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dizocilpine maleate

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Description

Dizocilpine Maleate: A potent noncompetitive antagonist of the NMDA receptor (RECEPTORS, N-METHYL-D-ASPARTATE) used mainly as a research tool. The drug has been considered for the wide variety of neurodegenerative conditions or disorders in which NMDA receptors may play an important role. Its use has been primarily limited to animal and tissue experiments because of its psychotropic effects. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

dizocilpine maleate : A maleate salt obtained by reaction of dizocilpine with one equivalent of maleic acid. [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 CID6420042
CHEMBL ID344151
CHEBI ID176788
SCHEMBL ID122777
MeSH IDM0024898

Synonyms (72)

Synonym
CHEBI:176788
(5s,10r)-5-methyl-10,11-dihydro-5h-5,10-epiminodibenzo[a,d][7]annulene (2z)-but-2-enedioate
dizocilpine maleate (usan)
D03878
EU-0100872
(+)-mk-801 hydrogen maleate, powder
(+)-10,11-dihydro-5-methyl-5h-dibenzo(a,d)cyclohepten-5,10-imine maleate (1:1)
5h-dibenzo(a,d)cyclohepten-5,10-imine, 10,11-dihydro-5-methyl-, (+)-, (z)-2-butenedioate (1:1)
dizocilpine maleate [usan]
einecs 278-614-5
c16h15n.c4h4o4
PRESTWICK_903
dizocilpine maleate
77086-22-7
(+)-mk-801 hydrogen maleate
smr000326942
MLS000860084
(+)-mk 801 maleate
NCGC00094196-01
dizocilipine maleate
M-107
CHEMBL344151
HMS1568E20
HMS3262P05
HMS2095E20
dizocilpine hydrogen maleate
unii-6lr8c1b66q
6lr8c1b66q ,
tox21_113059
tox21_111251
dtxsid2045785 ,
dtxcid0025785
HMS2230A11
BCP9000949
HY-15084
CS-1290
LP00872
dizocilpine maleate [mart.]
dizocilpine maleate [mi]
S2876
CCG-220109
CCG-222176
SCHEMBL122777
tox21_500872
NCGC00261557-01
M3393
(5s,10r)-(+)-5-methyl-10,11-dihydro-5h-dibenzo[a,d]cyclohepten-5,10-imine maleate
HB0004
AKOS024458698
(+/-)-mk-801 hydrogen maleate
mfcd00082465
(+)-mk 801 (maleate)
EX-A566
(+)-mk801
(5s,10r)-5-methyl-10,11-dihydro-5h-5,10-epiminodibenzo[a,d][7]annulene maleate
sr-01000597866
SR-01000597866-1
SR-01000075457-4
SR-01000075457-5
sr-01000075457
SR-01000075457-1
HMS3712E20
(+)mk-801 maleate
BCP21811
HMS3675H14
AS-16649
HMS3411H14
HMS3884B22
Q27265120
BM162595
5h-dibenzo[a,d]cyclohepten-5,10-imine,?10,11-dihydro-5-methyl-, (5s,10r)-, (2z)-2-butenedioate?(1:1)
AC-36528

Research Excerpts

Overview

Dizocilpine maleate (MK-801) is a highly potent, noncompetitive N-methyl-D-aspartate (NMDA) receptor antagonist.

ExcerptReferenceRelevance
"Dizocilpine maleate (MK-801) is a highly potent, noncompetitive N-methyl-D-aspartate (NMDA) receptor antagonist. "( Altered responses to dizocilpine maleate administration in ethanol-withdrawn male and female rats.
Bartoo, G; Devaud, LL; Malthankar, G, 2002
)
2.08

Treatment

Dizocilpine maleate (MK-801), a non-competitive NMDA antagonist, did not affect the immediate peak of glutamate after CHI but significantly diminished the prolonged plateau after hypoxia. Pretreated animals responded rapidly to diazepam treatment, even after 60 min of status epilepticus.

ExcerptReferenceRelevance
"The dizocilpine maleate treatment alone did not induce significant change of GAD67 mRNA levels in the striatum, indicating that NMDA receptors may not have a major role in the transcriptional regulation of GAD67 in the adult rat striatum."( Repeated injections of dizocilpine maleate (MK-801) do not suppress the effects of nigrostriatal dopamine deafferentation on glutamate decarboxylase (GAD67) mRNA expression in the adult rat striatum.
Hajji, MD; Kerkerian-Le Goff, L; Salin, P, 1996
)
1.09
"Dizocilpine maleate-pretreated animals responded rapidly to diazepam treatment, even after 60 min of status epilepticus."( N-methyl-D-aspartate receptor activation regulates refractoriness of status epilepticus to diazepam.
DeLorenzo, RJ; Rice, AC, 1999
)
1.02
"Treatment with dizocilpine maleate an antagonist of the N-methyl-D-aspartate receptor increased the survival of motoneurons to alpha-bungarotoxin-treated soleus muscles."( 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
)
0.63
"Pre-treatment with dizocilpine maleate (MK-801), a non-competitive NMDA antagonist, did not affect the immediate peak of glutamate after CHI but significantly diminished the prolonged plateau after hypoxia."( The effect of MK-801 on extracellular neuroactive amino acids in hippocampus after closed head injury followed by hypoxia in rats.
Chigasaki, H; Katoh, H; Nawashiro, H; Sima, K; Wada, K, 1997
)
0.62
"Pretreatment with dizocilpine maleate (0.1 mM), a non-competitive antagonist of N-methyl-D-aspartate receptors, of the paraventricular nucleus by microdialysis probe attenuated the N-methyl-D-aspartate (1.5 mM)-induced elevations of both thromboxane B2 and plasma catecholamines."( Perfusion of the hypothalamic paraventricular nucleus with N-methyl-D-aspartate produces thromboxane A2 and centrally activates adrenomedullary outflow in rats.
Murakami, Y; Nishihara, M; Okada, S; Osumi, Y; Yokotani, K, 2000
)
0.63

