DGIdb - GABRA5 Gene Record

GABRA5 2558 Druggable Genome

Alternate Names:

2558
GAMMA-AMINOBUTYRIC ACID TYPE A RECEPTOR ALPHA5 SUBUNIT
GABRA5
137142
4079
ENSG00000186297
OTTHUMG00000171824
GABA(A) receptor subunit alpha-5
Gamma-aminobutyric acid receptor subunit alpha-5
P31644
GBRA5_HUMAN
GAMMA-AMINOBUTYRIC-ACID RECEPTOR ALPHA-5 SUBUNIT PRECURSOR (GABA(A) RECEPTOR). [SOURCE:UNIPROT/SWISSPROT;ACC:P31644]
408
gamma-aminobutyric acid (GABA) A receptor, alpha 5
NP_000801
NM_000810
α5
GABA<sub>A</sub> receptor α5 subunit
BE0000471
GABA(A) receptor alpha-5
T26368
GAMMA-AMINOBUTYRIC ACID TYPE A RECEPTOR SUBUNIT ALPHA5
EIEE79

Gene Info:

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

(10 More Sources)

Gene Categories: Category Details

TRANSPORTER
ION CHANNEL
DRUGGABLE GENOME

Publications:

Mehta et al., 1999, An update on GABAA receptors., Brain Res. Brain Res. Rev.
Yamakura et al., 2001, Anesthetics and ion channels: molecular models and sites of action., Annu. Rev. Pharmacol. Toxicol.
Knust H et al., 2009, The discovery and unique pharmacological profile of RO4938581 and RO4882224 as potent and selective GABAA alpha5 inverse agonists for the treatment of cognitive dysfunction., Bioorg Med Chem Lett
Walash et al., 1994, A selective fluorimetric method for the determination of some 1,4-benzodiazepine drugs containing a hydroxyl group at C-3., J Pharm Biomed Anal
Möhler et al., 2002, A new benzodiazepine pharmacology., J. Pharmacol. Exp. Ther.
Riss et al., 2008, Benzodiazepines in epilepsy: pharmacology and pharmacokinetics., Acta Neurol. Scand.
Clément et al., 2009, Pharmacological alterations of anxious behaviour in mice depending on both strain and the behavioural situation., PLoS ONE
Schove et al., 1994, Molecular determinants of recognition and activation at the cerebellar benzodiazepine receptor site., Bioorg. Med. Chem.
Mandrioli et al., 2008, Benzodiazepine metabolism: an analytical perspective., Curr. Drug Metab.
Giersch et al., 2010, Atypical behavioural effects of lorazepam: clues to the design of novel therapies?, Pharmacol. Ther.
Husain SS et al., 2006, Synthesis of trifluoromethylaryl diazirine and benzophenone derivatives of etomidate that are potent general anesthetics and effective photolabels for probing sites on ligand-gated ion channels., J Med Chem
Oblak et al., 2011, Reduced GABAA receptors and benzodiazepine binding sites in the posterior cingulate cortex and fusiform gyrus in autism., Brain Res.
Imming et al., 2006, Drugs, their targets and the nature and number of drug targets., Nat Rev Drug Discov
Overington et al., 2006, How many drug targets are there?, Nat Rev Drug Discov
You et al., 2010, Benzodiazepine modulation of the rat GABAA receptor α4β3γ2L subtype expressed in Xenopus oocytes., Neuropharmacology
Billard et al., 1988, Selective affinity of the benzodiazepines quazepam and 2-oxo-quazepam for BZ1 binding site and demonstration of 3H-2-oxo-quazepam as a BZ1 selective radioligand., Life Sci.
Meldrum et al., 1986, Benzodiazepine receptors and their relationship to the treatment of epilepsy., Epilepsia
Rho et al., 1997, Barbiturate-like actions of the propanediol dicarbamates felbamate and meprobamate., J. Pharmacol. Exp. Ther.
Gonzalez et al., 2009, Carisoprodol-mediated modulation of GABAA receptors: in vitro and in vivo studies., J. Pharmacol. Exp. Ther.
Derry et al., 2004, Identification of a residue in the gamma-aminobutyric acid type A receptor alpha subunit that differentially affects diazepam-sensitive and -insensitive benzodiazepine site binding., J. Neurochem.
Iorio et al., 1984, Selective affinity of 1-N-trifluoroethyl benzodiazepines for cerebellar type 1 receptor sites., Life Sci.
Wamsley et al., 1985, Autoradiographic demonstration of the selectivity of two 1-N-trifluoroethyl benzodiazepines for the BZD-1 receptors in the rat brain., Pharmacol. Biochem. Behav.
Braestrup et al., 1978, Pharmacological characterization of benzodiazepine receptors in the brain., Eur. J. Pharmacol.
Miller et al., 1987, Benzodiazepine receptor binding of triazolobenzodiazepines in vivo: increased receptor number with low-dose alprazolam., J. Neurochem.
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
Nakatsuka et al., 1985, Benzodiazepines and their metabolites: relationship between binding affinity to the benzodiazepine receptor and pharmacological activity., Life Sci.
Santhakumar et al., 2007, Ethanol acts directly on extrasynaptic subtypes of GABAA receptors to increase tonic inhibition., Alcohol
Davies, 2003, The role of GABAA receptors in mediating the effects of alcohol in the central nervous system., J Psychiatry Neurosci
Lahti et al., 1983, Pharmacological profile of the antidepressant adinazolam, a triazolobenzodiazepine., Neuropharmacology
Sethy et al., 1984, Determination of biological activity of adinazolam and its metabolites., J. Pharm. Pharmacol.
Ramerstorfer et al., 2010, The point mutation gamma 2F77I changes the potency and efficacy of benzodiazepine site ligands in different GABAA receptor subtypes., Eur. J. Pharmacol.
Nutt et al., 2010, Searching for perfect sleep: the continuing evolution of GABAA receptor modulators as hypnotics., J. Psychopharmacol. (Oxford)
Skerritt et al., 1983, Enhancement of GABA binding by benzodiazepines and related anxiolytics., Eur. J. Pharmacol.
Hanson et al., 2008, Structural requirements for eszopiclone and zolpidem binding to the gamma-aminobutyric acid type-A (GABAA) receptor are different., J. Med. Chem.
Kumar M et al., 2016, Assessment of direct gating and allosteric modulatory effects of meprobamate in recombinant GABA(A) receptors., Eur J Pharmacol

