Proteins > Gamma-aminobutyric acid receptor subunit gamma-2
Page last updated: 2024-08-07 16:05:37
Gamma-aminobutyric acid receptor subunit gamma-2
A gamma-aminobutyric acid receptor subunit gamma-2 that is encoded in the genome of human. [PRO:DNx, UniProtKB:P18507]
Synonyms
GABA(A) receptor subunit gamma-2
Research
Bioassay Publications (87)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 3 (3.45) | 18.7374 |
| 1990's | 14 (16.09) | 18.2507 |
| 2000's | 39 (44.83) | 29.6817 |
| 2010's | 25 (28.74) | 24.3611 |
| 2020's | 6 (6.90) | 2.80 |
Compounds (131)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| gamma-aminobutyric acid | Homo sapiens (human) | Ki | 0.1165 | 2 | 2 |
| phenytoin | Homo sapiens (human) | Ki | 100.0000 | 1 | 1 |
| alprazolam | Homo sapiens (human) | Ki | 0.0011 | 4 | 4 |
| chlordiazepoxide | Homo sapiens (human) | Ki | 0.4861 | 16 | 16 |
| clonazepam | Homo sapiens (human) | IC50 | 555,904.0000 | 1 | 1 |
| clonazepam | Homo sapiens (human) | Ki | 0.0008 | 1 | 1 |
| nordazepam | Homo sapiens (human) | IC50 | 106,414.0000 | 1 | 1 |
| diazepam | Homo sapiens (human) | IC50 | 30,898.7593 | 4 | 4 |
| diazepam | Homo sapiens (human) | Ki | 0.4292 | 41 | 41 |
| fipronil | Homo sapiens (human) | IC50 | 0.0023 | 1 | 1 |
| flumazenil | Homo sapiens (human) | Ki | 0.0117 | 15 | 40 |
| flunitrazepam | Homo sapiens (human) | IC50 | 263,027.0000 | 1 | 1 |
| flunitrazepam | Homo sapiens (human) | Ki | 0.2379 | 17 | 17 |
| fluoxetine | Homo sapiens (human) | IC50 | 5.2000 | 1 | 2 |
| hydroxyurea | Homo sapiens (human) | Ki | 113.0000 | 1 | 2 |
| isoguvacine | Homo sapiens (human) | Ki | 0.0550 | 1 | 2 |
| 4-piperidinecarboxylic acid | Homo sapiens (human) | Ki | 0.5056 | 1 | 2 |
| muscimol | Homo sapiens (human) | IC50 | 0.0160 | 1 | 1 |
| muscimol | Homo sapiens (human) | Ki | 0.0085 | 2 | 2 |
| nitrazepam | Homo sapiens (human) | IC50 | 100,000.0000 | 1 | 1 |
| cm 7116 | Homo sapiens (human) | IC50 | 500,035.0000 | 1 | 1 |
| propofol | Homo sapiens (human) | IC50 | 28.0000 | 3 | 3 |
| ro 15-4513 | Homo sapiens (human) | Ki | 0.0048 | 23 | 24 |
| temazepam | Homo sapiens (human) | IC50 | 62,517.3000 | 1 | 1 |
| triazolam | Homo sapiens (human) | Ki | 2.0009 | 5 | 5 |
| zolpidem | Homo sapiens (human) | Ki | 2.5942 | 36 | 63 |
| triiodothyronine | Homo sapiens (human) | IC50 | 23.0000 | 1 | 1 |
| bicuculline | Homo sapiens (human) | IC50 | 15.0000 | 1 | 1 |
| flavone | Homo sapiens (human) | Ki | 0.5085 | 2 | 2 |
| chlordesmethyldiazepam | Homo sapiens (human) | IC50 | 277,952.0014 | 2 | 2 |
| 6-aminonicotinic acid | Homo sapiens (human) | Ki | 4.2369 | 1 | 2 |
| halazepam | Homo sapiens (human) | IC50 | 10,864.3000 | 1 | 1 |
| phenazepam | Homo sapiens (human) | Ki | 0.0002 | 4 | 4 |
| progabide | Homo sapiens (human) | Ki | 40.0000 | 1 | 1 |
| duloxetine | Homo sapiens (human) | IC50 | 0.0190 | 1 | 2 |
| norharman | Homo sapiens (human) | IC50 | 1.6218 | 1 | 1 |
| baicalin | Homo sapiens (human) | Ki | 77.6247 | 1 | 1 |
| abecarnil | Homo sapiens (human) | Ki | 1.1082 | 10 | 10 |
| 2-aminonicotinic acid | Homo sapiens (human) | Ki | 100.0000 | 1 | 1 |
| n-desmethylflunitrazepam | Homo sapiens (human) | IC50 | 25,003.5000 | 1 | 1 |
| 7-aminonitrazepam | Homo sapiens (human) | IC50 | 2,588.2100 | 1 | 1 |
| ro 20-1815 | Homo sapiens (human) | IC50 | 15,381.5000 | 1 | 1 |
| brexanolone | Homo sapiens (human) | IC50 | 0.0220 | 1 | 1 |
| 2,5-dihydro-2-(4-methoxyphenyl)-3h-pyrazolo(4,3-c)quinolin-3-one | Homo sapiens (human) | IC50 | 0.0001 | 1 | 1 |
| methyl 6,7-dimethoxy-4-ethyl-beta-carboline-3-carboxylate | Homo sapiens (human) | Ki | 0.0146 | 34 | 34 |
| beta-carboline-3-carboxylic acid ethyl ester | Homo sapiens (human) | IC50 | 0.0050 | 1 | 1 |
| beta-carboline-3-carboxylic acid ethyl ester | Homo sapiens (human) | Ki | 0.4344 | 15 | 15 |
| beta-carboline-3-carboxylic acid methyl ester | Homo sapiens (human) | IC50 | 0.0050 | 1 | 1 |
| sr 95531 | Homo sapiens (human) | IC50 | 0.2763 | 3 | 3 |
| sr 95531 | Homo sapiens (human) | Ki | 0.2400 | 1 | 1 |
| bretazenil | Homo sapiens (human) | Ki | 0.0029 | 5 | 5 |
| cl 218872 | Homo sapiens (human) | Ki | 2.0494 | 23 | 23 |
| ro 15-3505 | Homo sapiens (human) | Ki | 0.0153 | 14 | 14 |
| zk 93426 | Homo sapiens (human) | Ki | 0.1370 | 4 | 4 |
| zk 93423 | Homo sapiens (human) | Ki | 0.2038 | 10 | 10 |
| 3-ethoxy-beta-carboline | Homo sapiens (human) | IC50 | 0.0240 | 1 | 1 |
| 3-ethoxy-beta-carboline | Homo sapiens (human) | Ki | 0.4051 | 14 | 14 |
| tert-butyl beta-carboline-3-carboxylate | Homo sapiens (human) | IC50 | 0.0100 | 1 | 1 |
| tert-butyl beta-carboline-3-carboxylate | Homo sapiens (human) | Ki | 1.0273 | 16 | 16 |
| 5-(4-piperidyl)isoxazol-3-ol | Homo sapiens (human) | IC50 | 500.5935 | 1 | 2 |
| 5-(4-piperidyl)isoxazol-3-ol | Homo sapiens (human) | Ki | 11.0000 | 1 | 1 |
| ro 14-7437 | Homo sapiens (human) | Ki | 0.0609 | 5 | 5 |
| 3',6-dinitroflavone | Homo sapiens (human) | Ki | 0.0120 | 1 | 1 |
| l 663581 | Homo sapiens (human) | Ki | 0.0464 | 5 | 5 |
| cgp 36742 | Homo sapiens (human) | IC50 | 508.0000 | 2 | 2 |
| pitrazepin | Homo sapiens (human) | IC50 | 0.2400 | 1 | 1 |
| 7-aminoclonazepam | Homo sapiens (human) | IC50 | 13,335.2000 | 1 | 1 |
| zg 63 | Homo sapiens (human) | Ki | 0.0145 | 10 | 10 |
| ro 5-3438 | Homo sapiens (human) | IC50 | 71,449.6000 | 1 | 1 |
| cocaine | Homo sapiens (human) | IC50 | 127.0000 | 1 | 1 |
| 6-bromoflavone | Homo sapiens (human) | Ki | 0.0708 | 1 | 1 |
| n-desmethylflunitrazepam | Homo sapiens (human) | IC50 | 666,807.0000 | 1 | 1 |
| ro 05-4082 | Homo sapiens (human) | IC50 | 454,988.0000 | 1 | 1 |
| l 364373 | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| etomidate | Homo sapiens (human) | IC50 | 577.0000 | 1 | 1 |
| eszopiclone | Homo sapiens (human) | Ki | 5.0920 | 3 | 3 |
| 1-(1h-indol-3-ylcarbonyl)-n-(4-methoxybenzyl)formamide | Homo sapiens (human) | Ki | 0.1622 | 1 | 1 |
| 2-[(2-ethoxyphenoxy)-phenylmethyl]morpholine | Homo sapiens (human) | IC50 | 0.0110 | 1 | 2 |
| panadiplon | Homo sapiens (human) | Ki | 0.2041 | 3 | 3 |
| meclonazepam | Homo sapiens (human) | IC50 | 833,681.0000 | 1 | 1 |
| isothaz | Homo sapiens (human) | IC50 | 16.0000 | 1 | 1 |
| n-(indol-3-ylglyoxylyl)benzylamine | Homo sapiens (human) | Ki | 0.1202 | 1 | 1 |
| 6-bromo-3'-nitroflavone | Homo sapiens (human) | Ki | 0.0010 | 1 | 1 |
| 3-propoxy-beta-carboline | Homo sapiens (human) | IC50 | 0.0110 | 1 | 1 |
| 3-propoxy-beta-carboline | Homo sapiens (human) | Ki | 0.3845 | 16 | 16 |
| apigenin | Homo sapiens (human) | Ki | 3.0200 | 1 | 1 |
| harman | Homo sapiens (human) | IC50 | 12.3027 | 1 | 1 |
| amentoflavone | Homo sapiens (human) | IC50 | 281,838.0000 | 1 | 1 |
| amentoflavone | Homo sapiens (human) | Ki | 0.0060 | 2 | 2 |
| baicalein | Homo sapiens (human) | Ki | 5.6234 | 1 | 1 |
| chrysin | Homo sapiens (human) | Ki | 3.0200 | 1 | 1 |
| hispidulin | Homo sapiens (human) | Ki | 1.0000 | 1 | 1 |
| scutellarein | Homo sapiens (human) | Ki | 12.0226 | 1 | 1 |
| wogonin | Homo sapiens (human) | Ki | 2.0417 | 1 | 1 |
| cholesta-3,5-dien-7-one | Homo sapiens (human) | IC50 | 10.6833 | 6 | 6 |
