Page last updated: 2024-08-07 16:07:17
Glutamate receptor 1
A glutamate receptor 1 that is encoded in the genome of rat. [OMA:P19490, PRO:DNx]
Synonyms
GluR-1;
AMPA-selective glutamate receptor 1;
GluR-A;
GluR-K1;
Glutamate receptor ionotropic, AMPA 1;
GluA1
Research
Bioassay Publications (75)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 1 (1.33) | 18.7374 |
| 1990's | 32 (42.67) | 18.2507 |
| 2000's | 34 (45.33) | 29.6817 |
| 2010's | 8 (10.67) | 24.3611 |
| 2020's | 0 (0.00) | 2.80 |
Compounds (179)
Drugs with Potency Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| dihydroxyphenylalanine | Rattus norvegicus (Norway rat) | Potency | 0.1585 | 1 | 0 |
| thioctic acid | Rattus norvegicus (Norway rat) | Potency | 0.5012 | 1 | 0 |
| catechin | Rattus norvegicus (Norway rat) | Potency | 2.5119 | 1 | 0 |
| 5,7-Dihydroxy-2-(3,4,5-trihydroxyphenyl)-3,4-dihydro-2H-chromen-3-yl 3,4,5-trihydroxybenzoate | Rattus norvegicus (Norway rat) | Potency | 0.0891 | 1 | 0 |
| 5-fluoroindole-2-carboxylic acid | Rattus norvegicus (Norway rat) | Potency | 0.1413 | 1 | 0 |
| aurintricarboxylic acid | Rattus norvegicus (Norway rat) | Potency | 0.0562 | 1 | 0 |
| dephostatin | Rattus norvegicus (Norway rat) | Potency | 25.1189 | 1 | 0 |
| diuron | Rattus norvegicus (Norway rat) | Potency | 31.6228 | 1 | 0 |
| ellipticine | Rattus norvegicus (Norway rat) | Potency | 7.9433 | 1 | 0 |
| 2,2',3,3',4,4'-hexahydroxy-1,1'-biphenyl-6,6'-dimethanol dimethyl ether | Rattus norvegicus (Norway rat) | Potency | 0.3162 | 1 | 0 |
| hycanthone | Rattus norvegicus (Norway rat) | Potency | 15.8489 | 1 | 0 |
| juglone | Rattus norvegicus (Norway rat) | Potency | 10.0000 | 1 | 0 |
| nimesulide | Rattus norvegicus (Norway rat) | Potency | 31.6228 | 1 | 0 |
| oxidopamine | Rattus norvegicus (Norway rat) | Potency | 0.5623 | 1 | 0 |
| quinone | Rattus norvegicus (Norway rat) | Potency | 7.0795 | 1 | 0 |
| protoporphyrin ix | Rattus norvegicus (Norway rat) | Potency | 11.2947 | 1 | 0 |
| 1,2,5,8-tetrahydroxy anthraquinone | Rattus norvegicus (Norway rat) | Potency | 3.9811 | 1 | 0 |
| quinacrine monohydrochloride | Rattus norvegicus (Norway rat) | Potency | 15.8489 | 1 | 0 |
| alizarin | Rattus norvegicus (Norway rat) | Potency | 15.8489 | 1 | 0 |
| acriflavine chloride | Rattus norvegicus (Norway rat) | Potency | 6.3096 | 1 | 0 |
| suramin sodium | Rattus norvegicus (Norway rat) | Potency | 8.9125 | 1 | 0 |
| eriodictyol | Rattus norvegicus (Norway rat) | Potency | 15.8489 | 1 | 0 |
| carmine | Rattus norvegicus (Norway rat) | Potency | 3.1623 | 1 | 0 |
| pontamine sky blue | Rattus norvegicus (Norway rat) | Potency | 12.5893 | 1 | 0 |
| daunorubicin | Rattus norvegicus (Norway rat) | Potency | 10.0000 | 1 | 0 |
| idarubicin | Rattus norvegicus (Norway rat) | Potency | 15.8489 | 1 | 0 |
| avobenzone | Rattus norvegicus (Norway rat) | Potency | 7.9433 | 1 | 0 |
| mitoxantrone hydrochloride | Rattus norvegicus (Norway rat) | Potency | 1.9953 | 1 | 0 |
| cy 208-243 | Rattus norvegicus (Norway rat) | Potency | 25.1189 | 1 | 0 |
| D-dopa | Rattus norvegicus (Norway rat) | Potency | 7.3842 | 1 | 0 |
| 2-(4-hydroxyphenyl)-5,6,7,8-tetrahydroxy-4H-1-benzopyran-4-one | Rattus norvegicus (Norway rat) | Potency | 0.5012 | 1 | 0 |
| 6-hydroxydopa | Rattus norvegicus (Norway rat) | Potency | 0.7943 | 1 | 0 |
| pyrophen | Rattus norvegicus (Norway rat) | Potency | 15.8489 | 1 | 0 |
| sch 45752 | Rattus norvegicus (Norway rat) | Potency | 19.9526 | 1 | 0 |
| n-phthaloylglutamic acid | Rattus norvegicus (Norway rat) | Potency | 28.1838 | 1 | 0 |
| sb 216763 | Rattus norvegicus (Norway rat) | Potency | 25.1189 | 1 | 0 |
| fonsecin | Rattus norvegicus (Norway rat) | Potency | 14.1254 | 1 | 0 |
| Poriol | Rattus norvegicus (Norway rat) | Potency | 4.4668 | 1 | 0 |
| 3-(2-Methylpropanoyloxy)-8-(2-methylbutanoyloxy)-9,10-epoxy-p-mentha-1,3,5-triene | Rattus norvegicus (Norway rat) | Potency | 11.2202 | 1 | 0 |
| 4,5,7-trihydroxy-9,10-dioxo-2-anthracenecarboxylic acid | Rattus norvegicus (Norway rat) | Potency | 14.1254 | 1 | 0 |
| carubicin | Rattus norvegicus (Norway rat) | Potency | 7.9433 | 1 | 0 |
| 3-Hydroxy-1-(4-hydroxyphenyl)-1-propanone | Rattus norvegicus (Norway rat) | Potency | 1.2589 | 1 | 0 |
| 2-[[2-methyl-5-(3-methyl-4-oxo-1-phthalazinyl)phenyl]sulfonylamino]acetic acid ethyl ester | Rattus norvegicus (Norway rat) | Potency | 10.0000 | 1 | 0 |
| caffeic acid | Rattus norvegicus (Norway rat) | Potency | 35.4813 | 1 | 0 |
| (2'-(4-aminophenyl)-(2,5'-bi-1h-benzimidazol)-5-amine) | Rattus norvegicus (Norway rat) | Potency | 15.8489 | 1 | 0 |
| 3-[[2-[[6-fluoro-2-(4-fluorophenyl)-4-quinazolinyl]thio]-1-oxoethyl]amino]benzoic acid | Rattus norvegicus (Norway rat) | Potency | 39.8107 | 1 | 0 |
