| Name | NR2B |
|---|---|
| Synonyms | GRIN2B; Glutamate [NMDA] receptor subunit epsilon 2; Glutamate [NMDA] receptor subunit epsilon 2 precursor; N methyl D aspartate receptor subtype 2B; N methyl D aspartate receptor subunit 2B; N methyl D aspartate receptor subunit 3; NMDAR2B; NR2B… |
| Name | piperazine |
|---|---|
| CAS | piperazine |
| PubMed | Abstract | RScore(About this table) | |
|---|---|---|---|
| 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. The competitive NMDA receptor antagonist (2R,3S)-(1-biphenylyl-4-carbonyl) piperazine-2,3-dicarboxylic acid (PBPD, 16b) displays an unusual selectivity with improved relative affinity for NR2C and NR2D vs NR2A and NR2B. |
84(1,1,1,4) | 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 |
36(0,1,1,6) | 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. Whereas most binding site antagonists display a common pattern of NR2 selectivity, NR2A > NR2B > NR2C > NR2D (high to low affinity), (2S*,3R*)-1-(phenanthrene-2-carbonyl) piperazine-2,3-dicarboxylic acid (PPDA) has a low selectivity for NR2C- and NR2D-containing NMDA receptors. |
34(0,1,1,4) | 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). |
9(0,0,1,4) | 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. 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. Further studies using selective antagonists for NR2A- and NR2B-containing NMDARs demonstrated that synaptic NMDARs are predominantly NR2A-containing and NR2B-containing receptors, whereas the extrasynaptic NMDARs are complex multimeric receptors with NR2A, NR2B, or NR2D subunits. |
1(0,0,0,1) | 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. The widely-used (NMDA) receptor antagonists (R)-4-(3-phosphonopropyl) piperazine-2-carboxylic acid ((R)-CPP) and (R)-2-amino-7-phosphonoheptanoate ((R)-AP7) are frequently used as general NMDA receptor antagonists and assumed not to display significant selectivity among NMDA receptor NR2 subunits. All antagonists displayed the potency order (high to low affinity) of NR2A > NR2B > NR2C > NR2D, however the longer chain antagonists (having 7 instead of 5 bond lengths between acidic groups) displayed much greater subunit selectivity than their short-chain homologues. |
1(0,0,0,1) | 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. Moreover, the hyperdopamine induced by GBR12909 significantly decreased the expression of both surface and intracellular NR2B proteins, as well as NR2B mRNA levels, suggesting an inhibition of protein synthesis. |
1(0,0,0,1) | 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. |
34(0,1,1,4) | 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. |
4(0,0,0,4) | 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. At recombinant receptors, PPDA displayed a 16-fold (NR2B) to 94-fold (NR2C) increase in affinity over PBPD. |
2(0,0,0,2) | 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. |
0(0,0,0,0) | Details |