| l 655,708 | Homo sapiens (human) | Ki | 0.0320 | 22 | 22 |
| ry 80 | Homo sapiens (human) | Ki | 0.0222 | 31 | 36 |
| 1-Ethyl-9H-pyrido[3,4-b]indole | Homo sapiens (human) | IC50 | 251.1890 | 1 | 1 |
| 3-[(1S)-1-phenylethyl]-4-imidazolecarboxylic acid ethyl ester | Homo sapiens (human) | IC50 | 295.0000 | 1 | 1 |
| ganaxolone | Homo sapiens (human) | IC50 | 0.0420 | 1 | 1 |
| mrk 016 | Homo sapiens (human) | Ki | 0.5504 | 8 | 8 |
| 6,6-dimethyl-3-(2-hydroxyethyl)thio-1-(thiazol-2-yl)-6,7-dihydro-2-benzothiophen-4(5h)-one | Homo sapiens (human) | Ki | 0.0144 | 8 | 8 |
| bis(7)-tacrine | Homo sapiens (human) | IC50 | 6.0000 | 1 | 1 |
| qh-ii-66 | Homo sapiens (human) | Ki | 0.3717 | 9 | 9 |
| l 838,417 | Homo sapiens (human) | Ki | 0.0012 | 7 | 7 |
| ry 024 | Homo sapiens (human) | Ki | 0.0159 | 22 | 22 |
| pwz-029 | Homo sapiens (human) | Ki | 0.7138 | 20 | 20 |
| naluzotan | Homo sapiens (human) | Ki | 2.0000 | 1 | 1 |
| basimglurant | Homo sapiens (human) | Ki | 3.1600 | 1 | 1 |
| ro 4956371 | Homo sapiens (human) | Ki | 3.1600 | 1 | 1 |
| mdv 3100 | Homo sapiens (human) | IC50 | 3.0000 | 1 | 1 |
| ns 11394 | Homo sapiens (human) | Ki | 0.0003 | 3 | 3 |
| valproate sodium | Homo sapiens (human) | Ki | 100.0000 | 1 | 1 |
| mrk-409 | Homo sapiens (human) | Ki | 0.0002 | 3 | 3 |
| 4-amino-8-(2-fluoro-6-methoxy-phenyl)-n-propylcinnoline-3-carboxamide | Homo sapiens (human) | Ki | 0.0003 | 1 | 1 |
| 4-amino-8-(2,5-dimethoxyphenyl)-n-propylcinnoline-3-carboxamide | Homo sapiens (human) | Ki | 0.0200 | 1 | 1 |
| apalutamide | Homo sapiens (human) | IC50 | 3.0000 | 1 | 1 |
Drugs with Activation Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| gamma-aminobutyric acid | Homo sapiens (human) | EC50 | 13.6289 | 17 | 27 |
| benzyl alcohol | Homo sapiens (human) | EC50 | 50,000.0000 | 1 | 1 |
| phenol | Homo sapiens (human) | EC50 | 50,500.0000 | 2 | 2 |
| diazepam | Homo sapiens (human) | EC50 | 0.0792 | 5 | 5 |
| flumazenil | Homo sapiens (human) | Kd | 0.0004 | 1 | 1 |
| flunitrazepam | Homo sapiens (human) | EC50 | 0.0014 | 1 | 1 |
| gaboxadol | Homo sapiens (human) | EC50 | 14.0627 | 1 | 2 |
| isoguvacine | Homo sapiens (human) | EC50 | 48.5342 | 9 | 12 |
| 4-piperidinecarboxylic acid | Homo sapiens (human) | EC50 | 264.1971 | 8 | 10 |
| muscimol | Homo sapiens (human) | EC50 | 0.3864 | 6 | 12 |
| pentobarbital | Homo sapiens (human) | EC50 | 50.0000 | 1 | 1 |
| piperidine-4-sulfonic acid | Homo sapiens (human) | EC50 | 61.8333 | 6 | 6 |
| propofol | Homo sapiens (human) | EC50 | 16.8369 | 8 | 8 |
| zaleplon | Homo sapiens (human) | EC50 | 0.9733 | 3 | 3 |
| zolpidem | Homo sapiens (human) | EC50 | 0.2100 | 2 | 2 |
| 2-isopropylphenol | Homo sapiens (human) | EC50 | 99.1498 | 2 | 2 |
| pyrogallol 1,3-dimethyl ether | Homo sapiens (human) | EC50 | 100,000.0000 | 2 | 2 |
| 2,4-di-tert-butylphenol | Homo sapiens (human) | EC50 | 100,000.0000 | 2 | 2 |
| osthol | Homo sapiens (human) | EC50 | 14.0000 | 1 | 1 |
| 2,6-xylenol | Homo sapiens (human) | EC50 | 162.7095 | 2 | 2 |
| 2,6-dibromophenol | Homo sapiens (human) | EC50 | 100,000.0000 | 2 | 2 |
| 6-aminonicotinic acid | Homo sapiens (human) | EC50 | 308.1140 | 1 | 2 |
| 2,6-di-tert-butylphenol | Homo sapiens (human) | EC50 | 100,000.0000 | 2 | 2 |
| oxypeucadanin, (s)-(-)-isomer | Homo sapiens (human) | EC50 | 25.0000 | 1 | 1 |
| magnolol | Homo sapiens (human) | EC50 | 4.8000 | 1 | 1 |
| honokiol | Homo sapiens (human) | EC50 | 76.2000 | 1 | 1 |
| brexanolone | Homo sapiens (human) | EC50 | 0.1985 | 2 | 2 |
| imidazoleacetic acid | Homo sapiens (human) | EC50 | 199.6960 | 10 | 14 |
| alphaxalone | Homo sapiens (human) | EC50 | 1.2875 | 4 | 4 |
| methyl 6,7-dimethoxy-4-ethyl-beta-carboline-3-carboxylate | Homo sapiens (human) | EC50 | 0.0090 | 4 | 4 |
| piperine | Homo sapiens (human) | EC50 | 29.1000 | 2 | 2 |
| etomidate | Homo sapiens (human) | EC50 | 17.8000 | 4 | 4 |
| loreclezole | Homo sapiens (human) | EC50 | 11.0000 | 1 | 1 |
| amentoflavone | Homo sapiens (human) | EC50 | 3.6000 | 1 | 1 |
| stiripentol | Homo sapiens (human) | EC50 | 46.0000 | 1 | 1 |
| 3-[(1S)-1-phenylethyl]-4-imidazolecarboxylic acid ethyl ester | Homo sapiens (human) | EC50 | 47.0000 | 1 | 1 |
| valerenic acid | Homo sapiens (human) | EC50 | 15.8000 | 2 | 2 |
| ganaxolone | Homo sapiens (human) | EC50 | 0.2600 | 1 | 1 |
| 4-iodo-2,6-diisopropylphenol | Homo sapiens (human) | EC50 | 26.1557 | 4 | 4 |
| ry 024 | Homo sapiens (human) | EC50 | 111.1600 | 5 | 5 |
| batatasin-iii | Homo sapiens (human) | EC50 | 71.7667 | 3 | 3 |
Drugs with Other Measurements
Five-Membered N-Heterocyclic Scaffolds as Novel Amino Bioisosteres at γ-Aminobutyric Acid (GABA) Type A Receptors and GABA Transporters.Journal of medicinal chemistry, , 06-27, Volume: 62, Issue:12, 2019
Nitrogenated honokiol derivatives allosterically modulate GABAA receptors and act as strong partial agonists.Bioorganic & medicinal chemistry, , Oct-15, Volume: 23, Issue:20, 2015
Synthesis and pharmacological evaluation of 6-aminonicotinic acid analogues as novel GABA(A) receptor agonists.European journal of medicinal chemistry, , Sep-12, Volume: 84, 2014
Synthesis and biological evaluation of 4-(aminomethyl)-1-hydroxypyrazole analogues of muscimol as γ-aminobutyric acid(a) receptor agonists.Journal of medicinal chemistry, , Feb-14, Volume: 56, Issue:3, 2013
5-Substituted imidazole-4-acetic acid analogues: synthesis, modeling, and pharmacological characterization of a series of novel gamma-aminobutyric acid(C) receptor agonists.Journal of medicinal chemistry, , Aug-23, Volume: 50, Issue:17, 2007
Bioisosteric determinants for subtype selectivity of ligands for heteromeric GABA(A) receptors.Bioorganic & medicinal chemistry letters, , Jun-18, Volume: 11, Issue:12, 2001
New anticonvulsants: Schiff bases of gamma-aminobutyric acid and gamma-aminobutyramide.Journal of medicinal chemistry, , Volume: 23, Issue:6, 1980
An orally bioavailable, functionally selective inverse agonist at the benzodiazepine site of GABAA alpha5 receptors with cognition enhancing properties.Journal of medicinal chemistry, , Nov-18, Volume: 47, Issue:24, 2004
Selective, orally active gamma-aminobutyric acidA alpha5 receptor inverse agonists as cognition enhancers.Journal of medicinal chemistry, , Apr-22, Volume: 47, Issue:9, 2004
3,4-Dihydronaphthalen-1(2H)-ones: novel ligands for the benzodiazepine site of alpha5-containing GABAA receptors.Bioorganic & medicinal chemistry letters, , Jun-07, Volume: 14, Issue:11, 2004
3-Heteroaryl-2-pyridones: benzodiazepine site ligands with functional delectivity for alpha 2/alpha 3-subtypes of human GABA(A) receptor-ion channels.Journal of medicinal chemistry, , Apr-25, Volume: 45, Issue:9, 2002
High affinity central benzodiazepine receptor ligands: synthesis and biological evaluation of a series of phenyltriazolobenzotriazindione derivatives.Journal of medicinal chemistry, , Apr-21, Volume: 48, Issue:8, 2005
Prediction of receptor properties and binding affinity of ligands to benzodiazepine/GABAA receptors using artificial neural networks.Journal of medicinal chemistry, , Feb-17, Volume: 38, Issue:4, 1995
