DGIdb - GABRA6 Gene Record

GABRA6 2559 Druggable Genome

Alternate Names:

2559
GAMMA-AMINOBUTYRIC ACID TYPE A RECEPTOR ALPHA6 SUBUNIT
GABRA6
137143
4080
ENSG00000145863
OTTHUMG00000130351
BE0000764
Q16445
GBRA6_HUMAN
GAMMA-AMINOBUTYRIC ACID RECEPTOR SUBUNIT ALPHA-6
GAMMA-AMINOBUTYRIC-ACID RECEPTOR ALPHA-6 SUBUNIT PRECURSOR (GABA(A) RECEPTOR). [SOURCE:UNIPROT/SWISSPROT;ACC:Q16445]
GABA(A) receptor subunit alpha-6
409
NP_000802
NM_000811
α6
gamma-aminobutyric acid (GABA) A receptor, alpha 6
GABA<sub>A</sub> receptor α6 subunit

Gene Info:

Human Readable Name	ION CHANNEL
Interpro Short Name	Neur_channel
Interpro Name	Neurotransmitter-gated ion-channel ligand-binding
Interpro Short Name	Neur_chan_lig-bd
Interpro Acc	IPR006202
Uniprot Status	Swiss-Prot
Human Readable Name	DRUGGABLE GENOME
Uniprot Evidence	2: Evidence at transcript level
Interpro Acc	IPR006201
Interpro Name	Neurotransmitter-gated ion-channel
Interpro Type	Domain
Interpro Type	Family
Target Main Class	Receptors
Target Subclass	cys-loop
Target Subclass	Channels
Transmembrane Helix Count	4
Target Subclass	Ligand_gated_ion_channels
Target Class	Receptors
Target Subclass	TC:1.A.9
GuideToPharmacology Gene Category Name	GABA<sub>A</sub> receptors
GuideToPharmacology Gene Category ID	72
GuideToPharmacology Gene Type	lgic
Gene Biotype	PROTEIN_CODING"

(7 More Sources)

Publications:

Riss et al., 2008, Benzodiazepines in epilepsy: pharmacology and pharmacokinetics., Acta Neurol. Scand.
Giersch et al., 2010, Atypical behavioural effects of lorazepam: clues to the design of novel therapies?, Pharmacol. Ther.
Yamakura et al., 2001, Anesthetics and ion channels: molecular models and sites of action., Annu. Rev. Pharmacol. Toxicol.
Mehta et al., 1999, An update on GABAA receptors., Brain Res. Brain Res. Rev.
Gonzalez et al., 2009, Carisoprodol-mediated modulation of GABAA receptors: in vitro and in vivo studies., J. Pharmacol. Exp. Ther.
Rho et al., 1997, Barbiturate-like actions of the propanediol dicarbamates felbamate and meprobamate., J. Pharmacol. Exp. Ther.
Möhler et al., 2002, A new benzodiazepine pharmacology., J. Pharmacol. Exp. Ther.
Olsen et al., 2011, GABA(A) receptors as molecular targets of general anesthetics: identification of binding sites provides clues to allosteric modulation., Can J Anaesth
You et al., 2010, Benzodiazepine modulation of the rat GABAA receptor α4β3γ2L subtype expressed in Xenopus oocytes., Neuropharmacology
Skilbeck et al., 2008, Antipsychotic drug administration differentially affects [3H]muscimol and [3H]flunitrazepam GABA(A) receptor binding sites., Prog. Neuropsychopharmacol. Biol. Psychiatry
Santhakumar et al., 2006, Contributions of the GABAA receptor alpha6 subunit to phasic and tonic inhibition revealed by a naturally occurring polymorphism in the alpha6 gene., J. Neurosci.

MEPROBAMATE GABRA6

Interaction Types:

agonist

Interaction Info:

Trial Name -

Novel drug target Established target

Mechanism of Interaction GABA-A receptor; anion channel agonist

Publications:

Gonzalez et al., 2009, Carisoprodol-mediated modulation of GABAA receptors: in vitro and in vivo studies., J. Pharmacol. Exp. Ther.

Rho et al., 1997, Barbiturate-like actions of the propanediol dicarbamates felbamate and meprobamate., J. Pharmacol. Exp. Ther.

