| Name | NR2C |
|---|---|
| Synonyms | GRIN2C; Glutamate [NMDA] receptor subunit epsilon 3; Glutamate [NMDA] receptor subunit epsilon 3 precursor; N methyl D aspartate receptor subtype 2C; N methyl D aspartate receptor subunit 2C; NMDAR2C; NR2C; Glutamate [NMDA] receptor subunit epsilon 3s… |
| Name | piperazine |
|---|---|
| CAS | piperazine |
| PubMed | Abstract | RScore(About this table) | |
|---|---|---|---|
| 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. |
32(0,1,1,2) | 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. About half of vagal afferents express immunoreactivity for NR2B subunit and about half of the NR2B expressing afferents also express NR2C or NR2D subunits. 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). |
2(0,0,0,2) | 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. Of these residues, mutational analysis and modeling suggest that A414, R712, and G713 (NR2B numbering) may be especially useful for developing NR2C- and NR2D-selective NMDA receptor antagonists and that residues A414 and T428 may determine subunit variations in agonist affinity. 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. |
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 |
| 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. |
84(1,1,1,4) | 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. 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. |
164(2,2,2,4) | Details |