Target Information

Target General Infomation
Target ID
T28722
Former ID
TTDI01774
Target Name
GABA A receptor
Gene Name
GABRG3
Synonyms
GABRG3
Target Type
Successful
Disease Anxiety disorder [ICD9: 300, 311; ICD10: F32, F40-F42]
Alzheimer disease [ICD9: 331; ICD10: G30]
Anesthesia [ICD9: 338; ICD10: R20.0]
Anxiolytic and sedative [ICD10: F40-F42]
Epilepsy [ICD10: G40]
Epileptic seizures [ICD9: 345.9, 780.3; ICD10: G40, P90, R56]
Generalized anxiety disorder [ICD9: 300, 300.02, 311; ICD10: F32, F40-F42, F41.1]
General anesthesia [ICD9: 338; ICD10: R20.0]
Insomnia [ICD9: 307.41, 307.42, 327.0, 780.51, 780.52; ICD10: F51.0, G47.0]
Major depressive disorder [ICD9: 296.2, 296.3, 710.0; ICD10: F32, F33, M32]
Neuropathic pain [ICD9: 356.0, 356.8; ICD10: G64, G90.0]
Neurodegenerative disease [ICD9: 330-337; ICD10: G30-G32]
Pain [ICD9: 338, 356.0, 356.8,780; ICD10: G64, G90.0, R52, G89]
Premenstrual syndrome [ICD10: N94.3]
Panic disorder [ICD9: 300.01, 300.21; ICD10: F41.0]
Stroke [ICD9: 434.91, 437.6, 453, 671.5, 671.9; ICD10: I61-I63, I80-I82]
Sedation [ICD9: 338; ICD10: R52, G89]
Unspecified [ICD code not available]
Function
Component of the heteropentameric receptor for GABA, the major inhibitory neurotransmitter in the vertebrate brain. Functions also as histamine receptor and mediates cellular responses to histamine. Functionsas receptor for diazepines and various anesthetics, such as pentobarbital; these are bound at a separate allosteric effector binding site. Functions as ligand- gated chloride channel (By similarity).
BioChemical Class
Ligand-gated ion channel
UniProt ID
Q99928
Sequence
MAPKLLLLLCLFSGLHARSRKVEEDEYEDSSSNQKWVLAPKSQDTDVTLILNKLLREYDK
KLRPDIGIKPTVIDVDIYVNSIGPVSSINMEYQIDIFFAQTWTDSRLRFNSTMKILTLNS
NMVGLIWIPDTIFRNSKTAEAHWITTPNQLLRIWNDGKILYTLRLTINAECQLQLHNFPM
DEHSCPLIFSSYGYPKEEMIYRWRKNSVEAADQKSWRLYQFDFMGLRNTTEIVTTSAGDY
VVMTIYFELSRRMGYFTIQTYIPCILTVVLSWVSFWIKKDATPARTALGITTVLTMTTLS
TIARKSLPRVSYVTAMDLFVTVCFLFVFAALMEYATLNYYSSCRKPTTTKKTTSLLHPDS
SRWIPERISLQAPSNYSLLDMRPPPTAMITLNNSVYWQEFEDTCVYECLDGKDCQSFFCC
YEECKSGSWRKGRIHIDILELDSYSRVFFPTSFLLFNLVYWVGYLYL
Drugs and Mode of Action
Drug(s) Bentazepam Drug Info Approved Anxiety disorder [1]
Clobazam - Lundbeck Drug Info Approved Unspecified [1]
Etomidate Drug Info Approved Anesthesia [2], [3]
Mebutamate Drug Info Approved Anxiolytic and sedative [1]
Metharbital Drug Info Approved Epilepsy [4], [5]
Stiripentol Drug Info Approved Epilepsy [6], [7]
Talbutal Drug Info Approved Sedation [8]
Thiamylal Drug Info Approved Anesthesia [9], [10]
Clomethiazole Drug Info Phase 3 Stroke [11]
Remimazolam Drug Info Phase 3 Anesthesia [12], [13]
Pagoclone Drug Info Phase 2/3 Anxiety disorder [14]
Etazolate Drug Info Phase 2 Neurodegenerative disease [15], [16]
EVT-201 Drug Info Phase 2 Insomnia [17]
SARIPIDEM Drug Info Phase 2 Anxiety disorder [18]
T-2007 Drug Info Phase 2 Epilepsy [19]
AZD-3043 Drug Info Phase 1 Anesthesia [20]