| N-(2-furanylmethyl)-2-(4-oxo-6-phenyl-3-thieno[2,3-d]pyrimidinyl)acetamide | Rattus norvegicus (Norway rat) | Potency | 8.9125 | 1 | 0 |
| N-[4-[[[(5-bromo-2-furanyl)-oxomethyl]hydrazo]-oxomethyl]phenyl]benzamide | Rattus norvegicus (Norway rat) | Potency | 15.8489 | 1 | 0 |
| N-cyclohexyl-2-[(8-methoxy-6-oxo-3-benzo[c][1]benzopyranyl)oxy]acetamide | Rattus norvegicus (Norway rat) | Potency | 5.6234 | 1 | 0 |
| N-[2-[(phenylmethyl)amino]-1,3-benzodioxol-2-yl]carbamic acid ethyl ester | Rattus norvegicus (Norway rat) | Potency | 28.1838 | 1 | 0 |
| N-[2-(propan-2-ylamino)-1,3-benzodioxol-2-yl]carbamic acid ethyl ester | Rattus norvegicus (Norway rat) | Potency | 0.0631 | 1 | 0 |
| 5-[(4-oxo-2,3-dihydro-1H-cyclopenta[c][1]benzopyran-7-yl)oxymethyl]-2-furancarboxylic acid | Rattus norvegicus (Norway rat) | Potency | 12.5893 | 1 | 0 |
| 2-[3-(2-furanylmethyl)-2,4-dioxo-6,7,8,9-tetrahydro-5H-cyclohepta[2,3]thieno[2,4-b]pyrimidin-1-yl]acetamide | Rattus norvegicus (Norway rat) | Potency | 10.0000 | 1 | 0 |
| 2-[[5-[(1,3-benzothiazol-2-ylthio)methyl]-4-ethyl-1,2,4-triazol-3-yl]thio]-1-(3,4-dihydroxyphenyl)ethanone | Rattus norvegicus (Norway rat) | Potency | 1.0000 | 1 | 0 |
| 2-[[5-(2-fluoroanilino)-1,3,4-thiadiazol-2-yl]thio]-N-(2-furanylmethyl)acetamide | Rattus norvegicus (Norway rat) | Potency | 15.8489 | 1 | 0 |
| 5,6-dichloro-3-pyridinecarboxylic acid [2-(2-furanylmethylamino)-2-oxoethyl] ester | Rattus norvegicus (Norway rat) | Potency | 17.7828 | 1 | 0 |
| 2-phenoxybenzoic acid [2-(2-furanylmethylamino)-2-oxoethyl] ester | Rattus norvegicus (Norway rat) | Potency | 14.1254 | 1 | 0 |
| 4-(dimethylsulfamoyl)benzoic acid [2-(2-furanylmethylamino)-2-oxoethyl] ester | Rattus norvegicus (Norway rat) | Potency | 14.1254 | 1 | 0 |
| 2-[[4-(4-fluorophenyl)-5-pyridin-4-yl-1,2,4-triazol-3-yl]thio]-N-[(2-furanylmethylamino)-oxomethyl]acetamide | Rattus norvegicus (Norway rat) | Potency | 15.8489 | 1 | 0 |
| diphenyleneiodium chloride | Rattus norvegicus (Norway rat) | Potency | 39.8107 | 1 | 0 |
| 1H-benzimidazole-5,6-diamine | Rattus norvegicus (Norway rat) | Potency | 44.6684 | 1 | 0 |
| 2-{5-[2-(Phenylthio)acetyl]-2-thienyl}acetic acid | Rattus norvegicus (Norway rat) | Potency | 17.7828 | 1 | 0 |
| 3-[[sulfanylidene-[[2,2,2-trichloro-1-[[(3-nitrophenyl)-oxomethyl]amino]ethyl]amino]methyl]amino]benzoic acid | Rattus norvegicus (Norway rat) | Potency | 141.2540 | 1 | 0 |
| 5-cyclopentylidene-2-sulfanylidene-4-thiazolidinone | Rattus norvegicus (Norway rat) | Potency | 14.1254 | 1 | 0 |
| k 858 | Rattus norvegicus (Norway rat) | Potency | 1.4125 | 1 | 0 |
| 5,7-dihydroxy-2-(4-hydroxyphenyl)-6-[3,4,5-trihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-2-yl]-8-(3,4,5-trihydroxytetrahydro-2H-pyran-2-yl)-4H-chromen-4-one | Rattus norvegicus (Norway rat) | Potency | 4.4668 | 1 | 0 |
| isovitexin | Rattus norvegicus (Norway rat) | Potency | 12.5893 | 1 | 0 |
| 2-hydroxy-5-[(4-methoxyphenyl)sulfamoyl]benzoic acid [2-[1-(3-bicyclo[2.2.1]heptanyl)ethylamino]-2-oxoethyl] ester | Rattus norvegicus (Norway rat) | Potency | 10.0000 | 1 | 0 |
| 2-(3-oxo-4H-1,4-benzothiazin-2-yl)acetic acid (7-acetamido-2-oxo-1-benzopyran-4-yl)methyl ester | Rattus norvegicus (Norway rat) | Potency | 35.4813 | 1 | 0 |
| gossypetin | Rattus norvegicus (Norway rat) | Potency | 0.5012 | 1 | 0 |
| quercetin 3-o-methyl ether | Rattus norvegicus (Norway rat) | Potency | 10.0000 | 1 | 0 |
| 3-methylkaempferol | Rattus norvegicus (Norway rat) | Potency | 2.8184 | 1 | 0 |
| sulfuretin | Rattus norvegicus (Norway rat) | Potency | 15.8489 | 1 | 0 |
| baicalein | Rattus norvegicus (Norway rat) | Potency | 0.6310 | 1 | 0 |
| fisetin | Rattus norvegicus (Norway rat) | Potency | 0.8913 | 1 | 0 |
| myricetin | Rattus norvegicus (Norway rat) | Potency | 7.0795 | 1 | 0 |
| rosmarinic acid | Rattus norvegicus (Norway rat) | Potency | 0.6310 | 1 | 0 |
| wedelolactone | Rattus norvegicus (Norway rat) | Potency | 4.4668 | 1 | 0 |
| ellagic acid | Rattus norvegicus (Norway rat) | Potency | 0.0141 | 1 | 0 |
| l-2-(carboxypropyl)glycine | Rattus norvegicus (Norway rat) | Potency | 2.5119 | 1 | 0 |
| fumarprotocetraric acid | Rattus norvegicus (Norway rat) | Potency | 11.2202 | 1 | 0 |
| ag 538 | Rattus norvegicus (Norway rat) | Potency | 0.1995 | 1 | 0 |
| 3,3'-di-o-methylellagic acid | Rattus norvegicus (Norway rat) | Potency | 0.4467 | 1 | 0 |
| nf023 | Rattus norvegicus (Norway rat) | Potency | 3.5481 | 1 | 0 |
| nf 449 | Rattus norvegicus (Norway rat) | Potency | 2.5119 | 1 | 0 |
| 2-[[5,6-bis(2-furanyl)-1,2,4-triazin-3-yl]thio]-1-(4-methoxyphenyl)ethanone | Rattus norvegicus (Norway rat) | Potency | 14.1254 | 1 | 0 |
| 1,5-anhydro-1-[2-(3,4-dihydroxyphenyl)-5,7-dihydroxy-4-oxo-4H-chromen-6-yl]hexitol | Rattus norvegicus (Norway rat) | Potency | 3.1623 | 1 | 0 |
