| Name | NMDA receptor (protein family or complex) |
|---|---|
| Synonyms | Glutamate [NMDA] receptor; Glutamate [NMDA] receptors; N methyl D aspartate receptor; N methyl D aspartate receptors; NMDA receptor; NMDA receptors |
| Name | piperazine |
|---|---|
| CAS | piperazine |
| PubMed | Abstract | RScore(About this table) | |
|---|---|---|---|
| 10755741 | Morita T, Sonoda R, Nakato K, Koshiya K, Wanibuchi F, Yamaguchi T: Phencyclidine-induced abnormal behaviors in rats as measured by the hole board apparatus. Psychopharmacology. 2000 Feb;148(3):281-8. The effects of D- (D- a coagonist of NMDA receptors, or neuroleptics, haloperidol, clozapine and on PCP-induced behavioral changes were investigated. |
1(0,0,0,1) | Details |
| 18987204 | Harney SC, Jane DE, Anwyl R: Extrasynaptic NR2D-containing NMDARs are recruited to the synapse during LTP of NMDAR-EPSCs. J Neurosci. 2008 Nov 5;28(45):11685-94. Long-term potentiation of NMDA-receptor-mediated synaptic transmission (NMDAR-LTP) is a little-understood form of plasticity. The extrasynaptic NMDARs were shown to be NR2D-containing, because the activation of extrasynaptic NMDARs by spillover was prevented by the NR2D-selective antagonists PPDA [(2R*,3S*)-1-(phenanthrenyl-2-carbonyl) piperazine-2,3-dicarboxylic acid] and UBP141. |
1(0,0,0,1) | Details |
| 15661577 | Lee HJ, Ban JY, Cho SO, Seong YH: Stimulation of 5-HT1A receptor with 8-OH-DPAT inhibits peroxide-induced neurotoxicity in cultured rat cortical cells. Pharmacol Res. 2005 Mar;51(3):261-8. H (2) O (2) produced a concentration-dependent reduction of cell viability, which was significantly reduced by (5R,10S)-(+)-5-methyl-10,11-dihydro-5H-dibenzo [a,d] cyclohepten-5,10-imine (MK-801), an (NMDA) receptor antagonist. The protective effect of 8-OH-DPAT (100 microM) was completely blocked by the simultaneous treatment of 1-(2-methoxyphenyl)-4-[4-(2-phthalimideo) butyl] piperazine (NAN-190, 10muM), a selective 5-HT (1A) receptor antagonist, but not in the presence of the receptor blocker spiperone (10 microM), indicating that the protective effect of 8-OH-DPAT was mediated via 5-HT (1A) receptors. |
1(0,0,0,1) | Details |
| 14769205 | Meng FJ, Guo J, Song B, Yan XB, Zhang GY: Competitive binding of postsynaptic density 95 and Ca2+-calmodulin dependent protein kinase II to N-methyl-D-aspartate receptor subunit 2B in rat brain. Acta Pharmacol Sin. 2004 Feb;25(2):176-80. The association-dissociation of PSD-95 and CaMKIIalpha to and from (NMDA) receptor induced by ischemia and reperfusion and the effects of 1-[N,O-bis-(5-isoquinolinesulfonyl)-N-methyl-L-tyrosyl]-4-phenyl-piperazin e (KN-62, a selective inhibitor of CaMKII) on these protein interactions were investigated. |
1(0,0,0,1) | Details |
| 17658512 | Dayanithi G, Desmadryl G, Travo C, Chabbert C, Sans A: Trimetazidine modulates AMPA/kainate receptors in rat vestibular ganglion neurons. Eur J Pharmacol. 2007 Nov 21;574(1):8-14. Epub 2007 Jul 10. Trimetazidine (1 [2,3,4-trimethoxy-benzyl] piperazine, 2 HCl) is an anti-ischemic agent frequently administered as a prophylactic treatment for episodes of angina pectoris and chorioretinal disturbances. Using Fura-2 fluorescence photometry and whole-cell patch-clamp recordings we investigated the effect of trimetazidine on the [Ca (2+)](i) and current responses induced by the application of non- (NMDA) receptor agonists on low density vestibular ganglion neuronal cultures explanted from 3 day s postnatal rats. |
