 dopamine neurons.
Ceci, A; French, ED, 1990
)
0.28
" Although the dose-response curve is hyperbolic with an ED50 of 78 microM, glutamate apparently activates 2 types of receptors on motoneurons."( Characterization of excitatory amino acid receptors expressed by embryonic chick motoneurons in vitro.
Fischbach, GD; O'Brien, RJ, 1986
)
0.27
" Kindling significantly increased the inhibitory effect of NMDA (10 microM) in slices prepared from animals 24 h after the last class 5 kindled seizure, resulting in a steepening of the dose-response curve for NMDA."( Biochemical evidence for enhanced sensitivity to N-methyl-D-aspartate in the hippocampal formation of kindled rats.
Chow, C; McNamara, JO; Morrisett, RA; Nadler, JV, 1989
)
0.28
" In the present study we examined dose-response effects of excitotoxins acting at the three subtypes of glutamate receptors: N-methyl-D-aspartate (AA1), quisqualate (AA2), and kainic acid (AA3)."( Differential sparing of somatostatin-neuropeptide Y and cholinergic neurons following striatal excitotoxin lesions.
Beal, MF; Ferrante, RJ; Kowall, NW; Martin, JB; Swartz, KJ, 1989
)
0.28
" At a concentration of 10 microM, CNQX reversibly antagonized responses to alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA), quisqualate and kainate; it produced a parallel shift in their log dose-response curves."( 6-Cyano-7-nitroquinoxaline-2,3-dione as an excitatory amino acid antagonist in area CA1 of rat hippocampus.
Blake, JF; Brown, MW; Collingridge, GL; Yates, RG, 1989
)
0.28
" The NMDA receptor antagonists D(-)-2-amino-5-phosphonovalerate (D-AP5), phencyclidine and Mg2+ shifted the NMDA dose-response curve to the right in a parallel manner."( A grease-gap method for studying the excitatory amino acid pharmacology of CA1 hippocampal pyramidal cells.
Bowe, MA; Martin, D; Nadler, JV, 1989
)
0.28
" CGS 19755 was studied using single and cumulative dosing procedures up to a dose of 10."( The competitive N-methyl-D-aspartate (NMDA) antagonist CGS 19755 attenuates the rate-decreasing effects of NMDA in rhesus monkeys without producing ketamine-like discriminative stimulus effects.
France, CP; Ornstein, P; Woods, JH, 1989
)
0.28
" The dosage of NMA was within the range of doses that was previously demonstrated to stimulate LH secretion in monkeys."( N-methyl-d, l-aspartate stimulates growth hormone but not luteinizing hormone secretion in the sheep.
Boling, JA; Estienne, MJ; Green, MA; Hileman, SM; Schillo, KK, 1989
)
0.28
" In this preparation, all these antagonists shifted the NMDA dose-response curve to the right in a parallel manner."( Quantitative studies on some antagonists of N-methyl D-aspartate in slices of rat cerebral cortex.
Harrison, NL; Simmonds, MA, 1985
)
0.27
" Analysis of iontophoretic dose-response curves indicated that DL-APV was a competitive antagonist."( Action of excitatory amino acids and their antagonists on hippocampal neurons.
Hablitz, JJ, 1985
)
0.27
" When applied in combination with fixed concentrations of cis-PDA, NMDA evoked concentration-dependent depolarizations superimposed upon the basal cis-PDA-evoked depolarizations, the dose-response curve for which intercepted the control dose-response curve and was subsequently moved to the right compared with the control curve."( Quantitative studies of N-methyl-D-aspartate, 2-amino-5-phosphonovalerate and cis-2,3-piperidine dicarboxylate interactions on the neonatal rat spinal cord in vitro.
Collins, KJ; Wheatley, PL, 1986
)
0.27
" A dose-response relation for NMDA activation indicated that bath application of 1 and 5 microM NMDA had little or no effect on the response to a paired stimulus pulse (triggered response) and did not induce spontaneous bursting."( The NMDA receptor antagonist 2-amino-5-phosphonovalerate blocks stimulus train-induced epileptogenesis but not epileptiform bursting in the rat hippocampal slice.
Anderson, WW; Swartzwelder, HS; Wilson, WA, 1987
)
0.27
" We found that excitatory amino acid agonists evoked somatostatin release in the following order of potency: quisqualate greater than glutamate = N-methyl-D-aspartate (NMDA) greater than kainate, as calculated from the dose-response curves."( Glutamate stimulates somatostatin release from diencephalic neurons in primary culture.
Astier, H; Tapia-Arancibia, L, 1988
)
0.27
" The dose-response relationship of EAA (N-methyl-D-aspartate (NMDA), kainate, quisqualate and glutamate)-induced activation revealed qualitative and quantitative differences in their pattern of action, suggesting that these agonists act at distinct receptors."( Behavioral classification of excitatory amino acid receptors in mouse spinal cord.
Raigorodsky, G; Urca, G, 1988
)
0.27
" Dose-response analysis reveals that the AA-gated cation conductance activated by kainate requires the binding of two agonist molecules."( Properties of two classes of rat brain acidic amino acid receptors induced by distinct mRNA populations in Xenopus oocytes.
Davidson, N; Fong, TM; Lester, HA, 1988
)
0.27
" Dose-response curves to the two compounds appeared parallel but NMDA was 30-fold more potent than QUIN."( Quinolinate mimics neurotoxic actions of N-methyl-D-aspartate in rat cerebellar slices.
Garthwaite, G; Garthwaite, J, 1987
)
0.27
" Dose-response curves and IC50 values were determined for these antagonists against all four agonists."( The action of quinolinate in the rat spinal cord in vitro.
Curry, K; Magnuson, DS; McLennan, H; Peet, MJ, 1987
)
0.27
" To determine if acidic amino acid pathways were involved in this elevation, a low dosage of a selective NMDA antagonist, 2-amino-7-phosphonoheptanoic acid (APH) was injected intracerebroventricularly 4 min before having rats swim 4 laps."( 2-Amino-7-phosphonoheptanoic acid, a selective N-methyl-D-aspartate antagonist, blocks swim-induced elevation of cerebellar cyclic guanosine monophosphate.
McCaslin, PP; Morgan, WW, 1986
)
0.27
" Dose-response curves revealed that adult animals were more than 10-fold less sensitive to NMDA than their younger counterparts."( Characterization and possible opioid modulation of N-methyl-D-aspartic acid induced increases in serum luteinizing hormone levels in the developing male rat.
Bell, RD; Cicero, TJ; Meyer, ER, 1988
)
0.27
" Two potent, selective and competitive NMDA antagonists, cis-4-(phosphonomethyl)-2-piperidine-carboxylic acid (CGS 19755) and 4-(3-phosphonopropyl)-2-piperazine-carboxylic acid (CPP), were characterized in the gerbil ischemia model with respect to dose-response and time course effects."( The N-methyl-D-aspartate antagonists CGS 19755 and CPP reduce ischemic brain damage in gerbils.
Boast, CA; Etienne, PE; Gerhardt, SC; Lehmann, J; Liebman, JM; Pastor, G, 1988
)
0.27
" The non-parallel shift of the NMDA dose-response curve suggests that ketamine is not acting as a competitive antagonist of NMDA."( Effect of ketamine on amino acid-evoked release of acetylcholine from rat cerebral cortex in vitro.
Johnston, GA; Lodge, D, 1985
)
0.27
" The EC50 obtained from the dose-response curves for GABA in eliciting a maximal response was comparable in neurons maintained in high K+ or in low K+ and treated with a single dose of NMDA, but that it increased significantly in cells maintained in low K+."( NMDA-mediated modulation of gamma-aminobutyric acid type A receptor function in cerebellar granule neurons.
Grayson, DR; Harris, BT; Vicini, S; Zhu, WJ, 1995
)
0.29
" Ethanol dose-response analysis revealed enhanced inhibitory efficacy of ethanol in the presence of subsaturating glycine concentrations at the NR1/NR2A, NR1/NR2C, and NR1/NR2D receptors."( Glycine modulates ethanol inhibition of heteromeric N-methyl-D-aspartate receptors expressed in Xenopus oocytes.
Buller, AL; Larson, HC; Monaghan, DT; Morrisett, RA, 1995
)
0.29
" Pretreatment with glycine, an agonist to the glycine/NMDA receptors, shifted the dose-response effect of felbamate to the right (ED50 = 56."( Excitatory amino acid neurotransmission through both NMDA and non-NMDA receptors is involved in the anticonvulsant activity of felbamate in DBA/2 mice.
Aguglia, U; Bertorelli, R; De Sarro, A; De Sarro, G; Ongini, E, 1994
)
0.29
" In contrast, mixed and pure neuronal cultures exposed to NMDA for 10 min, or to kainate for 24 hr, had similar injury dose-response curves, suggesting that glial glutamate uptake is a less important protective mechanism in these excitotoxic injuries."( Glia modulate the response of murine cortical neurons to excitotoxicity: glia exacerbate AMPA neurotoxicity.
Amagasu, SM; Bruno, VM; Dugan, LL; Giffard, RG, 1995
)
0.29
" The dosage and sampling schedule were chosen by the dose-response and time course of LH response to NMDA, respectively."( [Effect of pinealectomy on N-methyl-D-aspartate-facilitated receptivity in female rats].
Ho, ML; Hsu, C; Hsu, HK; Lue, SI, 1995
)
0.29
" In the present experiments, the selective sigma ligands DTG, (+)pentazocine, BD-737, JO-1784 and L-687,384 were studied to determine if they would also generate bell-shaped dose-response curves."( Biphasic effects of sigma ligands on the neuronal response to N-methyl-D-aspartate.
Bergeron, R; de Montigny, C; Debonnel, G, 1995
)
0.29
" Close correspondence between the dose-response curves of 45Ca2+ uptake and TRE-binding activity by NMDA or KA suggested that Ca2+ influx not only triggered sequential activation of Ca(2+)-signaling processes leading to the increase in TRE-binding activity, but also controlled its increased level."( Involvement of protein kinase C in Ca(2+)-signaling pathways to activation of AP-1 DNA-binding activity evoked via NMDA- and voltage-gated Ca2+ channels.
Iwata, E; Oh, E; Ohtani, K; Sakurai, H; Tsuchiya, T; Tsuda, M, 1995
)
0.29
" Dose-response functions for all four drugs were displaced to the left and average ED50 values were reduced by 3-fold or more under the low-dose compared to the high-dose training condition."( Effects of N-methyl-D-aspartate antagonists in rats discriminating different doses of cocaine: comparison with direct and indirect dopamine agonists.
Edwards, MA; Kantak, KM; Spealman, RD, 1995
)
0.29
" The dose-response for in vitro neuroprotection against both NMDA toxicity and combined oxygen-glucose deprivation (OGD) was determined in murine neocortical cultures."( Correlation of CGS 19755 neuroprotection against in vitro excitotoxicity and focal cerebral ischemia.
Giffard, RG; Maier, CM; Pérez-Pinzón, MA; Steinberg, GK; Sun, GH; Yoon, EJ, 1995
)
0.29
" pretreatment (25 min) with morphine sulfate, 8-OH-DPAT, buspirone and 5-CT shifted the morphine sulfate dose-response curve 3- to 5-fold to the right."( Differential roles of 5-hydroxytryptamine1A and 5-hydroxytryptamine1B receptor subtypes in modulating spinal nociceptive transmission in mice.
Alhaider, AA; Wilcox, GL, 1993
)
0.29
" The dose-response curve of PS action showed significant potentiation above 250 nM and a half-maximal effect at approximately 29 microM."( Pregnenolone sulfate potentiation of N-methyl-D-aspartate receptor channels in hippocampal neurons.
Bowlby, MR, 1993
)
0.29
" Morphine, pethidine and fentanyl, which showed a biphasic dose-response relationship with respect to seizure modulation, abolished the anticonvulsant activity of propofol to exhibit their own intrinsic activity in proconvulsant doses."( Interactions between opioid drugs and propofol in laboratory models of seizures.
