Proteins > Gamma-aminobutyric acid receptor subunit alpha-2
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Gamma-aminobutyric acid receptor subunit alpha-2
A gamma-aminobutyric acid receptor subunit alpha-2 that is encoded in the genome of human. [PRO:DNx, UniProtKB:P47869]
Synonyms
GABA(A) receptor subunit alpha-2
Research
Bioassay Publications (66)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 3 (4.55) | 18.7374 |
| 1990's | 10 (15.15) | 18.2507 |
| 2000's | 33 (50.00) | 29.6817 |
| 2010's | 15 (22.73) | 24.3611 |
| 2020's | 5 (7.58) | 2.80 |
Compounds (110)
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 | 0.0006 | 1 | 1 |
| chlordiazepoxide | Homo sapiens (human) | Ki | 0.4260 | 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 | 0.0163 | 12 | 12 |
| fipronil | Homo sapiens (human) | IC50 | 0.0023 | 1 | 1 |
| flumazenil | Homo sapiens (human) | Ki | 0.0049 | 7 | 32 |
| flunitrazepam | Homo sapiens (human) | IC50 | 263,027.0000 | 1 | 1 |
| flunitrazepam | Homo sapiens (human) | Ki | 0.0022 | 4 | 4 |
| 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 | 0.0031 | 5 | 6 |
| temazepam | Homo sapiens (human) | IC50 | 62,517.3000 | 1 | 1 |
| triazolam | Homo sapiens (human) | Ki | 0.0006 | 1 | 1 |
| zolpidem | Homo sapiens (human) | Ki | 1.5069 | 9 | 36 |
| 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 | 0.0001 | 1 | 1 |
| 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 | 0.0153 | 2 | 2 |
| 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 | 0.0110 | 8 | 8 |
| 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 | 0.0049 | 3 | 3 |
| beta-carboline-3-carboxylic acid methyl ester | Homo sapiens (human) | IC50 | 0.0050 | 1 | 1 |
| bretazenil | Homo sapiens (human) | Ki | 0.0006 | 1 | 1 |
| cl 218872 | Homo sapiens (human) | Ki | 1.7216 | 5 | 5 |
| ro 15-3505 | Homo sapiens (human) | Ki | 0.0163 | 3 | 3 |
| zk 93426 | Homo sapiens (human) | Ki | 0.1370 | 1 | 1 |
| zk 93423 | Homo sapiens (human) | Ki | 0.0042 | 2 | 2 |
| 3-ethoxy-beta-carboline | Homo sapiens (human) | IC50 | 0.0240 | 1 | 1 |
| 3-ethoxy-beta-carboline | Homo sapiens (human) | Ki | 0.0251 | 3 | 3 |
| tert-butyl beta-carboline-3-carboxylate | Homo sapiens (human) | IC50 | 0.0100 | 1 | 1 |
| tert-butyl beta-carboline-3-carboxylate | Homo sapiens (human) | Ki | 0.0150 | 3 | 3 |
| ro 14-7437 | Homo sapiens (human) | Ki | 0.0020 | 1 | 1 |
| 3',6-dinitroflavone | Homo sapiens (human) | Ki | 0.0120 | 1 | 1 |
| l 663581 | Homo sapiens (human) | Ki | 0.0021 | 1 | 1 |
| cgp 36742 | Homo sapiens (human) | IC50 | 508.0000 | 1 | 1 |
| 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 | 0.0216 | 2 | 2 |
| 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 |
| eszopiclone | Homo sapiens (human) | Ki | 0.1140 | 1 | 1 |
| 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 |
| 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 | 0.0523 | 3 | 3 |
| apigenin | Homo sapiens (human) | Ki | 3.0200 | 1 | 1 |
| harman | Homo sapiens (human) | IC50 | 12.3027 | 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 | 15.7000 | 1 | 1 |
| l 655,708 | Homo sapiens (human) | Ki | 0.0244 | 7 | 7 |
| ry 80 | Homo sapiens (human) | Ki | 0.0199 | 7 | 12 |
| 1-Ethyl-9H-pyrido[3,4-b]indole | Homo sapiens (human) | IC50 | 251.1890 | 1 | 1 |
| ganaxolone | Homo sapiens (human) | IC50 | 0.0420 | 1 | 1 |
| mrk 016 | Homo sapiens (human) | Ki | 0.0008 | 3 | 3 |
| 6,6-dimethyl-3-(2-hydroxyethyl)thio-1-(thiazol-2-yl)-6,7-dihydro-2-benzothiophen-4(5h)-one | Homo sapiens (human) | Ki | 0.0160 | 2 | 2 |
| bis(7)-tacrine | Homo sapiens (human) | IC50 | 6.0000 | 1 | 1 |
| qh-ii-66 | Homo sapiens (human) | Ki | 0.0421 | 2 | 2 |
| l 838,417 | Homo sapiens (human) | Ki | 0.0007 | 2 | 2 |
| ry 024 | Homo sapiens (human) | Ki | 0.0263 | 5 | 5 |
| pwz-029 | Homo sapiens (human) | Ki | 0.2760 | 5 | 5 |
| 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 |
| 4-amino-8-(2-fluoro-6-methoxy-phenyl)-n-propylcinnoline-3-carboxamide | Homo sapiens (human) | Ki | 0.0003 | 2 | 3 |
| 4-amino-8-(2,5-dimethoxyphenyl)-n-propylcinnoline-3-carboxamide | Homo sapiens (human) | Ki | 0.0134 | 2 | 3 |
| apalutamide | Homo sapiens (human) | IC50 | 3.0000 | 1 | 1 |
| nitd 609 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
Drugs with Activation Measurements
Drugs with Other Measurements
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
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
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
Synthesis and biological evaluation of 7,8,9,10-tetrahydroimidazo[1,2-c]pyrido[3,4-e]pyrimdin-5(6H)-ones as functionally selective ligands of the benzodiazepine receptor site on the GABA(A) receptor.Journal of medicinal chemistry, , Nov-07, Volume: 45, Issue:23, 2002
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
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-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
[no title available]Journal of medicinal chemistry, , 04-09, Volume: 63, Issue:7, 2020
Developing dual functional allosteric modulators of GABA(A) receptors.Bioorganic & medicinal chemistry, , Dec-01, Volume: 18, Issue:23, 2010
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
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
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