FLUMAZENIL GABRA5

Interaction Types & Directionality:

antagonist (inhibitory)

allosteric modulator

Interaction Info:

Novel drug target Established target

Trial Name -

Mechanism of Interaction GABA-A receptor; anion channel allosteric antagonist

Publications:

Clément et al., 2009, Pharmacological alterations of anxious behaviour in mice depending on both strain and the behavioural situation., PLoS ONE
PRAZEPAM GABRA5

Interaction Types & Directionality:

positive modulator (activating)

potentiator

Interaction Info:

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

Direct Interaction yes

Trial Name -

Publications:

Schove et al., 1994, Molecular determinants of recognition and activation at the cerebellar benzodiazepine receptor site., Bioorg. Med. Chem.
TRIAZOLAM GABRA5

Interaction Types & Directionality:

positive modulator (activating)

allosteric modulator

potentiator

Interaction Info:

Novel drug target Established target

Trial Name ARX-03, sufentanil + triazolam NanoTab

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

Publications:

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

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

FLUNITRAZEPAM GABRA5

Interaction Types & Directionality:

potentiator

allosteric modulator

Interaction Info:

Trial Name -

Novel drug target Established target

Specific Binding Site for Interaction benzodiazepine site

Publications:

Oblak et al., 2011, Reduced GABAA receptors and benzodiazepine binding sites in the posterior cingulate cortex and fusiform gyrus in autism., Brain Res.