Ahmad, I; Pleuvry, BJ, 1995
)
0.29
" Subtypes of glutamate receptors, including NMDA subtype, KA/AMPA subtype and metabotropic glutamate receptors were also expressed and the dose-response relations were studied."( [Amino acid neurotransmitter receptors of carp brain expressed in amphibian oocytes].
Bao, YD; Zhu, H; Zhu, X, 1995
)
0.29
" Dose-response curves showed that DCG-IV was weaker than NMDA but more potent than glutamate in eliciting agonist-gated currents."( Metabotropic glutamate receptor agonist DCG-IV as NMDA receptor agonist in immature rat hippocampal neurons.
Opitz, T; Pidoplichko, VI; Reymann, KG; Shinozaki, H; Wilsch, VW, 1994
)
0.29
" In addition, microinfusion of the same dosage of NMDA into the medial nucleus tractus solitarius (mNTS) produced significant decreases in MAP (-33 +/- 4 mmHg), HR (-33 +/- 6 bpm), renal blood flow, mesenteric blood flow and vascular resistance, and iliac blood flow and resistance."( Cardiovascular effects of NMDA and MK-801 infusion at area postrema and mNTS in rat.
Hartle, DK; Tian, B, 1994
)
0.29
" DX lessened the reduction in adenosine triphosphate (ATP) and increased lactate contents in mice dosed with KCN and also lessened the reduction in ATP in the TCA cycle and oxidative phosphorylation reactions caused by KCN (0."( Dextrorphan attenuates the behavioral consequences of ischemia and the biochemical consequences of anoxia: possible role of N-methyl-d-aspartate receptor antagonism and ATP replenishing action in its cerebroprotecting profile.
Akaike, N; Himori, N; Imai, M; Kurasawa, M; Matsukura, T; Mishima, K; Tanaka, Y; Ueno, K; Watanabe, H, 1993
)
0.29
" Dose-response curves were evaluated by means of an ethological method in which behavioral sequences typical of S and R animals were quantitated."( NMDA-dependent audiogenic seizures are differentially regulated by inferior colliculus subnuclei.
Garcia-Cairasco, N; Terra, VC, 1994
)
0.29
" We now show that an LH dose-response curve for NMDA at age 28 days demonstrates that in NMDA-treated rats the LH response to NMDA is less than in the control group."( A critical period for glutamate receptor-mediated induction of precocious puberty in female rats.
Smyth, C; Wilkinson, M, 1994
)
0.29
" Studying the dose-response curves for glycine in different Ca2+ solutions, we found that the apparent dissociation constant (EC50) for glycine decreases with increasing external Ca2+ concentrations."( Modulation of glycine affinity for NMDA receptors by extracellular Ca2+ in trigeminal neurons.
Gu, Y; Huang, LY, 1994
)
0.29
" Dose-response showed that DL-(tetrazol-5-yl)glycine was about 100 and 500 times more potent than cis-methanoglutamate and NMDA, respectively."( The NMDA receptor agonist DL-(tetrazol-5-yl)glycine is a highly potent excitotoxin.
Lunn, WH; McDonald, JW; Salhoff, CR; Schoepp, DD, 1994
)
0.29
" In keeping with previous data obtained with other sigma receptor ligands, low doses of sertraline and of clorgyline potentiated selectively with a bell-shaped dose-response curve the effect of N-methyl-D-aspartate (NMDA) on pyramidal neurons in the CA3 region of the rat dorsal hippocampus."( Modification of the N-methyl-D-aspartate response by antidepressant sigma receptor ligands.
Bergeron, R; De Montigny, C; Debonnel, G, 1993
)
0.29
"The dose-response curve and time window of efficacy for dextrorphan in permanent focal brain ischemia leading to infarction was studied in the rat."( A dose-response study of dextrorphan in permanent focal ischemia.
Chen, J; Graham, SH; Simon, RP, 1993
)
0.29
" We have taken advantage of this information to study the effects of NMDA on LH release and on changes in levels of LHRH mRNA in single neurons of adult rats treated neonatally with a high dosage of androgen."( N-methyl-D,L-aspartic acid differentially affects LH release and LHRH mRNA levels in estrogen-treated ovariectomized control and androgen-sterilized rats.
Barraclough, CA; Liaw, JJ, 1993
)
0.29
" Depolarization evoked by 50 microM N-methyl-D-aspartate was dose dependently facilitated by serotonin (5-HT) (1 to 100 microM) giving a bell-shaped dose-response curve with maximum enhancement at 30 microM."( Activation of 5-HT2 receptors facilitates depolarization of neocortical neurons by N-methyl-D-aspartate.
Neuman, RS; Rahman, S, 1993
)
0.29
" To examine such a relationship in vivo, we first established a dose-response curve for N-methyl-D-aspartate (NMDA)-induced neuronal death in the rat striatum."( Mitochondrial impairment reduces the threshold for in vivo NMDA-mediated neuronal death in the striatum.
Isacson, O; Simpson, JR, 1993
)
0.29
" Analysis of the dose-response relation for whole cell NMDA-activated currents indicated that propofol caused no significant change in the apparent affinity of the receptor for NMDA."( Inhibition by propofol (2,6 di-isopropylphenol) of the N-methyl-D-aspartate subtype of glutamate receptor in cultured hippocampal neurones.
Bertlik, M; MacDonald, JF; Orser, BA; Wang, LY, 1995
)
0.29
" The NGF-induced changes in NK1 receptor responses occurred in the absence of any detectable changes in either spinal cord NK1 receptor dose-response relationships or NK1 receptor mRNA levels."( Nerve growth factor induces mechanical allodynia associated with novel A fibre-evoked spinal reflex activity and enhanced neurokinin-1 receptor activation in the rat.
Dray, A; Krause, JE; McCarson, KE; Thompson, SWN; Urban, L, 1995
)
0.29
" We, therefore, studied the dose-response characteristics and the time window of efficacy of the AMPA antagonist NBQX in a rat model of permanent focal ischemia."( A dose-response study of neuroprotection using the AMPA antagonist NBQX in rat focal cerebral ischemia.
Chen, J; Graham, SH; Lan, JQ; Simon, RP, 1996
)
0.29
" In a third experiment the dose-response effects of central AMPA on LH secretion were examined more closely."( Photoperiod regulates the LH response to central glutamatergic stimulation in the male Syrian hamster.
Ebling, FJ; Hastings, MH; Hui, Y; Maywood, ES; Mirakhur, A, 1993
)
0.29
" Using the rat cortical wedge preparation, the latter series of experiments showed the expected rightward parallel shifts of the dose-response curves."( Functional partial agonism at ionotropic excitatory amino acid receptors.
Ebert, B; Krogsgaard-Larsen, P; Madsen, U; Søby, KK, 1996
)
0.29
" Dose-response curves of non inactivated and inactivated NMDA responses showed that the apparent receptor affinity for NMDA is not different under the two conditions."( Ca(2+)-dependent inactivation of NMDA receptors: fast kinetics and high Ca2+ sensitivity in rat dorsal horn neurons.
Albuquerque, C; Gu, J; Kyrozis, A; MacDermott, AB, 1996
)
0.29
" In addition, neuronal death induced by brief NMDA exposure in both mixed neuronal-glial and pure neuronal cultures was increased by TGFbeta2 (1-30 ng/ml) with a similar dose-response curve."( Transforming growth factor-beta2 increases NMDA receptor-mediated excitotoxicity in rat cerebral cortical neurons independently of glia.
Brown, GJ; Kane, CJ; Phelan, KD, 1996
)
0.29
"N-Methyl-D-aspartate (NMDA) receptor dose-response relationships that are based on macroscopic currents suggest that NMDA and a different agonist molecule, glycine, must together activate the channel."( Single-channel evidence for glycine and NMDA requirement in NMDA receptor activation.
Currás, MC; Pallotta, BS, 1996
)
0.29
" In the patient with the apparent poor metabolizer (PM) phenotype, a change in the DM preparation to a sustained-release form and increase in the dosing interval was required to lower DM plasma concentrations."( Dextromethorphan in nonketotic hyperglycinaemia: metabolic variation confounds the dose-response relationship.
Arnold, GL; Griebel, ML; Kearns, GL; Koroma, DM; Valentine, JL, 1997
)
0.3
" This potentiation is dose-dependent at doses between 1 and 1000 micrograms/kg, IV but bell-shaped dose-response curves are obtained."( Effects of low and high doses of selective sigma ligands: further evidence suggesting the existence of different subtypes of sigma receptors.
Bergeron, R; Debonnel, G, 1997
)
0.3
" We have shown that sigma ligands, such as di(2-tolyl)guanidin (DTG), potentiate dose-dependently, with bell-shaped dose-response curves, the neuronal response of pyramidal neurones to N-methyl-D-aspartate (NMDA) in the CA3 region of the rat dorsal hippocampus."( Effect of short-term and long-term treatments with sigma ligands on the N-methyl-D-aspartate response in the CA3 region of the rat dorsal hippocampus.
Bergeron, R; de Montigny, C; Debonnel, G, 1997
)
0.3
" CPPG produces rightward parallel shifts of the dose-response curves for both L-AP4- and (1S,3S)-ACPD, with Schild slope in each case close to unity, consistent with a competitive mechanism of antagonism."( Potent antagonists at the L-AP4- and (1S,3S)-ACPD-sensitive presynaptic metabotropic glutamate receptors in the neonatal rat spinal cord.
Jane, DE; Thomas, NK; Tse, HW; Watkins, JC, 1996
)
0.29
"5 mg/kg, respectively, in a bell-shaped dose-response relationship."( Uncompetitive NMDA receptor antagonists attenuate NMDA-induced impairment of passive avoidance learning and LTP.
Danysz, W; Frankiewicz, T; Parsons, CG; Zajaczkowski, W, 1997
)
0.3
" Cumulative dose-response analysis in the tail-flick test revealed an ED50 value for intrathecal (spinal) l-methadone of 15."( d-Methadone is antinociceptive in the rat formalin test.
Elliott, KJ; Inturrisi, CE; Shimoyama, M; Shimoyama, N, 1997
)
0.3
"We investigated the dose-response and time-course of c-fos antisense oligodeoxynucleotide (ASO) treatment against excitatory amino acid (EAA)-induced neurotoxicity in rat hippocampal neurons."( Neuroprotective role of c-fos antisense oligonucleotide: in vitro and in vivo studies.
Dave, JR; Garcia, GE; Lu, XC; Tortella, FC; Ved, HS, 1997
)
0.3
" External H-7 shifted the dose-response curve of GABA-activated currents downward without changing the EC50 significantly (from 15."( Modulation of nicotinic ACh-, GABAA- and 5-HT3-receptor functions by external H-7, a protein kinase inhibitor, in rat sensory neurones.
Hu, HZ; Li, ZW, 1997
)
0.3
" After NMDA treatment, the DPDPE dose-response curve shifted to the right (EC50 value increased approximately 7-fold, from 6 to 40 nM), and the maximal response induced by DPDPE was reduced by approximately 60%."( N-Methyl-D-aspartate attenuates opioid receptor-mediated G protein activation and this process involves protein kinase C.
Fan, GH; Jing, Q; Lou, LG; Ma, L; Pei, G; Wu, YL; Zhang, Z; Zhao, J, 1998
)
0.3
" Lu 28-179 and BD 1008 potentiated dose-dependently the NMDA response and generated bell-shaped dose-response curves."( Modulation of the neuronal response to N-methyl-D-aspartate by selective sigma2 ligands.
Couture, S; Debonnel, G, 1998
)
0.3
" NMDA shifted the dose-response curve of AA to the right."( Further insights into the anti-aggregating activity of NMDA in human platelets.
Alberti, L; De Montis, MG; Franconi, F; Miceli, M; Seghieri, G; Tagliamonte, A, 1998
)
0.3