1(0,0,0,1) | Details |
| 11595362 | Houston GC, Papadakis NG, Carpenter TA, Hall LD, Mukherjee B, James MF, Huang CL: Mapping of brain activation in response to pharmacological agents using fMRI in the rat. Magn Reson Imaging. 2001 Sep;19(7):905-19. The effects of dizocilpine (MK-801) an N-methyl-D-aspartate receptor antagonist and m-chlorophenylpiperazine (mCPP), a 5-HT (2b/2c)-receptor agonist on rat brain activity were investigated over a time interval of about 1 h and the results were compared to published utilisation and cerebral blood flow data. |
1(0,0,0,1) | Details |
| 18822964 | Li JQ, Huang LY, Chen XJ, Weng ZJ, Zhang CN: [Synthesis and central none-opioid analgesic activity of SIPI5047] . Yao Xue Xue Bao. 2008 Jun;43(6):611-8. Compound SIPI5047 was synthesize by using piperazine as starting material in five reaction steps, and its central none-opioid analgesic activity was studied. |
0(0,0,0,0) | Details |
| 14718249 | Feng B, Tse HW, Skifter DA, Morley R, Jane DE, Monaghan DT: Structure-activity analysis of a novel NR2C/NR2D-preferring NMDA receptor antagonist: 1-(phenanthrene-2-carbonyl) piperazine-2,3-dicarboxylic acid. Br J Pharmacol. 2004 Feb;141(3):508-16. Epub 2004 Jan 12. (2S*,3R*)-1-(biphenyl-4-carbonyl) piperazine-2,3-dicarboxylic acid (PBPD) is a moderate affinity, competitive (NMDA) receptor antagonist with an atypical pattern of selectivity among NMDA receptor 2 subunit (NR2) subunits. |
197(2,3,3,7) | Details |
| 19684252 | Costa BM, Feng B, Tsintsadze TS, Morley RM, Irvine MW, Tsintsadze V, Lozovaya NA, Jane DE, Monaghan DT: (NMDA) receptor NR2 subunit selectivity of a series of novel piperazine-2,3-dicarboxylate derivatives: preferential blockade of extrasynaptic NMDA receptors in the rat hippocampal CA3-CA1 synapse. J Pharmacol Exp Ther. 2009 Nov;331(2):618-26. Epub 2009 Aug 14. |
117(1,2,2,7) | Details |
| 17556637 | Wang D, Noda Y, Tsunekawa H, Zhou Y, Miyazaki M, Senzaki K, Nitta A, Nabeshima T: Role of N-methyl-D-aspartate receptors in antidepressant-like effects of sigma 1 receptor agonist 1-(3,4-dimethoxyphenethyl)-4-(3-phenylpropyl) piperazine dihydrochloride (SA-4503) in olfactory bulbectomized rats. J Pharmacol Exp Ther. 2007 Sep;322(3):1305-14. Epub 2007 Jun 7. |
64(0,2,2,4) | Details |
| 15801853 | Morley RM, Tse HW, Feng B, Miller JC, Monaghan DT, Jane DE: Synthesis and pharmacology of N1-substituted piperazine-2,3-dicarboxylic acid derivatives acting as NMDA receptor antagonists. J Med Chem. 2005 Apr 7;48(7):2627-37. |
63(0,2,2,3) | Details |
| 20007479 | Li YC, Xi D, Roman J, Huang YQ, Gao WJ: Activation of glycogen synthase kinase-3 beta is required for hyperdopamine and D2 receptor-mediated inhibition of synaptic NMDA receptor function in the rat prefrontal cortex. J Neurosci. 2009 Dec 9;29(49):15551-63. Here, we show the signaling pathways involved in hyperdopaminergic regulation of NMDA receptor functions in the prefrontal cortex by incubating cortical slices with high concentration of or administering reuptake inhibitor 1-(2-[bis-(4-fluorophenyl) methoxy] ethyl)- 4-(3-phenylpropyl) piperazine (GBR12909) in vivo. |
35(0,1,1,5) | Details |
