Target Validation Information
Target ID T76414
Target Name Glutamate [NMDA] receptor subunit epsilon 2
Target Type
Clinical Trial
Drug Potency against Target TRANSTORINE Drug Info IC50 = 16000 nM [531421]
L-695902 Drug Info IC50 = 6500 nM
4-Chloro-3-hydroxy-1H-quinolin-2-one Drug Info IC50 = 1400 nM
4,5,7-Trichloro-3-hydroxy-1H-quinolin-2-one Drug Info IC50 = 4500 nM
5,7-Dichloro-4-hydroxy-3-phenyl-1H-quinolin-2-one Drug Info IC50 = 97 nM
RPR-104632 Drug Info IC50 = 8.3 nM [525816]
4-Phosphonomethyl-piperidine-2-carboxylic acid Drug Info IC50 = 452 nM [533067]
4-Bromo-5,7-dichloro-3-hydroxy-1H-quinolin-2-one Drug Info IC50 = 2800 nM
7-chloro-3-hydroxyquinazoline-2,4-dione Drug Info Ki = 240 nM [528453]
Phe-Pro-Glu Drug Info Ki = 4850 nM [527903]
Nle-Pro-Glu Drug Info Ki = 19500 nM [527903]
N,N'-Bis-(4-hexyl-phenyl)-guanidine Drug Info IC50 = 7790 nM [534685]
L-701324 Drug Info Ki = 1.4 nM [527994]
(R)-2-Amino-5-phosphono-pentanoic acid Drug Info Ki = 280 nM [527496]
Phenethyl-(3-phenyl-propyl)-amine Drug Info IC50 = 7300 nM [534696]
Phenethyl-(4-phenyl-butyl)-amine Drug Info IC50 = 3500 nM [534696]
Conantokin-R Drug Info IC50 = 1000 nM [529118]
8-Fluoro-3-hydroxy-1H-benzo[b]azepine-2,5-dione Drug Info IC50 = 490 nM [534270]
6,7-Dichloro-3-hydroxy-1H-quinazoline-2,4-dione Drug Info IC50 = 430 nM [527036]
8-Ethyl-3-hydroxy-1H-benzo[b]azepine-2,5-dione Drug Info IC50 = 5100 nM [534270]
6-Chloro-1,4-dihydro-quinoxaline-2,3-dione Drug Info IC50 = 1800 nM [534504]
Conantokin-G Drug Info IC50 = 100 nM [529118]
PHENCYCLIDINE Drug Info IC50 = 9.8 nM [534286]
5,7-Dinitro-1,4-dihydro-quinoxaline-2,3-dione Drug Info IC50 = 170 nM
Benzyl 4-aminobutyl(3-aminopropyl)carbamate Drug Info IC50 = 17600 nM [528098]
2-(4-Phenoxy-benzyl)-1H-benzoimidazole Drug Info Ki = 260 nM [527020]
6-Methoxy-2-(4-phenoxy-benzyl)-1H-benzoimidazole Drug Info Ki = 8400 nM [527020]
2-(4-benzyl-piperidin-1-ylmethyl)-1H-indol-6-ol Drug Info IC50 = 1158 nM [528664]
4-(3,4-Dihydro-1H-isoquinolin-2-yl)-quinoline Drug Info Ki = 29 nM [526618]
N-(2-methoxybenzyl)cinnamamidine Drug Info IC50 = 6.6 nM [527787]
AP-7 Drug Info IC50 = 390 nM [526787]
7-Chloro-3-nitro-3,4-dihydro-1H-quinolin-2-one Drug Info IC50 = 410 nM
2-Methylamino-succinic acid(NMDA) Drug Info IC50 = 6000 nM [531531]
N-(3-phenethoxybenzyl)-4-hydroxybenzamide Drug Info Ki = 5.6 nM [529014]
RPR-118723 Drug Info IC50 = 28 nM [525816]
N-(4-(benzyloxy)phenethyl)pyridin-4-amine Drug Info IC50 = 102 nM [528635]
N,N'-Bis-(4-sec-butyl-phenyl)-guanidine Drug Info IC50 = 10100 nM [534685]
GLUTAMATE Drug Info IC50 = 70 nM [526787]
Ala-Pro-Glu Drug Info Ki = 2660 nM [527903]
Gly-Hyp-Glu Drug Info Ki = 9240 nM [527903]
Gly-Pip-Glu Drug Info Ki = 2390 nM [527903]
N,N'-Bis-(4-isopropyl-phenyl)-guanidine Drug Info IC50 = 17900 nM [534685]
H-Gly-D-dmP-Glu-OH Drug Info Ki = 330 nM [528176]
L-687414 Drug Info IC50 = 2700 nM
3-phenyl-4-hydroxyquinolin-2(1H)-one Drug Info Ki = 12200 nM [527994]