Rationalizing the binding and α subtype selectivity of synthesized imidazodiazepines and benzodiazepines at GABAA receptors by using molecular docking studies.Bioorganic & medicinal chemistry letters, , 04-15, Volume: 62, 2022
A new chromanone derivative isolated from Hypericum lissophloeus (Hypericaceae) potentiates GABAA receptor currents in a subunit specific fashion.Bioorganic & medicinal chemistry, , Feb-15, Volume: 24, Issue:4, 2016
Ion channels as therapeutic targets: a drug discovery perspective.Journal of medicinal chemistry, , Feb-14, Volume: 56, Issue:3, 2013
Developing dual functional allosteric modulators of GABA(A) receptors.Bioorganic & medicinal chemistry, , Dec-01, Volume: 18, Issue:23, 2010
4-quinolone derivatives: high-affinity ligands at the benzodiazepine site of brain GABA A receptors. synthesis, pharmacology, and pharmacophore modeling.Journal of medicinal chemistry, , Apr-20, Volume: 49, Issue:8, 2006
Discovery of imidazo[1,2-b][1,2,4]triazines as GABA(A) alpha2/3 subtype selective agonists for the treatment of anxiety.Journal of medicinal chemistry, , Feb-23, Volume: 49, Issue:4, 2006
Imidazo[1,2-a]pyrimidines as functionally selective and orally bioavailable GABA(A)alpha2/alpha3 binding site agonists for the treatment of anxiety disorders.Journal of medicinal chemistry, , Jan-12, Volume: 49, Issue:1, 2006
2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine and analogues as A2A adenosine receptor antagonists. Design, synthesis, and pharmacological characterization.Journal of medicinal chemistry, , Nov-03, Volume: 48, Issue:22, 2005
High affinity central benzodiazepine receptor ligands: synthesis and biological evaluation of a series of phenyltriazolobenzotriazindione derivatives.Journal of medicinal chemistry, , Apr-21, Volume: 48, Issue:8, 2005
7-(1,1-Dimethylethyl)-6-(2-ethyl-2H-1,2,4-triazol-3-ylmethoxy)-3-(2-fluorophenyl)-1,2,4-triazolo[4,3-b]pyridazine: a functionally selective gamma-aminobutyric acid(A) (GABA(A)) alpha2/alpha3-subtype selective agonist that exhibits potent anxiolytic activiJournal of medicinal chemistry, , Nov-17, Volume: 48, Issue:23, 2005
Discovery of functionally selective 7,8,9,10-tetrahydro-7,10-ethano-1,2,4-triazolo[3,4-a]phthalazines as GABA A receptor agonists at the alpha3 subunit.Journal of medicinal chemistry, , Mar-10, Volume: 48, Issue:5, 2005
Synthesis and biological evaluation of 3-heterocyclyl-7,8,9,10-tetrahydro-(7,10-ethano)-1,2,4-triazolo[3,4-a]phthalazines and analogues as subtype-selective inverse agonists for the GABA(A)alpha5 benzodiazepine binding site.Journal of medicinal chemistry, , Jul-01, Volume: 47, Issue:14, 2004
3-phenyl-6-(2-pyridyl)methyloxy-1,2,4-triazolo[3,4-a]phthalazines and analogues: high-affinity gamma-aminobutyric acid-A benzodiazepine receptor ligands with alpha 2, alpha 3, and alpha 5-subtype binding selectivity over alpha 1.Journal of medicinal chemistry, , Mar-25, Volume: 47, Issue:7, 2004
Benzodiazepine receptor ligands. 7. Synthesis and pharmacological evaluation of new 3-esters of the 8-chloropyrazolo[5,1-c][1,2,4]benzotriazine 5-oxide. 3-(2-Thienylmethoxycarbonyl) derivative: an anxioselective agent in rodents.Journal of medicinal chemistry, , Dec-19, Volume: 45, Issue:26, 2002
N-(indol-3-ylglyoxylyl)piperidines: high affinity agonists of human GABA-A receptors containing the alpha1 subunit.Bioorganic & medicinal chemistry letters, , Jun-19, Volume: 10, Issue:12, 2000
Pharmacophore/receptor models for GABA(A)/BzR subtypes (alpha1beta3gamma2, alpha5beta3gamma2, and alpha6beta3gamma2) via a comprehensive ligand-mapping approach.Journal of medicinal chemistry, , Jan-13, Volume: 43, Issue:1, 2000
High-affinity partial agonist imidazo[1,5-a]quinoxaline amides, carbamates, and ureas at the gamma-aminobutyric acid A/benzodiazepine receptor complex.Journal of medicinal chemistry, , Jan-05, Volume: 39, Issue:1, 1996
Prediction of receptor properties and binding affinity of ligands to benzodiazepine/GABAA receptors using artificial neural networks.Journal of medicinal chemistry, , Feb-17, Volume: 38, Issue:4, 1995
Antagonist, partial agonist, and full agonist imidazo[1,5-a]quinoxaline amides and carbamates acting through the GABAA/benzodiazepine receptor.Journal of medicinal chemistry, , Mar-18, Volume: 37, Issue:6, 1994
Quinazolines and 1,4-benzodiazepines. 90. Structure-activity relationship between substituted 2-amino-N-(2-benzoyl-4-chlorophenyl)acetamides and 1,4-benzodiazepinones.Journal of medicinal chemistry, , Volume: 25, Issue:9, 1982
Ion channels as therapeutic targets: a drug discovery perspective.Journal of medicinal chemistry, , Feb-14, Volume: 56, Issue:3, 2013
Structural requirements for eszopiclone and zolpidem binding to the gamma-aminobutyric acid type-A (GABAA) receptor are different.Journal of medicinal chemistry, , Nov-27, Volume: 51, Issue:22, 2008
High affinity central benzodiazepine receptor ligands: synthesis and biological evaluation of a series of phenyltriazolobenzotriazindione derivatives.Journal of medicinal chemistry, , Apr-21, Volume: 48, Issue:8, 2005
Benzodiazepine receptor ligands. 7. Synthesis and pharmacological evaluation of new 3-esters of the 8-chloropyrazolo[5,1-c][1,2,4]benzotriazine 5-oxide. 3-(2-Thienylmethoxycarbonyl) derivative: an anxioselective agent in rodents.Journal of medicinal chemistry, , Dec-19, Volume: 45, Issue:26, 2002
Pharmacophore/receptor models for GABA(A)/BzR subtypes (alpha1beta3gamma2, alpha5beta3gamma2, and alpha6beta3gamma2) via a comprehensive ligand-mapping approach.Journal of medicinal chemistry, , Jan-13, Volume: 43, Issue:1, 2000
Predictive models for GABAA/benzodiazepine receptor subtypes: studies of quantitative structure-activity relationships for imidazobenzodiazepines at five recombinant GABAA/benzodiazepine receptor subtypes [alphaxbeta3gamma2 (x = 1-3, 5, and 6)] via comparJournal of medicinal chemistry, , Oct-08, Volume: 41, Issue:21, 1998
Rationalizing the binding and α subtype selectivity of synthesized imidazodiazepines and benzodiazepines at GABAA receptors by using molecular docking studies.Bioorganic & medicinal chemistry letters, , 04-15, Volume: 62, 2022
Protein kinase C epsilon regulates gamma-aminobutyrate type A receptor sensitivity to ethanol and benzodiazepines through phosphorylation of gamma2 subunits.The Journal of biological chemistry, , Nov-09, Volume: 282, Issue:45, 2007
N-(indol-3-ylglyoxylyl)piperidines: high affinity agonists of human GABA-A receptors containing the alpha1 subunit.Bioorganic & medicinal chemistry letters, , Jun-19, Volume: 10, Issue:12, 2000
Pharmacophore/receptor models for GABA(A)/BzR subtypes (alpha1beta3gamma2, alpha5beta3gamma2, and alpha6beta3gamma2) via a comprehensive ligand-mapping approach.Journal of medicinal chemistry, , Jan-13, Volume: 43, Issue:1, 2000
Synthesis and evaluation of analogues of the partial agonist 6-(propyloxy)-4-(methoxymethyl)-beta-carboline-3-carboxylic acid ethyl ester (6-PBC) and the full agonist 6-(benzyloxy)-4-(methoxymethyl)-beta-carboline-3-carboxylic acid ethyl ester (Zk 93423) Journal of medicinal chemistry, , Jul-02, Volume: 41, Issue:14, 1998
