| Name | NR2A |
|---|---|
| Synonyms | GRIN2A; Glutamate [NMDA] receptor subunit epsilon 1; Glutamate [NMDA] receptor subunit epsilon 1 precursor; N methyl D aspartate receptor subtype 2A; N methyl D aspartate receptor subunit 2A; NMDAR2A; NR2A; hNR2A… |
| 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. |
85(1,1,1,5) | 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. |
33(0,1,1,3) | 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. The competitive antagonist R-(-)-3-(2-carboxypiperazine-4-yl)-propyl-1-phosphonic acid (D-CPP), which has higher affinity to NR2A than to NR2B subunits and lowest affinity at NR2D subunits, significantly slowed down the decay rate of the afterburst EPSC while leaving the kinetics of the control current unaffected. 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 |
| 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. Replacement of the biphenyl group of PBPD with a 9-oxofluorene ring system resulted in small changes in receptor affinity and subtype selectivity. 2'-Bromo substitution on the biphenyl group of PBPD reduced antagonist affinity 3- to 5-fold at NR2A-, NR2B- and NR2D-containing receptors, but had little effect on NR2C-containing receptors. |
2(0,0,0,2) | 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. 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. |
32(0,1,1,2) | 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 |