4-Benzyl-1-(2-phenoxy-ethyl)-piperidine Drug Info IC50 = 630 nM [525548]
N,N'-Bis-(4-butyl-phenyl)-guanidine Drug Info IC50 = 3320 nM [534685]
4-[2-(3-Phenyl-propylamino)-ethyl]-phenol Drug Info IC50 = 96 nM [534696]
4-[2-(6-Phenyl-hexylamino)-ethyl]-phenol Drug Info IC50 = 35 nM [534696]
4-[2-(5-Phenyl-pentylamino)-ethyl]-phenol Drug Info IC50 = 8 nM [534696]
2-(4-Phenoxy-benzyl)-3H-benzoimidazol-4-ol Drug Info Ki = 140 nM [527020]
6-Nitro-2-(4-phenoxy-benzyl)-1H-benzoimidazole Drug Info Ki = 5400 nM [527020]
6-Nitro-1,4-dihydro-quinoxaline-2,3-dione Drug Info IC50 = 3800 nM [534504]
8-Chloro-3-hydroxy-1H-benzo[b]azepine-2,5-dione Drug Info IC50 = 13 nM [534270]
4-[3-(5-Phenyl-pentylamino)-propyl]-phenol Drug Info IC50 = 45 nM [534696]
5,7-Dichloro-3-hydroxy-1H-quinazoline-2,4-dione Drug Info IC50 = 750 nM [527036]
3-Hydroxy-8-methyl-1H-benzo[b]azepine-2,5-dione Drug Info IC50 = 130 nM [534270]
4-[2-(4-Benzyl-piperidin-1-yl)-ethoxy]-phenol Drug Info IC50 = 25 nM [525548]
DNQX Drug Info IC50 = 4500 nM [529309]
4-[3-(4-Phenyl-butylamino)-propyl]-phenol Drug Info IC50 = 20 nM [525527]
Gly-b7Pro-Glu Drug Info Ki = 480 nM [527903]
Besonprodil Drug Info IC50 = 6.6 nM [528259]
L-698532 Drug Info Ki = 151 nM [527994]
4-hydroxy-5-phenylthieno[2,3-b]pyridin-6(7H)-one Drug Info Ki = 16400 nM [527994]
4-[2-(4-Phenyl-piperidin-1-yl)-ethoxy]-phenol Drug Info IC50 = 7700 nM [525548]
Gly-Amp-Glu Drug Info Ki = 15540 nM [527903]
(D)-Ala-Pro-Glu Drug Info Ki = 5400 nM [527903]
4,6-Dichloro-1H-indole-2-carboxylic acid Drug Info IC50 = 6000 nM [531421]
N,N'-Bis-(4-butoxy-phenyl)-guanidine Drug Info IC50 = 3480 nM [534685]
H-Gly-dmP-Glu-OH Drug Info Ki = 3790 nM [528176]
N,N'-Bis-(4-ethyl-phenyl)-guanidine Drug Info IC50 = 7910 nM [534685]
DITOLYLGUANIDINE Drug Info IC50 = 10200 nM [534685]
4-{2-[Ethyl-(4-phenyl-butyl)-amino]-ethyl}-phenol Drug Info IC50 = 300 nM [534696]
4-Benzyl-1-phenethyl-piperidine hydrochloride Drug Info IC50 = 1100 nM [534696]
2-(4-Phenoxy-benzyl)-3H-benzoimidazol-5-ylamine Drug Info Ki = 180 nM [527020]
4-[2-(4-Phenyl-butylamino)-ethyl]-phenol Drug Info IC50 = 43 nM [534696]
ELIPRODIL Drug Info IC50 = 1400 nM [525548]
3-Hydroxy-7-nitro-1H-benzo[b]azepine-2,5-dione Drug Info IC50 = 12000 nM [534270]
8-Bromo-3-hydroxy-1H-benzo[b]azepine-2,5-dione Drug Info IC50 = 79 nM [534270]
2-(4-Phenoxy-benzyl)-3H-benzoimidazol-5-ol Drug Info Ki = 3.2 nM [527020]
3-Benzoyl-7-chloro-4-hydroxy-1H-quinolin-2-one Drug Info IC50 = 3200 nM
4-[2-(4-Phenyl-butoxy)-ethyl]-phenol Drug Info IC50 = 3700 nM [534696]
(R)-2-Amino-7-phosphono-heptanoic acid Drug Info Ki = 640 nM [527496]
YM-90K Drug Info IC50 = 10400 nM [525786]
DIZOCILPINE Drug Info Ki = 2.2 nM [533655]
3-Hydroxy-1H-benzo[b]azepine-2,5-dione Drug Info IC50 = 830 nM [534270]
H-Gly-PMe-Glu-OH Drug Info Ki = 7960 nM [528176]
2-Pyridin-4-yl-1,2,3,4-tetrahydro-isoquinoline Drug Info Ki = 8 nM [526618]