Toxicity

ExcerptReferenceRelevance
" Our data provide evidence that NO, synthesized upon glutamate exposure, has not a primary toxic action in pure hippocampal neuronal cultures."( Blockade of nitric oxide formation does not prevent glutamate-induced neurotoxicity in neuronal cultures from rat hippocampus.
Leysen, JE; Pauwels, PJ, 1992
)
0.28
") were also resistant to the toxic effects of quisqualic acid, indicating the possible involvement of NMDA receptors in quisqualic acid toxicity."( Quisqualic acid-induced neurotoxicity is protected by NMDA and non-NMDA receptor antagonists.
Pai, KS; Ravindranath, V, 1992
)
0.28
"A putative role for endogenous excitatory amino acid systems in the mediation of the cardiovascular and toxic responses to acute administration of cocaine, was examined in spontaneously hypertensive and normal Wistar-Kyoto rats."( Antagonism of the toxicity of cocaine by MK-801: differential effects in spontaneously hypertensive and Wistar-Kyoto rats.
Acuff, CG; Ho, IK; Hoskins, B; Rockhold, RW; Surrett, RS; Zhang, T, 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
" Thus, depolarization appears to enhance the sensitivity of neurons to toxic NMDA receptor activation by glutamate."( Enhancement of NMDA receptor-mediated neurotoxicity in the hippocampal slice by depolarization and ischemia.
Coyle, JT; Vornov, JJ, 1991
)
0.28
" Reducing the glutamate level of macrophage SN, either by exposure to astrocytes or by enzymatic degradation abolished the toxic effect."( Murine brain macrophages induced NMDA receptor mediated neurotoxicity in vitro by secreting glutamate.
Cuénod, M; Do, KQ; Fontana, A; Frei, K; Piani, D, 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
" PCP and MK-801 block neurotoxicity induced by glutamate doses 50 times higher than the LD50 (LD50 in Mg2+-free medium, 10 microM) but only partially block the kainate neurotoxicity (LD50 in presence of Mg2+, 100 microM)."( Gangliosides prevent glutamate and kainate neurotoxicity in primary neuronal cultures of neonatal rat cerebellum and cortex.
Alho, H; Bertolino, M; Costa, E; Favaron, M; Ferret, B; Guidotti, A; Manev, H, 1988
)
0.27
" These data indicate that the polyamine spermine is toxic to neurons in vitro and that toxicity is prevented by the NMDA-associated channel antagonist dizocilpine."( Polyamine neurotoxicity is antagonized by dizocilpine in cultured chick cortical neurons.
Fahey, JM; Miller, LG; Pritchard, GA, 1993
)
0.29
" None of the protective drugs inhibited the initial 5-HT loss following MDMA, rendering unlikely any proposal that they are protective because they inhibit 5-HT release and the subsequent formation ofa toxic indole derivative."( A study of the mechanism of MDMA ('ecstasy')-induced neurotoxicity of 5-HT neurones using chlormethiazole, dizocilpine and other protective compounds.
Colado, MI; Green, AR, 1994
)
0.29
"Subcutaneous administration of the N-methyl-D-aspartic acid (NMDA) antagonist, MK-801, to adult rats causes a toxic vacuole reaction in neurons of the posterior cingulate cortex which is readily detected in histological sections 4 h following MK-801 administration."( Halothane prevents MK-801 neurotoxicity in the rat cingulate cortex.
Fukamauchi, F; Ishimaru, M; Olney, JW, 1995
)
0.29
" Therefore, administering alpha 2 adrenergic agonists together with NMDA antagonists may be a valuable strategy for preventing adverse side effects of NMDA antagonists and making these agents safer for various neurotherapeutic purposes."( alpha 2 adrenergic agonists prevent MK-801 neurotoxicity.
Duhan, NL; Farber, NB; Foster, J; Olney, JW, 1995
)
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
"A brief exposure of dissociated hippocampal culture to aluminum (AlCl3, 60 min) is toxic to neurons."( Aluminum toxicity in rat hippocampal neurons.
Brenner, SR; Yoon, KW, 1994
)
0.29
"Glutamate (Glu), the major excitatory neurotransmitter in the nervous system, is toxic to neurons when it accumulates at high concentrations in the extracellular space."( Rapid desensitization determines the pharmacology of glutamate neurotoxicity.
Moudy, AM; Rothman, SM; Yamada, KA, 1994
)
0.29
"Phencyclidine (PCP), dizocilpine maleate (MK801), and other NMDA antagonists are toxic to neurons in the posterior cingulate and retrosplenial cortex."( Cerebellar toxicity of phencyclidine.
Koistinaho, J; Näkki, R; Sagar, SM; Sharp, FR, 1995
)
0.61
" Accordingly, intracellular hydrogen ion concentrations were measured in cultured hippocampal neurons with the fluorescent dye BCECF during and after toxic exposures."( Changes in intracellular pH associated with glutamate excitotoxicity.
Dubinsky, JM; Hartley, Z, 1993
)
0.29
" Large (19-fold) increases in cortical cysteine sulphinate concentration were noted after injection of a toxic dose of cysteine."( Cysteine sulphinate and cysteate: mediators of cysteine toxicity in the neonatal rat brain?
Hagberg, H; Lehmann, A; Orwar, O; Sandberg, M, 1993
)
0.29
" Methotrexate alone was not toxic to astrocytes, neurons, or the neurite networking."( MK-801 and memantine protect cultured neurons from glutamate toxicity induced by glutamate carboxypeptidase-mediated cleavage of methotrexate.
Finiels-Marlier, F; Marini, AM; Martin, B; Paul, SM; Weller, M, 1993
)
0.29
" The pathogenesis of this syndrome implicates immunopathological and toxic events such as the production of cytokines."( Tetrodotoxin blocks HIV coat protein (gp120) toxicity in primary neuronal cultures.
Couratier, P; Diop, AG; Esclaire, F; Hugon, J; Lesort, M; Sindou, P, 1994
)
0.29
" Toxic exposure of neurons to glutamate results in an extended neuronal depolarization that precedes delayed neuronal death."( Excitotoxicity affects membrane potential and calmodulin kinase II activity in cultured rat cortical neurons.
Churn, SB; DeLorenzo, RJ; Sombati, S; Taft, WC, 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
" However, elevated concentrations of NO, interacting with oxygen radicals, become toxic and mediate glutamate-induced neurotoxicity in the cultured retinal neurons."( Dual actions of nitric oxide in N-methyl-D-aspartate receptor-mediated neurotoxicity in cultured retinal neurons.
Akaike, A; Honda, Y; Kaneda, K; Kashii, S; Kikuchi, M; Mandai, M; Tamura, Y, 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
" Cysteine was also toxic but higher concentrations were required."( Neurotoxicity of cysteine: interaction with glutamate.
Eriksson, P; Lehmann, A; Nilsson, M; Puka-Sundvall, M; Sandberg, M, 1995
)
0.29
"Copper and manganese, two essential metals involved in physiological and physiopathological processes in the brain, were measured in corpora striata of rats 7 days after intrastriatal injection of quinolinic acid (QUIN, 240 nmol/l microliters), an N-methyl-D-aspartate (NMDA) receptor agonist with toxic activity."( Quinolinic acid neurotoxicity: in vivo increased copper and manganese content in rat corpus striatum after quinolinate intrastriatal injection.
Flores, A; Galván-Arzate, S; Osorio-Rico, L; Pérez, P; Ríos, C; Santamaría, A; Solís, F, 1996
)
0.29
" 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
" Putrescine was moderately toxic but only at 500 microM concentration."( Neurotoxicity of polyamines and pharmacological neuroprotection in cultures of rat cerebellar granule cells.
Ciani, E; Contestabile, A; Dall'Olio, R; Gandolfi, O; Sparapani, M, 1997
)
0.3
" Pretreatment with rotenone significantly augmented the toxic effect of L-DOPA on DA neurons."( Metabolic inhibition enhances selective toxicity of L-DOPA toward mesencephalic dopamine neurons in vitro.
Itakura, T; Nakai, K; Nakao, N, 1997
)
0.3
"Recent clinical trials with non-competitive and competitive N-methyl-D-aspartate (NMDA) receptor antagonists in patients with stroke have shown that these patients develop more adverse effects, particularly psychomimetic effects such as hallucinations and agitation, than normal volunteers at equivalent doses."( Focal ischemia enhances the adverse effect potential of N-methyl-D-aspartate receptor antagonists in rats.
Löscher, W; Szabo, L; Wlaź, P, 1998
)
0.3
"In this study, the anticonvulsant and adverse effects of compounds that belong to four different categories of systemically available N-methyl-D-aspartate (NMDA) receptor ligands were compared, namely the competitive antagonist CGP 40116, the noncompetitive antagonist MK-801 (dizocilpine), the glycineB receptor antagonist L-701,324, and the glycineB receptor high-efficacy partial agonist D-cycloserine."( Anti-convulsant and adverse effects of the glycineB receptor ligands, D-cycloserine and L-701,324: comparison with competitive and non-competitive N-methyl-D-aspartate receptor antagonists.
Wlaź, P, 1998
)
0.3
"Glutamate can be toxic to neurons although it is a neurotransmitter."( Neurons depend on astrocytes in a coculture system for protection from glutamate toxicity.
Brown, DR, 1999
)
0.3
"Lidocaine is toxic in a dose dependent fashion to RGC in vitro."( Lidocaine toxicity to rat retinal ganglion cells.
Dreyer, EB; Freeman, EE; Grosskreutz, CL; Katowitz, WR, 1999
)
0.3
"Lidocaine is toxic to RGC both in vitro and in vivo."( Lidocaine toxicity to rat retinal ganglion cells.
Dreyer, EB; Freeman, EE; Grosskreutz, CL; Katowitz, WR, 1999
)
0.3
" Our findings suggest that the toxic effects of MPP+ on dopaminergic terminals are not mediated through a direct interaction with the NMDA subtype of glutamate receptor, but with the AMPA-kainate subtype."( The non-NMDA glutamate receptor antagonists 6-cyano-7-nitroquinoxaline-2,3-dione and 2,3-dihydroxy-6-nitro-7-sulfamoylbenzo(f)quinoxaline, but not NMDA antagonists, block the intrastriatal neurotoxic effect of MPP+.
Cano, J; Machado, A; Merino, M; Vizuete, ML, 1999
)
0.3
" Normally, PrP106-126 is not toxic to cultures containing neurones deficient in the cellular isoform of prion protein (PrPc)."( Prion protein peptide neurotoxicity can be mediated by astrocytes.
Brown, DR, 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
"Altered glial function in the substantia nigra in Parkinson's disease may lead to the release of toxic substances that cause dopaminergic cell death or increase neuronal vulnerability to neurotoxins."( Altered glial function causes neuronal death and increases neuronal susceptibility to 1-methyl-4-phenylpyridinium- and 6-hydroxydopamine-induced toxicity in astrocytic/ventral mesencephalic co-cultures.
Jenner, P; McNaught, KS, 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
" The present study was conducted to characterise the toxic effect of L-CPA in primary cell cultures of rat cerebellar granule cells in vitro."( Neurotoxic effect of L-2-chloropropionic acid on primary cultures of rat cerebellar granule cells.
Fonnum, F; Lock, EA; Rustad, A; Sturgess, NC, 2000
)
0.31
" In consequence of these acute processes delayed cell death in the MBN and persistent loss of cholinergic fibre projections to the neocortex appear as early as 3 days following the Abeta-induced toxic insult."( beta-amyloid neurotoxicity is mediated by a glutamate-triggered excitotoxic cascade in rat nucleus basalis.
Abrahám, I; Harkany, T; Kónya, C; Korf, J; Laskay, G; Luiten, PG; Nyakas, C; Penke, B; Sasvári, M; Sebens, JB; Soós, K; Timmerman, W; Tóth, B; Zarándi, M, 2000
)
0.31
"L-2-Chloropropionic acid is selectively toxic to the cerebellum in rats; the granule cell necrosis observed within 48 h can be prevented by prior administration of MK-801."( Neuroprotective effects of MK-801 on L-2-chloropropionic acid-induced neurotoxicity.
Bachelard, HS; Lock, EA; Williams, RE, 2001
)
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
"The developing cortical neurons have been well documented to be extremely vulnerable to the toxic effect of methylmercury (MeHg)."( Involvement of enhanced sensitivity of N-methyl-D-aspartate receptors in vulnerability of developing cortical neurons to methylmercury neurotoxicity.
Arimura, K; Eto, K; Fukuyama, N; Miyamoto, K; Moriguchi, S; Murao, K; Nakanishi, H; Osame, M; Wakamiya, J, 2001
)
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
" This side effect can be avoided by using the macrosphere MCAO technique with a limited number of spheres."( Neuroprotective effects of MK-801 in different rat stroke models for permanent middle cerebral artery occlusion: adverse effects of hypothalamic damage and strategies for its avoidance.
Bachmann, G; Fisher, M; Gerriets, T; Kaps, M; Stolz, E; Walberer, M, 2003
)
0.32
"Non-competitive N-methyl-D-aspartate (NMDA) receptor antagonists produce toxic effects in the limbic cortex of rodent brain."( Altered trkB neurotrophin receptor activation does not influence the N-methyl-D-aspartate receptor antagonist-mediated neurotoxicity in mouse posterior cingulate cortex.
Castrén, E; Koponen, E; Saarelainen, T; Väisänen, J, 2003
)
0.32
" These findings suggest that gp120 is toxic to neurons even in the absence of the virus and that the toxic mechanism involves primarily activation of CXCR4 receptor."( The chemokine receptor CXCR4 and not the N-methyl-D-aspartate receptor mediates gp120 neurotoxicity in cerebellar granule cells.
Bachis, A; Mocchetti, I, 2004
)
0.32
"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
" Coadministration of the donor with Tempol (1 mM), a one-electron oxidant that converts NO- to NO, prevented its toxic effect, as did the concomitant addition of Fe(III)TPPS."( Neurotoxicity of nitroxyl: insights into HNO and NO biochemical imbalance.
Espey, MG; Hewett, SJ; Uliasz, TF; Wink, DA, 2005
)
0.33
" Further, this EtOH exposure and withdrawal regimen sensitizes the hippocampus to the toxic effects of Abeta treatment in a manner reflecting over activity of NMDA receptor function."( Ethanol exposure and withdrawal sensitizes the rat hippocampal CA1 pyramidal cell region to beta-amyloid (25-35)-induced cytotoxicity: NMDA receptor involvement.
Mulholland, PJ; Prendergast, MA; Self, RL; Smith, KJ, 2005
)
0.33
" The test compound used was the metabotropic glutamate receptor antagonist, L(+)-2-amino-3-phosphonopropionic acid (L-AP3), which is known to be toxic in vivo after subchronic, but not acute, administration."( Long-term, repeated dose in vitro neurotoxicity of the glutamate receptor antagonist L-AP3, demonstrated in rat hippocampal slice cultures by using continuous propidium iodide incubation.
Blaabjerg, M; Kristensen, BW; Noraberg, J; Zimmer, J, 2007
)
0.34
" Thus, developing safe NMDAR antagonists is of high therapeutic interest."( Comparison of the pharmacological properties of GK11 and MK801, two NMDA receptor antagonists: towards an explanation for the lack of intrinsic neurotoxicity of GK11.
Becerril Ortega, J; Buisson, A; Crouzin, N; Desmadryl, G; Hirbec, H; Privat, A; Teigell, M; Vandame, D, 2007
)
0.34
"05-1mM, 24h) was highly toxic for mature CGNs while young CGNs were insensitive to the toxic effect of Glu."( Paraquat potentiates glutamate toxicity in immature cultures of cerebellar granule neurons.
Isaev, NK; Stelmashook, EV; Zorov, DB, 2007
)
0.34
" This study investigates the effects of the PCB mixture Aroclor 1254 (A1254) and two PCB congeners (coplanar, non-ortho PCB 126, and non coplanar PCB 99) on the expression of N-methyl-D-aspartate receptors (NMDARs) and the subsequent toxic effects using a human SHS5-SY neuroblastoma cell line."( Role of N-methyl-D-aspartate receptors in polychlorinated biphenyl mediated neurotoxicity.
Chan, HM; Ndountse, LT, 2009
)
0.35
" However, the neural mechanism by which extracellular 5-HT is elevated to a toxic level for the syndrome remains to be determined."( Assessment of 5-hydroxytryptamine efflux in rat brain during a mild, moderate and severe serotonin-toxicity syndrome.
Huang, X; Krishnamoorthy, S; Ma, Z; Tao, R; Vukovich, NP; Zhang, G, 2009
)
0.35
"A growing body of experimental evidence suggests that an intracerebral hematoma is toxic to neighboring cells."( Accelerated hemolysis and neurotoxicity in neuron-glia-blood clot co-cultures.
Chen, L; Chen-Roetling, J; Jaremko, KM; Regan, RF, 2010
)
0.36
" Either the blockade of ionotropic glutamate NMDA-receptors with MK-801 or APV or supplementation the medium with ruthenium red (mitochondrial Ca(2+) uniporter blocker) almost entirely protected CGNs from the toxic effect of ZnCl(2) during glucose deprivation (GD)."( Glucose starvation stimulates Zn2+ toxicity in cultures of cerebellar granule neurons.
Isaev, NK; Lozier, ER; Novikova, SV; Silachev, DN; Stelmashook, EV; Zorov, DB, 2012
)
0.38
"Collectively, our data show that HgCl₂-induced toxic effects on central neurons are triggered by an over-activation of NMDA receptors, leading to cytoskeleton instability."( Mercury-induced toxicity of rat cortical neurons is mediated through N-Methyl-D-Aspartate receptors.
Chen, L; Farkas, S; Kortbeek, S; Syed, NI; Xu, F; Zamponi, GW; Zhang, FX, 2012
)
0.38
" Our results suggest that GluN2B antagonists may represent valuable alternatives to unspecific NMDAR antagonists with robust antidepressant efficacy and a more favorable side-effect profile."( Pharmacological blockade of GluN2B-containing NMDA receptors induces antidepressant-like effects lacking psychotomimetic action and neurotoxicity in the perinatal and adult rodent brain.
Dormann, C; Gass, P; Inta, D; Köhr, G; Lima-Ojeda, JM; Pfeiffer, N; Sprengel, R; Vogt, MA, 2013
)
0.39
" Presently only Memantine is considered a safe NMDAR antagonist and is used clinically."( Development of NMDAR antagonists with reduced neurotoxic side effects: a study on GK11.
Hirbec, H; Nesic, O; Perez-Polo, R; Prieto-Cappellini, M; Privat, A; Teigell, M; Ulmann, L; Vandame, D; Vignon, J, 2013
)
0.39
" Mice treated with PGW5 (25 and 50mg/kg/d) for 28 days did not show toxic effects in terms of weight gain and blood-chemistry analysis."( A novel analog of olanzapine linked to sarcosinyl moiety (PGW5) demonstrates high efficacy and good safety profile in mouse models of schizophrenia.
Bidder, M; Gil-Ad, I; Kramer, M; Portnoy, M; Taler, M; Tarasenko, I; Weizman, A, 2014
)
0.4
"PGW5 is a novel and safe antipsychotic, efficacious against schizophrenia-like positive and negative symptoms at nonsedative doses."( A novel analog of olanzapine linked to sarcosinyl moiety (PGW5) demonstrates high efficacy and good safety profile in mouse models of schizophrenia.
Bidder, M; Gil-Ad, I; Kramer, M; Portnoy, M; Taler, M; Tarasenko, I; Weizman, A, 2014
)
0.4
" The aims of the present study were to examine the acute toxic effects of methadone, an opioid receptor agonist and NMDA receptor antagonist, as well as to evaluate the protective properties of recombinant human GH (rhGH) on methadone-induced toxicity."( Growth hormone is protective against acute methadone-induced toxicity by modulating the NMDA receptor complex.
Diwakarla, S; Grönbladh, A; Hallberg, M; Nyberg, F; Nylander, E; Zelleroth, S, 2016
)
0.43
"Despite the adverse effects of N-methyl-D-aspartate receptor (NMDAR) activity in cardiomyocytes, no study has yet examined the effects of NMDAR activity under ex vivo ischemic-reperfusion (I/R) conditions."( N-Methyl-D-Aspartate Receptor-Driven Calcium Influx Potentiates the Adverse Effects of Myocardial Ischemia-Reperfusion Injury Ex Vivo.
Hu, S; Liu, ZY; Ma, HM; Tian, CN; Yu, JJ; Zhong, QW, 2017
)
0.46
"NMDAR-driven calcium influx potentiates the adverse effects of myocardial I/R injury ex vivo."( N-Methyl-D-Aspartate Receptor-Driven Calcium Influx Potentiates the Adverse Effects of Myocardial Ischemia-Reperfusion Injury Ex Vivo.
Hu, S; Liu, ZY; Ma, HM; Tian, CN; Yu, JJ; Zhong, QW, 2017
)
0.46
"Although attention-deficit/hyperactivity disorder (ADHD) is widely studied, problems regarding the adverse effect risks and non-responder problems still need to be addressed."( Synergistic efficacy and diminished adverse effect profile of composite treatment of several ADHD medications.
Adil, KJ; Cheong, JH; Han, SH; Jeon, SJ; Kim, HJ; Kim, HY; Kim, R; Kwon, KJ; Mabunga, DFN; Park, D; Ryu, O; Shin, CY; Valencia, S, 2021
)
0.62
" Schizophrenia (SZ) is one of the neuropsychiatric disorders in human beings with rapid mortality and intense morbidity which can be treated with antipsychotics, but these commercial drugs exert adverse effects and have less efficacy to treat the full spectrum of SZ."( Reversal of oxidative stress, cytokine toxicity and DNA fragmentation by quercetin in dizocilpine-induced animal model of Schizophrenia.
Afzal, A; Batool, Z; Haider, S; Shahzad, S, 2022
)
0.72

