Proteins > Glutamate receptor ionotropic, NMDA 2D
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Glutamate receptor ionotropic, NMDA 2D
A glutamate receptor ionotropic, NMDA 2D that is encoded in the genome of rat. [OMA:Q62645, PRO:DNx]
Synonyms
GluN2D;
Glutamate [NMDA] receptor subunit epsilon-4;
N-methyl D-aspartate receptor subtype 2D;
NMDAR2D;
NR2D
Research
Bioassay Publications (134)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 2 (1.49) | 18.7374 |
| 1990's | 60 (44.78) | 18.2507 |
| 2000's | 45 (33.58) | 29.6817 |
| 2010's | 21 (15.67) | 24.3611 |
| 2020's | 6 (4.48) | 2.80 |
Compounds (150)
Drugs with Potency Measurements
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| beta-alanine | Rattus norvegicus (Norway rat) | IC50 | 11.6000 | 1 | 1 |
| 1-aminocyclopropane-1-carboxylic acid | Rattus norvegicus (Norway rat) | IC50 | 0.0400 | 1 | 1 |
| glycine | Rattus norvegicus (Norway rat) | IC50 | 0.3253 | 3 | 3 |
| glycine | Rattus norvegicus (Norway rat) | Ki | 0.1700 | 1 | 1 |
| quinolinic acid | Rattus norvegicus (Norway rat) | IC50 | 100.0000 | 1 | 1 |
| spermine | Rattus norvegicus (Norway rat) | IC50 | 232.0000 | 1 | 1 |
| 2,4-methanoglutamate | Rattus norvegicus (Norway rat) | IC50 | 0.1630 | 1 | 1 |
| 2-amino-5-phosphonovalerate | Rattus norvegicus (Norway rat) | IC50 | 0.2900 | 4 | 5 |
| 2-amino-5-phosphonovalerate | Rattus norvegicus (Norway rat) | Ki | 0.5600 | 3 | 3 |
| alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid | Rattus norvegicus (Norway rat) | IC50 | 100.0000 | 5 | 7 |
| alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid | Rattus norvegicus (Norway rat) | Ki | 100.0000 | 1 | 1 |
| 3-(2-carboxypiperazin-4-yl)propyl-1-phosphonic acid | Rattus norvegicus (Norway rat) | IC50 | 29.0683 | 10 | 10 |
| ibotenic acid | Rattus norvegicus (Norway rat) | IC50 | 100.0000 | 1 | 1 |
| 1-(3-chlorophenyl)piperazine | Rattus norvegicus (Norway rat) | Ki | 0.0090 | 1 | 1 |
| 5,7-dichlorokynurenic acid | Rattus norvegicus (Norway rat) | IC50 | 40.0928 | 4 | 5 |
| 5,7-dichlorokynurenic acid | Rattus norvegicus (Norway rat) | Ki | 1.2275 | 4 | 4 |
| 6,7-dichloroquinoxaline-2,3-dione | Rattus norvegicus (Norway rat) | IC50 | 2.0825 | 4 | 4 |
| 6,7-dichloroquinoxaline-2,3-dione | Rattus norvegicus (Norway rat) | Ki | 0.1600 | 1 | 1 |
| 7-chlorokynurenic acid | Rattus norvegicus (Norway rat) | IC50 | 67.8880 | 4 | 5 |
| amantadine | Rattus norvegicus (Norway rat) | IC50 | 180.6667 | 6 | 6 |
| arcaine | Rattus norvegicus (Norway rat) | IC50 | 75.0000 | 3 | 3 |
| alpha-amino-3-hydroxy-5-tert-butyl-4-isoxazolepropionate | Rattus norvegicus (Norway rat) | IC50 | 100.0000 | 3 | 3 |
| chlorpromazine | Rattus norvegicus (Norway rat) | IC50 | 1.3000 | 1 | 1 |
| 2-amino-6-phosphonohexanoic acid | Rattus norvegicus (Norway rat) | Ki | 0.5210 | 2 | 2 |
| racemethorphan | Rattus norvegicus (Norway rat) | IC50 | 1.2950 | 2 | 2 |
| 2-amino-7-phosphonoheptanoic acid | Rattus norvegicus (Norway rat) | IC50 | 63.6605 | 9 | 11 |
| 2-amino-7-phosphonoheptanoic acid | Rattus norvegicus (Norway rat) | Ki | 0.9413 | 2 | 3 |
| enoxacin | Rattus norvegicus (Norway rat) | IC50 | 10.0000 | 1 | 1 |
| haloperidol | Rattus norvegicus (Norway rat) | Ki | 10.0000 | 1 | 1 |
| ifenprodil | Rattus norvegicus (Norway rat) | IC50 | 0.2630 | 1 | 1 |
| ifenprodil | Rattus norvegicus (Norway rat) | Ki | 0.1432 | 1 | 1 |
| imipramine | Rattus norvegicus (Norway rat) | IC50 | 14.0000 | 1 | 1 |
| ketamine | Rattus norvegicus (Norway rat) | IC50 | 5.0200 | 4 | 4 |
| ketamine | Rattus norvegicus (Norway rat) | Ki | 0.1800 | 13 | 13 |
| kynurenic acid | Rattus norvegicus (Norway rat) | IC50 | 112.5000 | 3 | 4 |
| memantine | Rattus norvegicus (Norway rat) | IC50 | 22.5444 | 9 | 9 |
| memantine | Rattus norvegicus (Norway rat) | Ki | 0.7000 | 1 | 1 |
| aspartic acid | Rattus norvegicus (Norway rat) | IC50 | 1.6380 | 1 | 1 |
| cycloserine | Rattus norvegicus (Norway rat) | IC50 | 2.3000 | 1 | 1 |
| phencyclidine | Rattus norvegicus (Norway rat) | IC50 | 0.1299 | 3 | 3 |
| phencyclidine | Rattus norvegicus (Norway rat) | Ki | 0.0380 | 1 | 2 |
| 1-aminoanthraquinone | Rattus norvegicus (Norway rat) | IC50 | 179.0000 | 2 | 2 |
| 9,10-anthraquinone | Rattus norvegicus (Norway rat) | IC50 | 1,000.0000 | 2 | 2 |
| 1,3-ditolylguanidine | Rattus norvegicus (Norway rat) | Ki | 6.6900 | 1 | 1 |
| 1-amino-4-hydroxyanthraquinone | Rattus norvegicus (Norway rat) | IC50 | 168.5000 | 2 | 2 |
| 2-aminoanthraquinone | Rattus norvegicus (Norway rat) | IC50 | 117.5000 | 2 | 2 |
| 1,5-diaminoanthraquinone | Rattus norvegicus (Norway rat) | IC50 | 330.5000 | 2 | 2 |
| 2,6-diaminoanthraquinone | Rattus norvegicus (Norway rat) | IC50 | 1,000.0000 | 2 | 2 |
| indopan | Rattus norvegicus (Norway rat) | Ki | 10.0000 | 1 | 1 |
| kainic acid | Rattus norvegicus (Norway rat) | IC50 | 100.0000 | 5 | 6 |
| kainic acid | Rattus norvegicus (Norway rat) | Ki | 68.7667 | 3 | 3 |
| 1,2-diaminoanthraquinone | Rattus norvegicus (Norway rat) | IC50 | 508.0000 | 2 | 2 |
| disperse blue 1 | Rattus norvegicus (Norway rat) | IC50 | 1,000.0000 | 2 | 2 |
| 1,12-dodecamethylenediamine | Rattus norvegicus (Norway rat) | IC50 | 250.7400 | 5 | 5 |
| n-methylaspartate | Rattus norvegicus (Norway rat) | IC50 | 11.1400 | 4 | 5 |
| n-methylaspartate | Rattus norvegicus (Norway rat) | Ki | 6.2000 | 2 | 2 |
| 2,3-dihydroxyquinoxaline | Rattus norvegicus (Norway rat) | IC50 | 29.1333 | 3 | 3 |
| 1,4-diaminoanthraquinone | Rattus norvegicus (Norway rat) | IC50 | 489.5000 | 2 | 2 |
| glutamic acid | Rattus norvegicus (Norway rat) | IC50 | 0.1532 | 4 | 4 |
| glutamic acid | Rattus norvegicus (Norway rat) | Ki | 8.4950 | 5 | 6 |
| quisqualic acid | Rattus norvegicus (Norway rat) | IC50 | 100.0000 | 1 | 1 |
| besipirdine | Rattus norvegicus (Norway rat) | IC50 | 20.0000 | 2 | 2 |
| 3-n-butylphthalide | Rattus norvegicus (Norway rat) | Ki | 0.0148 | 1 | 1 |
| amantadine hydrochloride | Rattus norvegicus (Norway rat) | IC50 | 216.7000 | 2 | 2 |
| propamidine | Rattus norvegicus (Norway rat) | IC50 | 5.5400 | 1 | 1 |
| selfotel | Rattus norvegicus (Norway rat) | IC50 | 9.7055 | 13 | 13 |
| selfotel | Rattus norvegicus (Norway rat) | Ki | 0.4300 | 3 | 3 |
| n-(2-carboxyphenyl)glycine | Rattus norvegicus (Norway rat) | IC50 | 4.0000 | 1 | 2 |
| D-serine | Rattus norvegicus (Norway rat) | IC50 | 0.3000 | 1 | 1 |
| D-alanine | Rattus norvegicus (Norway rat) | IC50 | 90.9000 | 1 | 1 |
| 2-phenylquinoline | Rattus norvegicus (Norway rat) | Ki | 35.0000 | 1 | 1 |
| 6,7-dichloroquinoxaline-2,3-dione | Rattus norvegicus (Norway rat) | IC50 | 3.4500 | 3 | 4 |
| 1-aminocyclobutanecarboxylic acid | Rattus norvegicus (Norway rat) | IC50 | 19.0000 | 1 | 1 |
| 1-amino-1,3-dicarboxycyclopentane | Rattus norvegicus (Norway rat) | IC50 | 100.0000 | 1 | 1 |
| sr141716 | Rattus norvegicus (Norway rat) | Ki | 0.0250 | 1 | 1 |
| metaphit | Rattus norvegicus (Norway rat) | Ki | 0.5350 | 1 | 1 |
| marimastat | Rattus norvegicus (Norway rat) | IC50 | 10.0000 | 1 | 1 |
