Proteins > Gamma-aminobutyric acid receptor subunit beta-2
Page last updated: 2024-08-07 16:43:06
Gamma-aminobutyric acid receptor subunit beta-2
A gamma-aminobutyric acid receptor subunit beta-2 that is encoded in the genome of human. [PRO:DNx, UniProtKB:P47870]
Synonyms
GABA(A) receptor subunit beta-2
Research
Bioassay Publications (62)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 3 (4.84) | 18.7374 |
| 1990's | 11 (17.74) | 18.2507 |
| 2000's | 18 (29.03) | 29.6817 |
| 2010's | 27 (43.55) | 24.3611 |
| 2020's | 3 (4.84) | 2.80 |
Compounds (111)
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 |
| 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 | 41,198.3400 | 3 | 3 |
| diazepam | Homo sapiens (human) | Ki | 1.1774 | 12 | 12 |
| fipronil | Homo sapiens (human) | IC50 | 0.0023 | 1 | 1 |
| flumazenil | Homo sapiens (human) | Ki | 0.0055 | 5 | 30 |
| flunitrazepam | Homo sapiens (human) | IC50 | 263,027.0000 | 1 | 1 |
| flunitrazepam | Homo sapiens (human) | Ki | 0.0030 | 5 | 5 |
| 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 |
| kynurenic acid | Homo sapiens (human) | IC50 | 2,900.0000 | 1 | 1 |
| 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 |
| ro 15-4513 | Homo sapiens (human) | Ki | 0.0051 | 9 | 10 |
| temazepam | Homo sapiens (human) | IC50 | 62,517.3000 | 1 | 1 |
| zolpidem | Homo sapiens (human) | Ki | 2.2165 | 5 | 32 |
| 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 |
| 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 |
| beta-carboline-3-carboxylic acid ethyl ester | Homo sapiens (human) | IC50 | 0.0050 | 1 | 1 |
| 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 |
| ro 15-3505 | Homo sapiens (human) | Ki | 0.0108 | 3 | 3 |
| 3-ethoxy-beta-carboline | Homo sapiens (human) | IC50 | 0.0240 | 1 | 1 |
| tert-butyl beta-carboline-3-carboxylate | Homo sapiens (human) | IC50 | 0.0100 | 1 | 1 |
| 5-(4-piperidyl)isoxazol-3-ol | Homo sapiens (human) | IC50 | 500.5935 | 1 | 2 |
| 3',6-dinitroflavone | Homo sapiens (human) | Ki | 0.0120 | 1 | 1 |
| 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 |
| 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 |
| 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 |
| ry 80 | Homo sapiens (human) | Ki | 0.0261 | 4 | 4 |
| 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 |
| bis(7)-tacrine | Homo sapiens (human) | IC50 | 6.0000 | 1 | 1 |
| qh-ii-66 | Homo sapiens (human) | Ki | 0.0432 | 4 | 4 |
| ry 024 | Homo sapiens (human) | Ki | 0.0192 | 4 | 4 |
| 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 |
| valproate sodium | Homo sapiens (human) | Ki | 100.0000 | 1 | 1 |
| apalutamide | Homo sapiens (human) | IC50 | 3.0000 | 1 | 1 |
| nitd 609 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
Drugs with Activation Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| gamma-aminobutyric acid | Homo sapiens (human) | EC50 | 5.3824 | 13 | 22 |
| phenol | Homo sapiens (human) | EC50 | 50,500.0000 | 2 | 2 |
| diazepam | Homo sapiens (human) | EC50 | 0.0925 | 2 | 2 |
| flunitrazepam | Homo sapiens (human) | EC50 | 0.0014 | 1 | 1 |
| gaboxadol | Homo sapiens (human) | EC50 | 14.0627 | 1 | 2 |
| isoguvacine | Homo sapiens (human) | EC50 | 7.0684 | 3 | 6 |
| 4-piperidinecarboxylic acid | Homo sapiens (human) | EC50 | 20.4927 | 2 | 4 |
| muscimol | Homo sapiens (human) | EC50 | 2.4336 | 7 | 13 |
| pentobarbital | Homo sapiens (human) | EC50 | 50.0000 | 1 | 1 |
| propofol | Homo sapiens (human) | EC50 | 15.6791 | 5 | 5 |
| zaleplon | Homo sapiens (human) | EC50 | 0.2900 | 1 | 1 |
| 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 | 20.8000 | 2 | 2 |
| honokiol | Homo sapiens (human) | EC50 | 47.5400 | 5 | 5 |
| brexanolone | Homo sapiens (human) | EC50 | 0.1774 | 4 | 4 |
| imidazoleacetic acid | Homo sapiens (human) | EC50 | 14.9510 | 3 | 6 |
| alphaxalone | Homo sapiens (human) | EC50 | 1.5667 | 3 | 3 |
| methyl 6,7-dimethoxy-4-ethyl-beta-carboline-3-carboxylate | Homo sapiens (human) | EC50 | 0.0090 | 1 | 1 |
| 4-methoxyhonokiol | Homo sapiens (human) | EC50 | 27.2000 | 1 | 1 |
| piperine | Homo sapiens (human) | EC50 | 29.1000 | 2 | 2 |
| etomidate | Homo sapiens (human) | EC50 | 17.8000 | 4 | 4 |
| 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 | 12.6000 | 1 | 1 |
| ganaxolone | Homo sapiens (human) | EC50 | 0.2097 | 3 | 3 |
| 4-iodo-2,6-diisopropylphenol | Homo sapiens (human) | EC50 | 20.8114 | 2 | 2 |
| batatasin-iii | Homo sapiens (human) | EC50 | 74.0500 | 2 | 2 |
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
Design, Synthesis, and Pharmacological Evaluation of Fluorescent and Biotinylated Antagonists of ρ1 GABAC Receptors.ACS medicinal chemistry letters, , Apr-11, Volume: 4, Issue:4, 2013
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
p-(4-Azipentyl)propofol: a potent photoreactive general anesthetic derivative of propofol.Journal of medicinal chemistry, , Dec-08, Volume: 54, Issue:23, 2011
Novel gamma-aminobutyric acid rho1 receptor antagonists; synthesis, pharmacological activity and structure-activity relationships.Journal of medicinal chemistry, , Jul-10, Volume: 51, Issue:13, 2008
New anticonvulsants: Schiff bases of gamma-aminobutyric acid and gamma-aminobutyramide.Journal of medicinal chemistry, , Volume: 23, Issue:6, 1980
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
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