| 19193935 | Guard DB, Swartz TD, Ritter RC, Burns GA, Covasa M: Blockade of hindbrain NMDA receptors containing NR2 subunits increases intake. Am J Physiol Regul Integr Comp Physiol. 2009 Apr;296(4):R921-8. Epub 2009 Feb 4. To test this, we measured deprivation-induced intake of 15% solution following fourth ventricle and intra-nucleus of the solitary tract (intra-NTS) injections of Conantokin G (Con G; NR2B blocker), d-3-(2-carboxypiperazin-4-yl)-1-propenyl-1- (d-CPPene; NR2B/2A blocker), and (+/-)-cis-1-(phenanthren-2yl-carbonyl) piperazine-2,3-dicarboxylic acid (PPDA; NR2D/C blocker). |
5(0,0,0,5) | Details |
| 16632817 | Eger EI 2nd, Liao M, Laster MJ, Won A, Popovich J, Raines DE, Solt K, Dutton RC, Cobos FV 2nd, Sonner JM: Contrasting roles of the N-methyl-D-aspartate receptor in the production of immobilization by conventional and aromatic anesthetics. Anesth Analg. 2006 May;102(5):1397-406. To test this hypothesis, we measured the effect of IV infusion of the blockers dizocilpine (MK-801) and (R)-4-(3-phosphonopropyl) piperazine-2-carboxylic acid (CPP) to decrease the MAC (the minimum alveolar concentration of anesthetic that prevents movement in 50% of subjects given a noxious stimulation) of 8 conventional anesthetics (cyclopropane, desflurane, enflurane, halothane, isoflurane, nitrous oxide, sevoflurane, and xenon) and 8 aromatic compounds fluorobenzene, o-difluorobenzene, p-difluorobenzene, 1,2,4-trifluorobenzene, 1,3,5-trifluorobenzene, pentafluorobenzene, and hexafluorobenzene) and, for comparison, etomidate. |
4(0,0,0,4) | Details |
| 19816675 | Hoque KE, Indorkar RP, Sammut S, West AR: Impact of - interactions on striatal neuronal nitric oxide synthase activity. Psychopharmacology. 2010 Jan;207(4):571-81. Epub 2009 Oct 9. RESULTS: Administration of the neuronal NOS inhibitor N (G)-propyl- (NPA), the D1 receptor antagonist SCH 23390, and the NMDA receptor antagonist 3-phosphonopropyl-piperazine-2-carboxylic acid (CPP) all attenuated staining selectively in the striatum. |
34(0,1,1,4) | Details |
| 15721167 | Feng B, Morley RM, Jane DE, Monaghan DT: The effect of competitive antagonist chain length on NMDA receptor subunit selectivity. Neuropharmacology. 2005 Mar;48(3):354-9. Epub 2005 Jan 25. For example (R)-CPP displayed a 50-fold difference in affinity between NR2A-containing and NR2D-containing NMDA receptors, while the shorter chain homologue 4-(phosphonomethyl) piperazine-2-carboxylic acid (PMPA) displayed only a 5-fold variation in affinity. |
33(0,1,1,3) | Details |
| 12941378 | Ayala GX, Tapia R: Expression of heat shock protein 70 induced by 4-aminopyridine through -mediated excitotoxic stress in rat hippocampus in vivo. Neuropharmacology. 2003 Oct;45(5):649-60. The (NMDA) receptor antagonists MK-801 and (3-phosphonopropyl)-piperazine-2-carboxylic acid prevented the seizures, the neurodegeneration and the expression of HSP70. |
31(0,1,1,1) | Details |
| 18789952 | Ayala GX, Tapia R: HSP70 expression protects against hippocampal neurodegeneration induced by endogenous in vivo. Neuropharmacology. 2008 Dec;55(8):1383-90. Epub 2008 Sep 9. All these effects of 4-AP are prevented by the NMDA receptor antagonists 3-phosphonopropyl-piperazine-2-carboxilic acid (CPP) and (+) 5-methyl-10,11-dyhydro-5H-dibenzo (a,d) cyclohepten-5,10-imine (MK-801), indicating that they are due to NMDA receptor overactivation by excessive extracellular synaptic |
31(0,1,1,1) | Details |