GABOXADOL GABRA6

Interaction Types:

agonist

Interaction Info:

Mechanism of Interaction GABA-A receptor; agonist GABA site agonist

Direct Interaction yes

Specific Binding Site for Interaction GABA site

Publications:
CLOBAZAM GABRA6

Interaction Types:

positive allosteric modulator

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Direct Interaction yes

Trial Name Clobazam

Publications:
ISOGUVACINE GABRA6

Interaction Types:

agonist

Interaction Info:

Specific Binding Site for Interaction GABA site

Specific Action of the Ligand Full agonist

Endogenous Drug? False

Publications:
ISONIPECOTIC ACID GABRA6

Interaction Types:

agonist

Interaction Info:

Specific Binding Site for Interaction GABA site

Specific Action of the Ligand Full agonist

Details of Interaction relatively high efficacy

Publications:
MUSCIMOL GABRA6

Interaction Types:

agonist

Interaction Info:

Specific Binding Site for Interaction GABA site

Specific Action of the Ligand Full agonist

Endogenous Drug? False

Publications:
CHEMBL34155 GABRA6

Interaction Types:

agonist

Interaction Info:

Specific Binding Site for Interaction GABA site

Specific Action of the Ligand Full agonist

Details of Interaction low efficacy

Publications:
CGS-8216 GABRA6

Interaction Types:

agonist

Interaction Info:

Specific Action of the Ligand Inverse agonist

Endogenous Drug? False

Direct Interaction? False

Publications:
CHEMBL70176 GABRA6

Interaction Types:

allosteric modulator

Interaction Info:

Specific Binding Site for Interaction benzodiazepine site

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Publications:
BRETAZENIL GABRA6

Interaction Types:

allosteric modulator

Interaction Info:

Specific Binding Site for Interaction benzodiazepine site

Specific Action of the Ligand Full agonist

Endogenous Drug? False

Publications:
CHEMBL274866 GABRA6

Interaction Types:

allosteric modulator

Interaction Info:

Specific Binding Site for Interaction benzodiazepine site

Specific Action of the Ligand Full agonist

Endogenous Drug? False

Publications:
Ro-154513 GABRA6

Interaction Types:

allosteric modulator

Interaction Info:

Specific Binding Site for Interaction benzodiazepine site

Specific Action of the Ligand Full agonist

Endogenous Drug? False

Publications:
ZINC ION GABRA6

Interaction Types:

allosteric modulator

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? True

Direct Interaction? False

Publications:
FLUMAZENIL GABRA6

Interaction Types:

allosteric modulator

Interaction Info:

Specific Binding Site for Interaction benzodiazepine site

Specific Action of the Ligand Partial agonist

Details of Interaction low affinity

Publications:
METHOCTRAMINE GABRA6

Interaction Types:

allosteric modulator

Interaction Info:

Specific Action of the Ligand Potentiation

Endogenous Drug? True

Direct Interaction? False

Publications:
BICUCULLINE GABRA6

Interaction Types:

antagonist

Interaction Info:

Specific Binding Site for Interaction GABA site

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Publications:
GABAZINE GABRA6

Interaction Types:

antagonist

Interaction Info:

Specific Binding Site for Interaction GABA site

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Publications:
PICROTOXIN GABRA6

Interaction Types:

channel blocker

Interaction Info:

Specific Action of the Ligand None

Endogenous Drug? False

Direct Interaction? False

Publications:
T-BUTYLBICYCLOPHOSPHOROTHIONATE GABRA6

Interaction Types:

channel blocker

Interaction Info:

Specific Action of the Ligand None

Endogenous Drug? False

Direct Interaction? False

Publications:
CLORAZEPATE DIPOTASSIUM GABRA6

Interaction Types:

positive allosteric modulator

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Direct Interaction yes

Publications:
CHLORDIAZEPOXIDE GABRA6

Interaction Types:

positive allosteric modulator

Interaction Info:

Trial Name -

Novel drug target Established target

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Publications:
DIAZEPAM GABRA6

Interaction Types:

positive allosteric modulator

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Direct Interaction yes

Publications:
ALPRAZOLAM GABRA6

Interaction Types:

positive allosteric modulator

Interaction Info:

Trial Name alprazolam,Xanax, Xanax XR

Novel drug target Established target

Trial Name AZ-002, Staccato alprazolam

Publications:
CLONAZEPAM GABRA6

Interaction Types:

positive allosteric modulator

Interaction Info:

Trial Name JZP-8

Novel drug target Established target

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Publications:
ESTAZOLAM GABRA6

Interaction Types:

positive allosteric modulator

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Direct Interaction yes

Publications:
BUTABARBITAL SODIUM GABRA6

Interaction Types:

positive allosteric modulator

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Direct Interaction yes

Publications:
LORAZEPAM GABRA6

Interaction Types:

positive allosteric modulator

Interaction Info:

Trial Name -

Novel drug target Established target

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Publications:
METHOHEXITAL SODIUM GABRA6