NSD-788 Drug Info Phase 1 Anxiety disorder [21]
Org-25435 Drug Info Phase 1 Epilepsy [22]
RWJ-51204 Drug Info Preclinical Anxiety disorder [23]
Suriclone Drug Info Discontinued in Preregistration Anxiety disorder [24]
Ocinaplon Drug Info Discontinued in Phase 3 Generalized anxiety disorder [25], [26]
PAZINACLONE Drug Info Discontinued in Phase 3 Anxiety disorder [27]
Y-23684 Drug Info Discontinued in Phase 3 Anxiety disorder [28]
LORECLEZOLE Drug Info Discontinued in Phase 2 Epileptic seizures [29], [30]
NGD 91-3 Drug Info Discontinued in Phase 2 Anxiety disorder [31]
RESEQUINIL Drug Info Discontinued in Phase 2 Epilepsy [32]
RO-48-6791 Drug Info Discontinued in Phase 2 Anxiety disorder [33]
SL-65.1498 Drug Info Discontinued in Phase 2 Anxiety disorder [34]
Suritozole Drug Info Discontinued in Phase 2 Major depressive disorder [35]
CCD-3693 Drug Info Discontinued in Phase 1 Anxiety disorder [36]
CTP-354 Drug Info Discontinued in Phase 1 Pain [37]
Org-21465 Drug Info Discontinued in Phase 1 Anesthesia [38]
RO-48-8684 Drug Info Discontinued in Phase 1 Anxiety disorder [39]
Co-152791 Drug Info Terminated Epilepsy [40]
Girisopam Drug Info Terminated Anxiety disorder [41]
NSD-721 Drug Info Terminated Anxiety disorder [42]
Ro-15-3505 Drug Info Terminated Discovery agent [43]
Ro-19-8022 Drug Info Terminated Anxiety disorder [44]
RU-33965 Drug Info Terminated Alzheimer disease [45]
ZK-91296 Drug Info Terminated Alzheimer disease [46]
ZK-93426 Drug Info Terminated Alzheimer disease [47], [48]
Modulator AA-29504 Drug Info [49]
AZD-3043 Drug Info [50]
Bentazepam Drug Info [51], [1]
C-21191 Drug Info [49]
CCD-3693 Drug Info [52]
Clobazam - Lundbeck Drug Info [53]
Clomethiazole Drug Info
Co-152791 Drug Info [54]
CP-409092 Drug Info [55]
CTP-354 Drug Info [56]
DOV-51892 Drug Info [49]
Etazolate Drug Info [15]
Etomidate Drug Info [53]
EVT-201 Drug Info [49]
GIDAZEPAM Drug Info [57]
Girisopam Drug Info
HZ-166 Drug Info [49]
LORECLEZOLE Drug Info [58]
Mebutamate Drug Info [53]
Metharbital Drug Info [53]
NGD 96-3 Drug Info [49]
NSD-721 Drug Info [49]
NSD-788 Drug Info [49]
Ocinaplon Drug Info [59]
Org-21465 Drug Info [60]
Org-25435 Drug Info [61]
Pagoclone Drug Info [62]
PAZINACLONE Drug Info [63]
PNU 101017 Drug Info
Ro-15-3505 Drug Info
Ro-19-8022 Drug Info
RO-48-6791 Drug Info [64]
RO-48-8684 Drug Info [65]
RU-33965 Drug Info [66]
RWJ-51204 Drug Info [67]
SARIPIDEM Drug Info [18]
Short-acting etomidate analogue Drug Info [49]
Stiripentol Drug Info [6], [1]
Suriclone Drug Info [68]
Suritozole Drug Info [69]
Talbutal Drug Info [53]
Thiamylal Drug Info [53]
UC-2024 Drug Info [49]
UC-2029 Drug Info [49]
Y-23684 Drug Info [70]
ZK-91296 Drug Info
ZK-93426 Drug Info
Modulator (allosteric modulator) alpha3IA Drug Info [49]
alpha5IA Drug Info [49]
DMCM Drug Info [49]
tetrahydrodeoxycorticosterone Drug Info [49]
TP003 Drug Info [49]
[11C]flumazenil Drug Info [49]