| 19394821 | Nguyen KT, Luethi E, Syed S, Urwyler S, Bertrand S, Bertrand D, Reymond JL: 3-(aminomethyl) piperazine-2,5-dione as a novel site inhibitor from the chemical universe database GDB. Bioorg Med Chem Lett. 2009 Jul 15;19(14):3832-5. Epub 2009 Apr 10. Docking of randomly selected compounds from the chemical universe database GDB-11, which contains all organic molecules up to 11 atoms of C, N, O, F possible under consideration of simple chemical stability and synthetic feasibility rules, into the NMDA receptor site (1pb7.pdb) lead to the identification of 3-(aminomethyl) piperazine-2,5-dione 3 and its close analog 5-(aminomethyl) piperazine-2,3-dione 4 as possible new ligands for this drug target, which is implicated in synaptic plasticity, neuronal development, learning and memory. |
31(0,1,1,1) | Details |
| 15742360 | D'Antuono M, de Guzman P, Kano T, Avoli M: Ripple activity in the dentate gyrus of dishinibited hippocampus-entorhinal cortex slices. J Neurosci Res. 2005 Apr 1;80(1):92-103. Ripples, which were also recorded in "minislices" only of the dentate gyrus, were unaffected by application of the mu-opioid receptor agonist (D-Ala2-N-Me-Phe,Gly-ol) enkephalin (10 microM; n = 6) or the (NMDA) receptor antagonist 3-(2-carboxy-piperazine-4-yl)-propyl-l-phosphonate (10 microM; n = 5). |
31(0,1,1,1) | Details |
| 15743930 | Kinarsky L, Feng B, Skifter DA, Morley RM, Sherman S, Jane DE, Monaghan DT: Identification of subunit- and antagonist-specific amino acid residues in the N-Methyl-D-aspartate receptor -binding pocket. J Pharmacol Exp Ther. 2005 Jun;313(3):1066-74. Epub 2005 Mar 2. To test the predictive value of these models, all four stereoisomers of the antagonist 1-(phenanthren-2-carbonyl) piperazine-2,3-dicarboxylic acid (PPDA) were docked into the NR2B -binding site model. |
3(0,0,0,3) | Details |
| 16307611 | Guitton MJ, Pujol R, Puel JL: m-Chlorophenylpiperazine exacerbates perception of -induced tinnitus in rats. Eur J Neurosci. 2005 Nov;22(10):2675-8. The demonstration that cochlear NMDA receptor blockade abolishes the exacerbated perception of tinnitus is highly relevant in terms of treatment. |
2(0,0,0,2) | Details |
| 16682960 | Kim HW, Kwon YB, Roh DH, Yoon SY, Han HJ, Kim KW, Beitz AJ, Lee JH: Intrathecal treatment with sigma1 receptor antagonists reduces formalin-induced phosphorylation of NMDA receptor subunit 1 and the second phase of formalin test in mice. Br J Pharmacol. 2006 Jun;148(4):490-8. Epub 2006 May 8. |
2(0,0,0,2) | Details |
| 15051155 | Husson I, Mesples B, Medja F, Leroux P, Kosofsky B, Gressens P: Methylphenidate and MK-801, an N-methyl-d-aspartate receptor antagonist: shared biological properties. Neuroscience. 2004;125(1):163-70. |
2(0,0,0,2) | Details |
| 15146049 | Lozovaya NA, Grebenyuk SE, Tsintsadze TSh, Feng B, Monaghan DT, Krishtal OA: Extrasynaptic NR2B and NR2D subunits of NMDA receptors shape 'superslow' afterburst EPSC in rat hippocampus. J Physiol. 2004 Jul 15;558(Pt 2):451-63. Epub 2004 May 14. In contrast, ifenprodil, a highly selective NR2B antagonist, and [+/-]-cis-1-[phenanthren-2yl-carbonyl] piperazine-2,3-dicarboxylic acid (PPDA), a competitive antagonist that is moderately selective for NR2D subunits, more strongly inhibited the late component of the afterburst EPSC |
2(0,0,0,2) | Details |
| 16307739 | Bennett S, Gronier B: Modulation of striatal release in vitro by agonists of the glycineB site of NMDA receptors; interaction with antipsychotics. Eur J Pharmacol. 2005 Dec 19;527(1-3):52-9. Epub 2005 Nov 22. The effect of on spontaneous release was abolished by the non-competitive antagonists 5R,10S-(+)-5-methyl-10,11-dihydro-5H-dibenzo [a,d] cyclohepten-5,10-imine (MK-801, 10 microM) and ifenprodil (5 microM), but was only partially suppressed by the competitive antagonist 4-(3-phosphonopropyl)-piperazine-2-carboxylic acid (CPP, 10 microM). |