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
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
[no title available]Journal of natural products, , 03-26, Volume: 84, Issue:3, 2021
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
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
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
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
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
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
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
Synthesis and biological evaluation of 7,8,9,10-tetrahydroimidazo[1,2-c]pyrido[3,4-e]pyrimdin-5(6H)-ones as functionally selective ligands of the benzodiazepine receptor site on the GABA(A) receptor.Journal of medicinal chemistry, , Nov-07, Volume: 45, Issue:23, 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
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
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
Developing dual functional allosteric modulators of GABA(A) receptors.Bioorganic & medicinal chemistry, , Dec-01, Volume: 18, Issue:23, 2010
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
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
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
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
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
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
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
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
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
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
[no title available]Journal of medicinal chemistry, , 04-09, Volume: 63, Issue:7, 2020
Ion channels as therapeutic targets: a drug discovery perspective.Journal of medicinal chemistry, , Feb-14, Volume: 56, Issue:3, 2013
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
[no title available]Journal of medicinal chemistry, , 04-09, Volume: 63, Issue:7, 2020
Ion channels as therapeutic targets: a drug discovery perspective.Journal of medicinal chemistry, , Feb-14, Volume: 56, Issue:3, 2013
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
Ion channels as therapeutic targets: a drug discovery perspective.Journal of medicinal chemistry, , Feb-14, Volume: 56, Issue:3, 2013
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
[no title available]Journal of medicinal chemistry, , 04-09, Volume: 63, Issue:7, 2020
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
[no title available]Journal of medicinal chemistry, , 04-09, Volume: 63, Issue:7, 2020
Development and SAR of functionally selective allosteric modulators of GABAA receptors.Bioorganic & medicinal chemistry, , May-01, Volume: 19, Issue:9, 2011
[no title available]Journal of medicinal chemistry, , 04-09, Volume: 63, Issue:7, 2020
Development and SAR of functionally selective allosteric modulators of GABAA receptors.Bioorganic & medicinal chemistry, , May-01, Volume: 19, Issue:9, 2011
Enables
This protein enables 5 target(s):
| Target | Category | Definition |
|---|
| protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
| benzodiazepine receptor activity | molecular function | Combining with benzodiazepines, a class of drugs with hypnotic, anxiolytic, anticonvulsive, amnestic and myorelaxant properties, to initiate a change in cell activity. [GOC:jl] |
| 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] |
| ligand-gated monoatomic ion channel activity involved in regulation of presynaptic membrane potential | molecular function | Any ligand-gated ion channel activity, occurring in the presynaptic membrane, that is involved in regulation of presynaptic membrane potential. [GOC:dos, PMID:15145529, PMID:19558451] |
| 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] |
Located In
This protein is located in 7 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] |
| synaptic vesicle membrane | cellular component | The lipid bilayer surrounding a synaptic vesicle. [GOC:mah] |
| neuronal cell body | cellular component | The portion of a neuron that includes the nucleus, but excludes cell projections such as axons and dendrites. [GOC:go_curators] |
| inhibitory synapse | cellular component | A synapse in which an action potential in the presynaptic cell reduces the probability of an action potential occurring in the postsynaptic cell. [GOC:dph, GOC:ef] |
| 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 |
|---|
| postsynapse | cellular component | The part of a synapse that is part of the post-synaptic cell. [GOC:dos] |
| 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] |
| 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/] |
| 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] |
| dendrite membrane | cellular component | The portion of the plasma membrane surrounding a dendrite. [GOC:mah] |
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 6 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] |
| regulation of presynaptic membrane potential | biological process | Any process that modulates the potential difference across a presynaptic membrane. [GOC:dph, GOC:ef] |
| 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] |
| 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] |