| bn82002 | Rattus norvegicus (Norway rat) | Potency | 0.2818 | 1 | 0 |
| biapigenin | Rattus norvegicus (Norway rat) | Potency | 1.9953 | 1 | 0 |
| 5,7-dihydroxy-2-(4-hydroxyphenyl)-4-oxo-4H-1-benzopyran-3-yl 6-O-(6-deoxyhexopyranosyl)hexopyranoside | Rattus norvegicus (Norway rat) | Potency | 3.1623 | 1 | 0 |
| (R)-Bitalin A | Rattus norvegicus (Norway rat) | Potency | 10.0000 | 1 | 0 |
| 5,7-dihydroxy-2-(4-hydroxyphenyl)-4-oxo-4H-1-benzopyran-3-yl 2-O-hexopyranosylhexopyranoside | Rattus norvegicus (Norway rat) | Potency | 17.7828 | 1 | 0 |
| violaceol II | Rattus norvegicus (Norway rat) | Potency | 14.1254 | 1 | 0 |
| cefamandole nafate | Rattus norvegicus (Norway rat) | Potency | 39.8107 | 1 | 0 |
| cephapirin sodium | Rattus norvegicus (Norway rat) | Potency | 7.9433 | 1 | 0 |
| hematein | Rattus norvegicus (Norway rat) | Potency | 1.4125 | 1 | 0 |
| thiolactomycin | Rattus norvegicus (Norway rat) | Potency | 1.9953 | 1 | 0 |
| lomofungin | Rattus norvegicus (Norway rat) | Potency | 17.7828 | 1 | 0 |
| N-(4-methoxyphenyl)-2-[[6-[(4-methylphenyl)sulfonylamino]-4-oxo-1H-pyrimidin-2-yl]thio]acetamide | Rattus norvegicus (Norway rat) | Potency | 39.8107 | 1 | 0 |
| galloflavin | Rattus norvegicus (Norway rat) | Potency | 0.1259 | 1 | 0 |
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| quinolinic acid | Rattus norvegicus (Norway rat) | IC50 | 100.0000 | 1 | 1 |
| 2-amino-5-phosphonovalerate | Rattus norvegicus (Norway rat) | Ki | 100.0000 | 1 | 1 |
| alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid | Rattus norvegicus (Norway rat) | IC50 | 12.6374 | 8 | 8 |
| alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid | Rattus norvegicus (Norway rat) | Ki | 0.0110 | 2 | 2 |
| 3-(2-carboxypiperazin-4-yl)propyl-1-phosphonic acid | Rattus norvegicus (Norway rat) | Ki | 100.0000 | 1 | 1 |
| ibotenic acid | Rattus norvegicus (Norway rat) | IC50 | 76.0000 | 1 | 1 |
| 5,7-dichlorokynurenic acid | Rattus norvegicus (Norway rat) | IC50 | 75.0000 | 1 | 1 |
| 5,7-dichlorokynurenic acid | Rattus norvegicus (Norway rat) | Ki | 38.0000 | 2 | 3 |
| 6,7-dichloroquinoxaline-2,3-dione | Rattus norvegicus (Norway rat) | Ki | 1.6400 | 1 | 1 |
| 7-chlorokynurenic acid | Rattus norvegicus (Norway rat) | IC50 | 153.0000 | 1 | 1 |
| alpha-amino-3-hydroxy-5-tert-butyl-4-isoxazolepropionate | Rattus norvegicus (Norway rat) | IC50 | 30.7750 | 4 | 4 |
| 2-amino-7-phosphonoheptanoic acid | Rattus norvegicus (Norway rat) | Ki | 100.0000 | 1 | 1 |
| gyki 52466 | Rattus norvegicus (Norway rat) | IC50 | 15.3200 | 4 | 5 |
| kynurenic acid | Rattus norvegicus (Norway rat) | IC50 | 101.0000 | 1 | 1 |
| methaqualone | Rattus norvegicus (Norway rat) | IC50 | 10.0000 | 1 | 1 |
| mecloqualone | Rattus norvegicus (Norway rat) | IC50 | 10.0000 | 1 | 1 |
| kainic acid | Rattus norvegicus (Norway rat) | IC50 | 16.2500 | 7 | 8 |
| kainic acid | Rattus norvegicus (Norway rat) | Ki | 0.4770 | 1 | 1 |
| n-methylaspartate | Rattus norvegicus (Norway rat) | IC50 | 100.0000 | 2 | 2 |
| d-glutamate | Rattus norvegicus (Norway rat) | IC50 | 100.0000 | 1 | 1 |
| glutamic acid | Rattus norvegicus (Norway rat) | IC50 | 0.5885 | 4 | 4 |
| glutamic acid | Rattus norvegicus (Norway rat) | Ki | 0.6345 | 2 | 2 |
| quisqualic acid | Rattus norvegicus (Norway rat) | IC50 | 5.1000 | 2 | 3 |
| selfotel | Rattus norvegicus (Norway rat) | Ki | 100.0000 | 1 | 1 |
| sym 2081 | Rattus norvegicus (Norway rat) | IC50 | 100.0000 | 1 | 1 |
| 1-amino-1,3-dicarboxycyclopentane | Rattus norvegicus (Norway rat) | IC50 | 100.0000 | 1 | 1 |
| jstx-3 | Rattus norvegicus (Norway rat) | IC50 | 0.0650 | 1 | 1 |
| argiotoxin-636 | Rattus norvegicus (Norway rat) | IC50 | 60.7378 | 5 | 5 |
| 2-amino-3-(3-(carboxymethoxy)-5-methylisoxazol-4-yl)propionic acid | Rattus norvegicus (Norway rat) | IC50 | 49.0000 | 2 | 2 |
| 5-fluorowillardiine | Rattus norvegicus (Norway rat) | Ki | 0.0029 | 1 | 1 |
| gyki 53655 | Rattus norvegicus (Norway rat) | IC50 | 1.0000 | 1 | 2 |
| 2-amino-3-(3-hydroxy-5-phenylisoxazol-4-yl)propionic acid | Rattus norvegicus (Norway rat) | IC50 | 100.0000 | 1 | 1 |
| 2-amino-3-(3-hydroxy-5-phenylisoxazol-4-yl)propionic acid | Rattus norvegicus (Norway rat) | Ki | 286.0000 | 1 | 1 |
| ly 293558 | Rattus norvegicus (Norway rat) | IC50 | 3.5879 | 10 | 14 |
| 1-naphthylacetylspermine | Rattus norvegicus (Norway rat) | IC50 | 0.6900 | 2 | 2 |
| agatoxin-489 | Rattus norvegicus (Norway rat) | IC50 | 0.0110 | 1 | 1 |
| alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid | Rattus norvegicus (Norway rat) | IC50 | 0.1049 | 7 | 8 |
| alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid | Rattus norvegicus (Norway rat) | Ki | 0.0220 | 2 | 2 |