2(0,0,0,2) | Details |
| 19911010 | Baron A, Montagne A, Casse F, Launay S, Maubert E, Ali C, Vivien D: NR2D-containing NMDA receptors mediate tissue plasminogen activator-promoted neuronal excitotoxicity. Cell Death Differ. 2009 Nov 13. We show that tPA-mediated signalling and neurotoxicity through the NMDAR are blocked by co-application of an NR2D antagonist (phenanthrene derivative (2S (*), 3R (*))-1-(phenanthrene-2-carbonyl) piperazine-2,3-dicarboxylic acid, PPDA) or knockdown of neuronal NR2D expression. |
2(0,0,0,2) | Details |
| 19799710 | Park DJ, West AR: Regulation of striatal synthesis by local and interactions. J Neurochem. 2009 Dec;111(6):1457-65. Epub 2009 Oct 3. To study the impact of local manipulations of D1/5 and glutamatergic NMDA receptors on striatal nNOS activity, we combined the techniques of in vivo amperometry and reverse microdialysis. NO efflux elicited by systemic administration of SKF-81297 was blocked following intrastriatal infusion of: (i) the D1/5 receptor antagonist SCH-23390, (ii) the nNOS inhibitor 7-nitroindazole, (iii) the non-specific ionotropic glutamate receptor antagonist and (iv) the selective NMDA receptor antagonist 3-phosphonopropyl-piperazine-2-carboxylic acid. |
1(0,0,0,1) | Details |
| 12486804 | Tsai CL, Wang LH, Tsai CC: Role of and in the behavioral thermoregulation of female tilapia during the prespawning phase. J Exp Zool. 2002 Oct 1;293(5):443-9. This effect was mimicked by the agonist of 5-HT1A, 1B, and 2C receptors, N-3-trifluoromethylphenyl piperazine. Both agonist and antagonist of and MK-801 (1.0 x 10 (-6) M), a noncompetitive blocker of NMDA receptor, significantly decreased the preferred temperature. |
1(0,0,0,1) | Details |
| 11182540 | Noda A, Noda Y, Kamei H, Ichihara K, Mamiya T, Nagai T, Sugiura S, Furukawa H, Nabeshima T: Phencyclidine impairs latent learning in mice: interaction between glutamatergic systems and sigma (1) receptors. Neuropsychopharmacology. 2001 Apr;24(4):451-60. When PCP (1mg/kg i.p.) was administered before the training trial, the finding latency was significantly prolonged in comparison with that in the saline-treated mice, indicating that PCP induced impairment of latent learning. 1-(3,4-Dimethoxy-phenethyl)-4-(3-phenylpropyl) piperazine dihydrochloride (SA4503: 0.3 mg/kg s.c.) and (+)-pentazocine (1 mg/kg s.c.), selective sigma (1) receptor agonists, or D-cycloserine (10 and 30mg/kg, s.c.), a binding site agonist, significantly counteracted the PCP-induced impairment of latent learning, whereas (+)-SKF-10,047 (0.1-3 mg/kg s.c.), a putative sigma (1) receptor agonist, did not. SA4503 also ameliorated the impairment of latent learning induced by dizocilpine, a non-competitive N-methyl-D-aspartate receptor antagonist, the effect being antagonized by NE-100. |
1(0,0,0,1) | Details |
| 12177685 | Hoerr R, Noeldner M: Ensaculin (KA-672 HCl): a multitransmitter approach to dementia treatment. CNS Drug Rev. 2002 Summer;8(2):143-58. Ensaculin, a novel benzopyranone substituted with a piperazine moiety, showed memory-enhancing effects in paradigms of passive and conditioned avoidance in both normal and artificially amnesic rodents. The compound could be characterized as a weak NMDA receptor-operated channel blocker. |
1(0,0,0,1) | Details |