MDL-105519 Drug Info IC50 = 157 nM [527438]
3-Hydroxy-6-methyl-1H-benzo[b]azepine-2,5-dione Drug Info IC50 = 13000 nM [534270]
NBQX Drug Info IC50 = 200 nM [526134]
The Effect of Target Knockout, Knockdown or Genetic Variations We investigated the effect of intrathecal (i.t.) injection of siRNAs targeting NMDA-R2B receptor subunit protein (NR2B) receptors, a subunit of NMDA receptor, for the modulationof pain. The results indicate that the use of siRNA targeting the NR2B subunit not only decreased the expression of NR2B mRNA and its associated protein, as demonstrated by real-time PCR and Western blotting, but also abolished formalin-induced pain behaviors in rat model. The peak effect occurred on day 3 for mRNA and day 7 for its protein, following i.t. injection of 5 microg of siRNA-NR2B. These data prove the feasibility of i.t. siRNAs in the investigation of functional gene expression in the context of whole animal behavior for the management of chronic pain. [531421]
References
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Ref 525816J Med Chem. 2000 Jun 15;43(12):2371-81.Indeno[1,2-b]pyrazin-2,3-diones: a new class of antagonists at the glycine site of the NMDA receptor with potent in vivo activity.
Ref 533067J Med Chem. 1989 Sep;32(9):2171-8.4-(Phosphonoalkyl)- and 4-(phosphonoalkenyl)-2-piperidinecarboxylic acids: synthesis, activity at N-methyl-D-aspartic acid receptors, and anticonvulsant activity.
Ref 528453J Med Chem. 2006 Oct 5;49(20):6015-26.Structural investigation of the 7-chloro-3-hydroxy-1H-quinazoline-2,4-dione scaffold to obtain AMPA and kainate receptor selective antagonists. Synthesis, pharmacological, and molecular modeling studies.
Ref 527903Bioorg Med Chem Lett. 2006 Mar 1;16(5):1392-6.New Gly-Pro-Glu (GPE) analogues: expedite solid-phase synthesis and biological activity.
Ref 527903Bioorg Med Chem Lett. 2006 Mar 1;16(5):1392-6.New Gly-Pro-Glu (GPE) analogues: expedite solid-phase synthesis and biological activity.
Ref 534685J Med Chem. 1998 Aug 13;41(17):3298-302.Synthesis and pharmacological evaluation of N,N'-diarylguanidines as potent sodium channel blockers and anticonvulsant agents.
Ref 527994J Med Chem. 2006 Feb 9;49(3):864-71.Synthesis of thieno[2,3-b]pyridinones acting as cytoprotectants and as inhibitors of [3H]glycine binding to the N-methyl-D-aspartate (NMDA) receptor.
Ref 527496J Med Chem. 2005 Apr 7;48(7):2627-37.Synthesis and pharmacology of N1-substituted piperazine-2,3-dicarboxylic acid derivatives acting as NMDA receptor antagonists.
Ref 534696J Med Chem. 1998 Aug 27;41(18):3499-506.Structure-activity relationships for a series of bis(phenylalkyl)amines: potent subtype-selective inhibitors of N-methyl-D-aspartate receptors.
Ref 534696J Med Chem. 1998 Aug 27;41(18):3499-506.Structure-activity relationships for a series of bis(phenylalkyl)amines: potent subtype-selective inhibitors of N-methyl-D-aspartate receptors.