Interaction Types:

positive allosteric modulator

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Direct Interaction yes

Publications:
METHYPRYLON GABRA6

Interaction Types:

positive allosteric modulator

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Direct Interaction yes

Publications:
MIDAZOLAM HYDROCHLORIDE GABRA6

Interaction Types:

positive allosteric modulator

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Direct Interaction yes

Publications:
PENTOBARBITAL SODIUM GABRA6

Interaction Types:

positive allosteric modulator

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Direct Interaction yes

Publications:
SEVOFLURANE GABRA6

Interaction Types:

positive allosteric modulator

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Direct Interaction yes

Publications:
THIAMYLAL SODIUM GABRA6

Interaction Types:

positive allosteric modulator

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Direct Interaction yes

Publications:
FLURAZEPAM HYDROCHLORIDE GABRA6

Interaction Types:

positive allosteric modulator

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Direct Interaction yes

Publications:
HALAZEPAM GABRA6

Interaction Types:

positive allosteric modulator

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Direct Interaction yes

Publications:
HALOTHANE GABRA6

Interaction Types:

positive allosteric modulator

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Direct Interaction yes

Publications:
ISOFLURANE GABRA6

Interaction Types:

positive allosteric modulator

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Direct Interaction yes

Publications:
PF-06372865 GABRA6

Interaction Types:

agonist

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel agonist

Direct Interaction yes

Publications:
PROPOFOL GABRA6

Interaction Types:

positive allosteric modulator

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Direct Interaction yes

Publications:
Lorediplon GABRA6

Interaction Types:

positive allosteric modulator

Interaction Info:

Mechanism of Interaction GABA-A receptor; benzodiazepine site positive allosteric modulator

Direct Interaction yes

Publications:
PENTOBARBITAL GABRA6

Interaction Types:

positive allosteric modulator

Interaction Info:

Trial Name -

Novel drug target Established target

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Publications:
ADIPIPLON GABRA6

Interaction Types:

partial agonist

Interaction Info:

Trial Name NG2-73

Novel drug target Established target

Mechanism of Interaction GABA-A receptor; benzodiazepine site partial agonist

Publications:
CHLORDIAZEPOXIDE HYDROCHLORIDE GABRA6

Interaction Types:

positive allosteric modulator

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Direct Interaction yes

Publications:
ESZOPICLONE GABRA6

Interaction Types:

positive allosteric modulator

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Direct Interaction yes

Publications:
DESFLURANE GABRA6

Interaction Types:

positive allosteric modulator

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Direct Interaction yes

Publications:
QUAZEPAM GABRA6

Interaction Types:

positive allosteric modulator

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Direct Interaction yes

Publications:
SECOBARBITAL SODIUM GABRA6

Interaction Types:

positive allosteric modulator

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Direct Interaction yes

Publications:
THIOPENTAL SODIUM GABRA6

Interaction Types:

positive allosteric modulator

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Direct Interaction yes

Publications:
RESEQUINIL GABRA6

Interaction Types:

inverse agonist

Interaction Info:

Mechanism of Interaction GABA-A receptor; benzodiazepine site inverse agonist

Direct Interaction yes

Publications:
PRAZEPAM GABRA6

Interaction Types:

positive allosteric modulator

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Direct Interaction yes

Publications:

TEMAZEPAM GABRA6

Interaction Types:

potentiator

positive allosteric modulator

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Direct Interaction yes

Trial Name -

Publications:

Riss et al., 2008, Benzodiazepines in epilepsy: pharmacology and pharmacokinetics., Acta Neurol. Scand.

Giersch et al., 2010, Atypical behavioural effects of lorazepam: clues to the design of novel therapies?, Pharmacol. Ther.

BUTALBITAL GABRA6

Interaction Types:

potentiator

positive allosteric modulator

Interaction Info:

Trial Name -

Novel drug target Established target

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Publications:

Yamakura et al., 2001, Anesthetics and ion channels: molecular models and sites of action., Annu. Rev. Pharmacol. Toxicol.

Mehta et al., 1999, An update on GABAA receptors., Brain Res. Brain Res. Rev.

TALBUTAL GABRA6

Interaction Types:

potentiator

positive allosteric modulator

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Direct Interaction yes

Trial Name -

Publications:

Yamakura et al., 2001, Anesthetics and ion channels: molecular models and sites of action., Annu. Rev. Pharmacol. Toxicol.

Mehta et al., 1999, An update on GABAA receptors., Brain Res. Brain Res. Rev.

SECOBARBITAL GABRA6

Interaction Types:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

Publications:

Yamakura et al., 2001, Anesthetics and ion channels: molecular models and sites of action., Annu. Rev. Pharmacol. Toxicol.

Mehta et al., 1999, An update on GABAA receptors., Brain Res. Brain Res. Rev.