| 1-(1-(2-benzo(b)thienyl)cyclohexyl)piperidine | Rattus norvegicus (Norway rat) | Ki | 10.0000 | 1 | 1 |
| 2-amino-3-(3-(carboxymethoxy)-5-methylisoxazol-4-yl)propionic acid | Rattus norvegicus (Norway rat) | IC50 | 100.0000 | 1 | 2 |
| (tetrazol-5-yl)glycine | Rattus norvegicus (Norway rat) | IC50 | 0.0980 | 1 | 1 |
| furamidine | Rattus norvegicus (Norway rat) | IC50 | 5.8550 | 2 | 2 |
| 2-amino-3-(3-hydroxy-5-phenylisoxazol-4-yl)propionic acid | Rattus norvegicus (Norway rat) | IC50 | 100.0000 | 2 | 2 |
| ly 293558 | Rattus norvegicus (Norway rat) | IC50 | 21.9769 | 11 | 13 |
| butamidine | Rattus norvegicus (Norway rat) | IC50 | 17.7000 | 1 | 1 |
| d-apv | Rattus norvegicus (Norway rat) | IC50 | 0.8800 | 1 | 1 |
| d-apv | Rattus norvegicus (Norway rat) | Ki | 21.0000 | 1 | 1 |
| ym 872 | Rattus norvegicus (Norway rat) | IC50 | 100.0000 | 2 | 2 |
| besonprodil | Rattus norvegicus (Norway rat) | IC50 | 0.0053 | 2 | 2 |
| alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid | Rattus norvegicus (Norway rat) | IC50 | 100.0000 | 5 | 5 |
| alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid | Rattus norvegicus (Norway rat) | Ki | 100.0000 | 1 | 1 |
| 3-(2-carboxyindol-3-yl)propionic acid | Rattus norvegicus (Norway rat) | IC50 | 30.5000 | 2 | 2 |
| alpha-amino-3-(hydroxy)-5-methyl-4-isoxazoleacetic acid | Rattus norvegicus (Norway rat) | IC50 | 28.3750 | 4 | 4 |
| homocysteic acid | Rattus norvegicus (Norway rat) | Ki | 2.7000 | 1 | 1 |
| dizocilpine | Rattus norvegicus (Norway rat) | IC50 | 0.0149 | 6 | 6 |
| dizocilpine | Rattus norvegicus (Norway rat) | Ki | 0.0392 | 5 | 8 |
| esketamine | Rattus norvegicus (Norway rat) | Ki | 0.4950 | 2 | 2 |
| etravirine | Rattus norvegicus (Norway rat) | IC50 | 0.0100 | 1 | 1 |
| latrepirdine | Rattus norvegicus (Norway rat) | IC50 | 1.5800 | 1 | 1 |
| rpr 104632 | Rattus norvegicus (Norway rat) | IC50 | 0.0082 | 2 | 2 |
| zk 200775 | Rattus norvegicus (Norway rat) | IC50 | 5.9833 | 3 | 3 |
| cocaine | Rattus norvegicus (Norway rat) | Ki | 10.0000 | 1 | 1 |
| mdl29,951 | Rattus norvegicus (Norway rat) | IC50 | 119.4367 | 3 | 3 |
| (R)-ketamine | Rattus norvegicus (Norway rat) | Ki | 1.9850 | 2 | 2 |
| N-(3-cyano-4,5,6,7-tetrahydro-1-benzothiophen-2-yl)-1-naphthalenecarboxamide | Rattus norvegicus (Norway rat) | IC50 | 0.3162 | 1 | 1 |
| d-ap7 | Rattus norvegicus (Norway rat) | IC50 | 0.9120 | 1 | 1 |
| 6,7-dichloro-3-hydroxy-2-quinoxalinecarboxylic acid | Rattus norvegicus (Norway rat) | IC50 | 0.4600 | 1 | 1 |
| 7-chloro-thiokynurenate | Rattus norvegicus (Norway rat) | IC50 | 0.4000 | 1 | 1 |
| ro 60-0175 | Rattus norvegicus (Norway rat) | Ki | 0.0023 | 1 | 1 |
| 2,3-dioxo-6-nitro-7-sulfamoylbenzo(f)quinoxaline | Rattus norvegicus (Norway rat) | IC50 | 99.5200 | 9 | 10 |
| 2,3-dioxo-6-nitro-7-sulfamoylbenzo(f)quinoxaline | Rattus norvegicus (Norway rat) | Ki | 100.0000 | 2 | 3 |
| fg 9041 | Rattus norvegicus (Norway rat) | IC50 | 13.8250 | 4 | 4 |
| fg 9041 | Rattus norvegicus (Norway rat) | Ki | 0.3900 | 1 | 3 |
| 6-nitro-1,4-dihydroquinoxaline-2,3-dione | Rattus norvegicus (Norway rat) | IC50 | 6.0500 | 2 | 2 |
| leukotriene d4 | Rattus norvegicus (Norway rat) | IC50 | 0.0007 | 1 | 1 |
| leukotriene d4 | Rattus norvegicus (Norway rat) | Ki | 0.0003 | 1 | 1 |
| (alpha-carboxycyclopropyl)glycine, (1r-(1alpha(s*),2alpha))-isomer | Rattus norvegicus (Norway rat) | Ki | 0.0090 | 1 | 1 |
| 2r,4r-4-aminopyrrolidine-2,4-dicarboxylate | Rattus norvegicus (Norway rat) | IC50 | 100.0000 | 1 | 1 |
| l 745870 | Rattus norvegicus (Norway rat) | Ki | 10.0000 | 1 | 1 |
| ml 10302 | Rattus norvegicus (Norway rat) | Ki | 0.0050 | 1 | 2 |
| mdl 105519 | Rattus norvegicus (Norway rat) | IC50 | 0.1570 | 1 | 1 |
| levorphanol | Rattus norvegicus (Norway rat) | IC50 | 4.4500 | 2 | 2 |
| dextromethorphan | Rattus norvegicus (Norway rat) | Ki | 2.2460 | 1 | 1 |
| licostinel | Rattus norvegicus (Norway rat) | IC50 | 0.0068 | 5 | 5 |
| lofepramine hydrochloride | Rattus norvegicus (Norway rat) | IC50 | 12.8625 | 7 | 8 |
| lofepramine hydrochloride | Rattus norvegicus (Norway rat) | Ki | 62.2000 | 4 | 5 |
| cgp 37849 | Rattus norvegicus (Norway rat) | Ki | 0.5175 | 2 | 2 |
| dizocilpine maleate | Rattus norvegicus (Norway rat) | Ki | 0.0024 | 1 | 2 |
| sdz eaa 494 | Rattus norvegicus (Norway rat) | IC50 | 0.0400 | 1 | 1 |
| 3-(2-carboxypiperazine-4-yl)-1-propenyl-1-phosphonic acid | Rattus norvegicus (Norway rat) | Ki | 0.0400 | 1 | 1 |
| gavestinel | Rattus norvegicus (Norway rat) | IC50 | 0.0080 | 2 | 2 |
| gavestinel | Rattus norvegicus (Norway rat) | Ki | 0.0030 | 1 | 1 |
| mdl 105519 | Rattus norvegicus (Norway rat) | IC50 | 0.0110 | 2 | 2 |
| ampa, (r)-isomer | Rattus norvegicus (Norway rat) | IC50 | 100.0000 | 2 | 3 |
| l 689560 | Rattus norvegicus (Norway rat) | IC50 | 0.0078 | 1 | 1 |
| l 689560 | Rattus norvegicus (Norway rat) | Ki | 0.0020 | 1 | 1 |
| ro 25-6981 | Rattus norvegicus (Norway rat) | IC50 | 0.0580 | 3 | 3 |
| ik 682 | Rattus norvegicus (Norway rat) | IC50 | 10.3400 | 1 | 1 |
| levomilnacipran | Rattus norvegicus (Norway rat) | IC50 | 6.3000 | 4 | 4 |
| eaa-090 | Rattus norvegicus (Norway rat) | IC50 | 0.0202 | 3 | 3 |
| 4-(4-chlorophenyl)-3-methylbut-3-en-2-oxime | Rattus norvegicus (Norway rat) | IC50 | 2.8000 | 1 | 1 |
| (4-benzylpiperidin-1-yl)-(6-hydroxy-1h-indol-2-yl)methanone | Rattus norvegicus (Norway rat) | IC50 | 0.0165 | 4 | 4 |
| tqx 173 | Rattus norvegicus (Norway rat) | IC50 | 68.0000 | 1 | 1 |
| tqx 173 | Rattus norvegicus (Norway rat) | Ki | 33.5000 | 1 | 1 |
| n,n-diallyl-5-methoxytryptamine | Rattus norvegicus (Norway rat) | Ki | 0.3991 | 1 | 2 |
| l 701324 | Rattus norvegicus (Norway rat) | IC50 | 0.0057 | 3 | 3 |
| 7-chloro-3-[cyclopropyl(oxo)methyl]-4-hydroxy-1H-quinolin-2-one | Rattus norvegicus (Norway rat) | IC50 | 0.4197 | 3 | 3 |
| mdl 104653 | Rattus norvegicus (Norway rat) | IC50 | 0.1720 | 1 | 1 |
Drugs with Activation Measurements
Drugs with Other Measurements
[no title available]Journal of medicinal chemistry, , 01-13, Volume: 65, Issue:1, 2022
Design, synthesis and structure-activity relationships of novel strychnine-insensitive glycine receptor ligands.Bioorganic & medicinal chemistry letters, , May-17, Volume: 9, Issue:10, 1999
The glycine site on the NMDA receptor: structure-activity relationships and therapeutic potential.Journal of medicinal chemistry, , Nov-25, Volume: 37, Issue:24, 1994
Tricyclic quinoxalinediones: 5,6-dihydro-1H-pyrrolo[1,2,3-de] quinoxaline-2,3-diones and 6,7-dihydro-1H,5H-pyrido[1,2,3-de] quinoxaline-2,3-diones as potent antagonists for the glycine binding site of the NMDA receptor.Journal of medicinal chemistry, , Nov-11, Volume: 37, Issue:23, 1994
Potent quinoxaline-spaced phosphono alpha-amino acids of the AP-6 type as competitive NMDA antagonists: synthesis and biological evaluation.Journal of medicinal chemistry, , Feb-05, Volume: 36, Issue:3, 1993
Synthesis and evaluation of 3-substituted 17-methylmorphinan analogs as potential anticonvulsant agents.Journal of medicinal chemistry, , Oct-30, Volume: 35, Issue:22, 1992