Ref 529118J Biol Chem. 2007 Dec 21;282(51):36905-13. Epub 2007 Oct 25.Novel conantokins from Conus parius venom are specific antagonists of N-methyl-D-aspartate receptors.
Ref 534270J Med Chem. 1996 Nov 8;39(23):4643-53.Analogs of 3-hydroxy-1H-1-benzazepine-2,5-dione: structure-activity relationship at N-methyl-D-aspartate receptor glycine sites.
Ref 527036Bioorg Med Chem Lett. 2004 May 3;14(9):2345-9.3-hydroxy-quinazoline-2,4-dione as a useful scaffold to obtain selective Gly/NMDA and AMPA receptor antagonists.
Ref 534270J Med Chem. 1996 Nov 8;39(23):4643-53.Analogs of 3-hydroxy-1H-1-benzazepine-2,5-dione: structure-activity relationship at N-methyl-D-aspartate receptor glycine sites.
Ref 534504J Med Chem. 1997 Oct 24;40(22):3679-86.5-(N-oxyaza)-7-substituted-1,4-dihydroquinoxaline-2,3-diones: novel, systemically active and broad spectrum antagonists for NMDA/glycine, AMPA, and kainate receptors.
Ref 529118J Biol Chem. 2007 Dec 21;282(51):36905-13. Epub 2007 Oct 25.Novel conantokins from Conus parius venom are specific antagonists of N-methyl-D-aspartate receptors.
Ref 534286J Med Chem. 1996 Nov 22;39(24):4844-52.Synthesis and biological activity of conformationally restricted analogs of milnacipran: (1S,2R)-1-phenyl-2-[(S)-1-aminopropyl]-N,N-diethylcyclopropanecarboxamide, an efficient noncompetitive N-methyl-D-aspartic acid receptor antagonist.
Ref 528098Bioorg Med Chem Lett. 2006 Jun 1;16(11):2837-41. Epub 2006 Mar 24.Polyamines and the NMDA receptor: modifying intrinsic activities with aromatic substituents.
Ref 527020J Med Chem. 2004 Apr 8;47(8):2089-96.NR2B-selective N-methyl-D-aspartate antagonists: synthesis and evaluation of 5-substituted benzimidazoles.
Ref 527020J Med Chem. 2004 Apr 8;47(8):2089-96.NR2B-selective N-methyl-D-aspartate antagonists: synthesis and evaluation of 5-substituted benzimidazoles.
Ref 528664J Med Chem. 2007 Mar 8;50(5):901-14. Epub 2007 Feb 10.Selective NR1/2B N-methyl-D-aspartate receptor antagonists among indole-2-carboxamides and benzimidazole-2-carboxamides.
Ref 526618Bioorg Med Chem Lett. 2003 May 19;13(10):1759-62.4-(3,4-dihydro-1H-isoquinolin-2yl)-pyridines and 4-(3,4-dihydro-1H-isoquinolin-2-yl)-quinolines as potent NR1/2B subtype selective NMDA receptor antagonists.
Ref 527787Bioorg Med Chem Lett. 2005 Dec 15;15(24):5439-41. Epub 2005 Oct 5.Indole-2-carboxamidines as novel NR2B selective NMDA receptor antagonists.
Ref 526787J Med Chem. 1992 Dec 11;35(25):4720-6.Bioisosteric replacement of the alpha-amino carboxylic acid functionality in 2-amino-5-phosphonopentanoic acid yields unique 3,4-diamino-3-cyclobutene-1,2-dione containing NMDA antagonists.
Ref 531531J Med Chem. 1990 Oct;33(10):2772-7.2,4-Dihydro-3H-1,2,4-triazol-3-ones as anticonvulsant agents.
Ref 529014Bioorg Med Chem Lett. 2007 Oct 15;17(20):5537-42. Epub 2007 Aug 19.Structure-activity relationship study of novel NR2B-selective antagonists with arylamides to avoid reactive metabolites formation.
Ref 525816J Med Chem. 2000 Jun 15;43(12):2371-81.Indeno[1,2-b]pyrazin-2,3-diones: a new class of antagonists at the glycine site of the NMDA receptor with potent in vivo activity.
Ref 528635J Med Chem. 2007 Feb 22;50(4):807-19. Epub 2007 Jan 24.Identification and characterization of 4-methylbenzyl 4-[(pyrimidin-2-ylamino)methyl]piperidine-1-carboxylate, an orally bioavailable, brain penetrant NR2B selective N-methyl-D-aspartate receptor antagonist.