"Chronic dosing with the glycine partial NMDA agonist, 1-aminocyclopropanecarboxylic acid (ACPC) elicited an altered allosteric regulation of cortical NMDA receptor binding."( Chronic dosing with 1-aminocyclopropanecarboxylic acid, a glycine partial agonist, modulates NMDA inhibition of muscarinic-coupled PI hydrolysis in rat cortical slices.
Boje, KM; Lakhman, SS, 1998
)
0.3
" Morphine dose-response curves were carried out for morphine and fixed doses of ACEA 1021 (12 microg) or AP-5 (10 microg)."( Effects of intrathecal NMDA and non-NMDA antagonists on acute thermal nociception and their interaction with morphine.
Nishiyama, T; Weber, E; Yaksh, TL, 1998
)
0.3
" Dose-response experiment showed that there was a biphasic action of NMDA on GnRH mRNA levels: GnRH mRNA levels were increased by NMDA at lower concentrations (10 and 100 microM), but not at higher concentrations (1 and 10 mM)."( Gonadotropin-releasing hormone (GnRH) gene regulation by N-methyl-D-aspartic acid in GT1-1 neuronal cells: differential involvement of c-fos and c-jun protooncogenes.
Cho, S; Jung, N; Kim, K; Lee, H; Shim, C; Sun, W, 1998
)
0.3
" In a separate series of experiments, dose-response curves were measured for cells in the visual cortex in response to iontophoresis of NMDA or alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA), and the effect of an injection of MK-801 on these curves was measured."( Injection of MK-801 affects ocular dominance shifts more than visual activity.
Beaver, CJ; Czepita, D; Daw, NW; Flavin, HJ; Fox, KD; Gordon, B; Ji, Q; Kirsch, JD; Reid, SN, 1999
)
0.3
" Sulpiride increased the maximum effect afforded by different concentrations of NMDA and shifted the dose-response curve of NMDA to the left (EC50 value from 12."( Neuroleptics with differential affinities at dopamine D2 receptors and sigma receptors affect differently the N-methyl-D-aspartate-induced increase in intracellular calcium concentration: involvement of protein kinase.
Hayashi, T; Kagaya, A; Nishida, A; Shimizu, M; Su, TP; Yamawaki, S, 1999
)
0.3
" A dose-response relationship was established for the K+ channel blockers."( Differential effects of potassium channel blockers on the activity of the locomotor network in neonatal rat.
Cazalets, JR; Magoul, R; Sqalli-Houssaini, Y, 1999
)
0.3
" The ACPC steady-state dose-response curve had both stimulatory and inhibitory phases."( Putative partial agonist 1-aminocyclopropanecarboxylic acid acts concurrently as a glycine-site agonist and a glutamate-site antagonist at N-methyl-D-aspartate receptors.
Benveniste, M; Fossom, LH; Nahum-Levy, R; Skolnick, P, 1999
)
0.3
" NMDA (10 microM-1 mM) dose-response curves produced in the presence of con-G or con-T (1 or 3 microM) resulted in a downward shift of the current response at saturation with NMDA, without affecting the EC50."( Inhibition of NMDA-induced currents by conantokin-G and conantokin-T in cultured embryonic murine hippocampal neurons.
Castellino, FJ; Galdzicki, Z; Klein, RC, 1999
)
0.3
" LY354740 and LY379268 were protective against transient global ischemia in gerbils when dosed intraperitoneally."( Neuroprotective actions of novel and potent ligands of group I and group II metabotropic glutamate receptors.
Battaglia, G; Bond, A; Bruno, V; Clark, BP; Harris, JR; Kingston, AE; Lodge, D; Monn, JA; Nicoletti, F; O'Neill, MJ; Schoepp, DD, 1999
)
0.3
" A dose-response effect was observed."( Behavioural motor effects of MK-801 and DNQX parenteral administration in adult cats: dose-response analysis. Modulatory role of dopaminergic D1 and D2 antagonists on MK-801 induced motor behaviours.
Gonzalez, M; Infante, C; Motles, E, 2000
)
0.31
") was administered prior to a cumulative DZP or PCP dose-response determination."( Modulation of the ethanol-like discriminative stimulus effects of diazepam and phencyclidine by L-type voltage-gated calcium-channel ligands in rats.
Grant, KA; Green-Jordan, K, 2000
)
0.31
" Plasma concentrations of corticosterone and cholinergic fibre loss after Abeta(1-42) or NMDA injection showed a clear U-shaped dose-response relationship."( Chronic corticosterone administration dose-dependently modulates Abeta(1-42)- and NMDA-induced neurodegeneration in rat magnocellular nucleus basalis.
Abrahám, I; Harkany, T; Horvath, KM; Luiten, PG; Nyakas, C; Penke, B; Veenema, AH, 2000
)
0.31
" Using the intraluminal filament method of middle cerebral artery occlusion as an in vivo rat model of transient focal brain ischemia, the neuroprotective dose-response effect of Con-G administration beginning 30 min postocclusion was evaluated after 2 h of ischemia and 22 h of reperfusion."( Neuroprotective efficacy and therapeutic window of the high-affinity N-methyl-D-aspartate antagonist conantokin-G: in vitro (primary cerebellar neurons) and in vivo (rat model of transient focal brain ischemia) studies.
Dave, JR; Lin, Y; McCabe, RT; Phillips, JB; Tortella, FC; Williams, AJ, 2000
)
0.31
" Following the dose-response curve, a dose of 3 nmol of NMDA was selected."( Nitric oxide mediates depressor responses by activation of N-methyl-D-aspartate receptors in the nucleus tractus solitarius of cat.
Chai, CY; Wu, WC; Yang, CY, 2000
)
0.31
" In the presence of tetrodotoxin, NMDA produced a bell-shaped dose-response curve with stimulation of phospho-ERK2 at 10, 25, and 50 microm NMDA and reduced stimulation at 100 microm NMDA."( N-methyl D-aspartate receptor-mediated bidirectional control of extracellular signal-regulated kinase activity in cortical neuronal cultures.
Chandler, LJ; Dorairaj, NR; Norwood, D; Sutton, G, 2001
)
0.31
" The noncompetitive antagonist MK-801 and a glycine-site blocker were equally neuroprotective in both normal and reduced conditions, but there was a significant rightward shift in the dose-response curves of the competitive antagonists APV and CPP and the uncompetitive antagonist memantine."( Reducing conditions significantly attenuate the neuroprotective efficacy of competitive, but not other NMDA receptor antagonists in vitro.
Eshak, M; Iannotti, F; Pringle, AK; Self, J, 2000
)
0.31
" Pretreatment with phencyclidine [PCP] at a dose of 3 mg/kg shifted the DOM dose-response relationship to the left."( Potentiation of DOM-induced stimulus control by non-competitive NMDA antagonists: a link between the glutamatergic and serotonergic hypotheses of schizophrenia.
Doat, M; Rabin, RA; Winter, JC, 2000
)
0.31
" Dose-response analysis showed that IL-2 ( > 50 ng/ml) increased the maximal I(NMDA), without changing the EC(50), indicating that IL-2 potentiates I(NMDA) by increasing the efficacy of the NMDAR."( Interleukin-2 modulates N-methyl-D-aspartate receptors of native mesolimbic neurons.
Tao, L; Ye, JH; Zalcman, SS, 2001
)
0.31
"This article briefly summarizes the occurrence of biphasic dose-response relationships associated with 5-hydroxytryptamine (5-HT) receptor systems, as well as 5-HT agonists and antagonists."( 5-Hydroxytryptamine (serotonin): biphasic dose responses.
Calabrese, EJ, 2001
)
0.31
" Dose-response determinations for dizocilpine [IG and intramuscular (IM)], PCP (IM) and ketamine (IM) were made under two training intervals (30 and 60 min)."( Characterization of the discriminative stimulus effects of N-methyl- D-aspartate ligands under different ethanol training conditions in the cynomolgus monkey ( Macaca fascicularis).
Grant, KA; Jordan, K; Szeliga, KT; Vivian, JA; Waters, CA, 2002
)
0.31
" This is the first report demonstrating non-linear dose-response effects of cycloheximide in low and ultra-low concentration ranges."( Non-linear effects of cycloheximide in glutamate-treated cultured rat cerebellar neurons.
Banaudha, K; Ives, J; Jonas, WB; Maharaj, S; Marini, A; Marotta, D; Morrissette, CR, 2002
)
0.31
" Using a mouse hot-plate test, dose-response relationships were first determined for all compounds individually and then for opioids co-administered with fixed doses of clonidine, ketamine or dextromethorphan."( Interactions of NMDA antagonists and an alpha 2 agonist with mu, delta and kappa opioids in an acute nociception assay.
Baker, AK; Hoffmann, VL; Meert, TF, 2002
)
0.31
" N-Methyl-D-aspartate (NMDA)-evoked currents were greatly and reversibly potentiated by bath application of nefiracetam resulting in a bell-shaped dose-response curve."( Potentiation of N-methyl-D-aspartate-induced currents by the nootropic drug nefiracetam in rat cortical neurons.
Marszalec, W; Moriguchi, S; Narahashi, T; Yeh, JZ; Zhao, X, 2003
)
0.32
" Further, dose-response studies with NMDA revealed that whereas high (10 microM) doses of NMDA themselves elicit cytotoxic responses, low (1-5 microM) concentrations of NMDA can effectively oppose DEX-induced cell death."( Ionotropic and metabotropic glutamate receptor mediation of glucocorticoid-induced apoptosis in hippocampal cells and the neuroprotective role of synaptic N-methyl-D-aspartate receptors.
Almeida, OF; Goula, D; Lu, J; Sousa, N, 2003
)
0.32
" (+)-HA-966 was evaluated as pretreatment on a complete dose-response for cocaine self-administration."( Effects on cocaine and food self-administration of (+)-HA-966, a partial agonist at the glycine/NMDA modulatory site, in rats.
Carnovali, F; Cervo, L; Cocco, A, 2004
)
0.32
"3 microM, respectively; whereas the dose-response curve of D,L-homocysteine revealed an IC50 of 401 microM."( Implications for hyperhomocysteinemia: not homocysteine but its oxidized forms strongly inhibit neuronal network activity.
Fleischer, W; Görtz, P; Hoinkes, A; Otto, F; Schwahn, B; Siebler, M; Wendel, U, 2004
)
0.32
" NMDA currents recorded in Mg2+-free media without addition of glycine were reversibly potentiated by bath and U-tube applications of galantamine at 10 to 10,000 nM, showing a bell-shaped dose-response relationship."( Mechanism of action of galantamine on N-methyl-D-aspartate receptors in rat cortical neurons.
Marszalec, W; Moriguchi, S; Narahashi, T; Yeh, JZ; Zhao, X, 2004
)
0.32
" D-aspartate concentration-dependently shifted the dose-response curve of kainate to the right."( D-aspartate and NMDA, but not L-aspartate, block AMPA receptors in rat hippocampal neurons.
Bai, D; Frandsen, A; Gong, XQ; Lu, WY; Pickering, DS; Wan, Y; Zabek, RL, 2005
)
0.33
" In a randomised double-blinded cross over study design we therefore administered placebo or memantine either as a single dosage or as an ascending dosage over 8 days."( The NMDA antagonist memantine affects training induced motor cortex plasticity--a study using transcranial magnetic stimulation.
Malin, JP; Pleger, B; Schwenkreis, P; Tegenthoff, M; Witscher, K, 2005
)
0.33
" A single dosage of memantine had no significant effect on this training-induced plasticity, whereas memantine administered in an ascending dosage over 8 days was able to block the cortical effect of the motor training."( The NMDA antagonist memantine affects training induced motor cortex plasticity--a study using transcranial magnetic stimulation.
Malin, JP; Pleger, B; Schwenkreis, P; Tegenthoff, M; Witscher, K, 2005
)
0.33
" At present, the best options for medication treatment are tricyclic antidepressants in lower dosage than usual in psychiatric disorders and a wide range of anticonvulsants."( Current trends in neuropathic pain treatments with special reference to fibromyalgia.
Ackenheil, M; Offenbaecher, M, 2005
)
0.33