Pharmacokinetics

ExcerptReferenceRelevance
" The finding that motor impairing but not anticonvulsant effects of MK-801 were potentiated by D-cycloserine suggests that different pharmacodynamic actions of NMDA receptor antagonists are differentially modulated by the glycine receptor, which could be related to the regional heterogeneity of the NMDA receptor complex in the brain."( Effect of the glycine/NMDA receptor partial agonist, D-cycloserine, on seizure threshold and some pharmacodynamic effects of MK-801 in mice.
Baran, H; Löscher, W; Wlaź, P, 1994
)
0.29
" However, the central nervous system (CNS) pharmacokinetic profile of agmatine remains minimally defined."( Pharmacodynamic and pharmacokinetic studies of agmatine after spinal administration in the mouse.
Fairbanks, CA; Grocholski, BM; Kitto, KF; Roberts, JC, 2005
)
0.33
" Importantly, our findings posit that 40 Hz ASSR is a pharmacodynamic biomarker for cortical NMDA function that is also robustly translatable."( 40 Hz Auditory Steady-State Response Is a Pharmacodynamic Biomarker for Cortical NMDA Receptors.
Ahlijanian, MK; Benitex, Y; Chen, P; Fernandes, A; Li, YW; Senapati, A; Sivarao, DV; Whiterock, V; Yang, Y, 2016
)
0.43

Compound-Compound Interactions

ExcerptReferenceRelevance
" In some experiments hypoxia was combined with glucose withdrawal."( Effect of MK-801 on dopamine release evoked by hypoxia combined with hypoglycemia.
Milusheva, E, 1992
)
0.28
" This research is designed to investigate the neuroprotective effects of long-term treatment with EGb761 (a standard form of the extract of Ginkgo biloba leaf) in combination with MgSO(4), FK506, or MK-801 on the infarct volume of male gerbils' brain induced by unilateral middle cerebral artery occlusion (MCAO)."( Ginkgo biloba leaf extract (EGb761) combined with neuroprotective agents reduces the infarct volumes of gerbil ischemic brain.
Cheng, FC; Chung, SY; Lee, MS; Lin, JY; Lin, MC; Wang, MF, 2006
)
0.33
" This study evaluated lamotrigine alone or in combination with phenobarbital, phenytoin, or the glutamate antagonist (+)-5-methyl-10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5,10-imine hydrogen maleate (MK-801) for a proapoptotic action in the developing rat brain."( Effects of lamotrigine alone and in combination with MK-801, phenobarbital, or phenytoin on cell death in the neonatal rat brain.
Gale, K; Katz, I; Kim, J; Kondratyev, A, 2007
)
0.34
"We examined whether MK-801 in combination with CA receptor ligands, which inhibit CAergic neuronal activities, could induce anesthesia including LORR."( Selective blockade of N-methyl-D-aspartate channels in combination with dopamine receptor antagonism induces loss of the righting reflex in mice, but not immobility.
Irifune, M; Kanematsu, T; Kikuchi, N; Morioka, N; Morita, K; Nakata, Y; Sakai, N; Shimizu, Y; Yoshida, K, 2015
)
0.42
" In contrast, MK-801 in combination with a small dose of the dopamine (DA) receptor antagonist haloperidol (0."( Selective blockade of N-methyl-D-aspartate channels in combination with dopamine receptor antagonism induces loss of the righting reflex in mice, but not immobility.
Irifune, M; Kanematsu, T; Kikuchi, N; Morioka, N; Morita, K; Nakata, Y; Sakai, N; Shimizu, Y; Yoshida, K, 2015
)
0.42
"The aim of study was to investigate the effects of pyrroloquinoline quinone (PQQ) combined with d-serine on the modulation of glycine sites in the brain of rats using social recognition test."( Modulation of glycine sites enhances social memory in rats using PQQ combined with d-serine.
Liu, D; Mao, S; Peng, Y; Qin, X; Zhang, R; Zhou, X, 2016
)
0.43
"Clinical studies that focused on treating schizophrenia showed that Calculus Bovis Sativus (CBS), a substitute of Calculus Bovis, when used in combination with haloperidol could significantly lower the dosage of haloperidol compared with treatment with haloperidol alone, whereas efficacy was maintained."( Investigation of the synergistic effects of haloperidol combined with Calculus Bovis Sativus in treating MK-801-induced schizophrenia in rats.
He, GF; He, GZ; Lei, K; Li, J; Li, XP; Liu, D; Liu, YN; Ren, XH; Zhang, CL, 2018
)
0.48

Bioavailability

ExcerptReferenceRelevance
" The differing neurotoxicity of MK-801 between rat strains and between lines within a strain may reflect genetic variation and/or differences in hepatic biotransformation and thus the bioavailability of the drug between strains and lines within a strain."( Strain and colony differences in the neurotoxic sequelae of MK-801 visualized with the amino-cupric-silver method.
Bueno, A; de Olmos, J; de Olmos, S; Desmond, NL; Manzini, F, 2003
)
0.32
" AVN-101 shows a good oral bioavailability and facilitated brain-blood barrier permeability, low toxicity, and reasonable efficacy in animal models of CNS diseases."( AVN-101: A Multi-Target Drug Candidate for the Treatment of CNS Disorders.
Ivachtchenko, AV; Lavrovsky, Y; Okun, I, 2016
)
0.43
" We also assessed the pharmacokinetics of MK-801 in rat blood plasma and its bioavailability in brain tissue."( Effects of the N-methyl-d-aspartate receptor antagonist, MK-801, on spatial memory and influence of the route of administration.
Dambrova, M; Grinberga, S; Pugovics, O; Sevostjanovs, E; Stelfa, G; Svalbe, B; Vavers, E; Zvejniece, B; Zvejniece, L, 2019
)
0.51
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51