Prediction of receptor properties and binding affinity of ligands to benzodiazepine/GABAA receptors using artificial neural networks.Journal of medicinal chemistry, , Feb-17, Volume: 38, Issue:4, 1995
Synthesis and pharmacological evaluation of 6-aminonicotinic acid analogues as novel GABA(A) receptor agonists.European journal of medicinal chemistry, , Sep-12, Volume: 84, 2014
Synthesis and biological evaluation of 4-(aminomethyl)-1-hydroxypyrazole analogues of muscimol as γ-aminobutyric acid(a) receptor agonists.Journal of medicinal chemistry, , Feb-14, Volume: 56, Issue:3, 2013
2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine and analogues as A2A adenosine receptor antagonists. Design, synthesis, and pharmacological characterization.Journal of medicinal chemistry, , Nov-03, Volume: 48, Issue:22, 2005
New anticonvulsants: Schiff bases of gamma-aminobutyric acid and gamma-aminobutyramide.Journal of medicinal chemistry, , Volume: 23, Issue:6, 1980
[no title available]European journal of medicinal chemistry, , May-15, Volume: 194, 2020
Synthesis, structure-activity relationships at the GABA(A) receptor in rat brain, and differential electrophysiological profile at the recombinant human GABA(A) receptor of a series of substituted 1,2-diphenylimidazoles.Journal of medicinal chemistry, , Apr-07, Volume: 48, Issue:7, 2005
4D-QSAR analysis of a set of propofol analogues: mapping binding sites for an anesthetic phenol on the GABA(A) receptor.Journal of medicinal chemistry, , Jul-18, Volume: 45, Issue:15, 2002
Alpha-amino acid phenolic ester derivatives: novel water-soluble general anesthetic agents which allosterically modulate GABA(A) receptors.Journal of medicinal chemistry, , Oct-25, Volume: 44, Issue:22, 2001
Propofol analogues. Synthesis, relationships between structure and affinity at GABAA receptor in rat brain, and differential electrophysiological profile at recombinant human GABAA receptors.Journal of medicinal chemistry, , May-21, Volume: 41, Issue:11, 1998
Structural requirements for eszopiclone and zolpidem binding to the gamma-aminobutyric acid type-A (GABAA) receptor are different.Journal of medicinal chemistry, , Nov-27, Volume: 51, Issue:22, 2008
Synthesis, in vitro affinity, and efficacy of a bis 8-ethynyl-4H-imidazo[1,5a]- [1,4]benzodiazepine analogue, the first bivalent alpha5 subtype selective BzR/GABA(A) antagonist.Journal of medicinal chemistry, , Dec-18, Volume: 46, Issue:26, 2003
Pharmacophore/receptor models for GABA(A)/BzR subtypes (alpha1beta3gamma2, alpha5beta3gamma2, and alpha6beta3gamma2) via a comprehensive ligand-mapping approach.Journal of medicinal chemistry, , Jan-13, Volume: 43, Issue:1, 2000
Predictive models for GABAA/benzodiazepine receptor subtypes: studies of quantitative structure-activity relationships for imidazobenzodiazepines at five recombinant GABAA/benzodiazepine receptor subtypes [alphaxbeta3gamma2 (x = 1-3, 5, and 6)] via comparJournal of medicinal chemistry, , Oct-08, Volume: 41, Issue:21, 1998
High-affinity partial agonist imidazo[1,5-a]quinoxaline amides, carbamates, and ureas at the gamma-aminobutyric acid A/benzodiazepine receptor complex.Journal of medicinal chemistry, , Jan-05, Volume: 39, Issue:1, 1996
Synthesis and pharmacological properties of novel 8-substituted imidazobenzodiazepines: high-affinity, selective probes for alpha 5-containing GABAA receptors.Journal of medicinal chemistry, , Apr-26, Volume: 39, Issue:9, 1996
Antagonist, partial agonist, and full agonist imidazo[1,5-a]quinoxaline amides and carbamates acting through the GABAA/benzodiazepine receptor.Journal of medicinal chemistry, , Mar-18, Volume: 37, Issue:6, 1994
Design, synthesis, and biological evaluation of fluorinated imidazo[1,2-a]pyridine derivatives with potential antipsychotic activity.European journal of medicinal chemistry, , Nov-29, Volume: 124, 2016
Design, synthesis, and subtype selectivity of 3,6-disubstituted β-carbolines at Bz/GABA(A)ergic receptors. SAR and studies directed toward agents for treatment of alcohol abuse.Bioorganic & medicinal chemistry, , Nov-01, Volume: 18, Issue:21, 2010
Structural requirements for eszopiclone and zolpidem binding to the gamma-aminobutyric acid type-A (GABAA) receptor are different.Journal of medicinal chemistry, , Nov-27, Volume: 51, Issue:22, 2008
4-quinolone derivatives: high-affinity ligands at the benzodiazepine site of brain GABA A receptors. synthesis, pharmacology, and pharmacophore modeling.Journal of medicinal chemistry, , Apr-20, Volume: 49, Issue:8, 2006
7-(1,1-Dimethylethyl)-6-(2-ethyl-2H-1,2,4-triazol-3-ylmethoxy)-3-(2-fluorophenyl)-1,2,4-triazolo[4,3-b]pyridazine: a functionally selective gamma-aminobutyric acid(A) (GABA(A)) alpha2/alpha3-subtype selective agonist that exhibits potent anxiolytic activiJournal of medicinal chemistry, , Nov-17, Volume: 48, Issue:23, 2005
Discovery of functionally selective 7,8,9,10-tetrahydro-7,10-ethano-1,2,4-triazolo[3,4-a]phthalazines as GABA A receptor agonists at the alpha3 subunit.Journal of medicinal chemistry, , Mar-10, Volume: 48, Issue:5, 2005
Synthesis and biological evaluation of 3-heterocyclyl-7,8,9,10-tetrahydro-(7,10-ethano)-1,2,4-triazolo[3,4-a]phthalazines and analogues as subtype-selective inverse agonists for the GABA(A)alpha5 benzodiazepine binding site.Journal of medicinal chemistry, , Jul-01, Volume: 47, Issue:14, 2004
3-phenyl-6-(2-pyridyl)methyloxy-1,2,4-triazolo[3,4-a]phthalazines and analogues: high-affinity gamma-aminobutyric acid-A benzodiazepine receptor ligands with alpha 2, alpha 3, and alpha 5-subtype binding selectivity over alpha 1.Journal of medicinal chemistry, , Mar-25, Volume: 47, Issue:7, 2004
Pharmacophore/receptor models for GABA(A)/BzR subtypes (alpha1beta3gamma2, alpha5beta3gamma2, and alpha6beta3gamma2) via a comprehensive ligand-mapping approach.Journal of medicinal chemistry, , Jan-13, Volume: 43, Issue:1, 2000
Synthesis and evaluation of analogues of the partial agonist 6-(propyloxy)-4-(methoxymethyl)-beta-carboline-3-carboxylic acid ethyl ester (6-PBC) and the full agonist 6-(benzyloxy)-4-(methoxymethyl)-beta-carboline-3-carboxylic acid ethyl ester (Zk 93423) Journal of medicinal chemistry, , Jul-02, Volume: 41, Issue:14, 1998
Synthesis and binding affinity of 2-phenylimidazo[1,2-alpha]pyridine derivatives for both central and peripheral benzodiazepine receptors. A new series of high-affinity and selective ligands for the peripheral type.Journal of medicinal chemistry, , Sep-12, Volume: 40, Issue:19, 1997
3D-QSAR model of flavonoids binding at benzodiazepine site in GABAA receptors.Journal of medicinal chemistry, , Jun-07, Volume: 44, Issue:12, 2001
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Prediction of receptor properties and binding affinity of ligands to benzodiazepine/GABAA receptors using artificial neural networks.Journal of medicinal chemistry, , Feb-17, Volume: 38, Issue:4, 1995
Quinazolines and 1,4-benzodiazepines. 90. Structure-activity relationship between substituted 2-amino-N-(2-benzoyl-4-chlorophenyl)acetamides and 1,4-benzodiazepinones.Journal of medicinal chemistry, , Volume: 25, Issue:9, 1982