" In the continuous flow experiments, the dose-response curve of glutamate-induced current was shifted to the right-hand side in co-expression oocytes compared with oocytes expressing NMDAR alone."( Glutamate transporter type 3 attenuates the activation of N-methyl-D-aspartate receptors co-expressed in Xenopus oocytes.
Fang, H; Zuo, Z, 2005
)
0.33
" RT-PCR was used to compare the tTG mRNA level in the cerebellum granular cells treated with NMDA of same dosage with/without thrombin pretreatment."( [Enhancement of NMDA receptor sensitivity by thrombin and its relationship with tissue transglutaminase].
Yu, SZ; Zeng, F; Zeng, QX, 2005
)
0.33
"Following neonatal hippocampal administration on postnatal day 1, the dose-response effects of the human immunodeficiency virus 1 protein glycoprotein 120 (gp120) were studied in vivo on prepulse inhibition (PPI) in adulthood."( Neonatal intrahippocampal glycoprotein 120 injection: the role of dopaminergic alterations in prepulse inhibition in adult rats.
Booze, RM; Fitting, S; Mactutus, CF, 2006
)
0.33
" In immunoblotting analysis, nefiracetam treatment increased the PKCalpha activity with a bell-shaped dose-response relationship peaking at 10 nM, thereby increasing phosphorylation of PKC substrate and NMDA receptor."( Nefiracetam potentiates N-methyl-D-aspartate (NMDA) receptor function via protein kinase C activation and reduces magnesium block of NMDA receptor.
Fukunaga, K; Maejima, H; Marszalec, W; Moriguchi, S; Narahashi, T; Shioda, N; Yeh, JZ; Zhao, X, 2007
)
0.34
" AMPA dose-response curves had similar EC50 but maximal responses increased in neurons isolated from DiA-labeled CIH (20."( Chronic intermittent hypoxia alters NMDA and AMPA-evoked currents in NTS neurons receiving carotid body chemoreceptor inputs.
de Paula, PM; Mifflin, S; Tolstykh, G, 2007
)
0.34
" It has advantages to cuvette techniques because cells have intact dendritic tree and synaptic function and it is a convenient method to obtain reliable dose-response curves for NMDA channel modulators on differentiated neural cells."( Measurements with fluorescent probes in primary neural cultures; improved multiwell techniques.
Ring, A; Tanso, R,
)
0.13
" Surprisingly and in contrast with most drugs that are being developed as therapeutic agents, the dose-response neuroprotective effect of xenon has been poorly studied, although this effect could be of major critical importance for its clinical development as a neuroprotectant."( Neuroprotective effects of xenon: a therapeutic window of opportunity in rats subjected to transient cerebral ischemia.
Abraini, JH; Apiou, G; Chazalviel, L; David, HN; Haelewyn, B; Lecoq, M; Lemaire, M; Risso, JJ; Rouillon, C, 2008
)
0.35
" Arterial rings were mounted in isolated tissue chambers equipped with isometric tension transducers to obtain pharmacologic dose-response curves."( N-methyl-D-aspartate (NMDA) antagonists--S(+)-ketamine, dextrorphan, and dextromethorphan--act as calcium antagonists on bovine cerebral arteries.
Carlsson, C; Chen, D; Harakal, C; Kamel, IR; Wendling, KS; Wendling, WW, 2008
)
0.35
" Following intravitreal injection, intracellular TcapQ activation occurred specifically in RGCs, identified individual apoptotic cells, showed a clear dose-response relationship with NMDA, and colocalized with TUNEL labeling in the retina."( Single-cell imaging of retinal ganglion cell apoptosis with a cell-penetrating, activatable peptide probe in an in vivo glaucoma model.
Barnett, EM; Chang, Q; Maxwell, D; Piwnica-Worms, D; Zhang, X, 2009
)
0.35
" In the rd10/rd10 mouse, a chronic model of inherited retinal degeneration, systemic dosing with BP3 on alternate days between post-natal day 18 and 25 preserved rod photoreceptor numbers and cone photoreceptor morphology."( A novel free radical scavenger rescues retinal cells in vivo.
Cotter, TG; Doonan, F; Messeguer, A; O'Driscoll, C; Sanvicens, N, 2011
)
0.37
" The results indicate that pretreatment with Parawixin 10 prevents the onset of seizures induced with kainic acid, N-methyl-D-aspartate, and pentylenetetrazole in a dose-response manner."( Neurobiological activity of Parawixin 10, a novel anticonvulsant compound isolated from Parawixia bistriata spider venom (Araneidae: Araneae).
Beleboni, RO; Coutinho-Netto, J; Cunha, AO; dos Santos, WF; Fachim, HA; Gobbo-Neto, L; Lopes, NP; Pereira, AC, 2011
)
0.37
" However, after the last ethanol dosing and during a time when ethanol concentrations remained high, I(NMDA) were significantly smaller than control values."( An in vitro model for studying the effects of continuous ethanol exposure on N-methyl-D-aspartate receptor function.
Agrawal, RG; Bergeson, SE; Bhakta, Y; Busari, K; Dertien, JS; Guerra, I; Nath, V; Neumann, MK; Popp, RL; Reneau, JC, 2012
)
0.38
" Thus, the identity (2A versus 2B) of the GluN2 CTD controls the toxicity dose-response to episodes of NMDAR activity."( The subtype of GluN2 C-terminal domain determines the response to excitotoxic insults.
Al-Mubarak, B; Bell, KF; Fowler, JH; Grant, SG; Hardingham, GE; Horsburgh, K; Kind, PC; Komiyama, NH; Martel, MA; McMahon, A; Ryan, TJ; Wyllie, DJ, 2012
)
0.38
" More importantly, subcutaneous co-administrations or even single dose of CBIO completely prevented or reversed morphine tolerance to analgesia (exhibited by a single dose or a dose-response curve of morphine) in both formalin-induced acute phase nociception and tonic phase pain."( Interactions of the potent D-amino acid oxidase inhibitor CBIO with morphine in pain and tolerance to analgesia.
Gong, N; Hashimoto, K; Ma, AN; Wang, HL; Wang, YC; Wang, YX, 2012
)
0.38
" Starting from the first day of the experiment, the rats in the (PONT+LBP) group and the (LBP) group were dosed with LBP; rats in the (PONT+PBS (phosphate buffered saline)) group and the (PBS) group were dosed with PBS via nasogastric tube every day until euthanized."( Effect of lycium barbarum (wolfberry) polysaccharides on preserving retinal function after partial optic nerve transection.
Chan, HH; Chin, MP; Chu, PH; Li, HY; So, KF, 2013
)
0.39
" These data also suggest the existence of an inverted-U dose-response curve in the potential therapeutic effect of this class of compounds."( Relationship between glycine transporter 1 inhibition as measured with positron emission tomography and changes in cognitive performances in nonhuman primates.
Carson, RE; Castner, SA; Gunn, RN; Herdon, H; Huang, Y; Laruelle, M; Murthy, NV; Rabiner, EA; Ridler, K; Roberts, BM; Weinzimmer, DP; Williams, GV; Zheng, MQ, 2014
)
0.4
" Further, administration of erythropoietin (EPO) in a clinically relevant postnatal dosing regimen following the prenatal injury protects the developing brain by reducing calpain activity, restoring oligomeric KCC2 expression and attenuating KCC2 fragmentation, thus providing the first report of a safe therapy to address deficits in KCC2 expression."( Erythropoietin attenuates loss of potassium chloride co-transporters following prenatal brain injury.
Firl, DJ; Getsy, PM; Jantzie, LL; Miller, RH; Robinson, S; Wilson, CG, 2014
)
0.4
" SNP, a nitric oxide donor, produced a bell-shaped dose-response profile on scototaxis."( Interactions between serotonin and glutamate-nitric oxide pathways in zebrafish scototaxis.
Herculano, AM; Lima, MG; Maximino, C; Miranda, V; Puty, B, 2015
)
0.42
" The evaluation of the side effects present shortly after dosing in the rotarod test has revealed neurotoxicity of Nic-BZA with experimentally determined TD50 value of 188."( Protective action of nicotinic acid benzylamide in a variety of chemically-induced seizures in mice.
Paruszewski, R; Świąder, K; Świąder, MJ; Turski, WA; Łuszczki, JJ, 2016
)
0.43
" Ethanol had a narrow dose-response effect on sleep."( Dose-dependent alcohol effects on electroencephalogram: Sedation/anesthesia is qualitatively distinct from sleep.
Abrahao, KP; Lovinger, DM; Pava, MJ, 2020
)
0.56
" Ocular histopathology was also conducted in the eyes collected 4 or 48 hr after dosing from 4 animals at each time period."( Outer retinal involvement in N-methyl-D-aspartate-induced inner retinal injury in rabbits assessed by optical coherence tomography.
Fujita, K; Iguchi, T; Kinoshita, J; Mori, K; Nishiya, T; Suzuki, T; Yasuno, K, 2020
)
0.56
" This specialized assessment may require dosing neonatal rats at postnatal day 7 at the peak of the brain growth spurt and evaluating brain tissue 24 to 48 hours following dosing."( Use of Both Fluoro-Jade B and Hematoxylin and Eosin to Detect Cell Death in the Juvenile Rat Brain Exposed to NMDA-Receptor Antagonists or GABA-Receptor Agonists in Safety Assessment.
Davis, S; Mendes, OR; Picut, CA; Swanson, C; Weil, DS, 2021
)
0.62
"Gene dosage imbalance caused by copy number variations (CNVs) is a prominent contributor to brain disorders."( CYFIP1 Dosages Exhibit Divergent Behavioral Impact via Diametric Regulation of NMDA Receptor Complex Translation in Mouse Models of Psychiatric Disorders.
Canzar, S; Christian, KM; Dawson, TM; Dawson, VL; Eacker, S; Hsu, KS; Kim, NS; Li, W; Lin, YT; Ming, GL; Nguyen, HN; Ringeling, FR; Song, H; Temme, SJ; Worley, P; Xiao, B; Yoon, KJ; Zhou, Y, 2022
)
0.72
" Our integrated analyses provide insight into how gene dosage imbalance caused by CNVs may contribute to divergent neuropsychiatric disorders."( CYFIP1 Dosages Exhibit Divergent Behavioral Impact via Diametric Regulation of NMDA Receptor Complex Translation in Mouse Models of Psychiatric Disorders.
Canzar, S; Christian, KM; Dawson, TM; Dawson, VL; Eacker, S; Hsu, KS; Kim, NS; Li, W; Lin, YT; Ming, GL; Nguyen, HN; Ringeling, FR; Song, H; Temme, SJ; Worley, P; Xiao, B; Yoon, KJ; Zhou, Y, 2022
)
0.72
" The role of NMDA receptor in the regulatory mechanisms of methadone dosage in heroin dependent patients is so far not clear."( Association of the D-amino acid oxidase gene with methadone dose in heroin dependent patients under methadone maintenance treatment.
Chen, ACH; Chung, RH; Fang, CP; Kuo, HW; Liu, SC; Liu, TH; Liu, YL; Tsou, HH; Wang, SC, 2022
)
0.72
" Microinjections of TFB-TBOA into the NAc, but not the ventral tegmental area (VTA), or dorsal striatum (DS), dose-dependently inhibited cocaine self-administration under fixed-ratio and progressive-ratio (PR) reinforcement schedules, shifted the cocaine dose-response curve downward, and inhibited intracranial BSR."( Elevation of Extracellular Glutamate by Blockade of Astrocyte Glutamate Transporters Inhibits Cocaine Reinforcement in Rats via a NMDA-GluN2B Receptor Mechanism.
Bi, GH; Gardner, EL; He, Y; Hempel, BJ; Xi, ZX; Yang, HJ; Zhang, HY, 2022
)
0.72
" Memantine demonstrated a bell-shaped dose-response curve of NP against NMDA."( Memantine has a nicotinic neuroprotective pathway in acute hippocampal slices after an NMDA insult.
Eterovic, VA; Ferchmin, PA; Ferrer-Acosta, Y; Martins, AH; Pérez, D; Rodriguez-Massó, S, 2022
)
0.72
" The results showed that d-cycloserine, a partial glycine agonist, was well tolerated, the 2 dosing strategies did not differ, and improvement was noted on the "lethargy/social withdrawal" and "stereotypic behavior" subscales of the Aberrant Behavior Checklist."( From Mouse to Man: N-Methyl-d-Aspartic Acid Receptor Activation as a Promising Pharmacotherapeutic Strategy for Autism Spectrum Disorders.
Burket, JA; Deutsch, SI, 2023
)
0.91
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (1)