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
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
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
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
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
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
Design, Synthesis, and Pharmacological Evaluation of Fluorescent and Biotinylated Antagonists of ρ1 GABAC Receptors.ACS medicinal chemistry letters, , Apr-11, Volume: 4, Issue:4, 2013
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
p-(4-Azipentyl)propofol: a potent photoreactive general anesthetic derivative of propofol.Journal of medicinal chemistry, , Dec-08, Volume: 54, Issue:23, 2011
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
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 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
Novel Cyclic Phosphinic Acids as GABAC ρ Receptor Antagonists: Design, Synthesis, and Pharmacology.ACS medicinal chemistry letters, , Jan-13, Volume: 2, Issue:1, 2011
Novel gamma-aminobutyric acid rho1 receptor antagonists; synthesis, pharmacological activity and structure-activity relationships.Journal of medicinal chemistry, , Jul-10, Volume: 51, Issue:13, 2008
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
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
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
Mixture-based synthetic combinatorial libraries.Journal of medicinal chemistry, , Sep-23, Volume: 42, Issue:19, 1999
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
Clerodane Diterpenes from Journal of natural products, , 05-27, Volume: 85, Issue:5, 2022
Modulation of GABAA-receptors by honokiol and derivatives: subtype selectivity and structure-activity relationship.Journal of medicinal chemistry, , Aug-11, Volume: 54, Issue:15, 2011
Nitrogenated honokiol derivatives allosterically modulate GABAA receptors and act as strong partial agonists.Bioorganic & medicinal chemistry, , Oct-15, Volume: 23, Issue:20, 2015
Modulation of GABAA-receptors by honokiol and derivatives: subtype selectivity and structure-activity relationship.Journal of medicinal chemistry, , Aug-11, Volume: 54, Issue:15, 2011
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
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
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
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
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
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
Enables
This protein enables 4 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] |
| 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 5 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] |
| cytoplasmic vesicle membrane | cellular component | The lipid bilayer surrounding a cytoplasmic vesicle. [GOC:mah] |
| extracellular exosome | cellular component | A vesicle that is released into the extracellular region by fusion of the limiting endosomal membrane of a multivesicular body with the plasma membrane. Extracellular exosomes, also simply called exosomes, have a diameter of about 40-100 nm. [GOC:BHF, GOC:mah, GOC:vesicles, PMID:15908444, PMID:17641064, PMID:19442504, PMID:19498381, PMID:22418571, PMID:24009894] |
| 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 3 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] |
| 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] |
| 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/] |
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 11 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] |
| chemical synaptic transmission | biological process | The vesicular release of classical neurotransmitter molecules from a presynapse, across a chemical synapse, the subsequent activation of neurotransmitter 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:jl, MeSH:D009435] |
| 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] |
| regulation of postsynaptic membrane potential | biological process | Any process that modulates the potential difference across a post-synaptic membrane. [GOC:dph, GOC:ef] |
| inner ear receptor cell development | biological process | The process whose specific outcome is the progression of an inner ear receptor cell over time, from its formation to the mature structure. Cell development does not include the steps involved in committing a cell to a specific fate. [GOC:dph] |
| innervation | biological process | The process in which a nerve invades a tissue and makes functional synaptic connection within the tissue. [GOC:dph, GOC:sart] |
| 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] |
| cochlea development | biological process | The progression of the cochlea over time from its formation to the mature structure. The cochlea is the snail-shaped portion of the inner ear that is responsible for the detection of sound. [GOC:dph, GOC:tb] |
| 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 membrane potential | biological process | Any process that modulates the establishment or extent of a membrane potential, the electric potential existing across any membrane arising from charges in the membrane itself and from the charges present in the media on either side of the membrane. [GOC:jl, GOC:mtg_cardio, GOC:tb, ISBN:0198506732] |