Synthesis and anticonvulsant activity of novel bicyclic acidic amino acids.Journal of medicinal chemistry, , Jul-03, Volume: 46, Issue:14, 2003
Exploration of N-phosphonoalkyl-, N-phosphonoalkenyl-, and N-(phosphonoalkyl)phenyl-spaced alpha-amino acids as competitive N-methyl-D-aspartic acid antagonists.Journal of medicinal chemistry, , Apr-17, Volume: 35, Issue:8, 1992
Modeling of competitive phosphono amino acid NMDA receptor antagonists.Journal of medicinal chemistry, , May-01, Volume: 35, Issue:9, 1992
Synthesis and biological evaluation of cyclopropyl analogues of 2-amino-5-phosphonopentanoic acid.Journal of medicinal chemistry, , Volume: 34, Issue:1, 1991
New and versatile approaches to the synthesis of CPP-related competitive NMDA antagonists. Preliminary structure-activity relationships and pharmacological evaluation.Journal of medicinal chemistry, , Volume: 33, Issue:10, 1990
4-hydroxy-1,2,5-oxadiazol-3-yl moiety as bioisoster of the carboxy function. Synthesis, ionization constants, and molecular pharmacological characterization at ionotropic glutamate receptors of compounds related to glutamate and its homologues.Journal of medicinal chemistry, , May-27, Volume: 53, Issue:10, 2010
Novel 1-hydroxyazole bioisosteres of glutamic acid. Synthesis, protolytic properties, and pharmacology.Journal of medicinal chemistry, , Jan-03, Volume: 45, Issue:1, 2002
Resolution, absolute stereochemistry, and pharmacology of the S-(+)- and R-(-)-isomers of the apparent partial AMPA receptor agonist (R,S)-2-amino-3-(3-hydroxy-5-phenylisoxazol-4-yl)propionic acid [(R,S)-APPA].Journal of medicinal chemistry, , Apr-01, Volume: 37, Issue:7, 1994
Excitatory amino acid receptor ligands. Synthesis and biological activity of 3-isoxazolol amino acids structurally related to homoibotenic acid.Journal of medicinal chemistry, , Sep-18, Volume: 35, Issue:19, 1992
Design, synthesis, SAR, and biological evaluation of highly potent benzimidazole-spaced phosphono-alpha-amino acid competitive NMDA antagonists of the AP-6 type.Journal of medicinal chemistry, , May-10, Volume: 44, Issue:10, 2001
Synthesis, resolution, and SAR of (+/-)-2-amino-N-methyl-alpha-(3-methyl-2-thienyl)benzeneethanamine++ + and related analogs as noncompetitive NMDA antagonists with neuroprotective properties.Journal of medicinal chemistry, , Sep-16, Volume: 37, Issue:19, 1994
Potent quinoxaline-spaced phosphono alpha-amino acids of the AP-6 type as competitive NMDA antagonists: synthesis and biological evaluation.Journal of medicinal chemistry, , Feb-05, Volume: 36, Issue:3, 1993
Exploration of N-phosphonoalkyl-, N-phosphonoalkenyl-, and N-(phosphonoalkyl)phenyl-spaced alpha-amino acids as competitive N-methyl-D-aspartic acid antagonists.Journal of medicinal chemistry, , Apr-17, Volume: 35, Issue:8, 1992
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.Journal of medicinal chemistry, , Dec-11, Volume: 35, Issue:25, 1992
New and versatile approaches to the synthesis of CPP-related competitive NMDA antagonists. Preliminary structure-activity relationships and pharmacological evaluation.Journal of medicinal chemistry, , Volume: 33, Issue:10, 1990
4-(Phosphonoalkyl)- and 4-(phosphonoalkenyl)-2-piperidinecarboxylic acids: synthesis, activity at N-methyl-D-aspartic acid receptors, and anticonvulsant activity.Journal of medicinal chemistry, , Volume: 32, Issue:9, 1989
Exploration of phenyl-spaced 2-amino-(5-9)-phosphonoalkanoic acids as competitive N-methyl-D-aspartic acid antagonists.Journal of medicinal chemistry, , Volume: 32, Issue:7, 1989
3-Hydroxy-1H-quinazoline-2,4-dione derivatives as new antagonists at ionotropic glutamate receptors: molecular modeling and pharmacological studies.European journal of medicinal chemistry, , Volume: 54, 2012
3-hydroxy-quinazoline-2,4-dione as a useful scaffold to obtain selective Gly/NMDA and AMPA receptor antagonists.Bioorganic & medicinal chemistry letters, , May-03, Volume: 14, Issue:9, 2004
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.Journal of medicinal chemistry, , Sep-13, Volume: 44, Issue:19, 2001
Effect of plasma protein binding on in vivo activity and brain penetration of glycine/NMDA receptor antagonists.Journal of medicinal chemistry, , Dec-05, Volume: 40, Issue:25, 1997
The glycine site on the NMDA receptor: structure-activity relationships and therapeutic potential.Journal of medicinal chemistry, , Nov-25, Volume: 37, Issue:24, 1994
Tricyclic quinoxalinediones: 5,6-dihydro-1H-pyrrolo[1,2,3-de] quinoxaline-2,3-diones and 6,7-dihydro-1H,5H-pyrido[1,2,3-de] quinoxaline-2,3-diones as potent antagonists for the glycine binding site of the NMDA receptor.Journal of medicinal chemistry, , Nov-11, Volume: 37, Issue:23, 1994
2-Carboxytetrahydroquinolines. Conformational and stereochemical requirements for antagonism of the glycine site on the NMDA receptor.Journal of medicinal chemistry, , May-29, Volume: 35, Issue:11, 1992
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.Journal of medicinal chemistry, , Volume: 34, Issue:4, 1991
Structure-activity relationships of 1,4-dihydro-(1H,4H)-quinoxaline-2,3-diones as N-methyl-D-aspartate (glycine site) receptor antagonists. 1. Heterocyclic substituted 5-alkyl derivatives.Journal of medicinal chemistry, , Jun-07, Volume: 44, Issue:12, 2001
Structure-activity relationships of 4-hydroxy-3-nitroquinolin-2(1H)-ones as novel antagonists at the glycine site of N-methyl-D-aspartate receptors.Journal of medicinal chemistry, , Nov-08, Volume: 39, Issue:23, 1996
Synthesis and structure-activity relationships of substituted 1,4-dihydroquinoxaline-2,3-diones: antagonists of N-methyl-D-aspartate (NMDA) receptor glycine sites and non-NMDA glutamate receptors.Journal of medicinal chemistry, , Oct-27, Volume: 38, Issue:22, 1995
The glycine site on the NMDA receptor: structure-activity relationships and therapeutic potential.Journal of medicinal chemistry, , Nov-25, Volume: 37, Issue:24, 1994
Tricyclic quinoxalinediones: 5,6-dihydro-1H-pyrrolo[1,2,3-de] quinoxaline-2,3-diones and 6,7-dihydro-1H,5H-pyrido[1,2,3-de] quinoxaline-2,3-diones as potent antagonists for the glycine binding site of the NMDA receptor.Journal of medicinal chemistry, , Nov-11, Volume: 37, Issue:23, 1994
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.Journal of medicinal chemistry, , Volume: 34, Issue:4, 1991
Effect of plasma protein binding on in vivo activity and brain penetration of glycine/NMDA receptor antagonists.Journal of medicinal chemistry, , Dec-05, Volume: 40, Issue:25, 1997
The glycine site on the NMDA receptor: structure-activity relationships and therapeutic potential.Journal of medicinal chemistry, , Nov-25, Volume: 37, Issue:24, 1994
2-Carboxytetrahydroquinolines. Conformational and stereochemical requirements for antagonism of the glycine site on the NMDA receptor.Journal of medicinal chemistry, , May-29, Volume: 35, Issue:11, 1992