Dosage Studied

ExcerptRelevanceReference
" 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
" There was a dose-response effect seen in muscimol-treated rabbits."( Protective effect of synaptic inhibition during cerebral ischemia in rats and rabbits.
Hedges, B; Lyden, PD, 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 purpose of the present study was to examine the dose-response relationship and the maximum time for which effective therapy could be delayed for the N-methyl-D-aspartate antagonist dizocilpine (MK-801) as a neuroprotective agent in a permanent focal ischaemia model in the rat."( The dose-response relationship and therapeutic window for dizocilpine (MK-801) in a rat focal ischaemia model.
Brazell, C; Gill, R; Hatfield, RH, 1992
)
0.28
" When ischemic animals were administered the multiple dosing regimen of (+)SKF 10,047, no hypothermic effect was noted in the temporalis muscle over 4 hours' postischemia."( Neuroprotective effects of SKF 10,047 in cultured rat cerebellar neurons and in gerbil global brain ischemia.
Feuerstein, G; Gagnon, RC; Gu, JL; Lysko, PG; Yue, TL, 1992
)
0.28
" The dose-response curves for induction of behavior was very different from that for increasing the concentration of i beta-E in plasma."( Phencyclidine increased release of beta-endorphin from anterior lobe of the pituitary.
Contreras, PC; Farah, JM; Jacobson, AE; Rice, KC, 1991
)
0.28
" In these experiments GR89696 was dosed 5 min, 4, 8, 12, 16, 20 and 24 h after occlusion on the first day and then three times daily for the next three days."( Neuroprotective actions of GR89696, a highly potent and selective kappa-opioid receptor agonist.
Birch, PJ; Hayes, AG; Hayward, NJ; Judd, DB; Naylor, A; Rogers, H; Scopes, DI; Tyers, MB, 1991
)
0.28
" Furthermore, pretreatment with the drug did not affect the dose-response curve for the inhibitory effects of the DA receptor agonist apomorphine or the mixed DA agonist/sigma-receptor ligand (+)-3-(3-hydroxyphenyl)-N-1-propyl)piperidine ((+)-3-PPP)."( Sigma-receptors: implication for the control of neuronal activity of nigral dopamine-containing neurons.
Engberg, G; Wikström, H, 1991
)
0.28
" Stimulation of binding induced by DCS in the presence of fixed concentrations of glycine resulted in a family of dose-response curves, consistent with the antibiotic having the property of a partial agonist at this glycine site."( D-cycloserine, a putative cognitive enhancer, facilitates activation of the N-methyl-D-aspartate receptor-ionophore complex in Alzheimer brain.
Bowen, DM; Chessell, IP; Francis, PT; Procter, AW, 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
" Determination of the pentobarbital dose-response curve under the fixed-ratio component resulted in a steep curve characterized by responding on the saline lever at low doses and on the drug lever at higher doses."( Effects of schedule of reinforcement on a pentobarbital discrimination in rats.
McMillan, DE; Snodgrass, SH, 1991
)
0.28
" Apomorphine-induced cage climbing behavior was partially decreased by lower dosages of GDEE, but was almost completely blocked by the highest dosage tested."( A possible role of AA2 excitatory amino acid receptors in the expression of stimulant drug effects.
Cannon-Spoor, HE; Freed, WJ, 1990
)
0.28
" Neither drug effected seizures in control rats, however, both GDEE and MK-801 produced a leftward shift in the strychnine-seizure dose-response curve in 3AP inferior olive-lesioned rats."( The effects of inferior olive lesion on strychnine seizure.
Anderson, MC; Chung, EY; Van Woert, MH, 1990
)
0.28
" Dizocilpine was active in this model at a dosage of 1 mg/kg."( Neuroprotective effect of memantine demonstrated in vivo and in vitro.
Krieglstein, J; Mennel, HD; Peruche, B; Rossberg, C; Seif el Nasr, M, 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
" 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
" Experimental conditions provided several different doses of drug during each of two daily 130 min sessions; as a result, a dose-response curve relating rate of responding to dose/injection for self-administered drug was obtained within each session."( Drug-reinforced responding: rapid determination of dose-response functions.
Palmer, RK; Winger, G; Woods, JH, 1989
)
0.28
" The low dosage reduced total AD accrued during each kindling stage but failed to alter kindling rate."( The NMDA-receptor antagonist, MK-801, suppresses limbic kindling and kindled seizures.
Gilbert, ME, 1988
)
0.27
" Consistently, 8 days after sciatic nerve ligation but not after a sham operation, an approximately 6-fold rightward shift occurred in the morphine antinociceptive dose-response curve."( Experimental mononeuropathy reduces the antinociceptive effects of morphine: implications for common intracellular mechanisms involved in morphine tolerance and neuropathic pain.
Mao, J; Mayer, DJ; Price, DD, 1995
)
0.29
" administration of 5 mg/kg morphine, a mu-opioid agonist, or U50488H (U50), a kappa 1-opioid agonist, for 5 days in male CD-1 mice results in a 2-3-fold shift to the right of the respective analgesic (tail flick) dose-response curves, indicating the development of tolerance."( The NMDA receptor antagonists, LY274614 and MK-801, and the nitric oxide synthase inhibitor, NG-nitro-L-arginine, attenuate analgesic tolerance to the mu-opioid morphine but not to kappa opioids.
Elliott, K; Inturrisi, CE; Kolesnikov, YA; Minami, N; Pasternak, GW, 1994
)
0.29
"5, 1, and 2 mg/kg for TCP, the second dosage corresponding to the minimal required for antiseizure activity."( Effects of TCP on spatial memory: comparison with MK-801.
Blanchet, G; Filliat, P,
)
0.13
" This indicates that the protective effects of MK-801 on MA-induced dopaminergic terminal degeneration varies among animals with complete protection in most animals and partial protection in the others using the present doses and dosing regimen."( Protective effects of MK-801 on methamphetamine-induced depletion of dopaminergic and serotonergic terminals and striatal astrocytic response: an immunohistochemical study.
Pu, C; Vorhees, CV, 1995
)
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
" Latency to acquisition of the lever discrimination for rats that had received prior exposure to amphetamine was shorter than for the saline-pretreated counterparts in each cocaine dosage group."( Development and expression of sensitization to cocaine's reinforcing properties: role of NMDA receptors.
Bankson, MG; Gibbs, S; Higley, D; Horger, BA; House, DT; McNamara, C; Schenk, S; Valadez, A, 1993
)
0.29
" After recovery from catheter implantations (5-7 days), intrathecal dose-response curves were established for the antihyperesthesia effects of clonidine (3, 6, 10, and 20 micrograms) and MK-801 (1, 3, 10, and 20 micrograms) alone to obtain the ED50 for each agent."( Analysis of drug interaction between intrathecal clonidine and MK-801 in peripheral neuropathic pain rat model.
Lee, YW; Yaksh, TL, 1995
)
0.29
" With the fixed-dose analysis, the log dose-response curves showed a left shift that considerably exceeds the theoretical curve made by a simple sum of the effects of clonidine alone and with MK-801 (1 microgram)."( Analysis of drug interaction between intrathecal clonidine and MK-801 in peripheral neuropathic pain rat model.
Lee, YW; Yaksh, TL, 1995
)
0.29
" Agonist dose-response curves were constructed, followed by bath applications of increasing concentrations of the antagonist D-AP5."( NMDA receptor responses in adult hippocampal CA1 region after neonatal treatment with MK-801: comparison with NMDA receptor responses in the immature rat.
Brady, RJ; Gorter, JA, 1994
)
0.29
" The increasing dosage of glutamate induced more calls and had a significant influence on frequency and intensity of emitted ultrasound."( High-frequency ultrasonic vocalization induced by intracerebral glutamate in rats.
Brudzynski, SM; Fu, XW, 1994
)
0.29
" The dose-response curve was bell-shaped which is typical for cognition enhancers."( PRE-084, a sigma selective PCP derivative, attenuates MK-801-induced impairment of learning in mice.
Maurice, T; Nabeshima, T; Parish, DW; Privat, A; Su, TP, 1994
)
0.29
" NMDA increased [Ca2+]i transients and MK-801 [(+)-5-methyl-10,11-dihydro-5H-dibenzo(a,d')cyclohepten-5,10-imine hydrogen] reduced them, in a dose-response manner."( Characterization of spontaneous and N-methyl-D-aspartate-induced calcium rise in rat cultured hypothalamic neurons.
Dayanithi, G; Rage, F; Richard, P; Tapia-Arancibia, L, 1995
)
0.29
" Here, adult female rats were dosed with PCP (10 mg/kg, IP), or (+)-MK-801 (0."( Phencyclidine and (+)-MK-801-induced circling preference: correlation with monoamine levels in striatum of the rat brain.
Ali, SF; Bracha, HS; Newport, GD,
)
0.13
" The dose-response effects of glutamate and serine were studied on the population spikes evoked in the granular cell layer."( Serine released from hippocampal slices during deprivation of oxygen and glucose enhances the effects of glutamate on neuronal function.
Hirai, H; Okada, Y, 1993
)
0.29
" In contrast, L-687,414 did not increase limbic CMRglc, nor evoke vacuolation when given in the neuroprotective dose-regime or at the higher dosage rate."( Lack of effect of L-687,414 ((+)-cis-4-methyl-HA-966), an NMDA receptor antagonist acting at the glycine site, on cerebral glucose metabolism and cortical neuronal morphology.
Hargreaves, RJ; Hill, RG; Rigby, M; Smith, D, 1993
)
0.29
" At the dosage used NBQX exerts an adverse effect."( Effects of MK-801 and NBQX on acute recovery of piglet cerebral metabolism after hypothermic circulatory arrest.
Aoki, M; Fackler, JC; Hickey, PR; Holtzman, D; Jonas, RA; Nomura, F; Stromski, ME; Tsuji, MK, 1994
)
0.29
" Once each of the two groups attained discrimination criterion, dose-response relationships with lower doses of ethanol indicated that the Fawn-Hooded rats were less sensitive (ED50 value = 579."( The NMDA receptor antagonist MK-801 produces ethanol-like discrimination in the rat.
Gordon, TL; McBurney, DM; Meehan, SM; Schechter, MD,
)
0.13
" In contrast, benactyzine and trihexyphenidyl showed a third profile of activity: There was a smaller increase in drug dosage required for anticonvulsant activity as seizure duration increased, and both drugs could terminate seizures that had progressed for 40 min."( Pharmacological modulation of soman-induced seizures.
McDonough, JH; Shih, TM, 1993
)
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
" There was no abnormal locomotor activity in the L-CPA rats treated with MK-801 except for the first 4 hr following dosing when animals were severely sedated."( L-2-chloropropionic acid-induced neurotoxicity is prevented by MK-801: possible role of NMDA receptors in the neuropathology.
Gyte, A; Lock, EA; Simpson, MG; Widdowson, PS; Wyatt, I, 1996
)
0.29
" Therefore, a dose-response curve of posttraining injection (intraperitoneal) of fluoxetine was carried out in an associative learning task (auto-shaping)."( Effect of fluoxetine on learning and memory involves multiple 5-HT systems.
Hong, E; Meneses, A, 1995
)
0.29
" The objective of this study was to conduct a dose-response analysis of the effects of (+)MK-801 on stereotyped behavior, ataxia, locomotor activity, and righting reflex latency in guinea pig."( A dose-response analysis of the behavioral effects of (+)MK-801 in guinea pig: comparison with CPP.
Darlington, CL; Jerram, AH; Smith, PF, 1996
)
0.29
" Once rats had acquired the discrimination, the criterion for stimulus control was set as at least 90% ethanol- or vehicle appropriate responding during ten consecutive sessions, an ethanol dose-response test (0."( Acamprosate and alcohol: III. Effects on alcohol discrimination in the rat.
Hundt, W; Spanagel, R; Zieglgänsberger, W, 1996
)
0.29
" Dose-response sensorimotor and activity tests suggested that this dose of MK-801 did not induce significant nonassociative effects."( Acute behavioral effects of MK-801 in the mouse.
Brosnan-Watters, G; Nardi, A; Olney, JW; Wozniak, DF, 1996
)
0.29
" To test this possibility, we performed a dose-response study of MK-801 on the high-affinity DA transport system in rat striatal synaptosomes."( MK-801 partially protects against the acute MPP+ depleting effect on dopamine levels in rat striatal slices.
Cano, J; Machado, A; Santiago, M; Venero, JL, 1996
)
0.29
" injections of morphine or fentanyl, produced antinociceptive tolerance as shown by a significant rightward displacement of the agonist dose-response curves compared to controls."( Competitive and non-competitive NMDA antagonists block the development of antinociceptive tolerance to morphine, but not to selective mu or delta opioid agonists in mice.
Bilsky, EJ; Hruby, VJ; Inturrisi, CE; Porreca, F; Sadée, W, 1996
)
0.29
" MK-801 increased CGRP in a dose-response manner in frontal cortex, and NKA-LI in occipital cortex."( Effects of electroconvulsive stimuli and MK-801 on neuropeptide Y, neurokinin A, and calcitonin gene-related peptide in rat brain.
Gruber, S; Jiménez, PA; Mathé, AA; Stenfors, C; Theodorsson, E, 1997
)
0.3
" boluses of ST to generate dose-response curves."( Spinal infusion of N-methyl-D-aspartate antagonist MK801 induces hypersensitivity to the spinal alpha-2 agonist ST91 in the rat.
Dunbar, SA; Yaksh, TL, 1997
)
0.3
" Neuronal degeneration was observed in the substantia nigra pars compacta (SN), ventral tegmental area (VTA) and retrorubral field (RRF) of only animals dosed in the low temperature environment."( Systemic administration of MPTP induces thalamic neuronal degeneration in mice.
Ali, SF; Freyaldenhoven, TE; Schmued, LC, 1997
)
0.3
"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
" Thus 1-log shift to the right of individual dose-response curves occurred with MK-801."( NMDA receptors mediate peripheral chemoreceptor afferent input in the conscious rat.
Gozal, D; Gozal, YM; Graff, GR; Ohtake, PJ; Torres, JE, 1998
)
0.3
"MK801 induces Fos-like immunoreactivity (FLI) in the paraventricular nucleus (PVN) in a sex, age, hormone and dosage dependent manner."( Sexually dimorphic MK801-induced c-fos in the rat hypothalamic paraventricular nucleus.
Nance, DM; Wilkinson, M; Wintrip, N, 1998
)
0.3
" MPTP-treated mice maintained at 4 degrees C demonstrated (1) a greater hypothermic response, (2) a significant reduction in striatal DA content and tyrosine hydroxylase (TH) activity, and (3) significantly greater striatal 1-methyl-4-phenylpyridinium (MPP+) levels, as compared to mice dosed with MPTP at room temperature."( Lowering ambient or core body temperature elevates striatal MPP+ levels and enhances toxicity to dopamine neurons in MPTP-treated mice.
Albers, DS; Moy, LY; Sonsalla, PK, 1998
)
0.3
" These studies examined the efficacy and potency with which L-glutamate produces receptor activation, channel opening and subsequent MK-801 binding as a function of increasing age by comparing dose-response curves (EC50 and Emax) from 6-, 12-, and 24-month-old F-344 rats."( Age-related changes in [3H]MK-801 binding in the Fischer 344 rat brain.
Anderson, KJ; Mitchell, JJ,
)
0.13
"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
" LTP was effectively abolished in a separate group of rats treated with an MK-801 dosing regimen (0."( L-687,414, a low efficacy NMDA receptor glycine site partial agonist in vitro, does not prevent hippocampal LTP in vivo at plasma levels known to be neuroprotective.
Hill, RG; Kemp, JA; Marshall, GR; Priestley, T, 1998
)
0.3
" Our results support the hypothesis that SS and LS mice differ in initial sensitivity to NMDAR antagonists and suggest that the line differences in the dose-response relationships for MK-801- and CPP-induced locomotor activity are qualitatively similar to those reported for ethanol."( Differences in NMDA receptor antagonist-induced locomotor activity and [3H]MK-801 binding sites in short-sleep and long-sleep mice.
Simpson, VJ; Velardo, MJ; Zahniser, NR, 1998
)
0.3
") was administered 30 min prior to a neurotoxic MeAmp dosage for this species (2 x 2 mg/kg, 4 h apart); control subjects received MeAmp."( Dizocilpine and reduced body temperature do not prevent methamphetamine-induced neurotoxicity in the vervet monkey: [11C]WIN 35,428 - positron emission tomography studies.
Harvey, DC; Huang, SC; Lacan, G; Melega, WP; Phelps, ME, 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
" Mice were dosed with 1 mg/kg MK-801 and tested on acquisition of a new "baited" hole at 5 or 12 h posttreatment."( Parallel recovery of MK-801-induced spatial learning impairment and neuronal injury in male mice.
Brosnan-Watters, G; Nardi, A; Olney, JW; Wozniak, DF, 1999
)
0.3
" After animals were trained to discriminate PCP from saline, they were inoculated with LP-BM5 and the PCP dose-response functions repeatedly determined."( Increased discriminative stimulus potency of phencyclidine in C57B1/6 mice infected with the LP-BM5 retrovirus.
Bruce, KH; English, JA; Paul, IA, 1999
)
0.3
" Glutamate treatment caused a dose-response increase of cyclic GMP levels in hippocampal slices."( Glutamate release is involved in PAF-increased cyclic GMP levels in hippocampus.
Calcerrada, MC; Catalán, RE; Martínez, AM, 1999
)
0.3
" A dose-response curve for dizocilpine (MK-801) was then constructed in conscious normothermic rats subjected to 75 min of MCAO."( Effects of RSR13, a synthetic allosteric modifier of hemoglobin, alone and in combination with dizocilpine, on outcome from transient focal cerebral ischemia in the rat.
Bart, RD; Grocott, HP; Pearlstein, RD; Sarraf-Yazdi, S; Sheng, H; Steffen, RP; Warner, DS, 1999
)
0.3
" In sham-operated rats, the dose-response effects of dizocilpine did not differ from those in intact rats at any time after the operation."( Two phases of behavioral plasticity in rats following unilateral excitotoxic lesion of the hippocampus.