Ref 534685J Med Chem. 1998 Aug 13;41(17):3298-302.Synthesis and pharmacological evaluation of N,N'-diarylguanidines as potent sodium channel blockers and anticonvulsant agents.
Ref 526787J Med Chem. 1992 Dec 11;35(25):4720-6.Bioisosteric replacement of the alpha-amino carboxylic acid functionality in 2-amino-5-phosphonopentanoic acid yields unique 3,4-diamino-3-cyclobutene-1,2-dione containing NMDA antagonists.
Ref 527903Bioorg Med Chem Lett. 2006 Mar 1;16(5):1392-6.New Gly-Pro-Glu (GPE) analogues: expedite solid-phase synthesis and biological activity.
Ref 527903Bioorg Med Chem Lett. 2006 Mar 1;16(5):1392-6.New Gly-Pro-Glu (GPE) analogues: expedite solid-phase synthesis and biological activity.
Ref 527903Bioorg Med Chem Lett. 2006 Mar 1;16(5):1392-6.New Gly-Pro-Glu (GPE) analogues: expedite solid-phase synthesis and biological activity.
Ref 534685J Med Chem. 1998 Aug 13;41(17):3298-302.Synthesis and pharmacological evaluation of N,N'-diarylguanidines as potent sodium channel blockers and anticonvulsant agents.
Ref 528176Bioorg Med Chem Lett. 2006 Jul 1;16(13):3396-400. Epub 2006 May 2.The neuroprotective activity of GPE tripeptide analogues does not correlate with glutamate receptor binding affinity.
Ref 527994J Med Chem. 2006 Feb 9;49(3):864-71.Synthesis of thieno[2,3-b]pyridinones acting as cytoprotectants and as inhibitors of [3H]glycine binding to the N-methyl-D-aspartate (NMDA) receptor.
Ref 525548J Med Chem. 1999 Jul 29;42(15):2993-3000.4-Hydroxy-1-[2-(4-hydroxyphenoxy)ethyl]-4-(4-methylbenzyl)piperidine: a novel, potent, and selective NR1/2B NMDA receptor antagonist.
Ref 534685J Med Chem. 1998 Aug 13;41(17):3298-302.Synthesis and pharmacological evaluation of N,N'-diarylguanidines as potent sodium channel blockers and anticonvulsant agents.
Ref 534696J Med Chem. 1998 Aug 27;41(18):3499-506.Structure-activity relationships for a series of bis(phenylalkyl)amines: potent subtype-selective inhibitors of N-methyl-D-aspartate receptors.
Ref 534696J Med Chem. 1998 Aug 27;41(18):3499-506.Structure-activity relationships for a series of bis(phenylalkyl)amines: potent subtype-selective inhibitors of N-methyl-D-aspartate receptors.
Ref 534696J Med Chem. 1998 Aug 27;41(18):3499-506.Structure-activity relationships for a series of bis(phenylalkyl)amines: potent subtype-selective inhibitors of N-methyl-D-aspartate receptors.
Ref 527020J Med Chem. 2004 Apr 8;47(8):2089-96.NR2B-selective N-methyl-D-aspartate antagonists: synthesis and evaluation of 5-substituted benzimidazoles.
Ref 527020J Med Chem. 2004 Apr 8;47(8):2089-96.NR2B-selective N-methyl-D-aspartate antagonists: synthesis and evaluation of 5-substituted benzimidazoles.
Ref 534504J Med Chem. 1997 Oct 24;40(22):3679-86.5-(N-oxyaza)-7-substituted-1,4-dihydroquinoxaline-2,3-diones: novel, systemically active and broad spectrum antagonists for NMDA/glycine, AMPA, and kainate receptors.
Ref 534270J Med Chem. 1996 Nov 8;39(23):4643-53.Analogs of 3-hydroxy-1H-1-benzazepine-2,5-dione: structure-activity relationship at N-methyl-D-aspartate receptor glycine sites.
Ref 534696J Med Chem. 1998 Aug 27;41(18):3499-506.Structure-activity relationships for a series of bis(phenylalkyl)amines: potent subtype-selective inhibitors of N-methyl-D-aspartate receptors.