| philanthotoxin 343 | Rattus norvegicus (Norway rat) | IC50 | 90.9767 | 3 | 3 |
| alpha-amino-3-(hydroxy)-5-methyl-4-isoxazoleacetic acid | Rattus norvegicus (Norway rat) | IC50 | 100.0000 | 3 | 3 |
| homoibotenic acid | Rattus norvegicus (Norway rat) | IC50 | 1.5000 | 1 | 1 |
| rpr 104632 | Rattus norvegicus (Norway rat) | IC50 | 10.0000 | 1 | 1 |
| zk 200775 | Rattus norvegicus (Norway rat) | IC50 | 0.1400 | 1 | 1 |
| eglumetad | Rattus norvegicus (Norway rat) | IC50 | 100.0000 | 1 | 1 |
| mycophenolic acid | Rattus norvegicus (Norway rat) | IC50 | 0.0140 | 1 | 1 |
| mdl29,951 | Rattus norvegicus (Norway rat) | IC50 | 273.0000 | 1 | 1 |
| (S)-ATPA | Rattus norvegicus (Norway rat) | IC50 | 1.8000 | 1 | 1 |
| (S)-ATPA | Rattus norvegicus (Norway rat) | Ki | 2.7800 | 1 | 1 |
| 4-bromohomoibotenic acid, (rs)-isomer | Rattus norvegicus (Norway rat) | IC50 | 0.6500 | 2 | 2 |
| mdl 100453 | Rattus norvegicus (Norway rat) | Ki | 100.0000 | 1 | 1 |
| 4-methylglutamic acid, threo-(l)-isomer | Rattus norvegicus (Norway rat) | IC50 | 10.0000 | 2 | 2 |
| 2,3-dioxo-6-nitro-7-sulfamoylbenzo(f)quinoxaline | Rattus norvegicus (Norway rat) | IC50 | 0.5781 | 14 | 16 |
| 2,3-dioxo-6-nitro-7-sulfamoylbenzo(f)quinoxaline | Rattus norvegicus (Norway rat) | Ki | 0.0883 | 6 | 6 |
| fg 9041 | Rattus norvegicus (Norway rat) | Ki | 0.3600 | 1 | 1 |
| 6-nitro-1,4-dihydroquinoxaline-2,3-dione | Rattus norvegicus (Norway rat) | Ki | 2.0000 | 1 | 1 |
| 2r,4r-4-aminopyrrolidine-2,4-dicarboxylate | Rattus norvegicus (Norway rat) | IC50 | 100.0000 | 1 | 1 |
| cp 99994 | Rattus norvegicus (Norway rat) | IC50 | 0.0006 | 1 | 1 |
| licostinel | Rattus norvegicus (Norway rat) | IC50 | 0.7660 | 1 | 1 |
| lofepramine hydrochloride | Rattus norvegicus (Norway rat) | IC50 | 0.3371 | 7 | 7 |
| lofepramine hydrochloride | Rattus norvegicus (Norway rat) | Ki | 0.0840 | 2 | 2 |
| piriqualone | Rattus norvegicus (Norway rat) | IC50 | 0.4600 | 1 | 1 |
| ubp 302 | Rattus norvegicus (Norway rat) | IC50 | 106.0000 | 2 | 2 |
| ubp 302 | Rattus norvegicus (Norway rat) | Ki | 117.0000 | 1 | 1 |
| gavestinel | Rattus norvegicus (Norway rat) | IC50 | 100.0000 | 1 | 1 |
| ampa, (r)-isomer | Rattus norvegicus (Norway rat) | IC50 | 40.4000 | 2 | 2 |
| tqx 173 | Rattus norvegicus (Norway rat) | Ki | 0.1400 | 4 | 4 |
| cp 465,022 | Rattus norvegicus (Norway rat) | IC50 | 0.0285 | 3 | 6 |
| ly 379268 | Rattus norvegicus (Norway rat) | IC50 | 100.0000 | 1 | 1 |
| ubp296 | Rattus norvegicus (Norway rat) | IC50 | 97.6000 | 1 | 1 |
Drugs with Activation Measurements
Drugs with Other Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| 5,7-dichlorokynurenic acid | Rattus norvegicus (Norway rat) | Kb | 16.5000 | 2 | 2 |
| 6,7-dichloroquinoxaline-2,3-dione | Rattus norvegicus (Norway rat) | Kb | 8.9050 | 2 | 2 |
| 7-chlorokynurenic acid | Rattus norvegicus (Norway rat) | Kb | 35.0000 | 2 | 2 |
| aniracetam | Rattus norvegicus (Norway rat) | EC2x | 1,440.0000 | 1 | 1 |
| aniracetam | Rattus norvegicus (Norway rat) | EC5X | 3,000.0000 | 1 | 2 |
| cyclothiazide | Rattus norvegicus (Norway rat) | EC2x | 1.6000 | 1 | 1 |
| cyclothiazide | Rattus norvegicus (Norway rat) | EC5X | 9.8000 | 1 | 2 |
| diazoxide | Rattus norvegicus (Norway rat) | EC2x | 448.0000 | 1 | 1 |
| diazoxide | Rattus norvegicus (Norway rat) | EC5X | 1,000.0000 | 1 | 2 |
| kynurenic acid | Rattus norvegicus (Norway rat) | Kb | 137.0000 | 2 | 2 |
| 2,3-dihydroxyquinoxaline | Rattus norvegicus (Norway rat) | Kb | 99.1000 | 2 | 2 |
| 6,7-dichloroquinoxaline-2,3-dione | Rattus norvegicus (Norway rat) | Kb | 17.7000 | 2 | 2 |
| acea 1011 | Rattus norvegicus (Norway rat) | Kb | 3.7000 | 1 | 1 |
| zk 200775 | Rattus norvegicus (Norway rat) | Activity | 0.1050 | 1 | 1 |
| (S)-ATPA | Rattus norvegicus (Norway rat) | pKi | 0.0035 | 1 | 1 |
| 2,3-dioxo-6-nitro-7-sulfamoylbenzo(f)quinoxaline | Rattus norvegicus (Norway rat) | Activity | 0.1500 | 1 | 1 |
| 2,3-dioxo-6-nitro-7-sulfamoylbenzo(f)quinoxaline | Rattus norvegicus (Norway rat) | Kb | 2.0000 | 1 | 1 |
| fg 9041 | Rattus norvegicus (Norway rat) | Kb | 0.5900 | 1 | 1 |
| 6-nitro-1,4-dihydroquinoxaline-2,3-dione | Rattus norvegicus (Norway rat) | Kb | 3.6850 | 2 | 2 |
| licostinel | Rattus norvegicus (Norway rat) | Kb | 1.5000 | 1 | 1 |
| lofepramine hydrochloride | Rattus norvegicus (Norway rat) | Activity | 0.2200 | 1 | 1 |
| cp 465,022 | Rattus norvegicus (Norway rat) | Concentration | 0.1690 | 2 | 2 |
| bpdz 44 | Rattus norvegicus (Norway rat) | EC2x | 1,000.0000 | 1 | 1 |
| bpdz 44 | Rattus norvegicus (Norway rat) | EC5X | 1,000.0000 | 1 | 2 |
Developing a complete pharmacology for AMPA receptors: a perspective on subtype-selective ligands.Bioorganic & medicinal chemistry, , Feb-15, Volume: 18, Issue:4, 2010