Nabeshima, T; Sasa, M; Yamada, K; Zou, LB, 1999
)
0.3
" Initial dosing commenced 30 min prior to the 2-min 'pre-conditioning' ischaemia."( NMDA receptor antagonism, but not AMPA receptor antagonism attenuates induced ischaemic tolerance in the gerbil hippocampus.
Bond, A; Hicks, CA; Lodge, D; O'Neill, MJ; Ward, MA, 1999
)
0.3
"075 mg/kg trained animals clozapine at 3 mg/kg failed to shift the MK-801 dose-response curve to the right."( Does MK-801 discrimination constitute an animal model of schizophrenia useful for detecting atypical antipsychotics?
Boyer-Millar, C; Goudie, AJ; Smith, JA, 1999
)
0.3
" Dose-response curves for spermine, spermidine, and diethylene-triamine (DET) show different potencies for inhibiting [3HDET."( [3H]Spermine binding to synaptosomal membranes from the chick retina.
Calderón, F; López, E; López-Colomé, AM; Pichardo, I, 1999
)
0.3
" We investigated the dose-response relationship for each alcohol and determined that the order of potency was methanol < EtOH << octanol, with EC(50) values of 291 mM, 39."( Effect of ethanol upon respiratory-related hypoglossal nerve output of neonatal rat brain stem slices.
Berger, AJ; Gibson, IC, 2000
)
0.31
" In addition, it may be used to investigate further dose-response relationships and the effects of other neurotoxicants."( MK-801 neurotoxicity in cupric silver-stained sections: lesion reconstruction by 3-dimensional computer image analysis.
Fix, AS; Ridder, GM; Stitzel, SR; Switzer, RC,
)
0.13
" 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
" 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
" When ethanol (10% v/v) was added to the sucrose reinforcer, MK-801 and pentobarbital dose-response curves were shifted significantly to the left."( The discriminative stimulus properties of self-administered ethanol are mediated by GABA(A) and NMDA receptors in rats.
Bratt, AM; Camarini, R; Cox, AA; Hodge, CW; Iller, K; Kelley, SP; Mehmert, KK; Nannini, MA; Olive, MF, 2001
)
0.31
" Immediately prior to dosing, 5 days per week (M--F), throughout the 2-year dosing period, an incremental repeated acquisition (IRA) task was used to assess learning and a progressive ratio (PR) task was used to assess motivation."( Differential effects of two NMDA receptor antagonists on cognitive-behavioral development in nonhuman primates I.
Allen, RR; Hammond, TG; Paule, MG; Pearson, EC; Popke, EJ,
)
0.13
" Throughout the 2-year dosing period, a conditioned position responding (CPR) task was used to assess color and position discrimination and a delayed matching-to-sample (DMTS) task was used to assess memory."( Differential effects of two NMDA receptor antagonists on cognitive--behavioral performance in young nonhuman primates II.
Allen, RR; Hammond, TG; Paule, MG; Pearson, EC; Popke, EJ,
)
0.13
" Four doses, administered at 2 h intervals, of 15 mg/kg (4x15 mg/kg) D-METH significantly decreased TH and dopamine levels to 50% of control in mice becoming hypothermic during dosing in a 13 degrees C environment."( Phenobarbital and dizocilpine can block methamphetamine-induced neurotoxicity in mice by mechanisms that are independent of thermoregulation.
Bowyer, JF; Holson, RR; Miller, DB; O'Callaghan, JP, 2001
)
0.31
" E(2) at low dosage increases the discharge rate of SFO neuron, an effect which may be related to the activation of NMDA receptors, whereas E(2) at high dosage decreases the discharge rate, an effect which may be attributed to the activation of NOS with resultant production of NO."( [Modulatory effects of 17beta-estradiol on the electrical activity of subfornical organ neurons].
He, RR; Wang, H; Wang, ZA, 2000
)
0.31
" In general, both drugs were well tolerated and produced no treatment-related effects during 2 years of dosing and assessment."( Assessing the potential toxicity of MK-801 and remacemide: chronic exposure in juvenile rhesus monkeys.
Allen, RR; Fogle, CM; Hammond, TG; Newport, GD; Patton, R; Paule, MG; Pearson, EC; Popke, EJ; Rushing, LG,
)
0.13
" MK-801 induced c-Fos in these brain regions in a nonlinear dose-response relationship."( Effects of MK-801 and electroconvulsive shock on c-Fos expression in the rat hippocampus and frontal cortex.
Ahn, YM; Kang, UG; Kim, YS; Park, JB, 2002
)
0.31
" Moreover, they support the notion of a bell-shaped dose-response curve previously reported for sigma ligands."( Effects of sigma ligands on NMDA receptor function in the bulbectomy model of depression: a behavioural study in the rat.
Bermack, J; Debonnel, G; Dryver, E; Lavoie, N, 2002
)
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
"Systemic or regional administration of the non-competitive NMDA antagonist dizocilpine into the VTA significantly increased the rate of heroin SA and shifted the heroin dose-response curve to the right."( Blockade of ionotropic glutamatergic transmission in the ventral tegmental area reduces heroin reinforcement in rat.
Stein, EA; Xi, ZX, 2002
)
0.31
" Dosing began at weaning and continued for nine months."( Chronic exposure to NMDA receptor and sodium channel blockers during development in monkeys and rats: long-term effects on cognitive function.
Allen, RR; Fogle, CM; Hammond, TG; Paule, MG; Pearson, EC; Popke, EJ, 2003
)
0.32
" The degree of the decrease was proportional to the dosage of MK-801 used."( [MK-801 inhibits formalin-induced cyclooxygenase-2 expression in the dorsal horn of the spinal cord in rats].
Ai, J; Chen, XL; Li, QJ; Li, SQ; Li, WB; Sun, XC, 2004
)
0.32
" Repetitive dosing with ethosuximide (i."( Ethosuximide reverses paclitaxel- and vincristine-induced painful peripheral neuropathy.
Bennett, GJ; Flatters, SJ, 2004
)
0.32
" In two dose-response studies, we showed that both drugs exhibited a tendency to attenuate prepulse-elicited reaction at higher doses when PPI was severely disrupted."( The Effects of dizocilpine and phencyclidine on prepulse inhibition of the acoustic startle reflex and on prepulse-elicited reactivity in C57BL6 mice.
Chang, DL; Feldon, J; Yee, BK, 2004
)
0.32
" We also observed that the apparent dose-response curve is very sensitive to the particular time window chosen for analysis because MK-801 affects both the time course and maximum value of stimulated locomotion."( Bimodal effects of MK-801 on locomotion and stereotypy in C57BL/6 mice.
Jin, M; Strong, JA; Wu, J; Xie, Q; Yu, J; Yu, L; Zhao, G; Zhou, X; Zou, H, 2005
)
0.33
"The non-competitive NMDA receptor antagonist MK-801 induces a complex pattern of behavioral modification in mice with respect to both the time course and the dose-response relationship of behavioral changes."( Bimodal effects of MK-801 on locomotion and stereotypy in C57BL/6 mice.
Jin, M; Strong, JA; Wu, J; Xie, Q; Yu, J; Yu, L; Zhao, G; Zhou, X; Zou, H, 2005
)
0.33
" Both agents produced a marked downward shift in the nicotine dose-response curve."( Drug discrimination analysis of NMDA receptor channel blockers as nicotinic receptor antagonists in rats.
Bespalov, AY; Danysz, W; Zakharova, ES, 2005
)
0.33
" 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
" These results highlight the complexity of the dose-response relation for MK-801-induced behaviors."( Paradoxical effects of very low dose MK-801.
Cui, Y; Jin, M; Strong, JA; Tang, Y; Xie, Q; Yu, L; Zhao, G; Zou, H, 2006
)
0.33
") were obtained from preliminary dose-response studies."( SCH 23390 in the prefrontal cortex enhances the effect of apomorphine on prepulse inhibition of rats.
de Jong, IE; van den Buuse, M, 2006
)
0.33
" Further, administration of DMSO could be delayed by up to 4 h after MK-801 dosing and still achieve between 80 and 86% reduction in neuronal loss."( Antioxidants attenuate MK-801-induced cortical neurotoxicity in the rat.
Ray, DE; Willis, CL, 2007
)
0.34
" As previously reported, when a within-subjects design and cumulative dosing was employed, no tolerance was observed in the 129P3/J strain."( Morphine analgesic tolerance in 129P3/J and 129S6/SvEv mice.
Bryant, CD; Byun, JS; Evans, CJ; Fanselow, MS; Roberts, KW, 2006
)
0.33
" The data suggest that chronic MK-801 treatment adversely affects the acquisition of IRA and AVD task performance and that the inclusion of phenytoin in the MK-801 dosing regimen blocks some of the adverse effects of chronic MK-801 treatment on IRA task acquisition."( Effect of chronic MK-801 and/or phenytoin on the acquisition of complex behaviors in rats.
Allen, RR; Hammond, TG; Paule, MG; Pearson, EC; Popke, EJ; Wright, LK,
)
0.13
" 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
" In order to ensure the occurrence of status epilepticus (SE) and decrease mortality, individual dosing of pilocarpine was performed by ramping up the dose until onset of SE."( Behavioral alterations in the pilocarpine model of temporal lobe epilepsy in mice.
Gröticke, I; Hoffmann, K; Löscher, W, 2007
)
0.34
"To develop a dose-response curve, adult rats were treated with varying doses of MK-801 and their spinal cords harvested and assessed for NR2A as well as AMPA GluR1 and GluR2 subunit protein levels."( MK-801 upregulates NR2A protein levels and induces functional recovery of the ipsilateral hemidiaphragm following acute C2 hemisection in adult rats.
Alilain, WJ; Goshgarian, HG, 2007
)
0.34
"SD rats were divided into five groups randomly, the sham operation group, the model group, the MK-801 group, the large and low dosage TXL groups (TXLL and TXLS)."( [Experimental study on effect of Tongxinluo on nerve cell apoptosis after cerebral ischemia in middle cerebral arterial obstructive model rats].
Jia, ZH; Wu, YL; Yuan, GQ, 2007
)
0.34
" Ketamine, PCP, and MK-801 enhanced catalepsy along inverted U-shaped dose-response curves likely because higher doses affected motor coordination, which limited their catalepsy-enhancing effects."( Cataleptic effects of gamma-hydroxybutyrate (GHB) and baclofen in mice: mediation by GABA(B) receptors, but differential enhancement by N-methyl-d-aspartate (NMDA) receptor antagonists.
France, CP; Koek, W, 2008
)
0.35
"Treatment with MPEP and dizocilpine significantly reduced cocaine self-administration, producing rightward and downward shifts in the ascending limb of the cocaine dose-response function."( Attenuation of cocaine self-administration in squirrel monkeys following repeated administration of the mGluR5 antagonist MPEP: comparison with dizocilpine.
Platt, DM; Rowlett, JK; Spealman, RD, 2008
)
0.35
" After treatment, a positive dose-response relationship of increasing NMDARS, increasing caspase-3 activity and cell death was observed in all PCB compounds."( Role of N-methyl-D-aspartate receptors in polychlorinated biphenyl mediated neurotoxicity.
Chan, HM; Ndountse, LT, 2009
)
0.35
" The present study directly addresses the hypothesis that MC4R activation may ameliorate ischemic brain injury by assessing the efficacy of a novel small molecule MC4R agonist RY767, administered in a pharmacokinetically guided and pharmacologically validated dosing regimen, in a rat stroke model of transient middle cerebral artery occlusion (tMCAO)."( Lack of protection with a novel, selective melanocortin receptor subtype-4 agonist RY767 in a rat transient middle cerebral artery occlusion stroke model.
Fong, T; Lynch, J; Nargund, R; Pollard, P; Regan, C; Reynolds, I; Shepherd, C; Strack, A; Weinberg, D; Ye, Z, 2009
)
0.35
" However, co-administration of these antagonists with morphine into the vPAG enhanced the acute antinociceptive effects of morphine as measured by a leftward shift in the morphine dose-response curves."( Glutamate modulation of antinociception, but not tolerance, produced by morphine microinjection into the periaqueductal gray of the rat.
Bobeck, EN; Ingram, SL; Morgan, MM, 2009
)
0.35
" Anticonvulsant effective doses (ED(50)) were determined using an up-down dosing procedure over successive animals."( Protection against sarin-induced seizures in rats by direct brain microinjection of scopolamine, midazolam or MK-801.
McDonough, JH; Shih, TM; Skovira, JW, 2010
)
0.36
"Experiment 1 examined the dose-response effects of PCP and (+)MK-801 on licking microstructure during sucrose consumption."( Analysis of licking microstructure provides no evidence for a reduction in reward value following acute or sub-chronic phencyclidine administration.
Dwyer, DM; Gilmour, G; Lydall, ES, 2010
)
0.36
" Only the group that received 2 postoperative injections and increased total dosage had improved analgesic indices."( Lack of beneficial effect for preemptive analgesia in postoperative pain control: verifying the efficacy of preemptive analgesia with N-methyl-D-aspartate receptor antagonists in a modified animal model of postoperative pain.
Chan, KH; Chang, WK; Chen, PT; Chu, YC; Chuang, CC; Tao, YX, 2011
)
0.37
" Increasing the duration of administration and/or total dosage had an incremental analgesic effect in comparison with a single injection."( Lack of beneficial effect for preemptive analgesia in postoperative pain control: verifying the efficacy of preemptive analgesia with N-methyl-D-aspartate receptor antagonists in a modified animal model of postoperative pain.
Chan, KH; Chang, WK; Chen, PT; Chu, YC; Chuang, CC; Tao, YX, 2011
)
0.37
" After rats were injected subcutaneously with nisoxetine, dose-response curves were constructed."( Nisoxetine produces local but not systemic analgesia against cutaneous nociceptive stimuli in the rat.
Chen, YC; Chen, YW; Chu, CC; Hung, CH; Shao, DZ; Wang, JJ, 2012
)
0.38
" Compounds were dosed 30 min before the learning trial of the task."( Phosphodiesterase type 5 (PDE5) inhibition improves object recognition memory: indications for central and peripheral mechanisms.
Akkerman, S; Blokland, A; Menniti, FS; Prickaerts, J; Reneerkens, OA; Rutten, K; Shaffer, CL; Steinbusch, HW, 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
" Mouse EEG was recorded in response to auditory stimuli after either vehicle or MK801 and the dose-response relationship for each measure was determined."( NMDA antagonist MK801 recreates auditory electrophysiology disruption present in autism and other neurodevelopmental disorders.
Gandal, MJ; Roberts, TP; Saunders, JA; Siegel, SJ, 2012
)
0.38
" For each drug treatment in each brain area, anticonvulsant ED₅₀ values were calculated using an up-down dosing procedure over successive animals."( Neuropharmacological specificity of brain structures involved in soman-induced seizures.
McDonough, JH; Shih, TM; Skovira, JW, 2012
)
0.38
" Repeated benzodiazepine dosing or combined application of benzodiazepines and NMDA receptor antagonists is more likely to be effective in treating TMDT poisoning."( Differential antagonism of tetramethylenedisulfotetramine-induced seizures by agents acting at NMDA and GABA(A) receptors.
Shakarjian, MP; Stanton, PK; Velíšek, L; Velíšková, J, 2012
)
0.38
" The inhibitory pattern on tau phosphorylation reveals a prolonged pharmacodynamic effect predicting less frequent dosing in humans."( AZD1080, a novel GSK3 inhibitor, rescues synaptic plasticity deficits in rodent brain and exhibits peripheral target engagement in humans.
Andersson, A; Arvidsson, PI; Berg, S; Bhat, RV; Doherty, J; Fälting, J; Georgievska, B; Gruber, S; Hellberg, S; Mörtberg, A; Neelissen, J; Nilsson, Y; Osswald, G; Sandin, J; Schött, P, 2013
)
0.39
" In the first series of experiments, we established a dose-response relationship for ghrelin on the passive avoidance paradigm."( The effect of ghrelin on MK-801 induced memory impairment in rats.
Goshadrou, F; Kermani, M; Ronaghi, A; Sajjadi, S, 2013
)
0.39
" The second experiment examined effects of repeated dosing with ketamine (3."( Dissociable effects of the noncompetitive NMDA receptor antagonists ketamine and MK-801 on intracranial self-stimulation in rats.
Hillhouse, TM; Negus, SS; Porter, JH, 2014
)
0.4
" Repeated dosing with ketamine produced dose-dependent tolerance to the rate-decreasing effects of ketamine (10."( Dissociable effects of the noncompetitive NMDA receptor antagonists ketamine and MK-801 on intracranial self-stimulation in rats.
Hillhouse, TM; Negus, SS; Porter, JH, 2014
)
0.4
"2 mg/kg) increased the GBO power, exhibiting an inverted U-shape dose-response curve; at higher doses (0."( Differential effects of NMDA receptor antagonists at lower and higher doses on basal gamma band oscillation power in rat cortical electroencephalograms.
Chaki, S; Hiyoshi, T; Kambe, D; Karasawa, J, 2014
)
0.4
" However, PHA-543613 had lower efficacy in the MK-801 induced transient amnesia model, as the pharmacologically induced memory deficit was only partially reversed and an inverted U-shaped dose-response was found."( Differential effects of α7 nicotinic receptor agonist PHA-543613 on spatial memory performance of rats in two distinct pharmacological dementia models.
Bali, ZK; Bruszt, N; Csurgyók, R; Hernádi, I; Horváth, H; Inkeller, J, 2015
)
0.42
" We therefore administered the same dosing regimen of MK801 to juvenile mice and compared them to juvenile SR-/- mice."( Subchronic pharmacological and chronic genetic NMDA receptor hypofunction differentially regulate the Akt signaling pathway and Arc expression in juvenile and adult mice.
Balu, DT; Coyle, JT; Takagi, S, 2015
)
0.42
" Dosing with dizocilpine (0."( Improvement of dizocilpine-induced social recognition deficits in mice by brexpiprazole, a novel serotonin-dopamine activity modulator.
Futamura, T; Hashimoto, K; Yoshimi, N, 2015
)
0.42
"MS and MK-801 showed biphasic and linear dose-response pattern, respectively."( The antinociceptive effects of magnesium sulfate and MK-801 in visceral inflammatory pain model: The role of NO/cGMP/K(+)ATP pathway.
Prostran, M; Savic Vujovic, K; Srebro, D; Vuckovic, S, 2015
)
0.42