Imming et al., 2006, Drugs, their targets and the nature and number of drug targets., Nat Rev Drug Discov

Overington et al., 2006, How many drug targets are there?, Nat Rev Drug Discov

MEPROBAMATE GABRA5

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Novel drug target Established target

Trial Name -

Mechanism of Interaction GABA-A receptor; anion channel agonist

Publications:

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

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

CHLORDIAZEPOXIDE GABRA5

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

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

Direct Interaction yes

Trial Name -

Publications:
PICROTOXIN GABRA5

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand None

Publications:
ALPRAZOLAM GABRA5

Interaction Types & Directionality:

positive modulator (activating)

allosteric modulator

Interaction Info:

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

Direct Interaction yes

Trial Name AZ-002, Staccato alprazolam

Publications:
CHLORDIAZEPOXIDE HYDROCHLORIDE GABRA5

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

Direct Interaction yes

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

Publications:
BICUCULLINE GABRA5

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Binding Site for Interaction GABA site

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Publications:
PROPOFOL GABRA5

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

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

Direct Interaction yes

Publications:
OCINAPLON GABRA5

Interaction Types & Directionality:

allosteric modulator

Interaction Info:

Trial Name ocinaplon

Novel drug target Established target

Specific Binding Site for Interaction benzodiazepine site

Publications:
BUTABARBITAL SODIUM GABRA5

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

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

Direct Interaction yes

Publications:
CLOBAZAM GABRA5

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

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

Direct Interaction yes

Novel drug target Established target

Publications:
THIOPENTAL SODIUM GABRA5

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

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

Direct Interaction yes

Publications:
ADIPIPLON GABRA5

Interaction Types & Directionality:

partial agonist (activating)

Interaction Info:

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

Direct Interaction yes

Trial Name NG2-73

Publications:
METHYPRYLON GABRA5

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

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

Direct Interaction yes

Publications:
ISOGUVACINE GABRA5

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Binding Site for Interaction GABA site

Specific Action of the Ligand Full agonist

Endogenous Drug? False

Publications:
PF-06372865 GABRA5

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel agonist

Direct Interaction yes

Publications:
GABOXADOL GABRA5

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

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

Direct Interaction yes

Trial Name gaboxadol

Publications:
DESFLURANE GABRA5

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

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

Direct Interaction yes

Publications:
LORAZEPAM GABRA5

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

Trial Name -

Novel drug target Established target

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

Publications:
PENTOBARBITAL SODIUM GABRA5

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

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

Direct Interaction yes

Publications:
CLORAZEPATE DIPOTASSIUM GABRA5

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

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

Direct Interaction yes

Publications:
CLONAZEPAM GABRA5

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

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

Direct Interaction yes

Trial Name JZP-8

Publications:
ISOFLURANE GABRA5

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

Direct Interaction yes

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

Publications:
THIAMYLAL SODIUM GABRA5

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

Direct Interaction yes

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

Publications:
RESEQUINIL GABRA5

Interaction Types & Directionality:

inverse agonist (inhibitory)

Interaction Info:

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

Direct Interaction yes

Publications:
MUSCIMOL GABRA5

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Binding Site for Interaction GABA site

Specific Action of the Ligand Full agonist

Endogenous Drug? False

Publications:
LOREDIPLON GABRA5

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

Direct Interaction yes

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

Publications:
SECOBARBITAL SODIUM GABRA5

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

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

Direct Interaction yes

Publications:
BRETAZENIL GABRA5

Interaction Types & Directionality:

allosteric modulator

Interaction Info:

Specific Binding Site for Interaction benzodiazepine site

Specific Action of the Ligand Full agonist

Endogenous Drug? False

Publications:
MIDAZOLAM HYDROCHLORIDE GABRA5

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

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

Direct Interaction yes

Publications:

BASMISANIL GABRA5

Interaction Types & Directionality:

allosteric modulator

Interaction Info:

Details of the Assay for Interaction Binding affinity determined in a radioligand displacement assay: test compound competition for [3H]flumazenil at α5β3γ2 GABAA channels transiently expressed in HEK293 cells.