Ref 527036Bioorg Med Chem Lett. 2004 May 3;14(9):2345-9.3-hydroxy-quinazoline-2,4-dione as a useful scaffold to obtain selective Gly/NMDA and AMPA receptor antagonists.
Ref 534270J Med Chem. 1996 Nov 8;39(23):4643-53.Analogs of 3-hydroxy-1H-1-benzazepine-2,5-dione: structure-activity relationship at N-methyl-D-aspartate receptor glycine sites.
Ref 525548J Med Chem. 1999 Jul 29;42(15):2993-3000.4-Hydroxy-1-[2-(4-hydroxyphenoxy)ethyl]-4-(4-methylbenzyl)piperidine: a novel, potent, and selective NR1/2B NMDA receptor antagonist.
Ref 529309J Med Chem. 1991 Apr;34(4):1243-52.Kynurenic acid derivatives. Structure-activity relationships for excitatory amino acid antagonism and identification of potent and selective antagonists at the glycine site on the N-methyl-D-aspartate receptor.
Ref 525527Bioorg Med Chem Lett. 1999 Jun 7;9(11):1619-24.Structure-activity relationship for a series of 2-substituted 1,2,3,4-tetrahydro-9H-pyrido[3,4-b]indoles: potent subtype-selective inhibitors of N-methyl-D-aspartate (NMDA) receptors.
Ref 527903Bioorg Med Chem Lett. 2006 Mar 1;16(5):1392-6.New Gly-Pro-Glu (GPE) analogues: expedite solid-phase synthesis and biological activity.
Ref 528259Bioorg Med Chem Lett. 2006 Sep 1;16(17):4638-40. Epub 2006 Jun 16.Benzimidazole-2-carboxamides as novel NR2B selective NMDA receptor antagonists.
Ref 527994J Med Chem. 2006 Feb 9;49(3):864-71.Synthesis of thieno[2,3-b]pyridinones acting as cytoprotectants and as inhibitors of [3H]glycine binding to the N-methyl-D-aspartate (NMDA) receptor.
Ref 527994J Med Chem. 2006 Feb 9;49(3):864-71.Synthesis of thieno[2,3-b]pyridinones acting as cytoprotectants and as inhibitors of [3H]glycine binding to the N-methyl-D-aspartate (NMDA) receptor.
Ref 525548J Med Chem. 1999 Jul 29;42(15):2993-3000.4-Hydroxy-1-[2-(4-hydroxyphenoxy)ethyl]-4-(4-methylbenzyl)piperidine: a novel, potent, and selective NR1/2B NMDA receptor antagonist.
Ref 527903Bioorg Med Chem Lett. 2006 Mar 1;16(5):1392-6.New Gly-Pro-Glu (GPE) analogues: expedite solid-phase synthesis and biological activity.
Ref 527903Bioorg Med Chem Lett. 2006 Mar 1;16(5):1392-6.New Gly-Pro-Glu (GPE) analogues: expedite solid-phase synthesis and biological activity.
Ref 531421J Med Chem. 1990 Nov;33(11):2944-6.3-(2-carboxyindol-3-yl)propionic acid derivatives: antagonists of the strychnine-insensitive glycine receptor associated with the N-methyl-D-aspartate receptor complex.
Ref 534685J Med Chem. 1998 Aug 13;41(17):3298-302.Synthesis and pharmacological evaluation of N,N'-diarylguanidines as potent sodium channel blockers and anticonvulsant agents.
Ref 528176Bioorg Med Chem Lett. 2006 Jul 1;16(13):3396-400. Epub 2006 May 2.The neuroprotective activity of GPE tripeptide analogues does not correlate with glutamate receptor binding affinity.
Ref 534685J Med Chem. 1998 Aug 13;41(17):3298-302.Synthesis and pharmacological evaluation of N,N'-diarylguanidines as potent sodium channel blockers and anticonvulsant agents.
Ref 534685J Med Chem. 1998 Aug 13;41(17):3298-302.Synthesis and pharmacological evaluation of N,N'-diarylguanidines as potent sodium channel blockers and anticonvulsant agents.
Ref 534696J Med Chem. 1998 Aug 27;41(18):3499-506.Structure-activity relationships for a series of bis(phenylalkyl)amines: potent subtype-selective inhibitors of N-methyl-D-aspartate receptors.