" Aripiprazole produced a U-shaped dose-response curve on MK-801-induced bar pressing behavior, a dose-dependent decrease in locomotor activity but no changes in IL pERK1/2 labeling."( Attenuation of MK-801-induced behavioral perseveration by typical and atypical antipsychotic pretreatment in rats.
Holahan, MR; Stocco, MR; Tuplin, EW, 2015
)
0.42
" The dose-response relationships of all 3 compounds in the forced swim test were also investigated in mice 30 min after IP administration."( Antidepressant-like effects of ketamine, norketamine and dehydronorketamine in forced swim test: Role of activity at NMDA receptor.
Drabik, U; Gajdosz, R; Librowski, T; Nowak, G; Popik, P; Sałat, K; Siwek, A; Starowicz, G, 2015
)
0.42
" In neuropharmacological studies their functioning strongly depends on testing conditions and the dosage of NMDAR antagonists."( MK-801 and memantine act differently on short-term memory tested with different time-intervals in the Morris water maze test.
Duda, W; Nekovarova, T; Ostaszewski, P; Stuchlik, A; Vales, K; Wesierska, M, 2016
)
0.43
" Co-treatment of maslinic acid and MK-801 at a subthreshold dosage obviously induced neuroprotection after ischemia."( Neuroprotection by Combined Administration with Maslinic Acid, a Natural Product from Olea europaea, and MK-801 in the Cerebral Ischemia Model.
Guan, T; Li, Y; Qian, Y; Sun, H; Tang, X, 2016
)
0.43
" Rings of BMCA were mounted in isolated tissue chambers equipped with isometric tension transducers to obtain pharmacologic dose-response curves."( Multiple Actions of Phencyclidine and (+)MK-801 on Isolated Bovine Cerebral Arteries.
Chen, D; Kamel, IR; Wendling, KS; Wendling, WW, 2018
)
0.48
"Clinical studies that focused on treating schizophrenia showed that Calculus Bovis Sativus (CBS), a substitute of Calculus Bovis, when used in combination with haloperidol could significantly lower the dosage of haloperidol compared with treatment with haloperidol alone, whereas efficacy was maintained."( Investigation of the synergistic effects of haloperidol combined with Calculus Bovis Sativus in treating MK-801-induced schizophrenia in rats.
He, GF; He, GZ; Lei, K; Li, J; Li, XP; Liu, D; Liu, YN; Ren, XH; Zhang, CL, 2018
)
0.48
" Dizocilpine impaired OST accuracy at doses that had no effect on a reference memory control task in both 2-choice and 10-choice conditions; however, the dose-response function was shifted to the left in the 10-choice tests."( Effects of NMDA antagonist dizocilpine (MK-801) are modulated by the number of distractor stimuli in the rodent odor span task of working memory.
Bruce, KE; Deal, M; Galizio, M; Mathews, M; Panoz-Brown, D; Prichard, A, 2019
)
0.51
" Interestingly, the dosage in both conditions is similar, and positive symptoms of schizophrenia appear before antidepressant effects emerge."( Brain NMDA Receptors in Schizophrenia and Depression.
Adell, A, 2020
)
0.56
" Both olanzapine and risperidone reversed the MK801-induced behavioral abnormalities as the dosage increased; however, they degenerated the hepatocytes in the liver and influenced the blood lipid levels and blood glucose levels."( Metformin attenuates antipsychotic-induced metabolic dysfunctions in MK801-induced schizophrenia-like rats.
Huang, H; Li, X; Liu, Y; Liu, Z; Luo, C; Mao, X; Wang, X; Zhao, J; Zhou, H, 2020
)
0.56
" Clearly more research is required to understand how NMDA-R antagonism and dosage affects processes contributing to MMN."( The effect of NMDA-R antagonist, MK-801, on neuronal mismatch along the rat auditory thalamocortical pathway.
Harms, L; Malmierca, MS; Michie, PT; Parras, GG; Valdés-Baizabal, C, 2020
)
0.56
"Findings will provide timely information on the safety, efficacy, and optimal dosing of t-PA to treat moderate/severe COVID-19-induced ARDS, which can be rapidly adapted to a phase III trial (NCT04357730; FDA IND 149634)."(
Abbasi, S; Abd El-Wahab, A; Abdallah, M; Abebe, G; Aca-Aca, G; Adama, S; Adefegha, SA; Adidigue-Ndiome, R; Adiseshaiah, P; Adrario, E; Aghajanian, C; Agnese, W; Ahmad, A; Ahmad, I; Ahmed, MFE; Akcay, OF; Akinmoladun, AC; Akutagawa, T; Alakavuklar, MA; Álava-Rabasa, S; Albaladejo-Florín, MJ; Alexandra, AJE; Alfawares, R; Alferiev, IS; Alghamdi, HS; Ali, I; Allard, B; Allen, JD; Almada, E; Alobaid, A; Alonso, GL; Alqahtani, YS; Alqarawi, W; Alsaleh, H; Alyami, BA; Amaral, BPD; Amaro, JT; Amin, SAW; Amodio, E; Amoo, ZA; Andia Biraro, I; Angiolella, L; Anheyer, D; Anlay, DZ; Annex, BH; Antonio-Aguirre, B; Apple, S; Arbuznikov, AV; Arinsoy, T; Armstrong, DK; Ash, S; Aslam, M; Asrie, F; Astur, DC; Atzrodt, J; Au, DW; Aucoin, M; Auerbach, EJ; Azarian, S; Ba, D; Bai, Z; Baisch, PRM; Balkissou, AD; Baltzopoulos, V; Banaszewski, M; Banerjee, S; Bao, Y; Baradwan, A; Barandika, JF; Barger, PM; Barion, MRL; Barrett, CD; Basudan, AM; Baur, LE; Baz-Rodríguez, SA; Beamer, P; Beaulant, A; Becker, DF; Beckers, C; Bedel, J; Bedlack, R; Bermúdez de Castro, JM; Berry, JD; Berthier, C; Bhattacharya, D; Biadgo, B; Bianco, G; Bianco, M; Bibi, S; Bigliardi, AP; Billheimer, D; Birnie, DH; Biswas, K; Blair, HC; Bognetti, P; Bolan, PJ; Bolla, JR; Bolze, A; Bonnaillie, P; Borlimi, R; Bórquez, J; Bottari, NB; Boulleys-Nana, JR; Brighetti, G; Brodeur, GM; Budnyak, T; Budnyk, S; Bukirwa, VD; Bulman, DM; Burm, R; Busman-Sahay, K; Butcher, TW; Cai, C; Cai, H; Cai, L; Cairati, M; Calvano, CD; Camacho-Ordóñez, A; Camela, E; Cameron, T; Campbell, BS; Cansian, RL; Cao, Y; Caporale, AS; Carciofi, AC; Cardozo, V; Carè, J; Carlos, AF; Carozza, R; Carroll, CJW; Carsetti, A; Carubelli, V; Casarotta, E; Casas, M; Caselli, G; Castillo-Lora, J; Cataldi, TRI; Cavalcante, ELB; Cavaleiro, A; Cayci, Z; Cebrián-Tarancón, C; Cedrone, E; Cella, D; Cereda, C; Ceretti, A; Ceroni, M; Cha, YH; Chai, X; Chang, EF; Chang, TS; Chanteux, H; Chao, M; Chaplin, BP; Chaturvedi, S; Chaturvedi, V; Chaudhary, DK; Chen, A; Chen, C; Chen, HY; Chen, J; Chen, JJ; Chen, K; Chen, L; Chen, Q; Chen, R; Chen, SY; Chen, TY; Chen, WM; Chen, X; Chen, Y; Cheng, G; Cheng, GJ; Cheng, J; Cheng, YH; Cheon, HG; Chew, KW; Chhoker, S; Chiu, WN; Choi, ES; Choi, MJ; Choi, SD; Chokshi, S; Chorny, M; Chu, KI; Chu, WJ; Church, AL; Cirrincione, A; Clamp, AR; Cleff, MB; Cohen, M; Coleman, RL; Collins, SL; Colombo, N; Conduit, N; Cong, WL; Connelly, MA; Connor, J; Cooley, K; Correa Ramos Leal, I; Cose, S; Costantino, C; Cottrell, M; Cui, L; Cundall, J; Cutaia, C; Cutler, CW; Cuypers, ML; da Silva Júnior, FMR; Dahal, RH; Damiani, E; Damtie, D; Dan-Li, W; Dang, Z; Dasa, SSK; Davin, A; Davis, DR; de Andrade, CM; de Jong, PL; de Oliveira, D; de Paula Dorigam, JC; Dean, A; Deepa, M; Delatour, C; Dell'Aiera, S; Delley, MF; den Boer, RB; Deng, L; Deng, Q; Depner, RM; Derdau, V; Derici, U; DeSantis, AJ; Desmarini, D; Diffo-Sonkoue, L; Divizia, M; Djenabou, A; Djordjevic, JT; Dobrovolskaia, MA; Domizi, R; Donati, A; Dong, Y; Dos Santos, M; Dos Santos, MP; Douglas, RG; Duarte, PF; Dullaart, RPF; Duscha, BD; Edwards, LA; Edwards, TE; Eichenwald, EC; El-Baba, TJ; Elashiry, M; Elashiry, MM; Elashry, SH; Elliott, A; Elsayed, R; Emerson, MS; Emmanuel, YO; Emory, TH; Endale-Mangamba, LM; Enten, GA; Estefanía-Fernández, K; Estes, JD; Estrada-Mena, FJ; Evans, S; Ezra, L; Faria de, RO; Farraj, AK; Favre, C; Feng, B; Feng, J; Feng, L; Feng, W; Feng, X; Feng, Z; Fernandes, CLF; Fernández-Cuadros, ME; Fernie, AR; Ferrari, D; Florindo, PR; Fong, PC; Fontes, EPB; Fontinha, D; Fornari, VJ; Fox, NP; Fu, Q; Fujitaka, Y; Fukuhara, K; Fumeaux, T; Fuqua, C; Fustinoni, S; Gabbanelli, V; Gaikwad, S; Gall, ET; Galli, A; Gancedo, MA; Gandhi, MM; Gao, D; Gao, K; Gao, M; Gao, Q; Gao, X; Gao, Y; Gaponenko, V; Garber, A; Garcia, EM; García-Campos, C; García-Donas, J; García-Pérez, AL; Gasparri, F; Ge, C; Ge, D; Ge, JB; Ge, X; George, I; George, LA; Germani, G; Ghassemi Tabrizi, S; Gibon, Y; Gillent, E; Gillies, RS; Gilmour, MI; Goble, S; Goh, JC; Goiri, F; Goldfinger, LE; Golian, M; Gómez, MA; Gonçalves, J; Góngora-García, OR; Gonul, I; González, MA; Govers, TM; Grant, PC; Gray, EH; Gray, JE; Green, MS; Greenwald, I; Gregory, MJ; Gretzke, D; Griffin-Nolan, RJ; Griffith, DC; Gruppen, EG; Guaita, A; Guan, P; Guan, X; Guerci, P; Guerrero, DT; Guo, M; Guo, P; Guo, R; Guo, X; Gupta, J; Guz, G; Hajizadeh, N; Hamada, H; Haman-Wabi, AB; Han, TT; Hannan, N; Hao, S; Harjola, VP; Harmon, M; Hartmann, MSM; Hartwig, JF; Hasani, M; Hawthorne, WJ; Haykal-Coates, N; Hazari, MS; He, DL; He, P; He, SG; Héau, C; Hebbar Kannur, K; Helvaci, O; Heuberger, DM; Hidalgo, F; Hilty, MP; Hirata, K; Hirsch, A; Hoffman, AM; Hoffmann, JF; Holloway, RW; Holmes, RK; Hong, S; Hongisto, M; Hopf, NB; Hörlein, R; Hoshino, N; Hou, Y; Hoven, NF; Hsieh, YY; Hsu, CT; Hu, CW; Hu, JH; Hu, MY; Hu, Y; Hu, Z; Huang, C; Huang, D; Huang, DQ; Huang, L; Huang, Q; Huang, R; Huang, S; Huang, SC; Huang, W; Huang, Y; Huffman, KM; Hung, CH; Hung, CT; Huurman, R; Hwang, SM; Hyun, S; Ibrahim, AM; Iddi-Faical, A; Immordino, P; Isla, MI; Jacquemond, V; Jacques, T; Jankowska, E; Jansen, JA; Jäntti, T; Jaque-Fernandez, F; Jarvis, GA; Jatt, LP; Jeon, JW; Jeong, SH; Jhunjhunwala, R; Ji, F; Jia, X; Jia, Y; Jian-Bo, Z; Jiang, GD; Jiang, L; Jiang, W; Jiang, WD; Jiang, Z; Jiménez-Hoyos, CA; Jin, S; Jobling, MG; John, CM; John, T; Johnson, CB; Jones, KI; Jones, WS; Joseph, OO; Ju, C; Judeinstein, P; Junges, A; Junnarkar, M; Jurkko, R; Kaleka, CC; Kamath, AV; Kang, X; Kantsadi, AL; Kapoor, M; Karim, Z; Kashuba, ADM; Kassa, E; Kasztura, M; Kataja, A; Katoh, T; Kaufman, JS; Kaupp, M; Kehinde, O; Kehrenberg, C; Kemper, N; Kerr, CW; Khan, AU; Khan, MF; Khan, ZUH; Khojasteh, SC; Kilburn, S; Kim, CG; Kim, DU; Kim, DY; Kim, HJ; Kim, J; Kim, OH; Kim, YH; King, C; Klein, A; Klingler, L; Knapp, AK; Ko, TK; Kodavanti, UP; Kolla, V; Kong, L; Kong, RY; Kong, X; Kore, S; Kortz, U; Korucu, B; Kovacs, A; Krahnert, I; Kraus, WE; Kuang, SY; Kuehn-Hajder, JE; Kurz, M; Kuśtrowski, P; Kwak, YD; Kyttaris, VC; Laga, SM; Laguerre, A; Laloo, A; Langaro, MC; Langham, MC; Lao, X; Larocca, MC; Lassus, J; Lattimer, TA; Lazar, S; Le, MH; Leal, DB; Leal, M; Leary, A; Ledermann, JA; Lee, JF; Lee, MV; Lee, NH; Leeds, CM; Leeds, JS; Lefrandt, JD; Leicht, AS; Leonard, M; Lev, S; Levy, K; Li, B; Li, C; Li, CM; Li, DH; Li, H; Li, J; Li, L; Li, LJ; Li, N; Li, P; Li, T; Li, X; Li, XH; Li, XQ; Li, XX; Li, Y; Li, Z; Li, ZY; Liao, YF; Lin, CC; Lin, MH; Lin, Y; Ling, Y; Links, TP; Lira-Romero, E; Liu, C; Liu, D; Liu, H; Liu, J; Liu, L; Liu, LP; Liu, M; Liu, T; Liu, W; Liu, X; Liu, XH; Liu, Y; Liuwantara, D; Ljumanovic, N; Lobo, L; Lokhande, K; Lopes, A; Lopes, RMRM; López-Gutiérrez, JC; López-Muñoz, MJ; López-Santamaría, M; Lorenzo, C; Lorusso, D; Losito, I; Lu, C; Lu, H; Lu, HZ; Lu, SH; Lu, SN; Lu, Y; Lu, ZY; Luboga, F; Luo, JJ; Luo, KL; Luo, Y; Lutomski, CA; Lv, W; M Piedade, MF; Ma, J; Ma, JQ; Ma, JX; Ma, N; Ma, P; Ma, S; Maciel, M; Madureira, M; Maganaris, C; Maginn, EJ; Mahnashi, MH; Maierhofer, M; Majetschak, M; Malla, TR; Maloney, L; Mann, DL; Mansuri, A; Marelli, E; Margulis, CJ; Marrella, A; Martin, BL; Martín-Francés, L; Martínez de Pinillos, M; Martínez-Navarro, EM; Martinez-Quintanilla Jimenez, D; Martínez-Velasco, A; Martínez-Villaseñor, L; Martinón-Torres, M; Martins, BA; Massongo, M; Mathew, AP; Mathews, D; Matsui, J; Matsumoto, KI; Mau, T; Maves, RC; Mayclin, SJ; Mayer, JM; Maynard, ND; Mayr, T; Mboowa, MG; McEvoy, MP; McIntyre, RC; McKay, JA; McPhail, MJW; McVeigh, AL; Mebazaa, A; Medici, V; Medina, DN; Mehmood, T; Mei-Li, C; Melku, M; Meloncelli, S; Mendes, GC; Mendoza-Velásquez, C; Mercadante, R; Mercado, MI; Merenda, MEZ; Meunier, J; Mi, SL; Michels, M; Mijatovic, V; Mikhailov, V; Milheiro, SA; Miller, DC; Ming, F; Mitsuishi, M; Miyashita, T; Mo, J; Mo, S; Modesto-Mata, M; Moeller, S; Monte, A; Monteiro, L; Montomoli, J; Moore, EE; Moore, HB; Moore, PK; Mor, MK; Moratalla-López, N; Moratilla Lapeña, L; Moreira, R; Moreno, MA; Mörk, AC; Morton, M; Mosier, JM; Mou, LH; Mougharbel, AS; Muccillo-Baisch, AL; Muñoz-Serrano, AJ; Mustafa, B; Nair, GM; Nakanishi, I; Nakanjako, D; Naraparaju, K; Nawani, N; Neffati, R; Neil, EC; Neilipovitz, D; Neira-Borrajo, I; Nelson, MT; Nery, PB; Nese, M; Nguyen, F; Nguyen, MH; Niazy, AA; Nicolaï, J; Nogueira, F; Norbäck, D; Novaretti, JV; O'Donnell, T; O'Dowd, A; O'Malley, DM; Oaknin, A; Ogata, K; Ohkubo, K; Ojha, M; Olaleye, MT; Olawande, B; Olomo, EJ; Ong, EWY; Ono, A; Onwumere, J; Ortiz Bibriesca, DM; Ou, X; Oza, AM; Ozturk, K; Özütemiz, C; Palacio-Pastrana, C; Palaparthi, A; Palevsky, PM; Pan, K; Pantanetti, S; Papachristou, DJ; Pariani, A; Parikh, CR; Parissis, J; Paroul, N; Parry, S; Patel, N; Patel, SM; Patel, VC; Pawar, S; Pefura-Yone, EW; Peixoto Andrade, BCO; Pelepenko, LE; Peña-Lora, D; Peng, S; Pérez-Moro, OS; Perez-Ortiz, AC; Perry, LM; Peter, CM; Phillips, NJ; Phillips, P; Pia Tek, J; Piner, LW; Pinto, EA; Pinto, SN; Piyachaturawat, P; Poka-Mayap, V; Polledri, E; Poloni, TE; Ponessa, G; Poole, ST; Post, AK; Potter, TM; Pressly, BB; Prouty, MG; Prudêncio, M; Pulkki, K; Pupier, C; Qian, H; Qian, ZP; Qiu, Y; Qu, G; Rahimi, S; Rahman, AU; Ramadan, H; Ramanna, S; Ramirez, I; Randolph, GJ; Rasheed, A; Rault, J; Raviprakash, V; Reale, E; Redpath, C; Rema, V; Remucal, CK; Remy, D; Ren, T; Ribeiro, LB; Riboli, G; Richards, J; Rieger, V; Rieusset, J; Riva, A; Rivabella Maknis, T; Robbins, JL; Robinson, CV; Roche-Campo, F; Rodriguez, R; Rodríguez-de-Cía, J; Rollenhagen, JE; Rosen, EP; Rub, D; Rubin, N; Rubin, NT; Ruurda, JP; Saad, O; Sabell, T; Saber, SE; Sabet, M; Sadek, MM; Saejio, A; Salinas, RM; Saliu, IO; Sande, D; Sang, D; Sangenito, LS; Santos, ALSD; Sarmiento Caldas, MC; Sassaroli, S; Sassi, V; Sato, J; Sauaia, A; Saunders, K; Saunders, PR; Savarino, SJ; Scambia, G; Scanlon, N; Schetinger, MR; Schinkel, AFL; Schladweiler, MC; Schofield, CJ; Schuepbach, RA; Schulz, J; Schwartz, N; Scorcella, C; Seeley, J; Seemann, F; Seinige, D; Sengoku, T; Seravalli, J; Sgromo, B; Shaheen, MY; Shan, L; Shanmugam, S; Shao, H; Sharma, S; Shaw, KJ; Shen, BQ; Shen, CH; Shen, P; Shen, S; Shen, Y; Shen, Z; Shi, J; Shi-Li, L; Shimoda, K; Shoji, Y; Shun, C; Silva, MA; Silva-Cardoso, J; Simas, NK; Simirgiotis, MJ; Sincock, SA; Singh, MP; Sionis, A; Siu, J; Sivieri, EM; Sjerps, MJ; Skoczen, SL; Slabon, A; Slette, IJ; Smith, MD; Smith, S; Smith, TG; Snapp, KS; Snow, SJ; Soares, MCF; Soberman, D; Solares, MD; Soliman, I; Song, J; Sorooshian, A; Sorrell, TC; Spinar, J; Staudt, A; Steinhart, C; Stern, ST; Stevens, DM; Stiers, KM; Stimming, U; Su, YG; Subbian, V; Suga, H; Sukhija-Cohen, A; Suksamrarn, A; Suksen, K; Sun, J; Sun, M; Sun, P; Sun, W; Sun, XF; Sun, Y; Sundell, J; Susan, LF; Sutjarit, N; Swamy, KV; Swisher, EM; Sykes, C; Takahashi, JA; Talmor, DS; Tan, B; Tan, ZK; Tang, L; Tang, S; Tanner, JJ; Tanwar, M; Tarazi, Z; Tarvasmäki, T; Tay, FR; Teketel, A; Temitayo, GI; Thersleff, T; Thiessen Philbrook, H; Thompson, LC; Thongon, N; Tian, B; Tian, F; Tian, Q; Timothy, AT; Tingle, MD; Titze, IR; Tolppanen, H; Tong, W; Toyoda, H; Tronconi, L; Tseng, CH; Tu, H; Tu, YJ; Tung, SY; Turpault, S; Tuynman, JB; Uemoto, AT; Ugurlu, M; Ullah, S; Underwood, RS; Ungell, AL; Usandizaga-Elio, I; Vakonakis, I; van Boxel, GI; van den Beucken, JJJP; van der Boom, T; van Slegtenhorst, MA; Vanni, JR; Vaquera, A; Vasconcellos, RS; Velayos, M; Vena, R; Ventura, G; Verso, MG; Vincent, RP; Vitale, F; Vitali, S; Vlek, SL; Vleugels, MPH; Volkmann, N; Vukelic, M; Wagner Mackenzie, B; Wairagala, P; Waller, SB; Wan, J; Wan, MT; Wan, Y; Wang, CC; Wang, H; Wang, J; Wang, JF; Wang, K; Wang, L; Wang, M; Wang, S; Wang, WM; Wang, X; Wang, Y; Wang, YD; Wang, YF; Wang, Z; Wang, ZG; Warriner, K; Weberpals, JI; Weerachayaphorn, J; Wehrli, FW; Wei, J; Wei, KL; Weinheimer, CJ; Weisbord, SD; Wen, S; Wendel Garcia, PD; Williams, JW; Williams, R; Winkler, C; Wirman, AP; Wong, S; Woods, CM; Wu, B; Wu, C; Wu, F; Wu, P; Wu, S; Wu, Y; Wu, YN; Wu, ZH; Wurtzel, JGT; Xia, L; Xia, Z; Xia, ZZ; Xiao, H; Xie, C; Xin, ZM; Xing, Y; Xing, Z; Xu, S; Xu, SB; Xu, T; Xu, X; Xu, Y; Xue, L; Xun, J; Yaffe, MB; Yalew, A; Yamamoto, S; Yan, D; Yan, H; Yan, S; Yan, X; Yang, AD; Yang, E; Yang, H; Yang, J; Yang, JL; Yang, K; Yang, M; Yang, P; Yang, Q; Yang, S; Yang, W; Yang, X; Yang, Y; Yao, JC; Yao, WL; Yao, Y; Yaqub, TB; Ye, J; Ye, W; Yen, CW; Yeter, HH; Yin, C; Yip, V; Yong-Yi, J; Yu, HJ; Yu, MF; Yu, S; Yu, W; Yu, WW; Yu, X; Yuan, P; Yuan, Q; Yue, XY; Zaia, AA; Zakhary, SY; Zalwango, F; Zamalloa, A; Zamparo, P; Zampini, IC; Zani, JL; Zeitoun, R; Zeng, N; Zenteno, JC; Zepeda-Palacio, C; Zhai, C; Zhang, B; Zhang, G; Zhang, J; Zhang, K; Zhang, Q; Zhang, R; Zhang, T; Zhang, X; Zhang, Y; Zhang, YY; Zhao, B; Zhao, D; Zhao, G; Zhao, H; Zhao, Q; Zhao, R; Zhao, S; Zhao, T; Zhao, X; Zhao, XA; Zhao, Y; Zhao, Z; Zheng, Z; Zhi-Min, G; Zhou, CL; Zhou, HD; Zhou, J; Zhou, W; Zhou, XQ; Zhou, Z; Zhu, C; Zhu, H; Zhu, L; Zhu, Y; Zitzmann, N; Zou, L; Zou, Y, 2022
)
0.72
" Ketamine dosing was studied up to 20 mg/kg intravenously for the single-dose neuropathology study and up to 60 mg/kg intraperitoneally for the multiple-dose neuropathology study."( A comparison of the pharmacokinetics and NMDAR antagonism-associated neurotoxicity of ketamine, (2R,6R)-hydroxynorketamine and MK-801.
Burke, RD; Elayan, I; Gould, TD; Lemke-Boutcher, LE; Lynch, DC; Mathew, S; Moaddel, R; Morris, PJ; Rao, DB; Sharma, AK; Thomas, CJ; Zanos, P; Zarate, CA,
)
0.13
" 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
"MK801 dose-response study was conducted in RHA and Roman Low-Avoidance (RLA) male rats."( Atypical antipsychotics attenuate MK801-induced social withdrawal and hyperlocomotion in the RHA rat model of schizophrenia-relevant features.
Cañete, T; Fernández-Teruel, A; Lavín, V; Oliveras, I; Río-Álamos, C; Sampedro-Viana, D; Sánchez-González, A; Sanna, F; Tapias-Espinosa, C; Tobeña, A; Torrecilla, P, 2023
)
0.91
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (5)