Pharmacophore/receptor models for GABA(A)/BzR subtypes (alpha1beta3gamma2, alpha5beta3gamma2, and alpha6beta3gamma2) via a comprehensive ligand-mapping approach.Journal of medicinal chemistry, , Jan-13, Volume: 43, Issue:1, 2000
Synthesis and evaluation of analogues of the partial agonist 6-(propyloxy)-4-(methoxymethyl)-beta-carboline-3-carboxylic acid ethyl ester (6-PBC) and the full agonist 6-(benzyloxy)-4-(methoxymethyl)-beta-carboline-3-carboxylic acid ethyl ester (Zk 93423) Journal of medicinal chemistry, , Jul-02, Volume: 41, Issue:14, 1998
Neuroactive Steroids. 2. 3α-Hydroxy-3β-methyl-21-(4-cyano-1H-pyrazol-1'-yl)-19-nor-5β-pregnan-20-one (SAGE-217): A Clinical Next Generation Neuroactive Steroid Positive Allosteric Modulator of the (γ-Aminobutyric Acid)Journal of medicinal chemistry, , 09-28, Volume: 60, Issue:18, 2017
Neuroactive Steroids. 1. Positive Allosteric Modulators of the (γ-Aminobutyric Acid)A Receptor: Structure-Activity Relationships of Heterocyclic Substitution at C-21.Journal of medicinal chemistry, , Apr-23, Volume: 58, Issue:8, 2015
Synthesis and in vitro activity of 3 beta-substituted-3 alpha-hydroxypregnan-20-ones: allosteric modulators of the GABAA receptor.Journal of medicinal chemistry, , Jan-03, Volume: 40, Issue:1, 1997
Five-Membered N-Heterocyclic Scaffolds as Novel Amino Bioisosteres at γ-Aminobutyric Acid (GABA) Type A Receptors and GABA Transporters.Journal of medicinal chemistry, , 06-27, Volume: 62, Issue:12, 2019
5-Substituted imidazole-4-acetic acid analogues: synthesis, modeling, and pharmacological characterization of a series of novel gamma-aminobutyric acid(C) receptor agonists.Journal of medicinal chemistry, , Aug-23, Volume: 50, Issue:17, 2007
Bioisosteric determinants for subtype selectivity of ligands for heteromeric GABA(A) receptors.Bioorganic & medicinal chemistry letters, , Jun-18, Volume: 11, Issue:12, 2001
Synthesis and pharmacological evaluation of neurosteroid photoaffinity ligands.European journal of medicinal chemistry, , Aug-18, Volume: 136, 2017
Synthesis, structure-activity relationships at the GABA(A) receptor in rat brain, and differential electrophysiological profile at the recombinant human GABA(A) receptor of a series of substituted 1,2-diphenylimidazoles.Journal of medicinal chemistry, , Apr-07, Volume: 48, Issue:7, 2005
Developing dual functional allosteric modulators of GABA(A) receptors.Bioorganic & medicinal chemistry, , Dec-01, Volume: 18, Issue:23, 2010
An orally bioavailable, functionally selective inverse agonist at the benzodiazepine site of GABAA alpha5 receptors with cognition enhancing properties.Journal of medicinal chemistry, , Nov-18, Volume: 47, Issue:24, 2004
Selective, orally active gamma-aminobutyric acidA alpha5 receptor inverse agonists as cognition enhancers.Journal of medicinal chemistry, , Apr-22, Volume: 47, Issue:9, 2004
3,4-Dihydronaphthalen-1(2H)-ones: novel ligands for the benzodiazepine site of alpha5-containing GABAA receptors.Bioorganic & medicinal chemistry letters, , Jun-07, Volume: 14, Issue:11, 2004
Identification of a novel, selective GABA(A) alpha5 receptor inverse agonist which enhances cognition.Journal of medicinal chemistry, , May-22, Volume: 46, Issue:11, 2003
6,7-Dihydro-2-benzothiophen-4(5H)-ones: a novel class of GABA-A alpha5 receptor inverse agonists.Journal of medicinal chemistry, , Mar-14, Volume: 45, Issue:6, 2002
3-Heteroaryl-2-pyridones: benzodiazepine site ligands with functional delectivity for alpha 2/alpha 3-subtypes of human GABA(A) receptor-ion channels.Journal of medicinal chemistry, , Apr-25, Volume: 45, Issue:9, 2002
Pharmacophore/receptor models for GABA(A)/BzR subtypes (alpha1beta3gamma2, alpha5beta3gamma2, and alpha6beta3gamma2) via a comprehensive ligand-mapping approach.Journal of medicinal chemistry, , Jan-13, Volume: 43, Issue:1, 2000
Synthesis and evaluation of analogues of the partial agonist 6-(propyloxy)-4-(methoxymethyl)-beta-carboline-3-carboxylic acid ethyl ester (6-PBC) and the full agonist 6-(benzyloxy)-4-(methoxymethyl)-beta-carboline-3-carboxylic acid ethyl ester (Zk 93423) Journal of medicinal chemistry, , Jul-02, Volume: 41, Issue:14, 1998
Design, synthesis, and subtype selectivity of 3,6-disubstituted β-carbolines at Bz/GABA(A)ergic receptors. SAR and studies directed toward agents for treatment of alcohol abuse.Bioorganic & medicinal chemistry, , Nov-01, Volume: 18, Issue:21, 2010
Pharmacophore/receptor models for GABA(A)/BzR subtypes (alpha1beta3gamma2, alpha5beta3gamma2, and alpha6beta3gamma2) via a comprehensive ligand-mapping approach.Journal of medicinal chemistry, , Jan-13, Volume: 43, Issue:1, 2000
Synthesis and evaluation of analogues of the partial agonist 6-(propyloxy)-4-(methoxymethyl)-beta-carboline-3-carboxylic acid ethyl ester (6-PBC) and the full agonist 6-(benzyloxy)-4-(methoxymethyl)-beta-carboline-3-carboxylic acid ethyl ester (Zk 93423) Journal of medicinal chemistry, , Jul-02, Volume: 41, Issue:14, 1998
Three-dimensional quantitative structure-activity relationships from molecular similarity matrices and genetic neural networks. 2. Applications.Journal of medicinal chemistry, , Dec-19, Volume: 40, Issue:26, 1997
Discovery of 2-(Imidazo[1,2- b]pyridazin-2-yl)acetic Acid as a New Class of Ligands Selective for the γ-Hydroxybutyric Acid (GHB) High-Affinity Binding Sites.Journal of medicinal chemistry, , 03-14, Volume: 62, Issue:5, 2019
Exploring the orthosteric binding site of the γ-aminobutyric acid type A receptor using 4-(Piperidin-4-yl)-1-hydroxypyrazoles 3- or 5-imidazolyl substituted: design, synthesis, and pharmacological evaluation.Journal of medicinal chemistry, , Aug-22, Volume: 56, Issue:16, 2013
Synthesis and evaluation of highly potent GABA(A) receptor antagonists based on gabazine (SR-95531).Bioorganic & medicinal chemistry letters, , Jul-15, Volume: 21, Issue:14, 2011
Potent 4-arylalkyl-substituted 3-isothiazolol GABA(A) competitive/noncompetitive antagonists: synthesis and pharmacology.Journal of medicinal chemistry, , Feb-23, Volume: 49, Issue:4, 2006
Design, synthesis, and subtype selectivity of 3,6-disubstituted β-carbolines at Bz/GABA(A)ergic receptors. SAR and studies directed toward agents for treatment of alcohol abuse.Bioorganic & medicinal chemistry, , Nov-01, Volume: 18, Issue:21, 2010
Discovery of functionally selective 7,8,9,10-tetrahydro-7,10-ethano-1,2,4-triazolo[3,4-a]phthalazines as GABA A receptor agonists at the alpha3 subunit.Journal of medicinal chemistry, , Mar-10, Volume: 48, Issue:5, 2005
3-phenyl-6-(2-pyridyl)methyloxy-1,2,4-triazolo[3,4-a]phthalazines and analogues: high-affinity gamma-aminobutyric acid-A benzodiazepine receptor ligands with alpha 2, alpha 3, and alpha 5-subtype binding selectivity over alpha 1.Journal of medicinal chemistry, , Mar-25, Volume: 47, Issue:7, 2004
Pharmacophore/receptor models for GABA(A)/BzR subtypes (alpha1beta3gamma2, alpha5beta3gamma2, and alpha6beta3gamma2) via a comprehensive ligand-mapping approach.Journal of medicinal chemistry, , Jan-13, Volume: 43, Issue:1, 2000