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.Journal of medicinal chemistry, , Volume: 34, Issue:4, 1991
Tryptophanol-derived oxazolopiperidone lactams: identification of a hit compound as NMDA receptor antagonist.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 24, Issue:15, 2014
New oxapolycyclic cage amines with NMDA receptor antagonist and trypanocidal activities.Bioorganic & medicinal chemistry, , Jan-01, Volume: 18, Issue:1, 2010
Synthesis and pharmacological evaluation of (2-oxaadamant-1-yl)amines.Bioorganic & medicinal chemistry, , Apr-15, Volume: 17, Issue:8, 2009
Synthesis and pharmacological evaluation of several ring-contracted amantadine analogs.Bioorganic & medicinal chemistry, , Dec-01, Volume: 16, Issue:23, 2008
Synthesis and structure-activity studies on acidic amino acids and related diacids as NMDA receptor ligands.Journal of medicinal chemistry, , Sep-30, Volume: 37, Issue:20, 1994
Excitatory amino acid receptor ligands. Synthesis and biological activity of 3-isoxazolol amino acids structurally related to homoibotenic acid.Journal of medicinal chemistry, , Sep-18, Volume: 35, Issue:19, 1992
Design, synthesis, SAR, and biological evaluation of highly potent benzimidazole-spaced phosphono-alpha-amino acid competitive NMDA antagonists of the AP-6 type.Journal of medicinal chemistry, , May-10, Volume: 44, Issue:10, 2001
Potent quinoxaline-spaced phosphono alpha-amino acids of the AP-6 type as competitive NMDA antagonists: synthesis and biological evaluation.Journal of medicinal chemistry, , Feb-05, Volume: 36, Issue:3, 1993
Exploration of N-phosphonoalkyl-, N-phosphonoalkenyl-, and N-(phosphonoalkyl)phenyl-spaced alpha-amino acids as competitive N-methyl-D-aspartic acid antagonists.Journal of medicinal chemistry, , Apr-17, Volume: 35, Issue:8, 1992
Modeling of competitive phosphono amino acid NMDA receptor antagonists.Journal of medicinal chemistry, , May-01, Volume: 35, Issue:9, 1992
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.Journal of medicinal chemistry, , Dec-11, Volume: 35, Issue:25, 1992
New and versatile approaches to the synthesis of CPP-related competitive NMDA antagonists. Preliminary structure-activity relationships and pharmacological evaluation.Journal of medicinal chemistry, , Volume: 33, Issue:10, 1990
Exploration of phenyl-spaced 2-amino-(5-9)-phosphonoalkanoic acids as competitive N-methyl-D-aspartic acid antagonists.Journal of medicinal chemistry, , Volume: 32, Issue:7, 1989
Repurposing of Drugs-The Ketamine Story.Journal of medicinal chemistry, , 11-25, Volume: 63, Issue:22, 2020
Synthesis and biological activity of conformationally restricted analogues of milnacipran: (1S, 2R)-1-phenyl-2-[(R)-1-amino-2-propynyl]-N,N- diethylcyclopropanecarboxamide is a novel class of NMDA receptor channel blocker.Journal of medicinal chemistry, , Aug-27, Volume: 41, Issue:18, 1998
Synthesis and biological activity of conformationally restricted analogs of milnacipran: (1S,2R)-1-phenyl-2-[(S)-1-aminopropyl]-N,N-diethylcyclopropanecarboxami de, an efficient noncompetitive N-methyl-D-aspartic acid receptor antagonist.Journal of medicinal chemistry, , Nov-22, Volume: 39, Issue:24, 1996
Synthesis and pharmacological evaluation of 4a-phenanthrenamine derivatives acting at the phencyclidine binding site of the N-methyl-D-aspartate receptor complex.Journal of medicinal chemistry, , Jul-09, Volume: 36, Issue:14, 1993
The glycine site on the NMDA receptor: structure-activity relationships and therapeutic potential.Journal of medicinal chemistry, , Nov-25, Volume: 37, Issue:24, 1994
2-Carboxytetrahydroquinolines. Conformational and stereochemical requirements for antagonism of the glycine site on the NMDA receptor.Journal of medicinal chemistry, , May-29, Volume: 35, Issue:11, 1992
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.Journal of medicinal chemistry, , Volume: 34, Issue:4, 1991
Identification of tetracyclic lactams as NMDA receptor antagonists with potential application in neurological disorders.European journal of medicinal chemistry, , May-15, Volume: 194, 2020
A novel class of multitarget anti-Alzheimer benzohomoadamantane‒chlorotacrine hybrids modulating cholinesterases and glutamate NMDA receptors.European journal of medicinal chemistry, , Oct-15, Volume: 180, 2019
New oxapolycyclic cage amines with NMDA receptor antagonist and trypanocidal activities.Bioorganic & medicinal chemistry, , Jan-01, Volume: 18, Issue:1, 2010
Synthesis and pharmacological evaluation of (2-oxaadamant-1-yl)amines.Bioorganic & medicinal chemistry, , Apr-15, Volume: 17, Issue:8, 2009
Comparisons of the influenza virus A M2 channel binding affinities, anti-influenza virus potencies and NMDA antagonistic activities of 2-alkyl-2-aminoadamantanes and analogues.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 18, Issue:23, 2008
Synthesis and pharmacological evaluation of several ring-contracted amantadine analogs.Bioorganic & medicinal chemistry, , Dec-01, Volume: 16, Issue:23, 2008
Emerging molecular approaches to pain therapy.Journal of medicinal chemistry, , May-06, Volume: 42, Issue:9, 1999
Design, synthesis and structure-activity relationships of novel strychnine-insensitive glycine receptor ligands.Bioorganic & medicinal chemistry letters, , May-17, Volume: 9, Issue:10, 1999
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Synthesis and biological activity of conformationally restricted analogs of milnacipran: (1S,2R)-1-phenyl-2-[(S)-1-aminopropyl]-N,N-diethylcyclopropanecarboxami de, an efficient noncompetitive N-methyl-D-aspartic acid receptor antagonist.Journal of medicinal chemistry, , Nov-22, Volume: 39, Issue:24, 1996
Identification, synthesis, and characterization of a unique class of N-methyl-D-aspartate antagonists. The 6,11-ethanobenzo[b]quinolizinium cation.Journal of medicinal chemistry, , Dec-23, Volume: 37, Issue:26, 1994
Synthesis and pharmacological evaluation of 4a-phenanthrenamine derivatives acting at the phencyclidine binding site of the N-methyl-D-aspartate receptor complex.Journal of medicinal chemistry, , Jul-09, Volume: 36, Issue:14, 1993
Synthesis and evaluation of 3-substituted 17-methylmorphinan analogs as potential anticonvulsant agents.Journal of medicinal chemistry, , Oct-30, Volume: 35, Issue:22, 1992
Use of the 4-Hydroxytriazole Moiety as a Bioisosteric Tool in the Development of Ionotropic Glutamate Receptor Ligands.Journal of medicinal chemistry, , 05-09, Volume: 62, Issue:9, 2019
Chemoenzymatic synthesis of new 2,4-syn-functionalized (S)-glutamate analogues and structure-activity relationship studies at ionotropic glutamate receptors and excitatory amino acid transporters.Journal of medicinal chemistry, , Feb-28, Volume: 56, Issue:4, 2013
4-hydroxy-1,2,5-oxadiazol-3-yl moiety as bioisoster of the carboxy function. Synthesis, ionization constants, and molecular pharmacological characterization at ionotropic glutamate receptors of compounds related to glutamate and its homologues.Journal of medicinal chemistry, , May-27, Volume: 53, Issue:10, 2010