RoleDescription
anaestheticSubstance which produces loss of feeling or sensation.
anticonvulsantA drug used to prevent seizures or reduce their severity.
neuroprotective agentAny compound that can be used for the treatment of neurodegenerative disorders.
nicotinic antagonistAn antagonist at the nicotinic cholinergic receptor.
NMDA receptor antagonistAny substance that inhibits the action of N-methyl-D-aspartate (NMDA) receptors. They tend to induce a state known as dissociative anesthesia, marked by catalepsy, amnesia, and analgesia, while side effects can include hallucinations, nightmares, and confusion. Due to their psychotomimetic effects, many NMDA receptor antagonists are used as recreational drugs.
[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 (2)

ClassDescription
maleate saltSalts from maleic acid.
tetracyclic antidepressantAn antidepressant whose molecular structure consists of four ring-like structures in a T-shape.
[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]

Protein Targets (13)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
TDP1 proteinHomo sapiens (human)Potency19.13490.000811.382244.6684AID686978; AID686979
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency8.91250.035520.977089.1251AID504332
potassium voltage-gated channel subfamily H member 2 isoform dHomo sapiens (human)Potency7.07950.01789.637444.6684AID588834
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency23.13530.000323.4451159.6830AID743065; AID743067
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency0.03980.050127.073689.1251AID588590
gemininHomo sapiens (human)Potency35.48130.004611.374133.4983AID624297
[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 ionotropic, NMDA 1 Rattus norvegicus (Norway rat)Ki0.00240.00030.86666.6900AID145123
Glutamate receptor ionotropic, NMDA 2A Rattus norvegicus (Norway rat)Ki0.00240.00030.68056.6900AID145123
Glutamate receptor ionotropic, NMDA 2BRattus norvegicus (Norway rat)Ki0.00240.00030.70716.6900AID145123
Glutamate receptor ionotropic, NMDA 2CRattus norvegicus (Norway rat)Ki0.00240.00030.81966.6900AID145123
Glutamate receptor ionotropic, NMDA 2DRattus norvegicus (Norway rat)Ki0.00240.00030.70726.6900AID145123
Glutamate receptor ionotropic, NMDA 3BRattus norvegicus (Norway rat)Ki0.00240.00030.70726.6900AID145123
Glutamate receptor ionotropic, NMDA 3ARattus norvegicus (Norway rat)Ki0.00240.00030.70726.6900AID145123
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Ceullar Components (2)