Specific Action of the Ligand Negative

Endogenous Drug? False

Publications:

HALOTHANE GABRA5

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

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

Direct Interaction yes

Publications:
METHOHEXITAL SODIUM GABRA5

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

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

Direct Interaction yes

Publications:
SEVOFLURANE GABRA5

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

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

Direct Interaction yes

Publications:
MK-0777 GABRA5

Interaction Types & Directionality:

allosteric modulator

Interaction Info:

Specific Binding Site for Interaction benzodiazepine site

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Publications:
GABAZINE GABRA5

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Binding Site for Interaction GABA site

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Publications:

BUTETHAL GABRA5

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

Publications:

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

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

PRIMIDONE GABRA5

Interaction Types & Directionality:

potentiator

positive modulator (activating)

Interaction Info:

Novel drug target Established target

Trial Name -

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

Publications:

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

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

CINOLAZEPAM GABRA5

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

Publications:

Walash et al., 1994, A selective fluorimetric method for the determination of some 1,4-benzodiazepine drugs containing a hydroxyl group at C-3., J Pharm Biomed Anal
OXAZEPAM GABRA5

Interaction Types & Directionality:

potentiator

positive modulator (activating)

Interaction Info:

Novel drug target Established target

Trial Name -

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

Publications:

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

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

BUTALBITAL GABRA5

Interaction Types & Directionality:

potentiator

positive modulator (activating)

Interaction Info:

Trial Name -

Novel drug target Established target

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

Publications:

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

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

CLOTIAZEPAM GABRA5

Interaction Types & Directionality:

potentiator

Interaction Info:

Novel drug target Established target

Trial Name -

Publications:

Mandrioli et al., 2008, Benzodiazepine metabolism: an analytical perspective., Curr. Drug Metab.

BARBITAL GABRA5

Interaction Types & Directionality:

potentiator

Interaction Info:

Publications:

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

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

TEMAZEPAM GABRA5

Interaction Types & Directionality:

positive modulator (activating)

potentiator

Interaction Info:

Direct Interaction yes

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

Trial Name -

Publications:

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

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

BROMAZEPAM GABRA5

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

Publications:

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

PENTOBARBITAL GABRA5

Interaction Types & Directionality:

positive modulator (activating)

potentiator

Interaction Info:

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

Direct Interaction yes

Trial Name -

Publications:

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

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

SECOBARBITAL GABRA5

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

Publications:

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

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

FLURAZEPAM GABRA5

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

Publications:

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

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

METHARBITAL GABRA5

Interaction Types & Directionality:

potentiator

positive modulator (activating)

Interaction Info:

Trial Name -

Novel drug target Established target

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

Publications:

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

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

QUAZEPAM GABRA5

Interaction Types & Directionality:

potentiator

positive modulator (activating)

Interaction Info:

Trial Name -

Novel drug target Established target

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

Publications:

Billard et al., 1988, Selective affinity of the benzodiazepines quazepam and 2-oxo-quazepam for BZ1 binding site and demonstration of 3H-2-oxo-quazepam as a BZ1 selective radioligand., Life Sci.

Meldrum et al., 1986, Benzodiazepine receptors and their relationship to the treatment of epilepsy., Epilepsia

TALBUTAL GABRA5

Interaction Types & Directionality:

positive modulator (activating)

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

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

Publications:

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

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

THIOPENTAL GABRA5

Interaction Types & Directionality:

potentiator

Interaction Info:

Novel drug target Established target

Trial Name -

Publications:

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

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

AMOBARBITAL GABRA5

Interaction Types & Directionality:

potentiator

Interaction Info:

Publications:

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

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

DIAZEPAM GABRA5

Interaction Types & Directionality:

positive modulator (activating)

potentiator

Interaction Info:

Trial Name diazepam rectal gel

Novel drug target Established target

Trial Name NRL-01

Publications:

Derry et al., 2004, Identification of a residue in the gamma-aminobutyric acid type A receptor alpha subunit that differentially affects diazepam-sensitive and -insensitive benzodiazepine site binding., J. Neurochem.