Synthesis and enantiopharmacology of new AMPA-kainate receptor agonists.Journal of medicinal chemistry, , Oct-07, Volume: 42, Issue:20, 1999
Synthesis and pharmacology of a new AMPA-kainate receptor agonist with potent convulsant activity.Journal of medicinal chemistry, , Sep-24, Volume: 41, Issue:20, 1998
Synthesis and pharmacology of highly selective carboxy and phosphono isoxazole amino acid AMPA receptor antagonists.Journal of medicinal chemistry, , Apr-12, Volume: 39, Issue:8, 1996
Resolution, absolute stereochemistry, and pharmacology of the S-(+)- and R-(-)-isomers of the apparent partial AMPA receptor agonist (R,S)-2-amino-3-(3-hydroxy-5-phenylisoxazol-4-yl)propionic acid [(R,S)-APPA].Journal of medicinal chemistry, , Apr-01, Volume: 37, Issue:7, 1994
Use of the 4-Hydroxytriazole Moiety as a Bioisosteric Tool in the Development of Ionotropic Glutamate Receptor Ligands.Journal of medicinal chemistry, , 05-09, Volume: 62, Issue:9, 2019
4-hydroxy-1,2,5-oxadiazol-3-yl moiety as bioisoster of the carboxy function. Synthesis, ionization constants, and molecular pharmacological characterization at ionotropic glutamate receptors of compounds related to glutamate and its homologues.Journal of medicinal chemistry, , May-27, Volume: 53, Issue:10, 2010
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DL-tetrazol-5-ylglycine, a highly potent NMDA agonist: its synthesis and NMDA receptor efficacy.Journal of medicinal chemistry, , Nov-27, Volume: 35, Issue:24, 1992
2,4-Dihydro-3H-1,2,4-triazol-3-ones as anticonvulsant agents.Journal of medicinal chemistry, , Volume: 33, Issue:10, 1990
Relationship between structure, conformational flexibility, and biological activity of agonists and antagonists at the N-methyl-D-aspartic acid subtype of excitatory amino acid receptors.Journal of medicinal chemistry, , Volume: 33, Issue:1, 1990
New and versatile approaches to the synthesis of CPP-related competitive NMDA antagonists. Preliminary structure-activity relationships and pharmacological evaluation.Journal of medicinal chemistry, , Volume: 33, Issue:10, 1990
Structure-activity relationships of 4-hydroxy-3-nitroquinolin-2(1H)-ones as novel antagonists at the glycine site of N-methyl-D-aspartate receptors.Journal of medicinal chemistry, , Nov-08, Volume: 39, Issue:23, 1996
Synthesis and structure-activity relationships of substituted 1,4-dihydroquinoxaline-2,3-diones: antagonists of N-methyl-D-aspartate (NMDA) receptor glycine sites and non-NMDA glutamate receptors.Journal of medicinal chemistry, , Oct-27, Volume: 38, Issue:22, 1995
The glycine site on the NMDA receptor: structure-activity relationships and therapeutic potential.Journal of medicinal chemistry, , Nov-25, Volume: 37, Issue:24, 1994
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.Journal of medicinal chemistry, , Volume: 34, Issue:4, 1991
Diverse Aromatic Metabolites in the Solitary Tunicate Journal of natural products, , 10-23, Volume: 83, Issue:10, 2020
Use of the 4-Hydroxytriazole Moiety as a Bioisosteric Tool in the Development of Ionotropic Glutamate Receptor Ligands.Journal of medicinal chemistry, , 05-09, Volume: 62, Issue:9, 2019
4-hydroxy-1,2,5-oxadiazol-3-yl moiety as bioisoster of the carboxy function. Synthesis, ionization constants, and molecular pharmacological characterization at ionotropic glutamate receptors of compounds related to glutamate and its homologues.Journal of medicinal chemistry, , May-27, Volume: 53, Issue:10, 2010
Chemo-enzymatic synthesis of (2S,4R)-2-amino-4-(3-(2,2-diphenylethylamino)-3-oxopropyl)pentanedioic acid: a novel selective inhibitor of human excitatory amino acid transporter subtype 2.Journal of medicinal chemistry, , Jul-24, Volume: 51, Issue:14, 2008
N-Hydroxypyrazolyl glycine derivatives as selective N-methyl-D-aspartic acid receptor ligands.Journal of medicinal chemistry, , Jul-24, Volume: 51, Issue:14, 2008
Synthesis, molecular modeling studies, and preliminary pharmacological characterization of all possible 2-(2'-sulfonocyclopropyl)glycine stereoisomers as conformationally constrained L-homocysteic acid analogs.Journal of medicinal chemistry, , Sep-20, Volume: 50, Issue:19, 2007
A rational approach to the design of selective substrates and potent nontransportable inhibitors of the excitatory amino acid transporter EAAC1 (EAAT3). new glutamate and aspartate analogues as potential neuroprotective agents.Journal of medicinal chemistry, , Aug-02, Volume: 44, Issue:16, 2001
DL-tetrazol-5-ylglycine, a highly potent NMDA agonist: its synthesis and NMDA receptor efficacy.Journal of medicinal chemistry, , Nov-27, Volume: 35, Issue:24, 1992
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.Journal of medicinal chemistry, , Dec-11, Volume: 35, Issue:25, 1992
New and versatile approaches to the synthesis of CPP-related competitive NMDA antagonists. Preliminary structure-activity relationships and pharmacological evaluation.Journal of medicinal chemistry, , Volume: 33, Issue:10, 1990
Discovery of {1-[4-(2-{hexahydropyrrolo[3,4-c]pyrrol-2(1H)-yl}-1H-benzimidazol-1-yl)piperidin-1-yl]cyclooctyl}methanol, systemically potent novel non-peptide agonist of nociceptin/orphanin FQ receptor as analgesic for the treatment of neuropathic pain: deBioorganic & medicinal chemistry, , Nov-01, Volume: 18, Issue:21, 2010
Design, synthesis, SAR, and biological evaluation of highly potent benzimidazole-spaced phosphono-alpha-amino acid competitive NMDA antagonists of the AP-6 type.Journal of medicinal chemistry, , May-10, Volume: 44, Issue:10, 2001
Design and synthesis of [2-(8,9-dioxo-2,6-diazabicyclo[5.2.0]non-1(7)-en-2-yl)-ethyl]phosphonic acid (EAA-090), a potent N-methyl-D-aspartate antagonist, via the use of 3-cyclobutene-1,2-dione as an achiral alpha-amino acid bioisostere.Journal of medicinal chemistry, , Jan-15, Volume: 41, Issue:2, 1998
Potent quinoxaline-spaced phosphono alpha-amino acids of the AP-6 type as competitive NMDA antagonists: synthesis and biological evaluation.Journal of medicinal chemistry, , Feb-05, Volume: 36, Issue:3, 1993
6-substituted decahydroisoquinoline-3-carboxylic acids as potent and selective conformationally constrained NMDA receptor antagonists.Journal of medicinal chemistry, , Sep-18, Volume: 35, Issue:19, 1992
Modeling of competitive phosphono amino acid NMDA receptor antagonists.Journal of medicinal chemistry, , May-01, Volume: 35, Issue:9, 1992
4-(Tetrazolylalkyl)piperidine-2-carboxylic acids. Potent and selective N-methyl-D-aspartic acid receptor antagonists with a short duration of action.Journal of medicinal chemistry, , Volume: 34, Issue:1, 1991
Synthesis and biological evaluation of cyclopropyl analogues of 2-amino-5-phosphonopentanoic acid.Journal of medicinal chemistry, , Volume: 34, Issue:1, 1991
New and versatile approaches to the synthesis of CPP-related competitive NMDA antagonists. Preliminary structure-activity relationships and pharmacological evaluation.Journal of medicinal chemistry, , Volume: 33, Issue:10, 1990