Processvia Protein(s)Taxonomy
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 (60)

Assay IDTitleYearJournalArticle
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.
AID478794Neuroprotective effect against H202-induced Sprague-Dawley rat neuron injury assessed as viable cells by annexin V-propidium iodide staining by flow cytometry (Rvb = 93.66%+/-2.19%)2010European journal of medicinal chemistry, May, Volume: 45, Issue:5
Design, synthesis and biological evaluation of new ionone derivatives as potential neuroprotective agents in cerebral ischemia.
AID478958Neuroprotective effect against H202-induced Sprague-Dawley rat neuron injury assessed as early apoptic cells by annexin V-propidium iodide staining by flow cytometry (Rvb = 3.09% +/- 1.40%)2010European journal of medicinal chemistry, May, Volume: 45, Issue:5
Design, synthesis and biological evaluation of new ionone derivatives as potential neuroprotective agents in cerebral ischemia.
AID380081Neuroprotective activity against glutamate-induced neurotoxicity in Sprague-Dawley rat cortical cells at 10 uM after 24 hrs by MTT assay relative to control2006Journal of natural products, Feb, Volume: 69, Issue:2
Neuroprotective 2-(2-phenylethyl)chromones of Imperata cylindrica.
AID380149Anticonvulsant activity against NMDA-induced seizures in mouse assessed as seizure latency at 0.3 mg/kg, ip administered 30 mins prior to NMDA challenge2006Journal of natural products, Mar, Volume: 69, Issue:3
Role of glutamate and dopamine receptors in the psychopharmacological profile of the indole alkaloid psychollatine.
AID524794Antiplasmodial activity against Plasmodium falciparum GB4 after 72 hrs by SYBR green assay2009Nature chemical biology, Oct, Volume: 5, Issue:10
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.
AID361436Neuroprotective activity against Sprague-Dawley rat cortical neurons assessed as glutamate-induced LDH release at 10 uM for 1 hr before glutamate challenge measured after 24 hrs by spectrophotometry2002Journal of natural products, Nov, Volume: 65, Issue:11
Four new neuroprotective iridoid glycosides from Scrophularia buergeriana roots.
AID328116Neuroprotective activity against rat cortical cells assessed as glutamate-induced neurotoxicity by MTT assay2008Journal of natural products, Feb, Volume: 71, Issue:2
Neuroprotective limonoids of root bark of Dictamnus dasycarpus.
AID478792Neuroprotective effect against H202-induced Sprague-Dawley rat neuron injury assessed as necrotic cells by annexin V-propidium iodide staining by flow cytometry (Rvb = 1.02% +/-0.4%)2010European journal of medicinal chemistry, May, Volume: 45, Issue:5
Design, synthesis and biological evaluation of new ionone derivatives as potential neuroprotective agents in cerebral ischemia.
AID328119Neuroprotective activity against rat cortical cells at 10.0 uM assessed as glutamate-induced neurotoxicity by MTT assay2008Journal of natural products, Feb, Volume: 71, Issue:2
Neuroprotective limonoids of root bark of Dictamnus dasycarpus.
AID361434Neuroprotective activity against Sprague-Dawley rat cortical neurons assessed as glutamate-induced LDH release at 0.1 uM for 1 hr before glutamate challenge measured after 24 hrs by spectrophotometry2002Journal of natural products, Nov, Volume: 65, Issue:11
Four new neuroprotective iridoid glycosides from Scrophularia buergeriana roots.
AID361435Neuroprotective activity against Sprague-Dawley rat cortical neurons assessed as glutamate-induced LDH release at 1 uM for 1 hr before glutamate challenge measured after 24 hrs by spectrophotometry2002Journal of natural products, Nov, Volume: 65, Issue:11
Four new neuroprotective iridoid glycosides from Scrophularia buergeriana roots.
AID132658Electrophysiological responses in closed channel block to NMDA were recorded in 13-day old mouse cortical neuronal cultures.1994Journal of medicinal chemistry, Dec-23, Volume: 37, Issue:26
Identification, synthesis, and characterization of a unique class of N-methyl-D-aspartate antagonists. The 6,11-ethanobenzo[b]quinolizinium cation.
AID271562Protective effect against L-glutamate-induced neurotoxicity in rat primary cortical neurons at 1 uM by trypan blue exclusion method2006Bioorganic & medicinal chemistry letters, Oct-01, Volume: 16, Issue:19
Synthesis and neuroprotective effects of serofendic acid analogues.
AID1866391Neuroprotective effect against NMDA-induced rat PC-12 cells assessed as prevention of morphological changes at 15 uM2022Bioorganic & medicinal chemistry, 04-01, Volume: 59Synthesis of novel 1-phenyl-benzopyrrolizidin-3-one derivatives and evaluation of their cytoneuroprotective effects against NMDA-induced injury in PC12 cells.
AID1141989Antiapoptotic activity against serum deprivation-induced human SK-N-BE(2) cells assessed as viable cells at 10 uM after 36 hrs incubation by DePsipher agent relative to control2014European journal of medicinal chemistry, Jun-10, Volume: 80Polycyclic propargylamine and acetylene derivatives as multifunctional neuroprotective agents.
AID1185665Displacement of [3H]-(+)-MK-801 from NMDA receptor PCP binding site in guinea pig brain cortex membranes2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Synthesis and pharmacological evaluation of 5-pyrrolidinylquinoxalines as a novel class of peripherally restricted κ-opioid receptor agonists.
AID751860Binding affinity to human PCP receptor by radioligand displacement assay2013European journal of medicinal chemistry, May, Volume: 63Synthesis and structure-activity relationship studies in serotonin 5-HT(1A) receptor agonists based on fused pyrrolidone scaffolds.
AID145123Binding affinity was determined towards NMDA receptor using [3H]thienylcyclidine as radioligand1994Journal of medicinal chemistry, Dec-23, Volume: 37, Issue:26
Identification, synthesis, and characterization of a unique class of N-methyl-D-aspartate antagonists. The 6,11-ethanobenzo[b]quinolizinium cation.
AID707048Neuroprotective activity in human SH-SY5Y cells assessed as protection against NMDA-induced cell death after 6 hrs by MTS assay2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Combining galantamine and memantine in multitargeted, new chemical entities potentially useful in Alzheimer's disease.
AID1866390Neuroprotective activity against NMDA-induced excitotoxicity in rat PC-12 cells assessed as increase in cell viability at 15 uM pretreated for 24 hr followed by NMDA addition and measured after 6 hrs by MTT assay2022Bioorganic & medicinal chemistry, 04-01, Volume: 59Synthesis of novel 1-phenyl-benzopyrrolizidin-3-one derivatives and evaluation of their cytoneuroprotective effects against NMDA-induced injury in PC12 cells.
AID1866389Neuroprotective activity against NMDA-induced excitotoxicity in rat PC-12 cells assessed as increase in cell viability at 5 uM pretreated for 24 hr followed by NMDA addition and measured after 6 hrs by MTT assay2022Bioorganic & medicinal chemistry, 04-01, Volume: 59Synthesis of novel 1-phenyl-benzopyrrolizidin-3-one derivatives and evaluation of their cytoneuroprotective effects against NMDA-induced injury in PC12 cells.
AID524796Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green assay2009Nature chemical biology, Oct, Volume: 5, Issue:10
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.
AID710414Inhibition of radioligand binding to N-methyl D-aspartate receptor phencyclidine binding site at 10 uM2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Identification of small molecule inhibitors of amyloid β-induced neuronal apoptosis acting through the imidazoline I(2) receptor.
AID524793Antiplasmodial activity against Plasmodium falciparum Dd2 after 72 hrs by SYBR green assay2009Nature chemical biology, Oct, Volume: 5, Issue:10
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.
AID752223Binding affinity to PCP receptor (unknown origin) by radioligand displacement assay2013Bioorganic & medicinal chemistry, May-15, Volume: 21, Issue:10
Synthesis and biological evaluation of 2-(5-methyl-4-phenyl-2-oxopyrrolidin-1-yl)-acetamide stereoisomers as novel positive allosteric modulators of sigma-1 receptor.
AID478793Neuroprotective effect against H202-induced Sprague-Dawley rat neuron injury assessed as late apoptic cells by annexin V-propidium iodide staining by flow cytometry (Rvb= 2.22%+/-0.70%)2010European journal of medicinal chemistry, May, Volume: 45, Issue:5
Design, synthesis and biological evaluation of new ionone derivatives as potential neuroprotective agents in cerebral ischemia.
AID231711Ratio between closed channel blockade to open channel blockade1994Journal of medicinal chemistry, Dec-23, Volume: 37, Issue:26
Identification, synthesis, and characterization of a unique class of N-methyl-D-aspartate antagonists. The 6,11-ethanobenzo[b]quinolizinium cation.
AID132659Electrophysiological responses in open channel block to NMDA were recorded in 13-day old mouse cortical neuronal cultures.1994Journal of medicinal chemistry, Dec-23, Volume: 37, Issue:26
Identification, synthesis, and characterization of a unique class of N-methyl-D-aspartate antagonists. The 6,11-ethanobenzo[b]quinolizinium cation.
AID1141991Inhibition of NMDA receptor in Wistar rat brain synaptoneurosomes homogenate assessed as calcium flux at 100 uM after 30 mins incubation by Fura-2/AM assay2014European journal of medicinal chemistry, Jun-10, Volume: 80Polycyclic propargylamine and acetylene derivatives as multifunctional neuroprotective agents.
AID710418Inhibition of imidazole receptor 2 in mouse hippocampal neurons assessed as reduction in tPA-induced Erk1/2 activation at 30 uM pre-incubated for 4 hrs before tPA stimulation by ELISA2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Identification of small molecule inhibitors of amyloid β-induced neuronal apoptosis acting through the imidazoline I(2) receptor.
AID707049Binding affinity to NMDAR in Sprague-Dawley rat cerebral cortex homogenates2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Combining galantamine and memantine in multitargeted, new chemical entities potentially useful in Alzheimer's disease.
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.
AID707052Displacement of [3H]Ifenprodil from NMDAR-2B in Sprague-Dawley rat frontal cortex homogenates after 2 hrs by liquid scintillation counting2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Combining galantamine and memantine in multitargeted, new chemical entities potentially useful in Alzheimer's disease.
AID704017Displacement of [3H]-(+)-MK-801 from PCP binding site of NMDA receptor in pig brain cortex2012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
Enantiomerically pure 1,3-dioxanes as highly selective NMDA and σ₁ receptor ligands.
AID1141990Inhibition of voltage gated calcium channel in Wistar rat brain synaptoneurosomes homogenate assessed as intracellular calcium at 100 uM after 30 mins incubation by Fura-2/AM assay2014European journal of medicinal chemistry, Jun-10, Volume: 80Polycyclic propargylamine and acetylene derivatives as multifunctional neuroprotective agents.
AID1866387Neuroprotective activity against NMDA-induced excitotoxicity in rat PC-12 cells assessed as increase in cell viability at 20 uM pretreated for 24 hr followed by NMDA addition and measured after 6 hrs by MTT assay2022Bioorganic & medicinal chemistry, 04-01, Volume: 59Synthesis of novel 1-phenyl-benzopyrrolizidin-3-one derivatives and evaluation of their cytoneuroprotective effects against NMDA-induced injury in PC12 cells.
AID1866388Neuroprotective activity against NMDA-induced excitotoxicity in rat PC-12 cells assessed as increase in cell viability pretreated for 24 hr followed by NMDA addition and measured after 6 hrs by MTT assay2022Bioorganic & medicinal chemistry, 04-01, Volume: 59Synthesis of novel 1-phenyl-benzopyrrolizidin-3-one derivatives and evaluation of their cytoneuroprotective effects against NMDA-induced injury in PC12 cells.
AID1141992Inhibition of MAO-B in baboon liver mitochondrial fraction using MPTP substrate at 300 uM2014European journal of medicinal chemistry, Jun-10, Volume: 80Polycyclic propargylamine and acetylene derivatives as multifunctional neuroprotective agents.
AID380417Inhibition of apomorphine-induced climbing behavior in mouse at 0.2 mg/kg, ip administered 30 mins prior to apomorphine challenge2006Journal of natural products, Mar, Volume: 69, Issue:3
Role of glutamate and dopamine receptors in the psychopharmacological profile of the indole alkaloid psychollatine.
AID1533825Inhibition of voltage-dependent L-type calcium channel in human SH-SY5Y cells assessed as reduction in KCl-stimulated calcium influx at 10 uM preincubated for 30 mins in presence of Mag-Fura-2/AM dye followed by KCl stimulation and measured over 35 secs b2019European journal of medicinal chemistry, Feb-01, Volume: 163Design, synthesis and evaluation of pentacycloundecane and hexacycloundecane propargylamine derivatives as multifunctional neuroprotective agents.
AID1866384Cytotoxicity against rat PC-12 cells assessed as increase in cell viability at 5 to 20 uM incubated for 24 hrs by MTT assay2022Bioorganic & medicinal chemistry, 04-01, Volume: 59Synthesis of novel 1-phenyl-benzopyrrolizidin-3-one derivatives and evaluation of their cytoneuroprotective effects against NMDA-induced injury in PC12 cells.
AID1866392Inhibition of NMDA-induced Ca2+ influx in rat PC-12 cells assessed as reduction in intracellular Ca2+ concentration at 15 uM pretreated for 24 hr followed by NMDA addition and measured after 6 hrs by Fluo2-AM staining based fluorescence microscopic method2022Bioorganic & medicinal chemistry, 04-01, Volume: 59Synthesis of novel 1-phenyl-benzopyrrolizidin-3-one derivatives and evaluation of their cytoneuroprotective effects against NMDA-induced injury in PC12 cells.
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.
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.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
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.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
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).
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (7,517)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990226 (3.01)18.7374
1990's3317 (44.13)18.2507
2000's2340 (31.13)29.6817
2010's1384 (18.41)24.3611
2020's250 (3.33)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials9 (0.12%)5.53%
Reviews96 (1.24%)6.00%
Case Studies6 (0.08%)4.05%
Observational1 (0.01%)0.25%
Other7,629 (98.55%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]