RoleDescription
neurotransmitter agentA substance used for its pharmacological action on any aspect of neurotransmitter systems. Neurotransmitter agents include agonists, antagonists, degradation inhibitors, uptake inhibitors, depleters, precursors, and modulators of receptor function.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (4)

ClassDescription
D-alpha-amino acid
D-aspartic acid derivativeA non-proteinogenic amino acid derivative resulting from the formal reaction of D-aspartic acid at the amino group or either carboxy group, or from the replacement of any hydrogen of D-aspartic acid by a heteroatom.
amino dicarboxylic acid
secondary amino compoundA compound formally derived from ammonia by replacing two hydrogen atoms by organyl groups.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Pathways (3)

PathwayProteinsCompounds
Metabolism of proteins1058144
Protein repair39
MECP2 and associated Rett syndrome011

Protein Targets (29)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, HADH2 proteinHomo sapiens (human)Potency25.11890.025120.237639.8107AID893
Chain B, HADH2 proteinHomo sapiens (human)Potency25.11890.025120.237639.8107AID893
Chain A, JmjC domain-containing histone demethylation protein 3AHomo sapiens (human)Potency22.38720.631035.7641100.0000AID504339
Chain A, 2-oxoglutarate OxygenaseHomo sapiens (human)Potency25.11890.177814.390939.8107AID2147
phosphopantetheinyl transferaseBacillus subtilisPotency78.11710.141337.9142100.0000AID1490
GLS proteinHomo sapiens (human)Potency5.62340.35487.935539.8107AID624146
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency39.81070.011212.4002100.0000AID1030
thyroid stimulating hormone receptorHomo sapiens (human)Potency0.79430.001318.074339.8107AID926
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency11.20480.035520.977089.1251AID504332
cytochrome P450 2C19 precursorHomo sapiens (human)Potency31.62280.00255.840031.6228AID899
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency35.48130.050127.073689.1251AID588590
gemininHomo sapiens (human)Potency2.59290.004611.374133.4983AID624296
muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Potency0.01410.00106.000935.4813AID943
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Glutamate receptor 1Rattus norvegicus (Norway rat)IC50 (µMol)100.00000.00011.617910.0000AID1553721; AID92499
Glutamate receptor 2Rattus norvegicus (Norway rat)IC50 (µMol)100.00000.00011.700010.0000AID1553721; AID92499
Glutamate receptor 3Rattus norvegicus (Norway rat)IC50 (µMol)100.00000.00011.700010.0000AID1553721; AID92499
Glutamate receptor 4Rattus norvegicus (Norway rat)IC50 (µMol)100.00000.00011.700010.0000AID1553721; AID92499
Glutamate receptor ionotropic, kainate 1Rattus norvegicus (Norway rat)IC50 (µMol)100.00000.00700.98217.0000AID93720
Glutamate receptor ionotropic, NMDA 1 Rattus norvegicus (Norway rat)IC50 (µMol)11.14000.00071.600310.0000AID144612; AID144747; AID144762; AID144902
Glutamate receptor ionotropic, NMDA 1 Rattus norvegicus (Norway rat)Ki6.20000.00030.86666.6900AID1553723; AID478464
Glutamate receptor ionotropic, kainate 2Rattus norvegicus (Norway rat)IC50 (µMol)100.00000.00701.01327.0000AID93720
Glutamate receptor ionotropic, kainate 3Rattus norvegicus (Norway rat)IC50 (µMol)100.00000.00701.01327.0000AID93720
Glutamate receptor ionotropic, NMDA 2A Rattus norvegicus (Norway rat)IC50 (µMol)11.14000.00071.630610.0000AID144612; AID144747; AID144762; AID144902
Glutamate receptor ionotropic, NMDA 2A Rattus norvegicus (Norway rat)Ki6.20000.00030.68056.6900AID1553723; AID478464
Glutamate receptor ionotropic, NMDA 2BRattus norvegicus (Norway rat)IC50 (µMol)11.14000.00061.525710.0000AID144612; AID144747; AID144762; AID144902
Glutamate receptor ionotropic, NMDA 2BRattus norvegicus (Norway rat)Ki6.20000.00030.70716.6900AID1553723; AID478464
Glutamate receptor ionotropic, NMDA 2CRattus norvegicus (Norway rat)IC50 (µMol)11.14000.00071.747210.0000AID144612; AID144747; AID144762; AID144902
Glutamate receptor ionotropic, NMDA 2CRattus norvegicus (Norway rat)Ki6.20000.00030.81966.6900AID1553723; AID478464
Glutamate receptor ionotropic, kainate 4Rattus norvegicus (Norway rat)IC50 (µMol)100.00000.00701.01327.0000AID93720
Glutamate receptor ionotropic, NMDA 2DRattus norvegicus (Norway rat)IC50 (µMol)11.14000.00071.741110.0000AID144612; AID144747; AID144762; AID144902
Glutamate receptor ionotropic, NMDA 2DRattus norvegicus (Norway rat)Ki6.20000.00030.70726.6900AID1553723; AID478464
Glutamate receptor ionotropic, kainate 5Rattus norvegicus (Norway rat)IC50 (µMol)100.00000.00701.01327.0000AID93720
Glutamate receptor ionotropic, NMDA 3BRattus norvegicus (Norway rat)IC50 (µMol)11.14000.00071.741110.0000AID144612; AID144747; AID144762; AID144902
Glutamate receptor ionotropic, NMDA 3BRattus norvegicus (Norway rat)Ki6.20000.00030.70726.6900AID1553723; AID478464
Glutamate receptor ionotropic, NMDA 3ARattus norvegicus (Norway rat)IC50 (µMol)11.14000.00071.741110.0000AID144612; AID144747; AID144762; AID144902
Glutamate receptor ionotropic, NMDA 3ARattus norvegicus (Norway rat)Ki6.20000.00030.70726.6900AID1553723; AID478464
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Glutamate receptor ionotropic, NMDA 1 Rattus norvegicus (Norway rat)EC50 (µMol)35.02670.00301.29038.3000AID144321; AID144322; AID339880; AID339882; AID339883; AID339885
Glutamate receptor ionotropic, NMDA 2A Rattus norvegicus (Norway rat)EC50 (µMol)52.28670.00301.02226.8600AID144321; AID144322; AID339880
Glutamate receptor ionotropic, NMDA 2BRattus norvegicus (Norway rat)EC50 (µMol)34.62000.00300.86696.8600AID144321; AID144322; AID339882
Glutamate receptor ionotropic, NMDA 2CRattus norvegicus (Norway rat)EC50 (µMol)34.95330.00301.11276.8600AID144321; AID144322; AID339885
Glutamate receptor ionotropic, NMDA 2DRattus norvegicus (Norway rat)EC50 (µMol)30.05330.00301.39378.3000AID144321; AID144322; AID339883
Glutamate receptor ionotropic, NMDA 3BRattus norvegicus (Norway rat)EC50 (µMol)40.93000.00300.90516.8600AID144321; AID144322
Glutamate receptor ionotropic, NMDA 3ARattus norvegicus (Norway rat)EC50 (µMol)40.93000.00300.90516.8600AID144321; AID144322
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Ceullar Components (2)