4-(Phosphonoalkyl)- and 4-(phosphonoalkenyl)-2-piperidinecarboxylic acids: synthesis, activity at N-methyl-D-aspartic acid receptors, and anticonvulsant activity.Journal of medicinal chemistry, , Volume: 32, Issue:9, 1989
[no title available]Journal of medicinal chemistry, , 01-13, Volume: 65, Issue:1, 2022
Design, synthesis and structure-activity relationships of novel strychnine-insensitive glycine receptor ligands.Bioorganic & medicinal chemistry letters, , May-17, Volume: 9, Issue:10, 1999
The glycine site on the NMDA receptor: structure-activity relationships and therapeutic potential.Journal of medicinal chemistry, , Nov-25, Volume: 37, Issue:24, 1994
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.Journal of medicinal chemistry, , Oct-24, Volume: 40, Issue:22, 1997
Structure-activity relationships of 4-hydroxy-3-nitroquinolin-2(1H)-ones as novel antagonists at the glycine site of N-methyl-D-aspartate receptors.Journal of medicinal chemistry, , Nov-08, Volume: 39, Issue:23, 1996
Synthesis and structure-activity relationships of substituted 1,4-dihydroquinoxaline-2,3-diones: antagonists of N-methyl-D-aspartate (NMDA) receptor glycine sites and non-NMDA glutamate receptors.Journal of medicinal chemistry, , Oct-27, Volume: 38, Issue:22, 1995
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.Journal of medicinal chemistry, , Volume: 34, Issue:4, 1991
alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) antagonists: from bench to bedside.Journal of medicinal chemistry, , Aug-12, Volume: 53, Issue:15, 2010
Bioisosteres of 9-carboxymethyl-4-oxo-imidazo[1,2-a]indeno-[1,2-e]pyrazin-2-carboxylic acid derivatives. Progress towards selective, potent in vivo AMPA antagonists with longer durations of action.Bioorganic & medicinal chemistry letters, , Jan-22, Volume: 11, Issue:2, 2001
Synthesis of anticonvulsive AMPA antagonists: 4-oxo-10-substituted-imidaz.Bioorganic & medicinal chemistry letters, , May-07, Volume: 11, Issue:9, 2001
Synthesis and potent anticonvulsant activities of 4-oxo-imidazo[1,2-a]inden.Bioorganic & medicinal chemistry letters, , Dec-18, Volume: 10, Issue:24, 2000
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.Bioorganic & medicinal chemistry letters, , May-15, Volume: 10, Issue:10, 2000
Spiro-imidazo[1,2-a]indeno[1,2-e]pyrazine-4-one derivatives are mixed AMPA and NMDA glycine-site antagonists active in vivo.Bioorganic & medicinal chemistry letters, , Oct-18, Volume: 9, Issue:20, 1999
Structure-activity studies of 6-(tetrazolylalkyl)-substituted decahydroisoquinoline-3-carboxylic acid AMPA receptor antagonists. 1. Effects of stereochemistry, chain length, and chain substitution.Journal of medicinal chemistry, , May-24, Volume: 39, Issue:11, 1996
Structure-activity studies of 6-substituted decahydroisoquinoline-3-carboxylic acid AMPA receptor antagonists. 2. Effects of distal acid bioisosteric substitution, absolute stereochemical preferences, and in vivo activity.Journal of medicinal chemistry, , May-24, Volume: 39, Issue:11, 1996
(3SR,4aRS,6SR,8aRS)-6-(1H-tetrazol-5-yl)decahydroisoquinoline-3-carboxylic acid, a novel, competitive, systemically active NMDA and AMPA receptor antagonist.Journal of medicinal chemistry, , Dec-08, Volume: 38, Issue:25, 1995
Augmentation of Anticancer Drug Efficacy in Murine Hepatocellular Carcinoma Cells by a Peripherally Acting Competitive N-Methyl-d-aspartate (NMDA) Receptor Antagonist.Journal of medicinal chemistry, , 12-14, Volume: 60, Issue:23, 2017
Synthesis and anticonvulsant activity of novel bicyclic acidic amino acids.Journal of medicinal chemistry, , Jul-03, Volume: 46, Issue:14, 2003
Benzimidazole-2-carboxamides as novel NR2B selective NMDA receptor antagonists.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 16, Issue:17, 2006
Indole-2-carboxamides as novel NR2B selective NMDA receptor antagonists.Bioorganic & medicinal chemistry letters, , Nov-03, Volume: 13, Issue:21, 2003
1,2,3-triazolyl amino acids as AMPA receptor ligands.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 20, Issue:24, 2010
Synthesis and enantiopharmacology of new AMPA-kainate receptor agonists.Journal of medicinal chemistry, , Oct-07, Volume: 42, Issue:20, 1999
Synthesis and pharmacology of a new AMPA-kainate receptor agonist with potent convulsant activity.Journal of medicinal chemistry, , Sep-24, Volume: 41, Issue:20, 1998
N-methyl-D-aspartic acid receptor agonists: resolution, absolute stereochemistry, and pharmacology of the enantiomers of 2-amino-2-(3-hydroxy-5-methyl-4-isoxazolyl)acetic acid.Journal of medicinal chemistry, , Jan-05, Volume: 39, Issue:1, 1996
A new highly selective metabotropic excitatory amino acid agonist: 2-amino-4-(3-hydroxy-5-methylisoxazol-4-yl)butyric acid.Journal of medicinal chemistry, , Aug-02, Volume: 39, Issue:16, 1996
Synthesis and structure-activity studies on acidic amino acids and related diacids as NMDA receptor ligands.Journal of medicinal chemistry, , Sep-30, Volume: 37, Issue:20, 1994
N-methyl-D-aspartic acid receptor agonists: resolution, absolute stereochemistry, and pharmacology of the enantiomers of 2-amino-2-(3-hydroxy-5-methyl-4-isoxazolyl)acetic acid.Journal of medicinal chemistry, , Jan-05, Volume: 39, Issue:1, 1996
A new highly selective metabotropic excitatory amino acid agonist: 2-amino-4-(3-hydroxy-5-methylisoxazol-4-yl)butyric acid.Journal of medicinal chemistry, , Aug-02, Volume: 39, Issue:16, 1996
Synthesis and structure-activity studies on acidic amino acids and related diacids as NMDA receptor ligands.Journal of medicinal chemistry, , Sep-30, Volume: 37, Issue:20, 1994
A novel class of negative allosteric modulators of NMDA receptor function.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 25, Issue:23, 2015
Chiral synthesis and pharmacological evaluation of NPS 1407: a potent, stereoselective NMDA receptor antagonist.Bioorganic & medicinal chemistry letters, , Nov-06, Volume: 10, Issue:21, 2000
Synthesis, biological activity, and absolute stereochemical assignment of NPS 1392: a potent and stereoselective NMDA receptor antagonist.Bioorganic & medicinal chemistry letters, , Jul-19, Volume: 9, Issue:14, 1999
Novel NMDA antagonists: replacement of the pyridinium ring of 6,11-ethanobenzo[b]quinolizinium cations with heteroisoquinolinium cations.Journal of medicinal chemistry, , May-12, Volume: 38, Issue:10, 1995
Synthesis and evaluation of 6,11-ethanohexahydrobenzo[b]quinolizidines: a new class of noncompetitive N-methyl-D-aspartate antagonists.Journal of medicinal chemistry, , Jun-23, Volume: 38, Issue:13, 1995
Synthesis, resolution, and SAR of (+/-)-2-amino-N-methyl-alpha-(3-methyl-2-thienyl)benzeneethanamine++ + and related analogs as noncompetitive NMDA antagonists with neuroprotective properties.Journal of medicinal chemistry, , Sep-16, Volume: 37, Issue:19, 1994
Synthesis and pharmacological evaluation of 4a-phenanthrenamine derivatives acting at the phencyclidine binding site of the N-methyl-D-aspartate receptor complex.Journal of medicinal chemistry, , Jul-09, Volume: 36, Issue:14, 1993