1H-cyclopentapyrimidine-2,4(1H,3H)-dione-related ionotropic glutamate receptors ligands. structure-activity relationships and identification of potent and Selective iGluR5 modulators.Journal of medicinal chemistry, , Oct-23, Volume: 51, Issue:20, 2008
A tetrazolyl-substituted subtype-selective AMPA receptor agonist.Journal of medicinal chemistry, , May-17, Volume: 50, Issue:10, 2007
Design, synthesis, and pharmacology of a highly subtype-selective GluR1/2 agonist, (RS)-2-amino-3-(4-chloro-3-hydroxy-5-isoxazolyl)propionic acid (Cl-HIBO).Journal of medicinal chemistry, , May-22, Volume: 46, Issue:11, 2003
Novel 1-hydroxyazole bioisosteres of glutamic acid. Synthesis, protolytic properties, and pharmacology.Journal of medicinal chemistry, , Jan-03, Volume: 45, Issue:1, 2002
AMPA receptor agonists: synthesis, protolytic properties, and pharmacology of 3-isothiazolol bioisosteres of glutamic acid.Journal of medicinal chemistry, , Feb-14, Volume: 40, Issue:4, 1997
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
Heterocyclic excitatory amino acids. Synthesis and biological activity of novel analogues of AMPA.Journal of medicinal chemistry, , Volume: 35, Issue:1, 1992
Enzymic resolution and binding to rat brain membranes of the glutamic acid agonist alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid.Journal of medicinal chemistry, , Volume: 26, Issue:6, 1983
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 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
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
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
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
4H-1,2,4-Pyridothiadiazine 1,1-dioxides and 2,3-dihydro-4H-1,2, 4-pyridothiadiazine 1,1-dioxides chemically related to diazoxide and cyclothiazide as powerful positive allosteric modulators of (R/S)-2-amino-3-(3-hydroxy-5-methylisoxazol-4-yl)propionic aciJournal of medicinal chemistry, , Jul-30, Volume: 41, Issue:16, 1998
AMPA receptor agonists: synthesis, protolytic properties, and pharmacology of 3-isothiazolol bioisosteres of glutamic acid.Journal of medicinal chemistry, , Feb-14, Volume: 40, Issue:4, 1997
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
4H-1,2,4-Pyridothiadiazine 1,1-dioxides and 2,3-dihydro-4H-1,2, 4-pyridothiadiazine 1,1-dioxides chemically related to diazoxide and cyclothiazide as powerful positive allosteric modulators of (R/S)-2-amino-3-(3-hydroxy-5-methylisoxazol-4-yl)propionic aciJournal of medicinal chemistry, , Jul-30, Volume: 41, Issue:16, 1998
4H-1,2,4-Pyridothiadiazine 1,1-dioxides and 2,3-dihydro-4H-1,2, 4-pyridothiadiazine 1,1-dioxides chemically related to diazoxide and cyclothiazide as powerful positive allosteric modulators of (R/S)-2-amino-3-(3-hydroxy-5-methylisoxazol-4-yl)propionic aciJournal of medicinal chemistry, , Jul-30, Volume: 41, Issue:16, 1998
New 7,8-ethylenedioxy-2,3-benzodiazepines as noncompetitive AMPA receptor antagonists.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 16, Issue:1, 2006
Methaqualone derivatives are potent noncompetitive AMPA receptor antagonists.Bioorganic & medicinal chemistry letters, , Jun-05, Volume: 10, Issue:11, 2000
Substituted 1,2-dihydrophthalazines: potent, selective, and noncompetitive inhibitors of the AMPA receptor.Journal of medicinal chemistry, , Jan-19, Volume: 39, Issue:2, 1996
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
Developing a complete pharmacology for AMPA receptors: a perspective on subtype-selective ligands.Bioorganic & medicinal chemistry, , Feb-15, Volume: 18, Issue:4, 2010
The glutamate receptor GluR5 agonist (S)-2-amino-3-(3-hydroxy-7,8-dihydro-6H-cyclohepta[d]isoxazol-4-yl)propionic acid and the 8-methyl analogue: synthesis, molecular pharmacology, and biostructural characterization.Journal of medicinal chemistry, , Aug-13, Volume: 52, Issue:15, 2009
1H-cyclopentapyrimidine-2,4(1H,3H)-dione-related ionotropic glutamate receptors ligands. structure-activity relationships and identification of potent and Selective iGluR5 modulators.Journal of medicinal chemistry, , Oct-23, Volume: 51, Issue:20, 2008
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
Heterocyclic excitatory amino acids. Synthesis and biological activity of novel analogues of AMPA.Journal of medicinal chemistry, , Volume: 35, Issue:1, 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
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
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
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
Tweaking Subtype Selectivity and Agonist Efficacy at (S)-2-Amino-3-(3-hydroxy-5-methyl-isoxazol-4-yl)propionic acid (AMPA) Receptors in a Small Series of BnTetAMPA Analogues.Journal of medicinal chemistry, , Mar-10, Volume: 59, Issue:5, 2016