Processvia Protein(s)Taxonomy
plasma membraneGlutamate receptor 1Rattus norvegicus (Norway rat)
plasma membraneGlutamate receptor 2Rattus norvegicus (Norway rat)
endoplasmic reticulum membraneGlutamate receptor ionotropic, NMDA 1 Rattus norvegicus (Norway rat)
plasma membraneGlutamate receptor ionotropic, NMDA 1 Rattus norvegicus (Norway rat)
endoplasmic reticulum membraneGlutamate receptor ionotropic, NMDA 2A Rattus norvegicus (Norway rat)
plasma membraneGlutamate receptor ionotropic, NMDA 2A Rattus norvegicus (Norway rat)
endoplasmic reticulum membraneGlutamate receptor ionotropic, NMDA 2BRattus norvegicus (Norway rat)
plasma membraneGlutamate receptor ionotropic, NMDA 2BRattus norvegicus (Norway rat)
endoplasmic reticulum membraneGlutamate receptor ionotropic, NMDA 2CRattus norvegicus (Norway rat)
plasma membraneGlutamate receptor ionotropic, NMDA 2CRattus norvegicus (Norway rat)
endoplasmic reticulum membraneGlutamate receptor ionotropic, NMDA 2DRattus norvegicus (Norway rat)
plasma membraneGlutamate receptor ionotropic, NMDA 2DRattus norvegicus (Norway rat)
endoplasmic reticulum membraneGlutamate receptor ionotropic, NMDA 3BRattus norvegicus (Norway rat)
plasma membraneGlutamate receptor ionotropic, NMDA 3BRattus norvegicus (Norway rat)
endoplasmic reticulum membraneGlutamate receptor ionotropic, NMDA 3ARattus norvegicus (Norway rat)
plasma membraneGlutamate receptor ionotropic, NMDA 3ARattus norvegicus (Norway rat)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (77)

Assay IDTitleYearJournalArticle
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1347049Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot screen2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347050Natriuretic polypeptide receptor (hNpr2) antagonism - Pilot subtype selectivity assay2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347410qHTS for inhibitors of adenylyl cyclases using a fission yeast platform: a pilot screen against the NCATS LOPAC library2019Cellular signalling, 08, Volume: 60A fission yeast platform for heterologous expression of mammalian adenylyl cyclases and high throughput screening.
AID1347151Optimization of GU AMC qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347058CD47-SIRPalpha protein protein interaction - HTRF assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347059CD47-SIRPalpha protein protein interaction - Alpha assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID588378qHTS for Inhibitors of ATXN expression: Validation
AID504836Inducers of the Endoplasmic Reticulum Stress Response (ERSR) in human glioma: Validation2002The Journal of biological chemistry, Apr-19, Volume: 277, Issue:16
Sustained ER Ca2+ depletion suppresses protein synthesis and induces activation-enhanced cell death in mast cells.
AID1347405qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS LOPAC collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347057CD47-SIRPalpha protein protein interaction - LANCE assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347045Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot counterscreen GloSensor control cell line2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID478463Displacement of [3H]KA from KA receptor in Sprague-Dawley rat brain membranes2010Journal of medicinal chemistry, May-27, Volume: 53, Issue:10
4-hydroxy-1,2,5-oxadiazol-3-yl moiety as bioisoster of the carboxy function. Synthesis, ionization constants, and molecular pharmacological characterization at ionotropic glutamate receptors of compounds related to glutamate and its homologues.
AID146063Effective concentration against NR1/NR2A receptor2000Journal of medicinal chemistry, Jul-13, Volume: 43, Issue:14
Ligands for glutamate receptors: design and therapeutic prospects.
AID339884Activity at rat recombinant NR1/NR2B receptor expressed in Xenopus oocytes by two voltage clamp electrophysiology relative to glutamate2008Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
N-Hydroxypyrazolyl glycine derivatives as selective N-methyl-D-aspartic acid receptor ligands.
AID339885Activity at rat recombinant NR1/NR2C receptor expressed in Xenopus oocytes assessed as effect on glutamate-induced current by two voltage clamp electrophysiology2008Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
N-Hydroxypyrazolyl glycine derivatives as selective N-methyl-D-aspartic acid receptor ligands.
AID478464Displacement of [3H]CGP39653 from NMDA receptor in Sprague-Dawley rat brain membranes2010Journal of medicinal chemistry, May-27, Volume: 53, Issue:10
4-hydroxy-1,2,5-oxadiazol-3-yl moiety as bioisoster of the carboxy function. Synthesis, ionization constants, and molecular pharmacological characterization at ionotropic glutamate receptors of compounds related to glutamate and its homologues.
AID337885Displacement of [3H]CGS19755 from excitatory NMDA receptor1993Journal of natural products, Apr, Volume: 56, Issue:4
The role of receptor binding in drug discovery.
AID144321Compound was evaluated for the inhibition of [3H]MK-801 binding at N-methyl-D-aspartate glutamate receptor1992Journal of medicinal chemistry, Nov-27, Volume: 35, Issue:24
DL-tetrazol-5-ylglycine, a highly potent NMDA agonist: its synthesis and NMDA receptor efficacy.
AID977602Inhibition of sodium fluorescein uptake in OATP1B3-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM2013Molecular pharmacology, Jun, Volume: 83, Issue:6
Structure-based identification of OATP1B1/3 inhibitors.
AID339883Activity at rat NR1/NR2D receptor expressed in Xenopus oocytes assessed as effect on glutamate-induced current by two voltage clamp electrophysiology2008Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
N-Hydroxypyrazolyl glycine derivatives as selective N-methyl-D-aspartic acid receptor ligands.
AID146058Effective concentration against NR1/NR2A receptor2000Journal of medicinal chemistry, Jul-13, Volume: 43, Issue:14
Ligands for glutamate receptors: design and therapeutic prospects.
AID339882Activity at rat recombinant NR1/NR2B receptor expressed in Xenopus oocytes assessed as effect on glutamate-induced current by two voltage clamp electrophysiology2008Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
N-Hydroxypyrazolyl glycine derivatives as selective N-methyl-D-aspartic acid receptor ligands.
AID205942Repolarization time for compound was measured by pattern firing by APN and KVN blockade1988Journal of medicinal chemistry, Apr, Volume: 31, Issue:4
Synthesis, resolution, and absolute configuration of the isomers of the neuronal excitant 1-amino-1,3-cyclopentanedicarboxylic acid.
AID144612Compound was evaluated for the inhibition of [3H]-CGS-19,755 binding at N-methyl-D-aspartate glutamate receptor1992Journal of medicinal chemistry, Nov-27, Volume: 35, Issue:24
DL-tetrazol-5-ylglycine, a highly potent NMDA agonist: its synthesis and NMDA receptor efficacy.
AID144762Inhibition of [3H]CPP binding to N-methyl-D-aspartate glutamate receptor of rat cortical or hippocampal membranes1990Journal of medicinal chemistry, Oct, Volume: 33, Issue:10
2,4-Dihydro-3H-1,2,4-triazol-3-ones as anticonvulsant agents.
AID521220Inhibition of neurosphere proliferation of mouse neural precursor cells by MTT assay2007Nature chemical biology, May, Volume: 3, Issue:5
Chemical genetics reveals a complex functional ground state of neural stem cells.
AID1553723Displacement of [3H]CGP39653 from NMDA receptor in rat brain synaptic cortical membranes after 60 mins by scintillation counting method2019Journal of medicinal chemistry, 05-09, Volume: 62, Issue:9
Use of the 4-Hydroxytriazole Moiety as a Bioisosteric Tool in the Development of Ionotropic Glutamate Receptor Ligands.
AID339887Activity at rat NR1/NR2D receptor expressed in Xenopus oocytes by two voltage clamp electrophysiology relative to glutamate2008Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
N-Hydroxypyrazolyl glycine derivatives as selective N-methyl-D-aspartic acid receptor ligands.
AID146059Effective concentration against NR1/NR2A receptor2000Journal of medicinal chemistry, Jul-13, Volume: 43, Issue:14
Ligands for glutamate receptors: design and therapeutic prospects.
AID144324Agonistic activity against N-methyl-D-aspartate glutamate receptor was determined in rat cortical slice preparation at concentration up to 5 mM1990Journal of medicinal chemistry, Jan, Volume: 33, Issue:1
Relationship between structure, conformational flexibility, and biological activity of agonists and antagonists at the N-methyl-D-aspartic acid subtype of excitatory amino acid receptors.
AID144747Compound was tested for inhibition of [3H]CPP binding from N-methyl-D-aspartate glutamate receptor in the rat cortical membranes.1990Journal of medicinal chemistry, Oct, Volume: 33, Issue:10
New and versatile approaches to the synthesis of CPP-related competitive NMDA antagonists. Preliminary structure-activity relationships and pharmacological evaluation.
AID92499Inhibitory activity against Ionotropic glutamate receptor AMPA using [3H]AMPA as radioligand1996Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1
N-methyl-D-aspartic acid receptor agonists: resolution, absolute stereochemistry, and pharmacology of the enantiomers of 2-amino-2-(3-hydroxy-5-methyl-4-isoxazolyl)acetic acid.
AID339886Activity at rat recombinant NR1/NR2C receptor expressed in Xenopus oocytes by two voltage clamp electrophysiology relative to glutamate2008Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
N-Hydroxypyrazolyl glycine derivatives as selective N-methyl-D-aspartic acid receptor ligands.
AID144185Agonistic activity at N-methyl-D-aspartate glutamate receptor was measured as [Ca2+] influx in rat cerebellar granule neurons at 100 uM concentration1998Journal of medicinal chemistry, May-07, Volume: 41, Issue:10
Synthesis and biology of the conformationally restricted ACPD analogue, 2-aminobicyclo[2.1.1]hexane-2,5-dicarboxylic acid-I, a potent mGluR agonist.
AID977599Inhibition of sodium fluorescein uptake in OATP1B1-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM2013Molecular pharmacology, Jun, Volume: 83, Issue:6
Structure-based identification of OATP1B1/3 inhibitors.
AID339880Activity at rat recombinant NR1/NR2A receptor expressed in Xenopus oocytes assessed as effect on glutamate-induced current by two voltage clamp electrophysiology2008Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
N-Hydroxypyrazolyl glycine derivatives as selective N-methyl-D-aspartic acid receptor ligands.
AID144902Inhibitory activity against N-methyl-D-aspartate glutamate receptor using [3H]CPP as radioligand1996Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1
N-methyl-D-aspartic acid receptor agonists: resolution, absolute stereochemistry, and pharmacology of the enantiomers of 2-amino-2-(3-hydroxy-5-methyl-4-isoxazolyl)acetic acid.
AID1553722Displacement of [3H]KA from KA receptor in rat brain synaptic cortical membranes after 60 mins by scintillation counting method2019Journal of medicinal chemistry, 05-09, Volume: 62, Issue:9
Use of the 4-Hydroxytriazole Moiety as a Bioisosteric Tool in the Development of Ionotropic Glutamate Receptor Ligands.
AID252416Effect of compound on cell viability in non-transformed neuronal/glial cells measured as percent reduction of MTT at 570 nm O.D. at 100 uM; Control value 0.56 %2005Bioorganic & medicinal chemistry letters, Jul-01, Volume: 15, Issue:13
Action of a novel pyrrolo[1,2-c][1.3]benzodiazepine on the viability of Jurkat and neuronal/glial cells.
AID144322Compound was evaluated for the inhibition of [3H]norepinephrine binding at N-methyl-D-aspartate glutamate receptor1992Journal of medicinal chemistry, Nov-27, Volume: 35, Issue:24
DL-tetrazol-5-ylglycine, a highly potent NMDA agonist: its synthesis and NMDA receptor efficacy.
AID1553721Displacement of [3H]AMPA from AMPA receptor in rat brain synaptic cortical membranes after 30 mins by scintillation counting method2019Journal of medicinal chemistry, 05-09, Volume: 62, Issue:9
Use of the 4-Hydroxytriazole Moiety as a Bioisosteric Tool in the Development of Ionotropic Glutamate Receptor Ligands.
AID478462Displacement of [3H]AMPA from AMPA receptor in Sprague-Dawley rat brain membranes2010Journal of medicinal chemistry, May-27, Volume: 53, Issue:10
4-hydroxy-1,2,5-oxadiazol-3-yl moiety as bioisoster of the carboxy function. Synthesis, ionization constants, and molecular pharmacological characterization at ionotropic glutamate receptors of compounds related to glutamate and its homologues.
AID339881Activity at rat recombinant NR1/NR2A receptor expressed in Xenopus oocytes by two voltage clamp electrophysiology relative to glutamate2008Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
N-Hydroxypyrazolyl glycine derivatives as selective N-methyl-D-aspartic acid receptor ligands.
AID187655Effect on fractional [3H]GABA release from rat forebrain neurons in culture1990Journal of medicinal chemistry, Jun, Volume: 33, Issue:6
Synthesis and bioactivity of a new class of rigid glutamate analogues. Modulators of the N-methyl-D-aspartate receptor.
AID146061Effective concentration against NR1/NR2A receptor2000Journal of medicinal chemistry, Jul-13, Volume: 43, Issue:14
Ligands for glutamate receptors: design and therapeutic prospects.
AID93720Inhibitory activity against Ionotropic glutamate receptor kainate using [3H]-kainic acid as radioligand1996Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1
N-methyl-D-aspartic acid receptor agonists: resolution, absolute stereochemistry, and pharmacology of the enantiomers of 2-amino-2-(3-hydroxy-5-methyl-4-isoxazolyl)acetic acid.
AID144328Antagonism of N-methyl-D-aspartate glutamate receptor was measured as [Ca2+] influx in rat cerebellar granule neurons at 100 uM concentration1998Journal of medicinal chemistry, May-07, Volume: 41, Issue:10
Synthesis and biology of the conformationally restricted ACPD analogue, 2-aminobicyclo[2.1.1]hexane-2,5-dicarboxylic acid-I, a potent mGluR agonist.
AID196567Electropharmacology on rat cortical slice preparation for EAA-evoked depolarizations; Depolarization evoked by the compound is antagonised by 10 uM of CPP.1999Journal of medicinal chemistry, Oct-07, Volume: 42, Issue:20
Synthesis and enantiopharmacology of new AMPA-kainate receptor agonists.
AID338169Displacement of [3H]CGS19755 from excitatory NMDA receptor assessed as specific binding relative to total binding1993Journal of natural products, Apr, Volume: 56, Issue:4
The role of receptor binding in drug discovery.
AID144333Binding affinity for glutamate-stimulated TCP binding site of N-methyl-D-aspartate glutamate receptor from rat brain by using [3H]-TCP as radioligand; ag = agonist1990Journal of medicinal chemistry, Oct, Volume: 33, Issue:10
New and versatile approaches to the synthesis of CPP-related competitive NMDA antagonists. Preliminary structure-activity relationships and pharmacological evaluation.
AID187656Effect on fractional [3H]GABA release from rat forebrain neurons in culture in the presence of [3H]GABA1990Journal of medicinal chemistry, Jun, Volume: 33, Issue:6
Synthesis and bioactivity of a new class of rigid glutamate analogues. Modulators of the N-methyl-D-aspartate receptor.
AID177860Effective dose against rat cortical slice cells using Electrophysiological experiment.1996Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1
N-methyl-D-aspartic acid receptor agonists: resolution, absolute stereochemistry, and pharmacology of the enantiomers of 2-amino-2-(3-hydroxy-5-methyl-4-isoxazolyl)acetic acid.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID540299A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis2010Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21
Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis.
AID588519A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities2011Antiviral research, Sep, Volume: 91, Issue:3
High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors.
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).2014Journal of biomolecular screening, Jul, Volume: 19, Issue:6
A High-Throughput Assay to Identify Inhibitors of the Apicoplast DNA Polymerase from Plasmodium falciparum.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).
AID1159550Human Phosphogluconate dehydrogenase (6PGD) Inhibitor Screening2015Nature cell biology, Nov, Volume: 17, Issue:11
6-Phosphogluconate dehydrogenase links oxidative PPP, lipogenesis and tumour growth by inhibiting LKB1-AMPK signalling.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (10,127)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990810 (8.00)18.7374
1990's4148 (40.96)18.2507
2000's3015 (29.77)29.6817
2010's1732 (17.10)24.3611
2020's422 (4.17)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 5.77