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

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

HEXOBARBITAL GABRA5

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

Publications:

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

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

APROBARBITAL GABRA5

Interaction Types & Directionality:

potentiator

Interaction Info:

Publications:

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

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

HALAZEPAM GABRA5

Interaction Types & Directionality:

positive modulator (activating)

potentiator

Interaction Info:

Direct Interaction yes

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

Trial Name -

Publications:

Iorio et al., 1984, Selective affinity of 1-N-trifluoroethyl benzodiazepines for cerebellar type 1 receptor sites., Life Sci.

Wamsley et al., 1985, Autoradiographic demonstration of the selectivity of two 1-N-trifluoroethyl benzodiazepines for the BZD-1 receptors in the rat brain., Pharmacol. Biochem. Behav.

ESTAZOLAM GABRA5

Interaction Types & Directionality:

positive modulator (activating)

potentiator

Interaction Info:

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

Direct Interaction yes

Trial Name -

Publications:

Braestrup et al., 1978, Pharmacological characterization of benzodiazepine receptors in the brain., Eur. J. Pharmacol.

Miller et al., 1987, Benzodiazepine receptor binding of triazolobenzodiazepines in vivo: increased receptor number with low-dose alprazolam., J. Neurochem.

MEPHOBARBITAL GABRA5

Interaction Types & Directionality:

potentiator

Interaction Info:

Novel drug target Established target

Trial Name -

Publications:

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

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

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

HEPTABARBITAL GABRA5

Interaction Types & Directionality:

potentiator

Interaction Info:

Publications:

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

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

FLUDIAZEPAM GABRA5

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

Publications:

Nakatsuka et al., 1985, Benzodiazepines and their metabolites: relationship between binding affinity to the benzodiazepine receptor and pharmacological activity., Life Sci.
MIDAZOLAM GABRA5

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

Publications:

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

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

ADINAZOLAM GABRA5

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

Publications:

Lahti et al., 1983, Pharmacological profile of the antidepressant adinazolam, a triazolobenzodiazepine., Neuropharmacology

Sethy et al., 1984, Determination of biological activity of adinazolam and its metabolites., J. Pharm. Pharmacol.

NITRAZEPAM GABRA5

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

Publications:

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

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

ZOPICLONE GABRA5

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

Publications:

Ramerstorfer et al., 2010, The point mutation gamma 2F77I changes the potency and efficacy of benzodiazepine site ligands in different GABAA receptor subtypes., Eur. J. Pharmacol.

Nutt et al., 2010, Searching for perfect sleep: the continuing evolution of GABAA receptor modulators as hypnotics., J. Psychopharmacol. (Oxford)

Skerritt et al., 1983, Enhancement of GABA binding by benzodiazepines and related anxiolytics., Eur. J. Pharmacol.

ESZOPICLONE GABRA5

Interaction Types & Directionality:

positive modulator (activating)

agonist (activating)

Interaction Info:

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

Direct Interaction yes

Trial Name Lunesta

Publications:

Nutt et al., 2010, Searching for perfect sleep: the continuing evolution of GABAA receptor modulators as hypnotics., J. Psychopharmacol. (Oxford)

Hanson et al., 2008, Structural requirements for eszopiclone and zolpidem binding to the gamma-aminobutyric acid type-A (GABAA) receptor are different., J. Med. Chem.