METHARBITAL GABRA6

Interaction Types:

potentiator

positive allosteric modulator

Interaction Info:

Trial Name -

Novel drug target Established target

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Publications:

Yamakura et al., 2001, Anesthetics and ion channels: molecular models and sites of action., Annu. Rev. Pharmacol. Toxicol.

Mehta et al., 1999, An update on GABAA receptors., Brain Res. Brain Res. Rev.

THIOPENTAL GABRA6

Interaction Types:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

Publications:

Yamakura et al., 2001, Anesthetics and ion channels: molecular models and sites of action., Annu. Rev. Pharmacol. Toxicol.

Mehta et al., 1999, An update on GABAA receptors., Brain Res. Brain Res. Rev.

PRIMIDONE GABRA6

Interaction Types:

potentiator

positive allosteric modulator

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Direct Interaction yes

Trial Name -

Publications:

Yamakura et al., 2001, Anesthetics and ion channels: molecular models and sites of action., Annu. Rev. Pharmacol. Toxicol.

Mehta et al., 1999, An update on GABAA receptors., Brain Res. Brain Res. Rev.

OXAZEPAM GABRA6

Interaction Types:

potentiator

positive allosteric modulator

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Direct Interaction yes

Trial Name -

Publications:

Riss et al., 2008, Benzodiazepines in epilepsy: pharmacology and pharmacokinetics., Acta Neurol. Scand.

Möhler et al., 2002, A new benzodiazepine pharmacology., J. Pharmacol. Exp. Ther.

MEPHOBARBITAL GABRA6

Interaction Types:

potentiator

Interaction Info:

Publications:

Yamakura et al., 2001, Anesthetics and ion channels: molecular models and sites of action., Annu. Rev. Pharmacol. Toxicol.

Mehta et al., 1999, An update on GABAA receptors., Brain Res. Brain Res. Rev.

Olsen et al., 2011, GABA(A) receptors as molecular targets of general anesthetics: identification of binding sites provides clues to allosteric modulation., Can J Anaesth

TRIAZOLAM GABRA6

Interaction Types:

potentiator

positive allosteric modulator

Interaction Info:

Trial Name ARX-03, sufentanil + triazolam NanoTab

Novel drug target Established target

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Publications:

Riss et al., 2008, Benzodiazepines in epilepsy: pharmacology and pharmacokinetics., Acta Neurol. Scand.

Möhler et al., 2002, A new benzodiazepine pharmacology., J. Pharmacol. Exp. Ther.

AMOBARBITAL GABRA6

Interaction Types:

potentiator

Interaction Info:

Publications:

Yamakura et al., 2001, Anesthetics and ion channels: molecular models and sites of action., Annu. Rev. Pharmacol. Toxicol.

Mehta et al., 1999, An update on GABAA receptors., Brain Res. Brain Res. Rev.

APROBARBITAL GABRA6

Interaction Types:

potentiator

Interaction Info:

Publications:

Yamakura et al., 2001, Anesthetics and ion channels: molecular models and sites of action., Annu. Rev. Pharmacol. Toxicol.

Mehta et al., 1999, An update on GABAA receptors., Brain Res. Brain Res. Rev.

BUTETHAL GABRA6

Interaction Types:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

Publications:

Yamakura et al., 2001, Anesthetics and ion channels: molecular models and sites of action., Annu. Rev. Pharmacol. Toxicol.

Mehta et al., 1999, An update on GABAA receptors., Brain Res. Brain Res. Rev.

HEPTABARBITAL GABRA6

Interaction Types:

potentiator

Interaction Info:

Publications:

Yamakura et al., 2001, Anesthetics and ion channels: molecular models and sites of action., Annu. Rev. Pharmacol. Toxicol.

Mehta et al., 1999, An update on GABAA receptors., Brain Res. Brain Res. Rev.

HEXOBARBITAL GABRA6

Interaction Types:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

Publications:

Yamakura et al., 2001, Anesthetics and ion channels: molecular models and sites of action., Annu. Rev. Pharmacol. Toxicol.

Mehta et al., 1999, An update on GABAA receptors., Brain Res. Brain Res. Rev.

BARBITAL GABRA6

Interaction Types:

potentiator

Interaction Info:

Publications:

Yamakura et al., 2001, Anesthetics and ion channels: molecular models and sites of action., Annu. Rev. Pharmacol. Toxicol.

Mehta et al., 1999, An update on GABAA receptors., Brain Res. Brain Res. Rev.