Synthesis and evaluation of analogues of the partial agonist 6-(propyloxy)-4-(methoxymethyl)-beta-carboline-3-carboxylic acid ethyl ester (6-PBC) and the full agonist 6-(benzyloxy)-4-(methoxymethyl)-beta-carboline-3-carboxylic acid ethyl ester (Zk 93423) Journal of medicinal chemistry, , Jul-02, Volume: 41, Issue:14, 1998
The GABA(A) receptor as a target for photochromic molecules.Bioorganic & medicinal chemistry, , Nov-15, Volume: 18, Issue:22, 2010
Selective influence on contextual memory: physiochemical properties associated with selectivity of benzodiazepine ligands at GABAA receptors containing the alpha5 subunit.Journal of medicinal chemistry, , Jul-10, Volume: 51, Issue:13, 2008
Pharmacophore/receptor models for GABA(A)/BzR subtypes (alpha1beta3gamma2, alpha5beta3gamma2, and alpha6beta3gamma2) via a comprehensive ligand-mapping approach.Journal of medicinal chemistry, , Jan-13, Volume: 43, Issue:1, 2000
Predictive models for GABAA/benzodiazepine receptor subtypes: studies of quantitative structure-activity relationships for imidazobenzodiazepines at five recombinant GABAA/benzodiazepine receptor subtypes [alphaxbeta3gamma2 (x = 1-3, 5, and 6)] via comparJournal of medicinal chemistry, , Oct-08, Volume: 41, Issue:21, 1998
Pharmacophore/receptor models for GABA(A)/BzR subtypes (alpha1beta3gamma2, alpha5beta3gamma2, and alpha6beta3gamma2) via a comprehensive ligand-mapping approach.Journal of medicinal chemistry, , Jan-13, Volume: 43, Issue:1, 2000
Synthesis and evaluation of analogues of the partial agonist 6-(propyloxy)-4-(methoxymethyl)-beta-carboline-3-carboxylic acid ethyl ester (6-PBC) and the full agonist 6-(benzyloxy)-4-(methoxymethyl)-beta-carboline-3-carboxylic acid ethyl ester (Zk 93423) Journal of medicinal chemistry, , Jul-02, Volume: 41, Issue:14, 1998
Design, synthesis, and subtype selectivity of 3,6-disubstituted β-carbolines at Bz/GABA(A)ergic receptors. SAR and studies directed toward agents for treatment of alcohol abuse.Bioorganic & medicinal chemistry, , Nov-01, Volume: 18, Issue:21, 2010
Pharmacophore/receptor models for GABA(A)/BzR subtypes (alpha1beta3gamma2, alpha5beta3gamma2, and alpha6beta3gamma2) via a comprehensive ligand-mapping approach.Journal of medicinal chemistry, , Jan-13, Volume: 43, Issue:1, 2000
Synthesis and evaluation of analogues of the partial agonist 6-(propyloxy)-4-(methoxymethyl)-beta-carboline-3-carboxylic acid ethyl ester (6-PBC) and the full agonist 6-(benzyloxy)-4-(methoxymethyl)-beta-carboline-3-carboxylic acid ethyl ester (Zk 93423) Journal of medicinal chemistry, , Jul-02, Volume: 41, Issue:14, 1998
Three-dimensional quantitative structure-activity relationships from molecular similarity matrices and genetic neural networks. 2. Applications.Journal of medicinal chemistry, , Dec-19, Volume: 40, Issue:26, 1997
Design, synthesis, and subtype selectivity of 3,6-disubstituted β-carbolines at Bz/GABA(A)ergic receptors. SAR and studies directed toward agents for treatment of alcohol abuse.Bioorganic & medicinal chemistry, , Nov-01, Volume: 18, Issue:21, 2010
Pharmacophore/receptor models for GABA(A)/BzR subtypes (alpha1beta3gamma2, alpha5beta3gamma2, and alpha6beta3gamma2) via a comprehensive ligand-mapping approach.Journal of medicinal chemistry, , Jan-13, Volume: 43, Issue:1, 2000
Synthesis and evaluation of analogues of the partial agonist 6-(propyloxy)-4-(methoxymethyl)-beta-carboline-3-carboxylic acid ethyl ester (6-PBC) and the full agonist 6-(benzyloxy)-4-(methoxymethyl)-beta-carboline-3-carboxylic acid ethyl ester (Zk 93423) Journal of medicinal chemistry, , Jul-02, Volume: 41, Issue:14, 1998
Three-dimensional quantitative structure-activity relationships from molecular similarity matrices and genetic neural networks. 2. Applications.Journal of medicinal chemistry, , Dec-19, Volume: 40, Issue:26, 1997
Novel 4-(piperidin-4-yl)-1-hydroxypyrazoles as gamma-aminobutyric acid(A) receptor ligands: synthesis, pharmacology, and structure-activity relationships.Journal of medicinal chemistry, , Apr-22, Volume: 53, Issue:8, 2010
4-aryl-5-(4-piperidyl)-3-isoxazolol GABAA antagonists: synthesis, pharmacology, and structure-activity relationships.Journal of medicinal chemistry, , Apr-19, Volume: 50, Issue:8, 2007
Novel Cyclic Phosphinic Acids as GABAC ρ Receptor Antagonists: Design, Synthesis, and Pharmacology.ACS medicinal chemistry letters, , Jan-13, Volume: 2, Issue:1, 2011
Phosphinic acid analogues of GABA. 2. Selective, orally active GABAB antagonists.Journal of medicinal chemistry, , Aug-18, Volume: 38, Issue:17, 1995
Pharmacophore/receptor models for GABA(A)/BzR subtypes (alpha1beta3gamma2, alpha5beta3gamma2, and alpha6beta3gamma2) via a comprehensive ligand-mapping approach.Journal of medicinal chemistry, , Jan-13, Volume: 43, Issue:1, 2000
Predictive models for GABAA/benzodiazepine receptor subtypes: studies of quantitative structure-activity relationships for imidazobenzodiazepines at five recombinant GABAA/benzodiazepine receptor subtypes [alphaxbeta3gamma2 (x = 1-3, 5, and 6)] via comparJournal of medicinal chemistry, , Oct-08, Volume: 41, Issue:21, 1998
Clerodane Diterpenes from Journal of natural products, , 05-27, Volume: 85, Issue:5, 2022
Efficient modulation of γ-aminobutyric acid type A receptors by piperine derivatives.Journal of medicinal chemistry, , Jul-10, Volume: 57, Issue:13, 2014
Synthesis, structure-activity relationships at the GABA(A) receptor in rat brain, and differential electrophysiological profile at the recombinant human GABA(A) receptor of a series of substituted 1,2-diphenylimidazoles.Journal of medicinal chemistry, , Apr-07, Volume: 48, Issue:7, 2005
2-(3-Methyl-3H-diaziren-3-yl)ethyl 1-(1-phenylethyl)-1H-imidazole-5-carboxylate: a derivative of the stereoselective general anesthetic etomidate for photolabeling ligand-gated ion channels.Journal of medicinal chemistry, , Mar-27, Volume: 46, Issue:7, 2003
Design, synthesis, and subtype selectivity of 3,6-disubstituted β-carbolines at Bz/GABA(A)ergic receptors. SAR and studies directed toward agents for treatment of alcohol abuse.Bioorganic & medicinal chemistry, , Nov-01, Volume: 18, Issue:21, 2010
Pharmacophore/receptor models for GABA(A)/BzR subtypes (alpha1beta3gamma2, alpha5beta3gamma2, and alpha6beta3gamma2) via a comprehensive ligand-mapping approach.Journal of medicinal chemistry, , Jan-13, Volume: 43, Issue:1, 2000
Synthesis and evaluation of analogues of the partial agonist 6-(propyloxy)-4-(methoxymethyl)-beta-carboline-3-carboxylic acid ethyl ester (6-PBC) and the full agonist 6-(benzyloxy)-4-(methoxymethyl)-beta-carboline-3-carboxylic acid ethyl ester (Zk 93423) Journal of medicinal chemistry, , Jul-02, Volume: 41, Issue:14, 1998
Three-dimensional quantitative structure-activity relationships from molecular similarity matrices and genetic neural networks. 2. Applications.Journal of medicinal chemistry, , Dec-19, Volume: 40, Issue:26, 1997
Synthesis and biological evaluation of 3-heterocyclyl-7,8,9,10-tetrahydro-(7,10-ethano)-1,2,4-triazolo[3,4-a]phthalazines and analogues as subtype-selective inverse agonists for the GABA(A)alpha5 benzodiazepine binding site.Journal of medicinal chemistry, , Jul-01, Volume: 47, Issue:14, 2004