Synthesis and binding properties of MK-801 isothiocyanates; (+)-3-isothiocyanato-5-methyl-10,11-dihydro-5H-dibenzo[a,d]cyclohepten- 5,10-imine hydrochloride: a new, potent and selective electrophilic affinity ligand for the NMDA receptor-coupled phencycliJournal of medicinal chemistry, , Aug-20, Volume: 36, Issue:17, 1993
Synthesis and evaluation of 3-substituted 17-methylmorphinan analogs as potential anticonvulsant agents.Journal of medicinal chemistry, , Oct-30, Volume: 35, Issue:22, 1992
Synthesis and pharmacological evaluation of a series of dibenzo[a,d]cycloalkenimines as N-methyl-D-aspartate antagonists.Journal of medicinal chemistry, , Volume: 33, Issue:2, 1990
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.Journal of medicinal chemistry, , Jun-15, Volume: 43, Issue:12, 2000
The glycine site on the NMDA receptor: structure-activity relationships and therapeutic potential.Journal of medicinal chemistry, , Nov-25, Volume: 37, Issue:24, 1994
alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) antagonists: from bench to bedside.Journal of medicinal chemistry, , Aug-12, Volume: 53, Issue:15, 2010
Synthesis of anticonvulsive AMPA antagonists: 4-oxo-10-substituted-imidaz.Bioorganic & medicinal chemistry letters, , May-07, Volume: 11, Issue:9, 2001
3-(2-Carboxyethyl)indole-2-carboxylic Acid Derivatives: Structural Requirements and Properties of Potent Agonists of the Orphan G Protein-Coupled Receptor GPR17.Journal of medicinal chemistry, , 09-27, Volume: 61, Issue:18, 2018
The glycine site on the NMDA receptor: structure-activity relationships and therapeutic potential.Journal of medicinal chemistry, , Nov-25, Volume: 37, Issue:24, 1994
N-(3-Cyano-4,5,6,7-tetrahydro-1-benzothien-2-yl)amides as potent, selective, inhibitors of JNK2 and JNK3.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 17, Issue:5, 2007
alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) antagonists: from bench to bedside.Journal of medicinal chemistry, , Aug-12, Volume: 53, Issue:15, 2010
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.Journal of medicinal chemistry, , Sep-13, Volume: 44, Issue:19, 2001
Bioisosteres of 9-carboxymethyl-4-oxo-imidazo[1,2-a]indeno-[1,2-e]pyrazin-2-carboxylic acid derivatives. Progress towards selective, potent in vivo AMPA antagonists with longer durations of action.Bioorganic & medicinal chemistry letters, , Jan-22, Volume: 11, Issue:2, 2001
Synthesis and potent anticonvulsant activities of 4-oxo-imidazo[1,2-a]inden.Bioorganic & medicinal chemistry letters, , Dec-18, Volume: 10, Issue:24, 2000
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.Bioorganic & medicinal chemistry letters, , May-15, Volume: 10, Issue:10, 2000
8-(1H-imidazol-1-yl)-7-nitro-4(5H)-imidazo[1,2-alpha]quinoxalinone and related compounds: synthesis and structure-activity relationships for the AMPA-type non-NMDA receptor.Journal of medicinal chemistry, , Jun-20, Volume: 40, Issue:13, 1997
Structure-activity relationships in a series of 2(1H)-quinolones bearing different acidic function in the 3-position: 6,7-dichloro-2(1H)-oxoquinoline-3-phosphonic acid, a new potent and selective AMPA/kainate antagonist with neuroprotective properties.Journal of medicinal chemistry, , Jan-05, Volume: 39, Issue:1, 1996
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.Journal of medicinal chemistry, , Dec-11, Volume: 35, Issue:25, 1992
alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) antagonists: from bench to bedside.Journal of medicinal chemistry, , Aug-12, Volume: 53, Issue:15, 2010
The glycine site on the NMDA receptor: structure-activity relationships and therapeutic potential.Journal of medicinal chemistry, , Nov-25, Volume: 37, Issue:24, 1994
Synthesis and excitatory amino acid pharmacology of a series of heterocyclic-fused quinoxalinones and quinazolinones.Journal of medicinal chemistry, , Sep-04, Volume: 35, Issue:18, 1992
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.Journal of medicinal chemistry, , Volume: 34, Issue:4, 1991
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.Journal of medicinal chemistry, , Oct-24, Volume: 40, Issue:22, 1997
Synthesis and structure-activity relationships of substituted 1,4-dihydroquinoxaline-2,3-diones: antagonists of N-methyl-D-aspartate (NMDA) receptor glycine sites and non-NMDA glutamate receptors.Journal of medicinal chemistry, , Oct-27, Volume: 38, Issue:22, 1995
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.Journal of medicinal chemistry, , Volume: 34, Issue:4, 1991
[no title available]Journal of medicinal chemistry, , 07-23, Volume: 63, Issue:14, 2020
Synthesis and structure activity relationship of tetrahydroisoquinoline-based potentiators of GluN2C and GluN2D containing N-methyl-D-aspartate receptors.Journal of medicinal chemistry, , Jul-11, Volume: 56, Issue:13, 2013
Development of 2'-substituted (2S,1'R,2'S)-2-(carboxycyclopropyl)glycine analogues as potent N-methyl-d-aspartic acid receptor agonists.Journal of medicinal chemistry, , May-23, Volume: 56, Issue:10, 2013
Synthesis, molecular modeling studies, and preliminary pharmacological characterization of all possible 2-(2'-sulfonocyclopropyl)glycine stereoisomers as conformationally constrained L-homocysteic acid analogs.Journal of medicinal chemistry, , Sep-20, Volume: 50, Issue:19, 2007
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 antagJournal of medicinal chemistry, , Feb-24, Volume: 48, Issue:4, 2005
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 antagJournal of medicinal chemistry, , Feb-24, Volume: 48, Issue:4, 2005
Structure-activity relationships of 1,4-dihydro-(1H,4H)-quinoxaline-2,3-diones as N-methyl-D-aspartate (glycine site) receptor antagonists. 1. Heterocyclic substituted 5-alkyl derivatives.Journal of medicinal chemistry, , Jun-07, Volume: 44, Issue:12, 2001
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.Journal of medicinal chemistry, , Jun-15, Volume: 43, Issue:12, 2000
Effect of plasma protein binding on in vivo activity and brain penetration of glycine/NMDA receptor antagonists.Journal of medicinal chemistry, , Dec-05, Volume: 40, Issue:25, 1997
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.Journal of medicinal chemistry, , Oct-24, Volume: 40, Issue:22, 1997
Synthesis and structure-activity relationships of substituted 1,4-dihydroquinoxaline-2,3-diones: antagonists of N-methyl-D-aspartate (NMDA) receptor glycine sites and non-NMDA glutamate receptors.Journal of medicinal chemistry, , Oct-27, Volume: 38, Issue:22, 1995
alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) antagonists: from bench to bedside.Journal of medicinal chemistry, , Aug-12, Volume: 53, Issue:15, 2010
Bioisosteres of 9-carboxymethyl-4-oxo-imidazo[1,2-a]indeno-[1,2-e]pyrazin-2-carboxylic acid derivatives. Progress towards selective, potent in vivo AMPA antagonists with longer durations of action.Bioorganic & medicinal chemistry letters, , Jan-22, Volume: 11, Issue:2, 2001