[18F]fluoroethylflumazenil Drug Info [49]
[3H]CGS8216 Drug Info [49]
[3H]Ro154513 Drug Info [49]
[3H]zolpidem Drug Info [49]
Agonist isonipecotic acid Drug Info [49]
JM-1232(-) Drug Info [49]
NGD 91-3 Drug Info [71]
piperidine-4-sulphonic acid Drug Info [49]
Remimazolam Drug Info [72]
RESEQUINIL Drug Info [73]
SL-65.1498 Drug Info [74]
T-2007 Drug Info [49]
[3H]muscimol Drug Info [49]
Blocker (channel blocker) TBPS Drug Info [49]
[35S]TBPS Drug Info [49]
Antagonist UC-1011 Drug Info [49]
Pathways
KEGG Pathway Neuroactive ligand-receptor interaction
Retrograde endocannabinoid signaling
GABAergic synapse
Morphine addiction
Nicotine addiction
Reactome Ligand-gated ion channel transport
GABA A receptor activation
WikiPathways SIDS Susceptibility Pathways
Neurotransmitter Receptor Binding And Downstream Transmission In The Postsynaptic Cell
Iron uptake and transport
References
REF 1Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
REF 2Anaesthetic drugs: linking molecular actions to clinical effects. Curr Pharm Des. 2006;12(28):3665-79.
REF 3(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 5463).
REF 4FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 008322.
REF 5(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7230).
REF 6Stiripentol, a putative antiepileptic drug, enhances the duration of opening of GABA-A receptor channels. Epilepsia. 2006 Apr;47(4):704-16.
REF 7(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 5469).
REF 8FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 009410.
REF 9(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7305).
REF 10Drug information of Thiamylal, 2008. eduDrugs.
REF 11ClinicalTrials.gov (NCT02374567) Pharmacovigilance in Gerontopsychiatric Patients. U.S. National Institutes of Health.
REF 12ClinicalTrials.gov (NCT02523859) Study Evaluating the Efficacy and Safety of Remimazolam in General Anesthesia in Adult Patients Undergoing Cardiac Surgery.
REF 13(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 8442).
REF 14ClinicalTrials.gov (NCT00830154) A Study to Assess the Efficacy and Safety of Pagoclone for Adults With Stuttering. U.S. National Institutes of Health.
REF 15Etazolate, a neuroprotective drug linking GABA(A) receptor pharmacology to amyloid precursor protein processing. J Neurochem. 2008 Jul;106(1):392-404.
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REF 17ClinicalTrials.gov (NCT00380003) Efficacy Study of EVT 201 to Treat Insomnia. U.S. National Institutes of Health.
REF 18Behavioural effects of novel benzodiazepine (omega) receptor agonists and partial agonists: increases in punished responding and antagonism of the pentylenetetrazole cue. Behav Pharmacol. 1995 Mar;6(2):116-126.
REF 19ClinicalTrials.gov (NCT00939653) T2007-002 Clofarabine, Etoposide, Cyclophosphamide in Relapsed Acute Myelogenous Leukemia (AML). U.S. National Institutes of Health.