Developing a complete pharmacology for AMPA receptors: a perspective on subtype-selective ligands.Bioorganic & medicinal chemistry, , Feb-15, Volume: 18, Issue:4, 2010
The glutamate receptor GluR5 agonist (S)-2-amino-3-(3-hydroxy-7,8-dihydro-6H-cyclohepta[d]isoxazol-4-yl)propionic acid and the 8-methyl analogue: synthesis, molecular pharmacology, and biostructural characterization.Journal of medicinal chemistry, , Aug-13, Volume: 52, Issue:15, 2009
1H-cyclopentapyrimidine-2,4(1H,3H)-dione-related ionotropic glutamate receptors ligands. structure-activity relationships and identification of potent and Selective iGluR5 modulators.Journal of medicinal chemistry, , Oct-23, Volume: 51, Issue:20, 2008
Synthesis and pharmacological characterization at glutamate receptors of the four enantiopure isomers of tricholomic acid.Journal of medicinal chemistry, , Apr-10, Volume: 51, Issue:7, 2008
Structure-activity relationship studies on N3-substituted willardiine derivatives acting as AMPA or kainate receptor antagonists.Journal of medicinal chemistry, , Apr-20, Volume: 49, Issue:8, 2006
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
Heterocyclic excitatory amino acids. Synthesis and biological activity of novel analogues of AMPA.Journal of medicinal chemistry, , Volume: 35, Issue:1, 1992
Enzymic resolution and binding to rat brain membranes of the glutamic acid agonist alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid.Journal of medicinal chemistry, , Volume: 26, Issue:6, 1983
Cyclobutane quisqualic acid analogues as selective mGluR5a metabotropic glutamic acid receptor ligands.Journal of medicinal chemistry, , May-06, Volume: 42, Issue:9, 1999
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
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
Novel 4-oxo-1,4-dihydroquinoline-3-carboxamide derivatives as new CB2 cannabinoid receptors agonists: synthesis, pharmacological properties and molecular modeling.Journal of medicinal chemistry, , Jan-12, Volume: 49, Issue:1, 2006
3D-QSAR studies on cannabinoid CB1 receptor agonists: G-protein activation as biological data.Journal of medicinal chemistry, , Jan-26, Volume: 49, Issue:2, 2006
Structure-activity relationship studies of argiotoxins: selective and potent inhibitors of ionotropic glutamate receptors.Journal of medicinal chemistry, , Feb-14, Volume: 56, Issue:3, 2013
General synthesis of β-alanine-containing spider polyamine toxins and discovery of nephila polyamine toxins 1 and 8 as highly potent inhibitors of ionotropic glutamate receptors.Journal of medicinal chemistry, , Nov-26, Volume: 55, Issue:22, 2012
Solid-phase synthesis and biological evaluation of Joro spider toxin-4 from Nephila clavata.Journal of natural products, , Mar-25, Volume: 74, Issue:3, 2011
Developing a complete pharmacology for AMPA receptors: a perspective on subtype-selective ligands.Bioorganic & medicinal chemistry, , Feb-15, Volume: 18, Issue:4, 2010
Heteroaryl analogues of AMPA. 2. Synthesis, absolute stereochemistry, photochemistry, and structure-activity relationships.Journal of medicinal chemistry, , Jul-02, Volume: 41, Issue:14, 1998
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
Synthesis of anticonvulsive AMPA antagonists: 4-oxo-10-substituted-imidaz.Bioorganic & medicinal chemistry letters, , May-07, Volume: 11, Issue:9, 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
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
Synthesis and potent anticonvulsant activities of 4-oxo-imidazo[1,2-a]inden.Bioorganic & medicinal chemistry letters, , Dec-18, Volume: 10, Issue:24, 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
Synthesis of polyamine derivatives having non-hypotensive Ca2 +-permeable AMPA receptor antagonist activity.Bioorganic & medicinal chemistry letters, , May-21, Volume: 11, Issue:10, 2001
Synthesis of diaminobutane derivatives as potent Ca(2+)-permeable AMPA receptor antagonists.Bioorganic & medicinal chemistry letters, , Oct-08, Volume: 11, Issue:19, 2001
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
Biostructural and pharmacological studies of bicyclic analogues of the 3-isoxazolol glutamate receptor agonist ibotenic acid.Journal of medicinal chemistry, , Dec-09, Volume: 53, Issue:23, 2010
(S)-2-Amino-3-(3-hydroxy-7,8-dihydro-6H-cyclohepta[d]isoxazol-4-yl)propionic acid, a potent and selective agonist at the GluR5 subtype of ionotropic glutamate receptors. Synthesis, modeling, and molecular pharmacology.Journal of medicinal chemistry, , Apr-10, Volume: 46, Issue:8, 2003
Synthesis and enantiopharmacology of new AMPA-kainate receptor agonists.Journal of medicinal chemistry, , Oct-07, Volume: 42, Issue:20, 1999