FLUNITRAZEPAM GABRA6

Interaction Types:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

Publications:

You et al., 2010, Benzodiazepine modulation of the rat GABAA receptor α4β3γ2L subtype expressed in Xenopus oocytes., Neuropharmacology

Skilbeck et al., 2008, Antipsychotic drug administration differentially affects [3H]muscimol and [3H]flunitrazepam GABA(A) receptor binding sites., Prog. Neuropsychopharmacol. Biol. Psychiatry

Santhakumar et al., 2006, Contributions of the GABAA receptor alpha6 subunit to phasic and tonic inhibition revealed by a naturally occurring polymorphism in the alpha6 gene., J. Neurosci.

BROMAZEPAM GABRA6

Interaction Types:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

Publications:

Riss et al., 2008, Benzodiazepines in epilepsy: pharmacology and pharmacokinetics., Acta Neurol. Scand.
NITRAZEPAM GABRA6

Interaction Types:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

Publications:

Riss et al., 2008, Benzodiazepines in epilepsy: pharmacology and pharmacokinetics., Acta Neurol. Scand.

Möhler et al., 2002, A new benzodiazepine pharmacology., J. Pharmacol. Exp. Ther.
PHENOBARBITAL GABRA6

Interaction Types:

n/a

Interaction Info:

Trial Name -

Novel drug target Established target

Publications:
GANAXOLONE GABRA6

Interaction Types:

n/a

Interaction Info:

Trial Name Ganaxolone

Novel drug target Established target

Publications:
METHOXYFLURANE GABRA6

Interaction Types:

n/a

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel positive modulator

Direct Interaction yes

Publications:
GLUTETHIMIDE GABRA6

Interaction Types:

n/a

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel positive modulator

Direct Interaction yes

Publications:
ENFLURANE GABRA6

Interaction Types:

n/a

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel positive modulator

Direct Interaction yes

Publications:
ETHCHLORVYNOL GABRA6

Interaction Types:

n/a

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel positive modulator

Direct Interaction yes

Publications:
ETOMIDATE GABRA6

Interaction Types:

n/a

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel positive modulator

Direct Interaction yes

Publications:
TOPIRAMATE GABRA6

Interaction Types:

n/a

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel positive modulator

Direct Interaction yes

Publications:
FLURAZEPAM GABRA6

Interaction Types:

n/a

Interaction Info:

Trial Name -

Novel drug target Established target

Publications:
BUTABARBITAL GABRA6

Interaction Types:

n/a

Interaction Info:

Trial Name -

Novel drug target Established target

Publications:
MIDAZOLAM GABRA6

Interaction Types:

n/a

Interaction Info:

Trial Name -

Novel drug target Established target

Publications:
CLORAZEPIC ACID GABRA6

Interaction Types:

n/a

Interaction Info:

Trial Name -

Novel drug target Established target

Publications:
TRICLOFOS SODIUM GABRA6

Interaction Types:

n/a

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel positive modulator

Direct Interaction yes

Publications:
ACAMPROSATE CALCIUM GABRA6

Interaction Types:

n/a

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel positive modulator

Direct Interaction yes

Publications:
OCINAPLON GABRA6

Interaction Types:

n/a

Interaction Info:

Trial Name ocinaplon

Novel drug target Established target

Publications:

Ensembl: ENSG00000145863
- Version: 90_38
Alternate Names:

GABRA6 Ensembl Gene Name

Gene Info:

Gene Biotype PROTEIN_CODING"

Publications:
GuideToPharmacologyGenes: 409
- Version: 4-March-2015
Alternate Names:

4080 HUGO Gene ID

gamma-aminobutyric acid (GABA) A receptor, alpha 6 HUGO Gene Name

GABRA6 Gene Symbol

Gene Info:

GuideToPharmacology Gene Category Name GABA<sub>A</sub> receptors

GuideToPharmacology Gene Category ID 72

GuideToPharmacology Gene Type lgic

Publications:
TEND: Q16445
- Version: 01-August-2011
Alternate Names:

GBRA6_HUMAN Uniprot Id

Q16445 Uniprot Accession

2559 Entrez Gene Id

Gene Info:

Target Main Class Receptors

Target Subclass cys-loop

Target Subclass Channels

Publications:
RussLampel: ENSG00000145863
- Version: 26-July-2011
Alternate Names:

ENSG00000145863 Ensembl Gene Id

GAMMA-AMINOBUTYRIC-ACID RECEPTOR ALPHA-6 SUBUNIT PRECURSOR (GABA(A) RECEPTOR). [SOURCE:UNIPROT/SWISSPROT;ACC:Q16445] Description

GABRA6 Display Id

Gene Info:

Human Readable Name DRUGGABLE GENOME

Publications:
TdgClinicalTrial: Q16445
- Version: January-2014
Alternate Names:

GABRA6 Gene Symbol

Gene Info:

Target Class Receptors

Target Subclass TC:1.A.9

Publications:
HopkinsGroom: Q16445
- Version: 11-September-2012
Alternate Names:

Q16445 Uniprot Accession

GAMMA-AMINOBUTYRIC ACID RECEPTOR SUBUNIT ALPHA-6 Uniprot Protein Name

GBRA6_HUMAN Uniprot Id

Gene Info:

Human Readable Name ION CHANNEL

Interpro Short Name Neur_channel

Interpro Name Neurotransmitter-gated ion-channel ligand-binding

Publications:

DrugBank: BE0000764

Version: 5.0.8

Alternate Names:

GABRA6 DrugBank Gene Name

Q16445 UniProt Accession

2559 Entrez Gene Id

Gene Info:

Publications:

Yamakura et al., 2001, Anesthetics and ion channels: molecular models and sites of action., Annu. Rev. Pharmacol. Toxicol.

Mehta et al., 1999, An update on GABAA receptors., Brain Res. Brain Res. Rev.

Olsen et al., 2011, GABA(A) receptors as molecular targets of general anesthetics: identification of binding sites provides clues to allosteric modulation., Can J Anaesth

GuideToPharmacologyInteractions: 409
- Version: 27-September-2017
Alternate Names:

GABA<sub>A</sub> receptor α6 subunit GuideToPharmacology Name

Q16445 UniProtKB ID

Gene Info:

Publications:
ChemblInteractions: GABRA6
- Version: chembl_23
Alternate Names:

GABRA6 GENE_SYMBOL

Gamma-aminobutyric acid receptor subunit alpha-6 UNIPROT

GABA(A) receptor subunit alpha-6 UNIPROT

Gene Info:

Publications:
GO: GABRA6
- Version: 27-September-2017
Alternate Names:

Q16445 UniProtKB ID

GBRA6_HUMAN GO Gene Synonym

Gene Info:

Publications:
HingoraniCasas: ENSG00000145863
- Version: 31-May-2017
Alternate Names:

ENSG00000145863 Gene Symbol

GABRA6 Ensembl Id

Gene Info:

Publications:

Trial Name	-
Novel drug target	Established target
Mechanism of Interaction	GABA-A receptor; anion channel agonist

Mechanism of Interaction	GABA-A receptor; agonist GABA site agonist
Direct Interaction	yes
Specific Binding Site for Interaction	GABA site

Mechanism of Interaction	GABA-A receptor; anion channel positive allosteric modulator
Direct Interaction	yes
Trial Name	Clobazam

Specific Binding Site for Interaction	GABA site
Specific Action of the Ligand	Full agonist
Endogenous Drug?	False

Specific Action of the Ligand	Inverse agonist
Endogenous Drug?	False
Direct Interaction?	False

Specific Binding Site for Interaction	benzodiazepine site
Specific Action of the Ligand	Antagonist
Endogenous Drug?	False

Specific Action of the Ligand	Inhibition
Endogenous Drug?	True
Direct Interaction?	False

Specific Action of the Ligand	Potentiation
Endogenous Drug?	True
Direct Interaction?	False

Specific Action of the Ligand	None
Endogenous Drug?	False
Direct Interaction?	False

Trial Name	alprazolam,Xanax, Xanax XR
Novel drug target	Established target
Trial Name	AZ-002, Staccato alprazolam

Trial Name	JZP-8
Novel drug target	Established target
Mechanism of Interaction	GABA-A receptor; anion channel positive allosteric modulator

Mechanism of Interaction	GABA-A receptor; benzodiazepine site positive allosteric modulator
Direct Interaction	yes

Trial Name	NG2-73
Novel drug target	Established target
Mechanism of Interaction	GABA-A receptor; benzodiazepine site partial agonist

Mechanism of Interaction	GABA-A receptor; benzodiazepine site inverse agonist
Direct Interaction	yes

Trial Name	ARX-03, sufentanil + triazolam NanoTab
Novel drug target	Established target
Mechanism of Interaction	GABA-A receptor; anion channel positive allosteric modulator

4080	HUGO Gene ID
gamma-aminobutyric acid (GABA) A receptor, alpha 6	HUGO Gene Name
GABRA6	Gene Symbol

GBRA6_HUMAN	Uniprot Id
Q16445	Uniprot Accession
2559	Entrez Gene Id

ENSG00000145863	Ensembl Gene Id
GAMMA-AMINOBUTYRIC-ACID RECEPTOR ALPHA-6 SUBUNIT PRECURSOR (GABA(A) RECEPTOR). [SOURCE:UNIPROT/SWISSPROT;ACC:Q16445]	Description
GABRA6	Display Id

GABRA6	DrugBank Gene Name
Q16445	UniProt Accession
2559	Entrez Gene Id

GABA<sub>A</sub> receptor α6 subunit	GuideToPharmacology Name
Q16445	UniProtKB ID

GABRA6 Gene Record

GABRA6 2559 Druggable Genome

Alternate Names:

Gene Info:

Publications:

Interaction Types: agonist

Interaction Info: Trial Name - Novel drug target Established target Mechanism of Interaction GABA-A receptor; anion channel agonist

Publications: Gonzalez et al., 2009, Carisoprodol-mediated modulation of GABAA receptors: in vitro and in vivo studies., J. Pharmacol. Exp. Ther. Rho et al., 1997, Barbiturate-like actions of the propanediol dicarbamates felbamate and meprobamate., J. Pharmacol. Exp. Ther.