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be weak demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index5.77 (24.57)
Research Supply Index9.26 (2.92)
Research Growth Index5.02 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (5.77)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials59 (0.57%)5.53%
Reviews401 (3.85%)6.00%
Case Studies35 (0.34%)4.05%
Observational0 (0.00%)0.25%
Other9,913 (95.24%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (25)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Caudal Versus Intravenous Magnesium Sulfate In The Prevention OF Emergence Agitation After Sevoflurane Anesthesia For Lower Abdominal Surgeries In Children. [NCT03846284]93 participants (Actual)Interventional2017-10-08Active, not recruiting
The Infusion of L-Ornithine L-aspart is as Effective as Nonabsorbable Disaccharides in the Management of Acute Hepatic Encephalopathy. [NCT01041755]Phase 430 participants (Actual)Interventional2009-11-30Completed
Comparison of Three Different Schemes:Lactulose, L-ornithine L-aspartate, or Rifaximin, Versus Placebo, as Primary Prophylaxis of the Development of Hepatic Encephalopathy After Acute Variceal Bleeding in Cirrhotic Patients [NCT02158182]Phase 488 participants (Actual)Interventional2014-07-31Completed
Efficacy of L-Ornithine L-Aspartate (LOLA) as an Adjunct to Branched Chain Amino Acids (BCAA) Enriched Solutions on Clinical Outcomes in ICU Patients With Hepatic Encephalopathy: a Randomized Controlled Trial [NCT05539027]Phase 4140 participants (Anticipated)Interventional2022-09-20Recruiting
Supplementation With L-ornithine Increases Representation Density of CD68+ and CD163+ Macrophages in Human Periodontitis Gingiva and Can Modulate Macrophages Phenotypes. Randomized Controlled Pilot Trial [NCT05042024]Phase 375 participants (Actual)Interventional2017-10-20Completed
An Observational Study on the Effect of L-ornithine-L-aspertate (LOLA) on the Flavonifractor Abundance in the Gut Microbiome in Liver Cirrhosis [NCT05737030]Phase 455 participants (Anticipated)Interventional2023-02-06Recruiting
Therapeutic Efficacy of Oral L-Ornithine-L-Aspartate on Liver Cirrhosis and Minimal Encephalopathy: a Single Center Placebo Control Double Blind Study [NCT00896831]Phase 496 participants (Anticipated)Interventional2008-11-30Enrolling by invitation
Randomized, Double Blind, Placebo Controlled Study of Parallel Groups to Evaluate the Effect of Chronic Supplementation of L-arginine in the Muscular Performance. [NCT00785811]Phase 436 participants (Actual)Interventional2008-10-31Terminated(stopped due to Required by the investigator. The site could not recruit patients anymore.)
Efficacy of Combined Oral L-ornithine-L-aspartate and Oral Lactulose in Patients With Hepatic Encephalopathy [NCT00740142]Phase 435 participants (Actual)Interventional2008-09-30Completed
Does a Single Intravenous Dose of Ketamine Reduce the Need for Supplemental Opioids in Post-Cesarean Section Patients? [NCT00486902]188 participants (Actual)Interventional2006-07-31Completed
Efficacy of L-ornithine L-aspartate and Therapeutic Plasma Exchange Versus Plasma Exchange Alone in Lowering Ammonia and Improving Outcomes in Pediatric Acute Liver Failure: A Randomized Controlled Trial [NCT05778461]32 participants (Anticipated)Interventional2023-03-15Not yet recruiting
Therapeutic Efficacy of L-Ornithine L-Aspartate Infusion in Patients With Acute Liver Failure: A Double- Blind, Randomized, Placebo- Controlled Study [NCT00470314]Phase 2150 participants (Actual)Interventional2005-01-31Active, not recruiting
NMDA Antagonists and Steroids for the Prevention of Persisting Post-Surgical Pain After Thoracoscopic Surgeries: A Randomized Controlled, Factorial Design, International, Multicentre Pilot Study [NCT02950233]Phase 327 participants (Actual)Interventional2017-05-04Terminated(stopped due to Recruitment was slower than expected and study drug reached expiry)
Elevated Initial APRI Value Was Associated With the Development of Sepsis-associated Liver Dysfunction in Adult Patients With Sepsis [NCT05999331]160 participants (Anticipated)Observational [Patient Registry]2019-01-01Recruiting
Double Blind Randomised Controlled Trial to Investigate the Efficacy of ANTOX (Vers) 1.2 and MGCT (Magnesiocard) for the Treatment of Hereditary Pancreatitis and Idiopathic Chronic Pancreatitis [NCT00142233]Phase 3295 participants (Actual)Interventional2005-06-06Completed
Repurposing Lithium as a Disease-modifying Therapy in Parkinson's Disease: A Phase I Trial [NCT06099886]Phase 115 participants (Anticipated)Interventional2023-10-12Enrolling by invitation
Functional Magnetic Resonance Imaging and Spectroscopy of the Brain in Patients With Chronic Hepatic Encephalopathy [NCT00305591]50 participants (Anticipated)Interventional2006-03-31Completed
Efficacy of Intravenous 'L-ornithine L-aspartate' in Reversal of Overt Acute Hepatic Encephalopathy in Patients With Liver Cirrhosis: a Prospective, Randomized, Double-blind, Placebo Controlled Trial [NCT01722578]Phase 4200 participants (Actual)Interventional2013-12-31Completed
HELP Trial: Efficacy of L-Ornithine L-Aspartate and Polyethylene Glycol in Cirrhotic Patients With Overt Hepatic Encephalopathy [NCT05920213]Phase 4360 participants (Anticipated)Interventional2023-10-31Not yet recruiting
The Effectiveness of L-ornithine-L-aspartate on Plasma Ammonia in Cirrhotic Patients After TIPS Procedure: a Prospective, Randomized, Controlled, Open-label Clinical Trial [NCT01440829]Phase 2/Phase 340 participants (Actual)Interventional2011-12-31Completed
Efficacy of a Three Days' Infusion of L-Ornithine-L-Aspartate as an Adjuvant Therapy in Cirrhotic Patients With Overt Hepatic Encephalopathy: A Placebo Controlled Study [NCT00433368]Phase 3108 participants Interventional2003-10-31Completed
The Efficacy and Safety of Ornithine Aspartic Acid Granules in Non-Alcoholic Fatty Liver Disease Against Silymarin Capsules: a Randomized, Double-Blind, Multicenter Clinical Trial [NCT05042245]Phase 4240 participants (Anticipated)Interventional2019-04-26Recruiting
Investigating Rapid Anti-Suicidal Ideation Effects of Intravenous (IV) Ketamine in Hospitalized Patients [NCT01507181]Phase 424 participants (Actual)Interventional2012-01-31Completed
[NCT02523703]36 participants (Actual)Interventional2007-09-10Completed
Glutamatergic Modulation of Motivation Enhancement: A Pilot Feasibility Trial [NCT02373124]Phase 1/Phase 24 participants (Actual)Interventional2014-12-31Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT00486902 (8) [back to overview]Cumulative Hydrocodone/Acetaminophen for Supplemental Analgesia to Treat Breakthrough Pain
NCT00486902 (8) [back to overview]Disturbing Dreams
NCT00486902 (8) [back to overview]Number of Subjects Requiring Supplemental Analgesia in the First 24 Hours Following Cesarean Delivery
NCT00486902 (8) [back to overview]Pain Score (0-10) at 2 Weeks Following Cesarean Delivery
NCT00486902 (8) [back to overview]Postoperative Nausea
NCT00486902 (8) [back to overview]Postoperative Vomiting
NCT00486902 (8) [back to overview]Postperative Pruritus
NCT00486902 (8) [back to overview]Verbal Pain Scores (0 to 10) at First Analgesia Request
NCT01507181 (8) [back to overview]Change in Beck Scale for Suicidal Ideation (BSSI)
NCT01507181 (8) [back to overview]Change in Beck Scale for Suicidal Ideation (BSSI)
NCT01507181 (8) [back to overview]Patient Rated Inventory of Side Effects (PRISE)
NCT01507181 (8) [back to overview]Suicidality Item of the MADRS (MADRS-SI)
NCT01507181 (8) [back to overview]Montgomery-Asberg Depression Rating Scale (MADRS)
NCT01507181 (8) [back to overview]The Brief Psychiatric Rating Scale (BPRS)
NCT01507181 (8) [back to overview]The Clinician-Administered Dissociative States Scale (CADSS)
NCT01507181 (8) [back to overview]The Young Mania Rating Scale (YMRS)
NCT02373124 (1) [back to overview]Cocaine Use

