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 Anxiolytic and sedative [ICD10: F40-F42]
Anxiety disorder [ICD9: 300, 311; ICD10: F32, F40-F42]
Alzheimer disease [ICD9: 331; ICD10: G30]
Anesthesia [ICD9: 338; ICD10: R20.0]
Epileptic seizures [ICD9: 345.9, 780.3; ICD10: G40, P90, R56]
Epilepsy [ICD10: G40]
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]
Panic disorder [ICD9: 300.01, 300.21; ICD10: F41.0]
Pain [ICD9: 338, 356.0, 356.8,780; ICD10: G64, G90.0, R52, G89]
Premenstrual syndrome [ICD10: N94.3]
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 [551871]
Clobazam - Lundbeck Drug Info Approved Unspecified [551871]
Etomidate Drug Info Approved Anesthesia [536300], [540865]
Mebutamate Drug Info Approved Anxiolytic and sedative [551871]
Metharbital Drug Info Approved Epilepsy [538407], [542246]
Stiripentol Drug Info Approved Epilepsy [528174], [540871]
Talbutal Drug Info Approved Sedation [538418]
Thiamylal Drug Info Approved Anesthesia [542327], [550765]
Clomethiazole Drug Info Phase 3 Stroke [525101]
Remimazolam Drug Info Phase 3 Anesthesia [525292], [543138]
Pagoclone Drug Info Phase 2/3 Anxiety disorder [522559]
Etazolate Drug Info Phase 2 Neurodegenerative disease [529410], [542359]
EVT-201 Drug Info Phase 2 Insomnia [521889]
SARIPIDEM Drug Info Phase 2 Anxiety disorder [525986]
T-2007 Drug Info Phase 2 Epilepsy [522725]
AZD-3043 Drug Info Phase 1 Anesthesia [522974]
NSD-788 Drug Info Phase 1 Anxiety disorder [548723]
Org-25435 Drug Info Phase 1 Epilepsy [522942]
RWJ-51204 Drug Info Preclinical Anxiety disorder [547383]
Suriclone Drug Info Discontinued in Preregistration Anxiety disorder [544682]
Ocinaplon Drug Info Discontinued in Phase 3 Generalized anxiety disorder [467614], [544880]
PAZINACLONE Drug Info Discontinued in Phase 3 Anxiety disorder [544719]
Y-23684 Drug Info Discontinued in Phase 3 Anxiety disorder [544030]
LORECLEZOLE Drug Info Discontinued in Phase 2 Epileptic seizures [540868], [546397]
NGD 91-3 Drug Info Discontinued in Phase 2 Anxiety disorder [546952]
RESEQUINIL Drug Info Discontinued in Phase 2 Epilepsy [546863]
RO-48-6791 Drug Info Discontinued in Phase 2 Anxiety disorder [546337]
SL-65.1498 Drug Info Discontinued in Phase 2 Anxiety disorder [547275]
Suritozole Drug Info Discontinued in Phase 2 Major depressive disorder [544851]
CCD-3693 Drug Info Discontinued in Phase 1 Anxiety disorder [546165]
CTP-354 Drug Info Discontinued in Phase 1 Pain [549484]
Org-21465 Drug Info Discontinued in Phase 1 Anesthesia [546127]
RO-48-8684 Drug Info Discontinued in Phase 1 Anxiety disorder [546340]
Co-152791 Drug Info Terminated Epilepsy [546908]
Girisopam Drug Info Terminated Anxiety disorder [545943]
NSD-721 Drug Info Terminated Anxiety disorder [546776]
Ro-15-3505 Drug Info Terminated Discovery agent [546017]
Ro-19-8022 Drug Info Terminated Anxiety disorder [544933]
RU-33965 Drug Info Terminated Alzheimer disease [544965]
ZK-91296 Drug Info Terminated Alzheimer disease [544676]
ZK-93426 Drug Info Terminated Alzheimer disease [467684], [544909]
Modulator AA-29504 Drug Info [543814]
AZD-3043 Drug Info [531883]
Bentazepam Drug Info [530960], [551871]
C-21191 Drug Info [543814]
CCD-3693 Drug Info [1572591]
Clobazam - Lundbeck Drug Info [556264]
Clomethiazole Drug Info
Co-152791 Drug Info [534715]
CP-409092 Drug Info [1572605]
CTP-354 Drug Info [550561]
DOV-51892 Drug Info [543814]
Etazolate Drug Info [529410]
Etomidate Drug Info [556264]
EVT-201 Drug Info [543814]
GIDAZEPAM Drug Info [525609]
Girisopam Drug Info
HZ-166 Drug Info [543814]
LORECLEZOLE Drug Info [534346]
Mebutamate Drug Info [556264]
Metharbital Drug Info [556264]
NGD 96-3 Drug Info [543814]
NSD-721 Drug Info [543814]
NSD-788 Drug Info [543814]
Ocinaplon Drug Info [531560]