Synthesis of anticonvulsive AMPA antagonists: 4-oxo-10-substituted-imidaz.Bioorganic & medicinal chemistry letters, , May-07, Volume: 11, Issue:9, 2001
Synthesis and potent anticonvulsant activities of 4-oxo-imidazo[1,2-a]inden.Bioorganic & medicinal chemistry letters, , Dec-18, Volume: 10, Issue:24, 2000
8-Methylureido-4,5-dihydro-4-oxo-10H-imidazo[1,2-a]indeno[1,2-e]pyrazines: highly potent in vivo AMPA antagonists.Bioorganic & medicinal chemistry letters, , Mar-20, Volume: 10, Issue:6, 2000
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.Bioorganic & medicinal chemistry letters, , May-15, Volume: 10, Issue:10, 2000
Spiro-imidazo[1,2-a]indeno[1,2-e]pyrazine-4-one derivatives are mixed AMPA and NMDA glycine-site antagonists active in vivo.Bioorganic & medicinal chemistry letters, , Oct-18, Volume: 9, Issue:20, 1999
8-(1H-imidazol-1-yl)-7-nitro-4(5H)-imidazo[1,2-alpha]quinoxalinone and related compounds: synthesis and structure-activity relationships for the AMPA-type non-NMDA receptor.Journal of medicinal chemistry, , Jun-20, Volume: 40, Issue:13, 1997
Structure-activity relationships in a series of 2(1H)-quinolones bearing different acidic function in the 3-position: 6,7-dichloro-2(1H)-oxoquinoline-3-phosphonic acid, a new potent and selective AMPA/kainate antagonist with neuroprotective properties.Journal of medicinal chemistry, , Jan-05, Volume: 39, Issue:1, 1996
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 antagJournal of medicinal chemistry, , Feb-24, Volume: 48, Issue:4, 2005
Enantiomerically pure tetrahydroquinoline derivatives as in vivo potent antagonists of the glycine binding site associated to the NMDA receptor.Bioorganic & medicinal chemistry letters, , Nov-03, Volume: 13, Issue:21, 2003
Effect of plasma protein binding on in vivo activity and brain penetration of glycine/NMDA receptor antagonists.Journal of medicinal chemistry, , Dec-05, Volume: 40, Issue:25, 1997
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 antagJournal of medicinal chemistry, , Feb-24, Volume: 48, Issue:4, 2005
The glycine site on the NMDA receptor: structure-activity relationships and therapeutic potential.Journal of medicinal chemistry, , Nov-25, Volume: 37, Issue:24, 1994
Tricyclic quinoxalinediones: 5,6-dihydro-1H-pyrrolo[1,2,3-de] quinoxaline-2,3-diones and 6,7-dihydro-1H,5H-pyrido[1,2,3-de] quinoxaline-2,3-diones as potent antagonists for the glycine binding site of the NMDA receptor.Journal of medicinal chemistry, , Nov-11, Volume: 37, Issue:23, 1994
4-Amido-2-carboxytetrahydroquinolines. Structure-activity relationships for antagonism at the glycine site of the NMDA receptor.Journal of medicinal chemistry, , May-29, Volume: 35, Issue:11, 1992
Benzimidazole-2-carboxamides as novel NR2B selective NMDA receptor antagonists.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 16, Issue:17, 2006
Indole-2-carboxamides as novel NR2B selective NMDA receptor antagonists.Bioorganic & medicinal chemistry letters, , Nov-03, Volume: 13, Issue:21, 2003
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.Bioorganic & medicinal chemistry letters, , Jun-07, Volume: 9, Issue:11, 1999
A method for designing conformationally restricted analogues based on allylic strain: synthesis of a novel class of noncompetitive NMDA receptor antagonists having the acrylamide structure.Journal of medicinal chemistry, , Dec-04, Volume: 46, Issue:25, 2003
Synthesis and biological activity of conformationally restricted analogues of milnacipran: (1S, 2R)-1-phenyl-2-[(R)-1-amino-2-propynyl]-N,N- diethylcyclopropanecarboxamide is a novel class of NMDA receptor channel blocker.Journal of medicinal chemistry, , Aug-27, Volume: 41, Issue:18, 1998
Synthesis and biological activity of conformationally restricted analogs of milnacipran: (1S,2R)-1-phenyl-2-[(S)-1-aminopropyl]-N,N-diethylcyclopropanecarboxami de, an efficient noncompetitive N-methyl-D-aspartic acid receptor antagonist.Journal of medicinal chemistry, , Nov-22, Volume: 39, Issue:24, 1996
(+/-)-(Z)-2-(aminomethyl)-1-phenylcyclopropanecarboxamide derivatives as a new prototype of NMDA receptor antagonists.Journal of medicinal chemistry, , Jul-21, Volume: 38, Issue:15, 1995
Prodrugs of perzinfotel with improved oral bioavailability.Journal of medicinal chemistry, , Feb-12, Volume: 52, Issue:3, 2009
Design and synthesis of [2-(8,9-dioxo-2,6-diazabicyclo[5.2.0]non-1(7)-en-2-yl)-ethyl]phosphonic acid (EAA-090), a potent N-methyl-D-aspartate antagonist, via the use of 3-cyclobutene-1,2-dione as an achiral alpha-amino acid bioisostere.Journal of medicinal chemistry, , Jan-15, Volume: 41, Issue:2, 1998
Kynurenic acid amides as novel NR2B selective NMDA receptor antagonists.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 17, Issue:2, 2007
Benzimidazole-2-carboxamides as novel NR2B selective NMDA receptor antagonists.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 16, Issue:17, 2006
Indole-2-carboxamidines as novel NR2B selective NMDA receptor antagonists.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 15, Issue:24, 2005
Indole-2-carboxamides as novel NR2B selective NMDA receptor antagonists.Bioorganic & medicinal chemistry letters, , Nov-03, Volume: 13, Issue:21, 2003
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.Journal of medicinal chemistry, , Sep-13, Volume: 44, Issue:19, 2001
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 antagJournal of medicinal chemistry, , Feb-24, Volume: 48, Issue:4, 2005
Effect of plasma protein binding on in vivo activity and brain penetration of glycine/NMDA receptor antagonists.Journal of medicinal chemistry, , Dec-05, Volume: 40, Issue:25, 1997
4-substituted-3-phenylquinolin-2(1H)-ones: acidic and nonacidic glycine site N-methyl-D-aspartate antagonists with in vivo activity.Journal of medicinal chemistry, , Feb-28, Volume: 40, Issue:5, 1997
The glycine site on the NMDA receptor: structure-activity relationships and therapeutic potential.Journal of medicinal chemistry, , Nov-25, Volume: 37, Issue:24, 1994
Effect of plasma protein binding on in vivo activity and brain penetration of glycine/NMDA receptor antagonists.Journal of medicinal chemistry, , Dec-05, Volume: 40, Issue:25, 1997
The glycine site on the NMDA receptor: structure-activity relationships and therapeutic potential.Journal of medicinal chemistry, , Nov-25, Volume: 37, Issue:24, 1994
3-Acyl-4-hydroxyquinolin-2(1H)-ones. Systemically active anticonvulsants acting by antagonism at the glycine site of the N-methyl-D-aspartate receptor complex.Journal of medicinal chemistry, , Oct-29, Volume: 36, Issue:22, 1993
Effect of plasma protein binding on in vivo activity and brain penetration of glycine/NMDA receptor antagonists.Journal of medicinal chemistry, , Dec-05, Volume: 40, Issue:25, 1997
4-substituted-3-phenylquinolin-2(1H)-ones: acidic and nonacidic glycine site N-methyl-D-aspartate antagonists with in vivo activity.Journal of medicinal chemistry, , Feb-28, Volume: 40, Issue:5, 1997