Heteroaryl analogues of AMPA. 2. Synthesis, absolute stereochemistry, photochemistry, and structure-activity relationships.Journal of medicinal chemistry, , Jul-02, Volume: 41, Issue:14, 1998
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
Enzymic resolution and binding to rat brain membranes of the glutamic acid agonist alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid.Journal of medicinal chemistry, , Volume: 26, Issue:6, 1983
Developing a complete pharmacology for AMPA receptors: a perspective on subtype-selective ligands.Bioorganic & medicinal chemistry, , Feb-15, Volume: 18, Issue:4, 2010
The effects of conformational constraints and steric bulk in the amino acid moiety of philanthotoxins on AMPAR antagonism.Journal of medicinal chemistry, , Jan-13, Volume: 48, Issue:1, 2005
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
Synthesis of anticonvulsive AMPA antagonists: 4-oxo-10-substituted-imidaz.Bioorganic & medicinal chemistry letters, , May-07, Volume: 11, Issue:9, 2001
5-Aminomethylquinoxaline-2,3-diones. Part I: A novel class of AMPA receptor antagonists.Bioorganic & medicinal chemistry letters, , Jan-06, Volume: 8, Issue:1, 1998
Synthesis, pharmacological characterization, and molecular modeling of heterobicyclic amino acids related to (+)-2-aminobicyclo[3.1.0] hexane-2,6-dicarboxylic acid (LY354740): identification of two new potent, selective, and systemically active agonists fJournal of medicinal chemistry, , Mar-25, Volume: 42, Issue:6, 1999
The glutamate receptor GluR5 agonist (S)-2-amino-3-(3-hydroxy-7,8-dihydro-6H-cyclohepta[d]isoxazol-4-yl)propionic acid and the 8-methyl analogue: synthesis, molecular pharmacology, and biostructural characterization.Journal of medicinal chemistry, , Aug-13, Volume: 52, Issue:15, 2009
(S)-2-Amino-3-(3-hydroxy-7,8-dihydro-6H-cyclohepta[d]isoxazol-4-yl)propionic acid, a potent and selective agonist at the GluR5 subtype of ionotropic glutamate receptors. Synthesis, modeling, and molecular pharmacology.Journal of medicinal chemistry, , Apr-10, Volume: 46, Issue:8, 2003
Design, synthesis, and pharmacology of a highly subtype-selective GluR1/2 agonist, (RS)-2-amino-3-(4-chloro-3-hydroxy-5-isoxazolyl)propionic acid (Cl-HIBO).Journal of medicinal chemistry, , May-22, Volume: 46, Issue:11, 2003
AMPA receptor agonists: synthesis, protolytic properties, and pharmacology of 3-isothiazolol bioisosteres of glutamic acid.Journal of medicinal chemistry, , Feb-14, Volume: 40, Issue:4, 1997
Developing a complete pharmacology for AMPA receptors: a perspective on subtype-selective ligands.Bioorganic & medicinal chemistry, , Feb-15, Volume: 18, Issue:4, 2010
Structure-activity relationship studies on N3-substituted willardiine derivatives acting as AMPA or kainate receptor antagonists.Journal of medicinal chemistry, , Apr-20, Volume: 49, Issue:8, 2006
Synthesis and pharmacology of willardiine derivatives acting as antagonists of kainate receptors.Journal of medicinal chemistry, , Dec-01, Volume: 48, Issue:24, 2005
Synthesis and biological evaluation of analogues of 7-chloro-4,5-dihydro-4- oxo-8-(1,2,4-triazol-4-yl)-1,2,4-triazolo[1,5-a]quinoxaline-2-carboxylic acid (TQX-173) as novel selective AMPA receptor antagonists.Journal of medicinal chemistry, , Jan-01, Volume: 47, Issue:1, 2004
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
Characterization of the mechanism of anticonvulsant activity for a selected set of putative AMPA receptor antagonists.Bioorganic & medicinal chemistry letters, , Feb-10, Volume: 13, Issue:3, 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
Quinazolin-4-one alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor antagonists: structure-activity relationship of the C-2 side chain tether.Journal of medicinal chemistry, , May-24, Volume: 44, Issue:11, 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
Atropisomeric quinazolin-4-one derivatives are potent noncompetitive alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor antagonists.Bioorganic & medicinal chemistry letters, , Jan-22, Volume: 11, Issue:2, 2001
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
Synthesis and potent anticonvulsant activities of 4-oxo-imidazo[1,2-a]inden.Bioorganic & medicinal chemistry letters, , Dec-18, Volume: 10, Issue:24, 2000
7-Chloro-4,5-dihydro-8-(1,2,4-triazol-4-yl)-4-oxo-1,2,4-triazolo[1, 5-a]quinoxaline-2- carboxylates as novel highly selective AMPA receptor antagonists.Journal of medicinal chemistry, , Oct-19, Volume: 43, Issue:21, 2000
Methaqualone derivatives are potent noncompetitive AMPA receptor antagonists.Bioorganic & medicinal chemistry letters, , Jun-05, Volume: 10, Issue:11, 2000
5-Aminomethylquinoxaline-2,3-diones. Part I: A novel class of AMPA receptor antagonists.Bioorganic & medicinal chemistry letters, , Jan-06, Volume: 8, Issue:1, 1998