CARISOPRODOL GABRA5

Interaction Types & Directionality:

modulator

Interaction Info:

Publications:

Kumar M et al., 2016, Assessment of direct gating and allosteric modulatory effects of meprobamate in recombinant GABA(A) receptors., Eur J Pharmacol

ETOMIDATE GABRA5

Interaction Types & Directionality:

n/a

Interaction Info:

Direct Interaction yes

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

Publications:

Husain SS et al., 2006, Synthesis of trifluoromethylaryl diazirine and benzophenone derivatives of etomidate that are potent general anesthetics and effective photolabels for probing sites on ligand-gated ion channels., J Med Chem

GANAXOLONE GABRA5

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name Ganaxolone

Novel drug target Established target

Publications:
PHENOBARBITAL GABRA5

Interaction Types & Directionality:

n/a

Interaction Info:

Novel drug target Established target

Trial Name -

Publications:
BUTABARBITAL GABRA5

Interaction Types & Directionality:

n/a

Interaction Info:

Novel drug target Established target

Trial Name -

Publications:
METHOXYFLURANE GABRA5

Interaction Types & Directionality:

n/a

Interaction Info:

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

Direct Interaction yes

Publications:
ETHCHLORVYNOL GABRA5

Interaction Types & Directionality:

n/a

Interaction Info:

Direct Interaction yes

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

Publications:
TRICLOFOS SODIUM GABRA5

Interaction Types & Directionality:

n/a

Interaction Info:

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

Direct Interaction yes

Publications:
TOPIRAMATE GABRA5

Interaction Types & Directionality:

n/a

Interaction Info:

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

Direct Interaction yes

Publications:
CLORAZEPIC ACID GABRA5

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name -

Novel drug target Established target

Publications:
ENFLURANE GABRA5

Interaction Types & Directionality:

n/a

Interaction Info:

Direct Interaction yes

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

Publications:
GLUTETHIMIDE GABRA5

Interaction Types & Directionality:

n/a

Interaction Info:

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

Direct Interaction yes

Publications:
REMIMAZOLAM GABRA5

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name CNS-7056

Novel drug target Established target

Publications:
ACAMPROSATE CALCIUM GABRA5

Interaction Types & Directionality:

n/a

Interaction Info:

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

Direct Interaction yes

Publications:

chembl:CHEMBL1077391 GABRA5

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Knust H et al., 2009, The discovery and unique pharmacological profile of RO4938581 and RO4882224 as potent and selective GABAA alpha5 inverse agonists for the treatment of cognitive dysfunction., Bioorg Med Chem Lett

AZIETOMIDATE GABRA5

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Husain SS et al., 2006, Synthesis of trifluoromethylaryl diazirine and benzophenone derivatives of etomidate that are potent general anesthetics and effective photolabels for probing sites on ligand-gated ion channels., J Med Chem

ALCOHOL GABRA5

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Santhakumar et al., 2007, Ethanol acts directly on extrasynaptic subtypes of GABAA receptors to increase tonic inhibition., Alcohol

Davies, 2003, The role of GABAA receptors in mediating the effects of alcohol in the central nervous system., J Psychiatry Neurosci

chembl:CHEMBL52030 GABRA5

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
AMENTOFLAVONE GABRA5

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
chembl:CHEMBL1080588 GABRA5

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
CI-218872 GABRA5

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Ensembl: ENSG00000186297
- Version: 101_38
Alternate Names:

GABRA5 Ensembl Gene Name

Gene Info:

Gene Biotype PROTEIN_CODING

Publications:
HopkinsGroom: P31644
- Version: 11-September-2012
Alternate Names:

ENSG00000186297 Ensembl Gene Id

GAMMA-AMINOBUTYRIC ACID RECEPTOR SUBUNIT ALPHA-5 Uniprot Protein Name

GBRA5_HUMAN Uniprot Id

Gene Info:

Interpro Type Domain

Human Readable Name DRUGGABLE GENOME

Interpro Acc IPR006201

Gene Categories:

ION CHANNEL, DRUGGABLE GENOME

Publications:
TdgClinicalTrial: P31644
- Version: January-2014
Alternate Names:

GABRA5 Gene Symbol

Gene Info:

Target Class Receptors

Target Subclass TC:1.A.9

Publications:
GuideToPharmacologyGenes: 408
- Version: 4-March-2015
Alternate Names:

gamma-aminobutyric acid (GABA) A receptor, alpha 5 HUGO Gene Name

4079 HUGO Gene ID

GABRA5 Gene Symbol

Gene Info:

GuideToPharmacology Gene Category Name GABAA receptors

GuideToPharmacology Gene Category ID 72

GuideToPharmacology Gene Type lgic

Gene Categories:

TRANSPORTER, ION CHANNEL

Publications:
TEND: P31644
- Version: 01-August-2011
Alternate Names:

2558 Entrez Gene Id

ENSG00000186297 Ensembl Gene Id

GBRA5_HUMAN Uniprot Id

Gene Info:

Target Main Class Receptors

Target Subclass Ligand_gated_ion_channels

Target Subclass Channels

Publications:
RussLampel: ENSG00000186297
- Version: 26-July-2011
Alternate Names:

GABRA5 Display Id

GAMMA-AMINOBUTYRIC-ACID RECEPTOR ALPHA-5 SUBUNIT PRECURSOR (GABA(A) RECEPTOR). [SOURCE:UNIPROT/SWISSPROT;ACC:P31644] Description

ENSG00000186297 Ensembl Gene Id

Gene Info:

Human Readable Name DRUGGABLE GENOME

Gene Categories:

DRUGGABLE GENOME

Publications:

DrugBank: BE0000471

Version: 5.1.7

Alternate Names:

GABRA5 DrugBank Gene Name

P31644 UniProt Accession

2558 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.

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

DTC: GABRA5

Version: 02-September-2020

Alternate Names:

Gene Info:

Publications:

Knust H et al., 2009, The discovery and unique pharmacological profile of RO4938581 and RO4882224 as potent and selective GABAA alpha5 inverse agonists for the treatment of cognitive dysfunction., Bioorg Med Chem Lett

Husain SS et al., 2006, Synthesis of trifluoromethylaryl diazirine and benzophenone derivatives of etomidate that are potent general anesthetics and effective photolabels for probing sites on ligand-gated ion channels., J Med Chem

HingoraniCasas: ENSG00000186297
- Version: 31-May-2017
Alternate Names:

ENSG00000186297 Gene Symbol

GABRA5 Ensembl Id

Gene Info:

Gene Categories:

DRUGGABLE GENOME

Publications:
ChemblInteractions: GABRA5
- Version: chembl_23
Alternate Names:

GABRA5 GENE_SYMBOL

Gamma-aminobutyric acid receptor subunit alpha-5 UNIPROT

GABA(A) receptor subunit alpha-5 UNIPROT

Gene Info:

Publications:
GuideToPharmacologyInteractions: ENSG00000186297
- Version: 20-July-2020
Alternate Names:

P31644 UniProtKB ID

GABAA receptor α5 subunit GuideToPharmacology Name

Gene Info:

Publications:
TTD: GABA(A) receptor alpha-5
- Version: 2020.06.01
Alternate Names:

GABRA5 TTD Gene Abbreviation

T26368 TTD Target ID

Gene Info:

Publications:
Pharos: GABRA5
- Version: 03-September-2020
Alternate Names:

Gamma-aminobutyric acid receptor subunit alpha-5 Gene Name

P31644 UniProt ID

Gene Info:

Gene Categories:

ION CHANNEL

Publications:
GO: GABRA5
- Version: 05-September-2020
Alternate Names:

Gene Info:

Gene Categories:

TRANSPORTER

Publications:

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

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

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

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

Trial Name	ocinaplon
Novel drug target	Established target
Specific Binding Site for Interaction	benzodiazepine site

Mechanism of Interaction	GABA-A receptor; benzodiazepine site partial agonist
Direct Interaction	yes
Trial Name	NG2-73

Mechanism of Interaction	GABA-A receptor; anion channel agonist
Direct Interaction	yes

Mechanism of Interaction	GABA-A receptor; agonist GABA site agonist
Direct Interaction	yes
Trial Name	gaboxadol