3-phenyl-6-(2-pyridyl)methyloxy-1,2,4-triazolo[3,4-a]phthalazines and analogues: high-affinity gamma-aminobutyric acid-A benzodiazepine receptor ligands with alpha 2, alpha 3, and alpha 5-subtype binding selectivity over alpha 1.Journal of medicinal chemistry, , Mar-25, Volume: 47, Issue:7, 2004
Synthesis, in vitro affinity, and efficacy of a bis 8-ethynyl-4H-imidazo[1,5a]- [1,4]benzodiazepine analogue, the first bivalent alpha5 subtype selective BzR/GABA(A) antagonist.Journal of medicinal chemistry, , Dec-18, Volume: 46, Issue:26, 2003
Pharmacophore/receptor models for GABA(A)/BzR subtypes (alpha1beta3gamma2, alpha5beta3gamma2, and alpha6beta3gamma2) via a comprehensive ligand-mapping approach.Journal of medicinal chemistry, , Jan-13, Volume: 43, Issue:1, 2000
Predictive models for GABAA/benzodiazepine receptor subtypes: studies of quantitative structure-activity relationships for imidazobenzodiazepines at five recombinant GABAA/benzodiazepine receptor subtypes [alphaxbeta3gamma2 (x = 1-3, 5, and 6)] via comparJournal of medicinal chemistry, , Oct-08, Volume: 41, Issue:21, 1998
A study of the structure-activity relationship of GABA(A)-benzodiazepine receptor bivalent ligands by conformational analysis with low temperature NMR and X-ray analysis.Bioorganic & medicinal chemistry, , Oct-01, Volume: 16, Issue:19, 2008
Determination of the stable conformation of GABA(A)-benzodiazepine receptor bivalent ligands by low temperature NMR and X-ray analysis.Bioorganic & medicinal chemistry letters, , Mar-22, Volume: 14, Issue:6, 2004
Synthesis, in vitro affinity, and efficacy of a bis 8-ethynyl-4H-imidazo[1,5a]- [1,4]benzodiazepine analogue, the first bivalent alpha5 subtype selective BzR/GABA(A) antagonist.Journal of medicinal chemistry, , Dec-18, Volume: 46, Issue:26, 2003
Pharmacophore/receptor models for GABA(A)/BzR subtypes (alpha1beta3gamma2, alpha5beta3gamma2, and alpha6beta3gamma2) via a comprehensive ligand-mapping approach.Journal of medicinal chemistry, , Jan-13, Volume: 43, Issue:1, 2000
Predictive models for GABAA/benzodiazepine receptor subtypes: studies of quantitative structure-activity relationships for imidazobenzodiazepines at five recombinant GABAA/benzodiazepine receptor subtypes [alphaxbeta3gamma2 (x = 1-3, 5, and 6)] via comparJournal of medicinal chemistry, , Oct-08, Volume: 41, Issue:21, 1998
Synthesis and pharmacological properties of novel 8-substituted imidazobenzodiazepines: high-affinity, selective probes for alpha 5-containing GABAA receptors.Journal of medicinal chemistry, , Apr-26, Volume: 39, Issue:9, 1996
Clerodane Diterpenes from Journal of natural products, , 05-27, Volume: 85, Issue:5, 2022
[no title available]Journal of medicinal chemistry, , 01-10, Volume: 62, Issue:1, 2019
Neuroactive Steroids. 1. Positive Allosteric Modulators of the (γ-Aminobutyric Acid)A Receptor: Structure-Activity Relationships of Heterocyclic Substitution at C-21.Journal of medicinal chemistry, , Apr-23, Volume: 58, Issue:8, 2015
Synthesis and in vitro activity of 3 beta-substituted-3 alpha-hydroxypregnan-20-ones: allosteric modulators of the GABAA receptor.Journal of medicinal chemistry, , Jan-03, Volume: 40, Issue:1, 1997
GABA allosteric modulators: An overview of recent developments in non-benzodiazepine modulators.European journal of medicinal chemistry, , Jun-01, Volume: 171, 2019
An orally bioavailable, functionally selective inverse agonist at the benzodiazepine site of GABAA alpha5 receptors with cognition enhancing properties.Journal of medicinal chemistry, , Nov-18, Volume: 47, Issue:24, 2004
Identification of a novel, selective GABA(A) alpha5 receptor inverse agonist which enhances cognition.Journal of medicinal chemistry, , May-22, Volume: 46, Issue:11, 2003
6,7-Dihydro-2-benzothiophen-4(5H)-ones: a novel class of GABA-A alpha5 receptor inverse agonists.Journal of medicinal chemistry, , Mar-14, Volume: 45, Issue:6, 2002
Rationalizing the binding and α subtype selectivity of synthesized imidazodiazepines and benzodiazepines at GABAA receptors by using molecular docking studies.Bioorganic & medicinal chemistry letters, , 04-15, Volume: 62, 2022
Pharmacophore/receptor models for GABA(A)/BzR subtypes (alpha1beta3gamma2, alpha5beta3gamma2, and alpha6beta3gamma2) via a comprehensive ligand-mapping approach.Journal of medicinal chemistry, , Jan-13, Volume: 43, Issue:1, 2000
4D-QSAR analysis of a set of propofol analogues: mapping binding sites for an anesthetic phenol on the GABA(A) receptor.Journal of medicinal chemistry, , Jul-18, Volume: 45, Issue:15, 2002
Propofol analogues. Synthesis, relationships between structure and affinity at GABAA receptor in rat brain, and differential electrophysiological profile at recombinant human GABAA receptors.Journal of medicinal chemistry, , May-21, Volume: 41, Issue:11, 1998
[no title available]Journal of medicinal chemistry, , 04-09, Volume: 63, Issue:7, 2020
Imidazo[1,2-a]pyrimidines as functionally selective and orally bioavailable GABA(A)alpha2/alpha3 binding site agonists for the treatment of anxiety disorders.Journal of medicinal chemistry, , Jan-12, Volume: 49, Issue:1, 2006
Selective influence on contextual memory: physiochemical properties associated with selectivity of benzodiazepine ligands at GABAA receptors containing the alpha5 subunit.Journal of medicinal chemistry, , Jul-10, Volume: 51, Issue:13, 2008
Synthesis, in vitro affinity, and efficacy of a bis 8-ethynyl-4H-imidazo[1,5a]- [1,4]benzodiazepine analogue, the first bivalent alpha5 subtype selective BzR/GABA(A) antagonist.Journal of medicinal chemistry, , Dec-18, Volume: 46, Issue:26, 2003
Pharmacophore/receptor models for GABA(A)/BzR subtypes (alpha1beta3gamma2, alpha5beta3gamma2, and alpha6beta3gamma2) via a comprehensive ligand-mapping approach.Journal of medicinal chemistry, , Jan-13, Volume: 43, Issue:1, 2000
Predictive models for GABAA/benzodiazepine receptor subtypes: studies of quantitative structure-activity relationships for imidazobenzodiazepines at five recombinant GABAA/benzodiazepine receptor subtypes [alphaxbeta3gamma2 (x = 1-3, 5, and 6)] via comparJournal of medicinal chemistry, , Oct-08, Volume: 41, Issue:21, 1998
Synthesis and pharmacological properties of novel 8-substituted imidazobenzodiazepines: high-affinity, selective probes for alpha 5-containing GABAA receptors.Journal of medicinal chemistry, , Apr-26, Volume: 39, Issue:9, 1996
The GABA(A) receptor as a target for photochromic molecules.Bioorganic & medicinal chemistry, , Nov-15, Volume: 18, Issue:22, 2010
Selective influence on contextual memory: physiochemical properties associated with selectivity of benzodiazepine ligands at GABAA receptors containing the alpha5 subunit.Journal of medicinal chemistry, , Jul-10, Volume: 51, Issue:13, 2008
Pharmacophore/receptor models for GABA(A)/BzR subtypes (alpha1beta3gamma2, alpha5beta3gamma2, and alpha6beta3gamma2) via a comprehensive ligand-mapping approach.Journal of medicinal chemistry, , Jan-13, Volume: 43, Issue:1, 2000