Org-21465 Drug Info [534520]
Org-25435 Drug Info [530997]
Pagoclone Drug Info [528204]
PAZINACLONE Drug Info [536090]
PNU 101017 Drug Info
Ro-15-3505 Drug Info
Ro-19-8022 Drug Info
RO-48-6791 Drug Info [534517]
RO-48-8684 Drug Info [534518]
RU-33965 Drug Info [526780]
RWJ-51204 Drug Info [526442]
SARIPIDEM Drug Info [525986]
Short-acting etomidate analogue Drug Info [543814]
Stiripentol Drug Info [528174], [551871]
Suriclone Drug Info [553196]
Suritozole Drug Info [533581]
Talbutal Drug Info [556264]
Thiamylal Drug Info [556264]
UC-2024 Drug Info [543814]
UC-2029 Drug Info [543814]
Y-23684 Drug Info [533803]
ZK-91296 Drug Info
ZK-93426 Drug Info
Modulator (allosteric modulator) alpha3IA Drug Info [543814]
alpha5IA Drug Info [543814]
DMCM Drug Info [543814]
tetrahydrodeoxycorticosterone Drug Info [543814]
TP003 Drug Info [543814]
[11C]flumazenil Drug Info [543814]
[18F]fluoroethylflumazenil Drug Info [543814]
[3H]CGS8216 Drug Info [543814]
[3H]Ro154513 Drug Info [543814]
[3H]zolpidem Drug Info [543814]
Agonist isonipecotic acid Drug Info [543814]
JM-1232(-) Drug Info [543814]
NGD 91-3 Drug Info [526675]
piperidine-4-sulphonic acid Drug Info [543814]
Remimazolam Drug Info [531293]
RESEQUINIL Drug Info [550144]
SL-65.1498 Drug Info [550122]
T-2007 Drug Info [543814]
[3H]muscimol Drug Info [543814]
Blocker (channel blocker) TBPS Drug Info [543814]
[35S]TBPS Drug Info [543814]
Antagonist UC-1011 Drug Info [543814]
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 467614(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 467684(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 521889ClinicalTrials.gov (NCT00380003) Efficacy Study of EVT 201 to Treat Insomnia. U.S. National Institutes of Health.
Ref 522559ClinicalTrials.gov (NCT00830154) A Study to Assess the Efficacy and Safety of Pagoclone for Adults With Stuttering. U.S. National Institutes of Health.
Ref 522725ClinicalTrials.gov (NCT00939653) T2007-002 Clofarabine, Etoposide, Cyclophosphamide in Relapsed Acute Myelogenous Leukemia (AML). U.S. National Institutes of Health.
Ref 522942ClinicalTrials.gov (NCT01062867) First Administration to Man Of Org 25435 a New Intravenous Anesthetic. U.S. National Institutes of Health.
Ref 522974ClinicalTrials.gov (NCT01086813) Phase I, Single Centre, Study to Assess Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of AZD3043. U.S. National Institutes of Health.
Ref 525101ClinicalTrials.gov (NCT02374567) Pharmacovigilance in Gerontopsychiatric Patients. U.S. National Institutes of Health.
Ref 525292ClinicalTrials.gov (NCT02523859) Study Evaluating the Efficacy and Safety of Remimazolam in General Anesthesia in Adult Patients Undergoing Cardiac Surgery.
Ref 525986Behavioural 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 528174Stiripentol, a putative antiepileptic drug, enhances the duration of opening of GABA-A receptor channels. Epilepsia. 2006 Apr;47(4):704-16.
Ref 529410Etazolate, a neuroprotective drug linking GABA(A) receptor pharmacology to amyloid precursor protein processing. J Neurochem. 2008 Jul;106(1):392-404.
Ref 536300Anaesthetic drugs: linking molecular actions to clinical effects. Curr Pharm Des. 2006;12(28):3665-79.
Ref 538407FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 008322.
Ref 538418FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 009410.
Ref 540865(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 540868(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 540871(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 542246(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 542327(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 542359(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: 7336).