Ref 534696J Med Chem. 1998 Aug 27;41(18):3499-506.Structure-activity relationships for a series of bis(phenylalkyl)amines: potent subtype-selective inhibitors of N-methyl-D-aspartate receptors.
Ref 527020J Med Chem. 2004 Apr 8;47(8):2089-96.NR2B-selective N-methyl-D-aspartate antagonists: synthesis and evaluation of 5-substituted benzimidazoles.
Ref 534696J Med Chem. 1998 Aug 27;41(18):3499-506.Structure-activity relationships for a series of bis(phenylalkyl)amines: potent subtype-selective inhibitors of N-methyl-D-aspartate receptors.
Ref 525548J Med Chem. 1999 Jul 29;42(15):2993-3000.4-Hydroxy-1-[2-(4-hydroxyphenoxy)ethyl]-4-(4-methylbenzyl)piperidine: a novel, potent, and selective NR1/2B NMDA receptor antagonist.
Ref 534270J Med Chem. 1996 Nov 8;39(23):4643-53.Analogs of 3-hydroxy-1H-1-benzazepine-2,5-dione: structure-activity relationship at N-methyl-D-aspartate receptor glycine sites.
Ref 534270J Med Chem. 1996 Nov 8;39(23):4643-53.Analogs of 3-hydroxy-1H-1-benzazepine-2,5-dione: structure-activity relationship at N-methyl-D-aspartate receptor glycine sites.
Ref 527020J Med Chem. 2004 Apr 8;47(8):2089-96.NR2B-selective N-methyl-D-aspartate antagonists: synthesis and evaluation of 5-substituted benzimidazoles.
Ref 534696J Med Chem. 1998 Aug 27;41(18):3499-506.Structure-activity relationships for a series of bis(phenylalkyl)amines: potent subtype-selective inhibitors of N-methyl-D-aspartate receptors.
Ref 527496J Med Chem. 2005 Apr 7;48(7):2627-37.Synthesis and pharmacology of N1-substituted piperazine-2,3-dicarboxylic acid derivatives acting as NMDA receptor antagonists.
Ref 525786Bioorg Med Chem Lett. 2000 May 15;10(10):1133-7.4,10-Dihydro-4-oxo-4H-imidazo[1,2-a]indeno[1,2-e]pyrazin-2-carboxylic acid derivatives: highly potent and selective AMPA receptors antagonists with in vivo activity.
Ref 533655J Med Chem. 1995 Jun 23;38(13):2483-9.Synthesis and evaluation of 6,11-ethanohexahydrobenzo[b]quinolizidines: a new class of noncompetitive N-methyl-D-aspartate antagonists.
Ref 534270J Med Chem. 1996 Nov 8;39(23):4643-53.Analogs of 3-hydroxy-1H-1-benzazepine-2,5-dione: structure-activity relationship at N-methyl-D-aspartate receptor glycine sites.
Ref 528176Bioorg Med Chem Lett. 2006 Jul 1;16(13):3396-400. Epub 2006 May 2.The neuroprotective activity of GPE tripeptide analogues does not correlate with glutamate receptor binding affinity.
Ref 526618Bioorg Med Chem Lett. 2003 May 19;13(10):1759-62.4-(3,4-dihydro-1H-isoquinolin-2yl)-pyridines and 4-(3,4-dihydro-1H-isoquinolin-2-yl)-quinolines as potent NR1/2B subtype selective NMDA receptor antagonists.
Ref 527438J Med Chem. 2005 Feb 24;48(4):995-1018.CoMFA, synthesis, and pharmacological evaluation of (E)-3-(2-carboxy-2-arylvinyl)-4,6-dichloro-1H-indole-2-carboxylic acids: 3-[2-(3-aminophenyl)-2-carboxyvinyl]-4,6-dichloro-1H-indole-2-carboxylic acid, a potent selective glycine-site NMDA receptor antagonist.
Ref 534270J Med Chem. 1996 Nov 8;39(23):4643-53.Analogs of 3-hydroxy-1H-1-benzazepine-2,5-dione: structure-activity relationship at N-methyl-D-aspartate receptor glycine sites.
Ref 526134J Med Chem. 2001 Sep 13;44(19):3157-65.Synthesis, ionotropic glutamate receptor binding affinity, and structure-activity relationships of a new set of 4,5-dihydro-8-heteroaryl-4-oxo-1,2,4-triazolo[1,5-a]quinoxaline-2-carboxylates analogues of TQX-173.

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