Interaction Types: agonist

Interaction Info: Mechanism of Interaction GABA-A receptor; agonist GABA site agonist Direct Interaction yes Specific Binding Site for Interaction GABA site

Publications:

Interaction Types: positive allosteric modulator

Interaction Info: Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator Direct Interaction yes Trial Name Clobazam

Publications:

Interaction Types: agonist

Interaction Info: Specific Binding Site for Interaction GABA site Specific Action of the Ligand Full agonist Endogenous Drug? False

Publications:

Interaction Types: agonist

Interaction Info: Specific Binding Site for Interaction GABA site Specific Action of the Ligand Full agonist Details of Interaction relatively high efficacy

Publications:

Interaction Types: agonist

Interaction Info: Specific Binding Site for Interaction GABA site Specific Action of the Ligand Full agonist Endogenous Drug? False

Publications:

Interaction Types: agonist

Interaction Info: Specific Binding Site for Interaction GABA site Specific Action of the Ligand Full agonist Details of Interaction low efficacy

Publications:

Interaction Types: agonist

Interaction Info: Specific Action of the Ligand Inverse agonist Endogenous Drug? False Direct Interaction? False

Publications:

Interaction Types: allosteric modulator

Interaction Info: Specific Binding Site for Interaction benzodiazepine site Specific Action of the Ligand Antagonist Endogenous Drug? False

Publications:

Interaction Types: allosteric modulator

Interaction Info: Specific Binding Site for Interaction benzodiazepine site Specific Action of the Ligand Full agonist Endogenous Drug? False

Publications:

Interaction Types: allosteric modulator

Interaction Info: Specific Binding Site for Interaction benzodiazepine site Specific Action of the Ligand Full agonist Endogenous Drug? False

Publications:

Interaction Types: allosteric modulator

Interaction Info: Specific Binding Site for Interaction benzodiazepine site Specific Action of the Ligand Full agonist Endogenous Drug? False

Publications:

Interaction Types: allosteric modulator

Interaction Info: Specific Action of the Ligand Inhibition Endogenous Drug? True Direct Interaction? False

Publications:

Interaction Types: allosteric modulator

Interaction Info: Specific Binding Site for Interaction benzodiazepine site Specific Action of the Ligand Partial agonist Details of Interaction low affinity

Publications:

Interaction Types: allosteric modulator

Interaction Info: Specific Action of the Ligand Potentiation Endogenous Drug? True Direct Interaction? False

Publications:

Interaction Types: antagonist

Interaction Info: Specific Binding Site for Interaction GABA site Specific Action of the Ligand Antagonist Endogenous Drug? False

Publications:

Interaction Types: antagonist

Interaction Info: Specific Binding Site for Interaction GABA site Specific Action of the Ligand Antagonist Endogenous Drug? False

Publications:

Interaction Types: channel blocker

Interaction Info: Specific Action of the Ligand None Endogenous Drug? False Direct Interaction? False

Publications:

Interaction Types: channel blocker

Interaction Info: Specific Action of the Ligand None Endogenous Drug? False Direct Interaction? False

Publications:

Interaction Types: positive allosteric modulator

Interaction Info: Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator Direct Interaction yes

Publications:

Interaction Types: positive allosteric modulator

Interaction Info: Trial Name - Novel drug target Established target Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Publications:

Interaction Types: positive allosteric modulator

Interaction Info: Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator Direct Interaction yes

Publications:

Interaction Types: positive allosteric modulator

Interaction Info: Trial Name alprazolam,Xanax, Xanax XR Novel drug target Established target Trial Name AZ-002, Staccato alprazolam

Publications:

Interaction Types: positive allosteric modulator

Interaction Info: Trial Name JZP-8 Novel drug target Established target Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Publications:

Interaction Types: positive allosteric modulator

Interaction Info: Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator Direct Interaction yes

Publications:

Interaction Types:

agonist

Interaction Info:

Trial Name -

Novel drug target Established target

Mechanism of Interaction GABA-A receptor; anion channel agonist

Publications:

Gonzalez et al., 2009, Carisoprodol-mediated modulation of GABAA receptors: in vitro and in vivo studies., J. Pharmacol. Exp. Ther.