Ref 543138(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 544030The pharmacological properties of Y-23684, a benzodiazepine receptor partial agonist.. Br J Pharmacol. 1994 April; 111(4): 1170-1178.
Ref 544676Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000552)
Ref 544682Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000574)
Ref 544719Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000717)
Ref 544851Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001322)
Ref 544880Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001407)
Ref 544909Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001474)
Ref 544933Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001584)
Ref 544965Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001729)
Ref 545943Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005437)
Ref 546017Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005900)
Ref 546127Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006459)
Ref 546165Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006723)
Ref 546337Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007556)
Ref 546340Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007572)
Ref 546397Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007906)
Ref 546776Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010233)
Ref 546863Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010724)
Ref 546908Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800011029)
Ref 546952Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800011480)
Ref 547275Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800014726)
Ref 547383Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800015754)
Ref 548723Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800028006)
Ref 549484Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800038187)
Ref 550765Drug information of Thiamylal, 2008. eduDrugs.
Ref 551871Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
Ref
Ref 525609Discriminative effects of phenazepam and gidazepam in rats: comparison with other GABA-related drugs. Pharmacol Biochem Behav. 1999 Oct;64(2):397-401.
Ref 525986Behavioural 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 5264425-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 526675Anxioselective compounds acting at the GABA(A) receptor benzodiazepine binding site. Curr Drug Targets CNS Neurol Disord. 2003 Aug;2(4):213-32.
Ref 526780Discriminative stimulus properties of RU 33965, a benzodiazepine receptor weak partial inverse agonist. Pharmacol Biochem Behav. 1992 Oct;43(2):583-8.
Ref 528174Stiripentol, a putative antiepileptic drug, enhances the duration of opening of GABA-A receptor channels. Epilepsia. 2006 Apr;47(4):704-16.
Ref 528204Evaluation of the abuse potential of pagoclone, a partial GABAA agonist. J Clin Psychopharmacol. 2006 Jun;26(3):268-73.
Ref 529410Etazolate, a neuroprotective drug linking GABA(A) receptor pharmacology to amyloid precursor protein processing. J Neurochem. 2008 Jul;106(1):392-404.
Ref 530960Prodynorphin 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 530997First administration to man of Org 25435, an intravenous anaesthetic: A Phase 1 Clinical Trial. BMC Anesthesiol. 2010 Jun 29;10:10.
Ref 531293Remimazolam, a short-acting GABA(A) receptor agonist for intravenous sedation and/or anesthesia in day-case surgical and non-surgical procedures. IDrugs. 2010 Dec;13(12):929-37.
Ref 531560Discriminative 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 531883AZD-3043: a novel, metabolically labile sedative-hypnotic agent with rapid and predictable emergence from hypnosis. Anesthesiology. 2012 Jun;116(6):1267-77.
Ref 533581Chronic 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 533803The pharmacological properties of Y-23684, a benzodiazepine receptor partial agonist. Br J Pharmacol. 1994 Apr;111(4):1170-8.
Ref 534346Direct activation of GABAA receptors by loreclezole, an anticonvulsant drug with selectivity for the beta-subunit. Neuropharmacology. 1996;35(12):1753-60.
Ref 534517Integrated pharmacokinetics and pharmacodynamics of Ro 48-6791, a new benzodiazepine, in comparison with midazolam during first administration to healthy male subjects. Br J Clin Pharmacol. 1997 Nov;44(5):477-86.
Ref 534518Integrated 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 534520Computer-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.
Ref 534715Substituted 3beta-phenylethynyl derivatives of 3alpha-hydroxy-5alpha-pregnan-20-one: remarkably potent neuroactive steroid modulators of gamma-aminobutyric acidA receptors. J Pharmacol Exp Ther. 1998Oct;287(1):198-207.
Ref 536090The benzodiazepine binding site of GABA(A) receptors as a target for the development of novel anxiolytics. Expert Opin Investig Drugs. 2005 May;14(5):601-18.
Ref 543814(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. (Target id: 415).
Ref 550122WO patent application no. 2005,0749,31, Pharmaceutical combinations comprising (s) -pantoprazole.
Ref 550144WO patent application no. 2010,0024,51, Naphthyridin derivatives.
Ref 550561Clinical pipeline report, company report or official report of Concert Pharmaceuticals.
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Ref 553196The effect of cyclopyrrolones on GABAA receptor function is different from that of benzodiazepines. Naunyn Schmiedebergs Arch Pharmacol. 1994 Sep;350(3):294-300.
Ref 556264Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
Ref 1572591Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.
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