Predictive models for GABAA/benzodiazepine receptor subtypes: studies of quantitative structure-activity relationships for imidazobenzodiazepines at five recombinant GABAA/benzodiazepine receptor subtypes [alphaxbeta3gamma2 (x = 1-3, 5, and 6)] via comparJournal of medicinal chemistry, , Oct-08, Volume: 41, Issue:21, 1998
Enables
This protein enables 6 target(s):
| Target | Category | Definition |
|---|
| GABA-A receptor activity | molecular function | Combining with the amino acid gamma-aminobutyric acid (GABA, 4-aminobutyrate) to initiate a change in cell activity. GABA-A receptors function as chloride channels. [PMID:8974333] |
| chloride channel activity | molecular function | Enables the facilitated diffusion of a chloride (by an energy-independent process) involving passage through a transmembrane aqueous pore or channel without evidence for a carrier-mediated mechanism. [GOC:mtg_transport, GOC:pr, ISBN:0815340729] |
| protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
| GABA-gated chloride ion channel activity | molecular function | Enables the transmembrane transfer of a chloride ion by a channel that opens when GABA has been bound by the channel complex or one of its constituent parts. [GOC:mtg_transport, ISBN:0815340729] |
| transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potential | molecular function | Any transmitter-gated ion channel activity that is involved in regulation of postsynaptic membrane potential. [GO_REF:0000061, GOC:TermGenie, PMID:20200227] |
| neurotransmitter receptor activity | molecular function | Combining with a neurotransmitter and transmitting the signal to initiate a change in cell activity. [GOC:jl, GOC:signaling] |
Located In
This protein is located in 6 target(s):
| Target | Category | Definition |
|---|
| plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
| axon | cellular component | The long process of a neuron that conducts nerve impulses, usually away from the cell body to the terminals and varicosities, which are sites of storage and release of neurotransmitter. [GOC:nln, ISBN:0198506732] |
| cytoplasmic vesicle membrane | cellular component | The lipid bilayer surrounding a cytoplasmic vesicle. [GOC:mah] |
| dendrite membrane | cellular component | The portion of the plasma membrane surrounding a dendrite. [GOC:mah] |
| GABA-ergic synapse | cellular component | A synapse that uses GABA as a neurotransmitter. These synapses are typically inhibitory. [GOC:dos] |
| postsynaptic specialization membrane | cellular component | The membrane component of the postsynaptic specialization. This is the region of the postsynaptic membrane in which the population of neurotransmitter receptors involved in synaptic transmission are concentrated. [GOC:dos] |
Active In
This protein is active in 5 target(s):
| Target | Category | Definition |
|---|
| neuron projection | cellular component | A prolongation or process extending from a nerve cell, e.g. an axon or dendrite. [GOC:jl, http://www.cogsci.princeton.edu/~wn/] |
| dendrite membrane | cellular component | The portion of the plasma membrane surrounding a dendrite. [GOC:mah] |
| synapse | cellular component | The junction between an axon of one neuron and a dendrite of another neuron, a muscle fiber or a glial cell. As the axon approaches the synapse it enlarges into a specialized structure, the presynaptic terminal bouton, which contains mitochondria and synaptic vesicles. At the tip of the terminal bouton is the presynaptic membrane; facing it, and separated from it by a minute cleft (the synaptic cleft) is a specialized area of membrane on the receiving cell, known as the postsynaptic membrane. In response to the arrival of nerve impulses, the presynaptic terminal bouton secretes molecules of neurotransmitters into the synaptic cleft. These diffuse across the cleft and transmit the signal to the postsynaptic membrane. [GOC:aruk, ISBN:0198506732, PMID:24619342, PMID:29383328, PMID:31998110] |
| plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
| postsynapse | cellular component | The part of a synapse that is part of the post-synaptic cell. [GOC:dos] |
Part Of
This protein is part of 3 target(s):
| Target | Category | Definition |
|---|
| GABA-A receptor complex | cellular component | A protein complex which is capable of GABA-A receptor activity. In human, it is usually composed of either two alpha, two beta and one gamma chain of the GABA-A receptor subunits or 5 chains of the GABA-A receptor subunits rho1-3 (formally known as GABA-C receptor). [GO_REF:0000088, GOC:bhm, GOC:TermGenie, PMID:18790874] |
| chloride channel complex | cellular component | An ion channel complex through which chloride ions pass. [GOC:mah] |
| transmembrane transporter complex | cellular component | A transmembrane protein complex which enables the transfer of a substance from one side of a membrane to the other. [GOC:bhm, GOC:TermGenie, PMID:18024586] |
Involved In
This protein is involved in 8 target(s):
| Target | Category | Definition |
|---|
| gamma-aminobutyric acid signaling pathway | biological process | The series of molecular signals generated by the binding of gamma-aminobutyric acid (GABA, 4-aminobutyrate), an amino acid which acts as a neurotransmitter in some organisms, to its receptor on the surface of a target cell. [GOC:mah] |
| post-embryonic development | biological process | The process whose specific outcome is the progression of the organism over time, from the completion of embryonic development to the mature structure. See embryonic development. [GOC:go_curators] |
| adult behavior | biological process | Behavior in a fully developed and mature organism. [GOC:mah, ISBN:0877797099] |
| synaptic transmission, GABAergic | biological process | The vesicular release of gamma-aminobutyric acid (GABA). from a presynapse, across a chemical synapse, the subsequent activation of GABA receptors at the postsynapse of a target cell (neuron, muscle, or secretory cell) and the effects of this activation on the postsynaptic membrane potential and ionic composition of the postsynaptic cytosol. This process encompasses both spontaneous and evoked release of neurotransmitter and all parts of synaptic vesicle exocytosis. Evoked transmission starts with the arrival of an action potential at the presynapse. [GOC:dos, ISBN:0126603030] |
| cellular response to histamine | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a histamine stimulus. Histamine, the biogenic amine 2-(1H-imidazol-4-yl)ethanamine, is involved in local immune responses as well as regulating physiological function in the gut and acting as a neurotransmitter. [GOC:mah] |
| chloride transmembrane transport | biological process | The process in which chloride is transported across a membrane. [GOC:TermGenie, GOC:vw] |
| inhibitory synapse assembly | biological process | The aggregation, arrangement and bonding together of a set of components to form an inhibitory synapse. [GO_REF:0000079, GOC:bf, GOC:PARL, GOC:TermGenie] |
| regulation of postsynaptic membrane potential | biological process | Any process that modulates the potential difference across a post-synaptic membrane. [GOC:dph, GOC:ef] |