Rho et al., 1997, Barbiturate-like actions of the propanediol dicarbamates felbamate and meprobamate., J. Pharmacol. Exp. Ther.

Interaction Types:

agonist

Interaction Info:

Mechanism of Interaction GABA-A receptor; agonist GABA site agonist

Direct Interaction yes

Specific Binding Site for Interaction GABA site

Interaction Types:

positive allosteric modulator

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Direct Interaction yes

Trial Name Clobazam

Interaction Types:

agonist

Interaction Info:

Specific Binding Site for Interaction GABA site

Specific Action of the Ligand Full agonist

Endogenous Drug? False

Interaction Types:

agonist

Interaction Info:

Specific Binding Site for Interaction GABA site

Specific Action of the Ligand Full agonist

Details of Interaction relatively high efficacy

Interaction Types:

agonist

Interaction Info:

Specific Binding Site for Interaction GABA site

Specific Action of the Ligand Full agonist

Endogenous Drug? False

Interaction Types:

agonist

Interaction Info:

Specific Binding Site for Interaction GABA site

Specific Action of the Ligand Full agonist

Details of Interaction low efficacy

Interaction Types:

agonist

Interaction Info:

Specific Action of the Ligand Inverse agonist

Endogenous Drug? False

Direct Interaction? False

Interaction Types:

allosteric modulator

Interaction Info:

Specific Binding Site for Interaction benzodiazepine site

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Interaction Types:

allosteric modulator

Interaction Info:

Specific Binding Site for Interaction benzodiazepine site

Specific Action of the Ligand Full agonist

Endogenous Drug? False

Interaction Types:

allosteric modulator

Interaction Info:

Specific Binding Site for Interaction benzodiazepine site

Specific Action of the Ligand Full agonist

Endogenous Drug? False

Interaction Types:

allosteric modulator

Interaction Info:

Specific Binding Site for Interaction benzodiazepine site

Specific Action of the Ligand Full agonist

Endogenous Drug? False

Interaction Types:

allosteric modulator

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? True

Direct Interaction? False

Interaction Types:

allosteric modulator

Interaction Info:

Specific Binding Site for Interaction benzodiazepine site

Specific Action of the Ligand Partial agonist

Details of Interaction low affinity

Interaction Types:

allosteric modulator

Interaction Info:

Specific Action of the Ligand Potentiation

Endogenous Drug? True

Direct Interaction? False

Interaction Types:

antagonist

Interaction Info:

Specific Binding Site for Interaction GABA site

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Interaction Types:

antagonist

Interaction Info:

Specific Binding Site for Interaction GABA site

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Interaction Types:

channel blocker

Interaction Info:

Specific Action of the Ligand None

Endogenous Drug? False

Direct Interaction? False

Interaction Types:

channel blocker

Interaction Info:

Specific Action of the Ligand None

Endogenous Drug? False

Direct Interaction? False

Interaction Types:

positive allosteric modulator

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Direct Interaction yes

Interaction Types:

positive allosteric modulator

Interaction Info:

Trial Name -

Novel drug target Established target

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Interaction Types:

positive allosteric modulator

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Direct Interaction yes

Interaction Types:

positive allosteric modulator

Interaction Info:

Trial Name alprazolam,Xanax, Xanax XR

Novel drug target Established target

Trial Name AZ-002, Staccato alprazolam

Interaction Types:

positive allosteric modulator

Interaction Info:

Trial Name JZP-8

Novel drug target Established target

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Interaction Types:

positive allosteric modulator

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Direct Interaction yes

Interaction Types:

positive allosteric modulator

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Direct Interaction yes

Interaction Types:

positive allosteric modulator

Interaction Info:

Trial Name -

Novel drug target Established target

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Interaction Types:

positive allosteric modulator

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Direct Interaction yes

Interaction Types:

positive allosteric modulator

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Direct Interaction yes

Interaction Types:

positive allosteric modulator

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Direct Interaction yes

Interaction Types:

positive allosteric modulator

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Direct Interaction yes

Interaction Types:

positive allosteric modulator

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Direct Interaction yes

Interaction Types:

positive allosteric modulator

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Direct Interaction yes

Interaction Types:

positive allosteric modulator

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Direct Interaction yes

Interaction Types:

positive allosteric modulator

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Direct Interaction yes

Interaction Types:

positive allosteric modulator

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Direct Interaction yes

GABRA6	GENE_SYMBOL
Gamma-aminobutyric acid receptor subunit alpha-6	UNIPROT
GABA(A) receptor subunit alpha-6	UNIPROT