REF 20ClinicalTrials.gov (NCT01086813) Phase I, Single Centre, Study to Assess Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of AZD3043. U.S. National Institutes of Health.
REF 21Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800028006)
REF 22ClinicalTrials.gov (NCT01062867) First Administration to Man Of Org 25435 a New Intravenous Anesthetic. U.S. National Institutes of Health.
REF 23Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800015754)
REF 24Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000574)
REF 25(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 4277).
REF 26Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001407)
REF 27Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000717)
REF 28The pharmacological properties of Y-23684, a benzodiazepine receptor partial agonist.. Br J Pharmacol. 1994 April; 111(4): 1170-1178.
REF 29(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 5466).
REF 30Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007906)
REF 31Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800011480)
REF 32Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010724)
REF 33Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007556)
REF 34Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800014726)
REF 35Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001322)
REF 36Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006723)
REF 37Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800038187)
REF 38Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006459)
REF 39Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007572)
REF 40Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800011029)
REF 41Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005437)
REF 42Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010233)
REF 43Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005900)
REF 44Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001584)
REF 45Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001729)
REF 46Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000552)
REF 47(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 4347).
REF 48Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001474)
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REF 50AZD-3043: a novel, metabolically labile sedative-hypnotic agent with rapid and predictable emergence from hypnosis. Anesthesiology. 2012 Jun;116(6):1267-77.
REF 51Prodynorphin gene deletion increased anxiety-like behaviours, impaired the anxiolytic effect of bromazepam and altered GABAA receptor subunits gene expression in the amygdala. J Psychopharmacol. 2011Jan;25(1):87-96.
REF 52Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.
REF 53Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
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REF 55The ChEMBL database in 2017.
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REF 58Direct activation of GABAA receptors by loreclezole, an anticonvulsant drug with selectivity for the beta-subunit. Neuropharmacology. 1996;35(12):1753-60.
REF 59Discriminative stimulus properties of GABAA receptor positive allosteric modulators TPA023, ocinaplon and NG2-73 in rats trained to discriminate chlordiazepoxide or zolpidem. Eur J Pharmacol. 2011 Oct 1;668(1-2):190-3.
REF 60Computer-controlled infusion of ORG 21465, a water soluble steroid i.v. anaesthetic agent, into human volunteers. Br J Anaesth. 1997 Oct;79(4):433-9.
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REF 62Evaluation of the abuse potential of pagoclone, a partial GABAA agonist. J Clin Psychopharmacol. 2006 Jun;26(3):268-73.
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REF 65Integrated pharmacokinetics and pharmacodynamics of Ro 48-8684, a new benzodiazepine, in comparison with midazolam during first administration to healthy male subjects. Br J Clin Pharmacol. 1997 Nov;44(5):487-93.
REF 66Discriminative stimulus properties of RU 33965, a benzodiazepine receptor weak partial inverse agonist. Pharmacol Biochem Behav. 1992 Oct;43(2):583-8.
REF 675-ethoxymethyl-7-fluoro-3-oxo-1,2,3,5-tetrahydrobenzo[4,5]imidazo[1,2a]pyridine-4-N-(2-fluorophenyl)carboxamide (RWJ-51204), a new nonbenzodiazepine anxiolytic. J Pharmacol Exp Ther. 2002 Nov;303(2):777-90.
REF 68The effect of cyclopyrrolones on GABAA receptor function is different from that of benzodiazepines. Naunyn Schmiedebergs Arch Pharmacol. 1994 Sep;350(3):294-300.
REF 69Chronic postinjury administration of MDL 26,479 (Suritozole), a negative modulator at the GABAA receptor, and cognitive impairment in rats following traumatic brain injury. J Neurosurg. 1995 Nov;83(5):878-83.
REF 70The pharmacological properties of Y-23684, a benzodiazepine receptor partial agonist. Br J Pharmacol. 1994 Apr;111(4):1170-8.
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