Cumulative Hydrocodone/Acetaminophen for Supplemental Analgesia to Treat Breakthrough Pain

Cumulative hydrocodone/acetaminophen for supplemental analgesia to treat breakthrough pain for 72 hours following cesarean delivery (NCT00486902)
Timeframe: 72 hours

Interventiontablets (Median)
Ketamine10
Placebo9

[back to top]

Disturbing Dreams

Number of subject reporting disturbing dreams at 72 hours post cesarean delivery (NCT00486902)
Timeframe: 72 hours

Interventionparticipants (Number)
Ketamine0
Placebo0

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Number of Subjects Requiring Supplemental Analgesia in the First 24 Hours Following Cesarean Delivery

Request for oral hydrocodone/acetaminophen for pain not controlled by around the clock non-steroidal antiflammatory drugs in the first 24 hours following cesarean delivery. (NCT00486902)
Timeframe: 24 hours

Interventionparticipants (Number)
Ketamine64
Placebo66

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Pain Score (0-10) at 2 Weeks Following Cesarean Delivery

Numeric rating for pain score (0 to 10) reported at 2 weeks following cesarean delivery. Zero is no pain and 10 is worst pain imaginable. (NCT00486902)
Timeframe: 2 weeks

InterventionScores on a scale (Median)
Ketamine2
Placebo2.6

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Postoperative Nausea

Number of subjects reporting nausea in first 24 hours following cesarean delivery (NCT00486902)
Timeframe: 24 hours

Interventionparticipants (Number)
Ketamine27
Placebo30

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Postoperative Vomiting

Number of subjects that vomited in the first 24 hours following cesarean delivery (NCT00486902)
Timeframe: 24 hours

Interventionparticipants (Number)
Ketamine13
Placebo13

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Postperative Pruritus

Number of subjects with pruritus in the first 24 hours following cesarean delivery (NCT00486902)
Timeframe: 24 hours

Interventionparticipants (Number)
Ketamine12
Placebo19

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Verbal Pain Scores (0 to 10) at First Analgesia Request

Numeric rating of pain scores (NRS) scale (0 to 10) at time of supplemental analgesia request. Zero is no pain and 10 is worst pain imaginable. (NCT00486902)
Timeframe: 24 hours

InterventionScores on a scale (Median)
Ketamine3
Placebo4

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Change in Beck Scale for Suicidal Ideation (BSSI)

Change in BSI score at 24 hours following treatment as compared to baseline. Beck Scale is a 21-item self or clinician administered instrumentation used to measure the current intensity of patients' specific attitudes, behaviors and plans to commit suicide. Score range 0-42, with higher score indicating higher intensity. (NCT01507181)
Timeframe: baseline and 24 hours post infusion

Interventionunits on a scale (Mean)
Ketamine10.8
Midazolam14.0

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Change in Beck Scale for Suicidal Ideation (BSSI)

Change in BSI score at 48 hours following treatment as compared to baseline. Beck Scale is a 21-item self or clinician administered instrumentation used to measure the current intensity of patients' specific attitudes, behaviors and plans to commit suicide. Score range 0-42, with higher score indicating higher intensity. (NCT01507181)
Timeframe: baseline and 48 hours post infusion

Interventionunits on a scale (Mean)
Ketamine8.8
Midazolam15.3

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Patient Rated Inventory of Side Effects (PRISE)

The PRISE assesses the presence of treatment side effects in nine organ/function systems (gastrointestinal, nervous system, heart, eyes/ears, skin, genital/urinary, sleep, sexual functioning, and other). Data reported in in Adverse Events section. (NCT01507181)
Timeframe: duration of study

Interventionevents (Number)
Ketamine29
Midazolam23

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Suicidality Item of the MADRS (MADRS-SI)

The MADRS-SI ranges from 0 to 6; a score of 2 corresponds to fleeting, passive SI; a score of 4 indicates that SI is frequent with at least moderate intensity but without specific plans or intention; a score of 6 corresponds to active intention and planning for suicide. (NCT01507181)
Timeframe: 24 hours post infusion

Interventionunits on a scale (Mean)
Ketamine1.8
Midazolam3.3

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Montgomery-Asberg Depression Rating Scale (MADRS)

The MADRS is a 10-item instrument used for the evaluation of depressive symptoms in adults and for the assessment of any changes to those symptoms. Higher MADRS score indicates more severe depression, and each item yields a score of 0 to 6. The overall score ranges from 0 to 60. (NCT01507181)
Timeframe: up to 7 days post infusion

,
Interventionunits on a scale (Mean)
24 hours48 hours72 hours7 days
Ketamine19.019.320.921.7
Midazolam26.22824.122.2

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The Brief Psychiatric Rating Scale (BPRS)

The BPRS measures psychomimetic effects with higher scores indicating more severe symptoms (scale range 7 - 49). (NCT01507181)
Timeframe: baseline, 40 minutes post infusion, and 240 minutes post infusion

,
Interventionunits on a scale (Mean)
baseline40 minutes post infusion240 minutes post infusion
Ketamine7.79.98.1
Midazolam7.77.97.0

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The Clinician-Administered Dissociative States Scale (CADSS)

The CADSS measures dissociation with higher scores indicating more severe symptoms (scale range 0 - 92). (NCT01507181)
Timeframe: baseline, 40 minutes post infusion and 240 minutes post infusion

,
Interventionunits on a scale (Mean)
baseline40 minutes post infusion240 minutes post infusion
Ketamine1.117.11.2
Midazolam4.03.31.3

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The Young Mania Rating Scale (YMRS)

An 11-item questionnaire, used to assess manic symptoms based on the patient's subjective report of his or her clinical condition. There are four items that are graded on a 0 to 8 scale (irritability, speech, thought content, and disruptive/aggressive behavior), while the remaining seven items are graded on a 0 to 4 scale. The scores from each question are added together to form a total score ranging from 0 to 60, with higher scores indicating a greater severity of symptoms. (NCT01507181)
Timeframe: baseline, 40 minutes post infusion, 240 minutes post infusion

,
Interventionunits on a scale (Mean)
baseline40 minutes post infusion240 minutes post infusion
Ketamine0.00.00.2
Midazolam0.10.30.2

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Cocaine Use

Participants were provided choices to use up to 5 hits of cocaine on up to 2 occasions (cocaine versus money). Participants who chose cocaine (1 or more hits) during the first choice opportunity are administered a 52 minute infusion of 0.71 mg/kg ketamine the following day. Another choice opportunity occurs 24 hours later. The primary outcome is the choice participants made during these occasions (NCT02373124)
Timeframe: 5 weeks

InterventionParticipants (Count of Participants)
first choice opportunity72037520second choice opportunity72037520
able to abstaincontinue to use
Open-label3
Open-label1
Open-label0

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