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
Substituted 1,2-dihydrophthalazines: potent, selective, and noncompetitive inhibitors of the AMPA receptor.Journal of medicinal chemistry, , Jan-19, Volume: 39, Issue:2, 1996
Synthesis of 1,4,7,8,9,10-hexahydro-9-methyl-6-nitropyrido[3,4-f]- quinoxaline-2,3-dione and related quinoxalinediones: characterization of alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (and N-methyl-D-aspartate) receptor and anticonvulsant actJournal of medicinal chemistry, , Sep-15, Volume: 38, Issue:19, 1995
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
Novel alpha-amino-3-hydroxy-5-methylisoxazole-4-propionate receptor antagonists: synthesis and structure-activity relationships of 6-(1H-imidazol-1-yl)-7-nitro-2,3(1H,4H)-pyrido[2,3-b]pyrazinedione and related compounds.Journal of medicinal chemistry, , Mar-15, Volume: 39, Issue:6, 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
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
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
Synthesis of anticonvulsive AMPA antagonists: 4-oxo-10-substituted-imidaz.Bioorganic & medicinal chemistry letters, , May-07, Volume: 11, Issue:9, 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
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-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
Synthesis and potent anticonvulsant activities of 4-oxo-imidazo[1,2-a]inden.Bioorganic & medicinal chemistry letters, , Dec-18, Volume: 10, Issue:24, 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
5-Aminomethylquinoxaline-2,3-diones. Part I: A novel class of AMPA receptor antagonists.Bioorganic & medicinal chemistry letters, , Jan-06, Volume: 8, Issue:1, 1998
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
Novel alpha-amino-3-hydroxy-5-methylisoxazole-4-propionate receptor antagonists: synthesis and structure-activity relationships of 6-(1H-imidazol-1-yl)-7-nitro-2,3(1H,4H)-pyrido[2,3-b]pyrazinedione and related compounds.Journal of medicinal chemistry, , Mar-15, Volume: 39, Issue:6, 1996
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.Journal of medicinal chemistry, , Oct-05, Volume: 49, Issue:20, 2006
Structure-activity relationship studies on N3-substituted willardiine derivatives acting as AMPA or kainate receptor antagonists.Journal of medicinal chemistry, , Apr-20, Volume: 49, Issue:8, 2006
Synthesis and pharmacology of willardiine derivatives acting as antagonists of kainate receptors.Journal of medicinal chemistry, , Dec-01, Volume: 48, Issue:24, 2005
Novel 4-oxo-1,4-dihydroquinoline-3-carboxamide derivatives as new CB2 cannabinoid receptors agonists: synthesis, pharmacological properties and molecular modeling.Journal of medicinal chemistry, , Jan-12, Volume: 49, Issue:1, 2006
3D-QSAR studies on cannabinoid CB1 receptor agonists: G-protein activation as biological data.Journal of medicinal chemistry, , Jan-26, Volume: 49, Issue:2, 2006
Novel 4-oxo-1,4-dihydroquinoline-3-carboxamide derivatives as new CB2 cannabinoid receptors agonists: synthesis, pharmacological properties and molecular modeling.Journal of medicinal chemistry, , Jan-12, Volume: 49, Issue:1, 2006
3D-QSAR studies on cannabinoid CB1 receptor agonists: G-protein activation as biological data.Journal of medicinal chemistry, , Jan-26, Volume: 49, Issue:2, 2006
Synthesis and biological evaluation of analogues of 7-chloro-4,5-dihydro-4- oxo-8-(1,2,4-triazol-4-yl)-1,2,4-triazolo[1,5-a]quinoxaline-2-carboxylic acid (TQX-173) as novel selective AMPA receptor antagonists.Journal of medicinal chemistry, , Jan-01, Volume: 47, Issue:1, 2004
Synthesis and biological evaluation of a new set of pyrazolo[1,5-c]quinazoline-2-carboxylates as novel excitatory amino acid antagonists.Journal of medicinal chemistry, , Feb-28, Volume: 45, Issue:5, 2002
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
7-Chloro-4,5-dihydro-8-(1,2,4-triazol-4-yl)-4-oxo-1,2,4-triazolo[1, 5-a]quinoxaline-2- carboxylates as novel highly selective AMPA receptor antagonists.Journal of medicinal chemistry, , Oct-19, Volume: 43, Issue:21, 2000
Synthesis, pharmacological characterization, and molecular modeling of heterobicyclic amino acids related to (+)-2-aminobicyclo[3.1.0] hexane-2,6-dicarboxylic acid (LY354740): identification of two new potent, selective, and systemically active agonists fJournal of medicinal chemistry, , Mar-25, Volume: 42, Issue:6, 1999
4H-1,2,4-Pyridothiadiazine 1,1-dioxides and 2,3-dihydro-4H-1,2, 4-pyridothiadiazine 1,1-dioxides chemically related to diazoxide and cyclothiazide as powerful positive allosteric modulators of (R/S)-2-amino-3-(3-hydroxy-5-methylisoxazol-4-yl)propionic aciJournal of medicinal chemistry, , Jul-30, Volume: 41, Issue:16, 1998