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

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

Details of the Assay for Interaction	Binding affinity determined in a radioligand displacement assay: test compound competition for [<sup>3</sup>H]flumazenil at α5β3γ2 GABA<sub>A</sub> channels transiently expressed in HEK293 cells.
Specific Action of the Ligand	Negative
Endogenous Drug?	False

Trial Name	diazepam rectal gel
Novel drug target	Established target
Trial Name	NRL-01

ENSG00000186297	Ensembl Gene Id
GAMMA-AMINOBUTYRIC ACID RECEPTOR SUBUNIT ALPHA-5	Uniprot Protein Name
GBRA5_HUMAN	Uniprot Id

gamma-aminobutyric acid (GABA) A receptor, alpha 5	HUGO Gene Name
4079	HUGO Gene ID
GABRA5	Gene Symbol

2558	Entrez Gene Id
ENSG00000186297	Ensembl Gene Id
GBRA5_HUMAN	Uniprot Id

GABRA5	Display Id
GAMMA-AMINOBUTYRIC-ACID RECEPTOR ALPHA-5 SUBUNIT PRECURSOR (GABA(A) RECEPTOR). [SOURCE:UNIPROT/SWISSPROT;ACC:P31644]	Description
ENSG00000186297	Ensembl Gene Id

GABRA5	DrugBank Gene Name
P31644	UniProt Accession
2558	Entrez Gene Id

GABRA5	GENE_SYMBOL
Gamma-aminobutyric acid receptor subunit alpha-5	UNIPROT
GABA(A) receptor subunit alpha-5	UNIPROT

P31644	UniProtKB ID
GABA<sub>A</sub> receptor α5 subunit	GuideToPharmacology Name

Gamma-aminobutyric acid receptor subunit alpha-5	Gene Name
P31644	UniProt ID

GABRA5 Gene Record

GABRA5 2558 Druggable Genome

Alternate Names:

Gene Info:

Gene Categories: Category Details

Publications:

Interaction Types & Directionality: antagonist (inhibitory) allosteric modulator

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

Publications: Clément et al., 2009, Pharmacological alterations of anxious behaviour in mice depending on both strain and the behavioural situation., PLoS ONE

Interaction Types & Directionality: positive modulator (activating) potentiator

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

Publications: Schove et al., 1994, Molecular determinants of recognition and activation at the cerebellar benzodiazepine receptor site., Bioorg. Med. Chem.

Interaction Types & Directionality: positive modulator (activating) allosteric modulator potentiator

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

Publications: Möhler et al., 2002, A new benzodiazepine pharmacology., J. Pharmacol. Exp. Ther. Riss et al., 2008, Benzodiazepines in epilepsy: pharmacology and pharmacokinetics., Acta Neurol. Scand.

Interaction Types & Directionality: potentiator allosteric modulator

Interaction Info: Trial Name - Novel drug target Established target Specific Binding Site for Interaction benzodiazepine site

Interaction Types & Directionality: agonist (activating)

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

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

Interaction Types & Directionality: positive modulator (activating)

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

Publications:

Interaction Types & Directionality: blocker (inhibitory)

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

Publications:

Interaction Types & Directionality: positive modulator (activating) allosteric modulator

Interaction Info: Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator Direct Interaction yes Trial Name AZ-002, Staccato alprazolam

Publications:

Interaction Types & Directionality: positive modulator (activating)

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

Publications:

Interaction Types & Directionality: antagonist (inhibitory)

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

Publications:

Interaction Types & Directionality: positive modulator (activating)

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

Publications:

Interaction Types & Directionality: allosteric modulator

Interaction Info: Trial Name ocinaplon Novel drug target Established target Specific Binding Site for Interaction benzodiazepine site

Publications:

Interaction Types & Directionality: positive modulator (activating)

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

Publications:

Interaction Types & Directionality: positive modulator (activating)

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

Publications:

Interaction Types & Directionality: positive modulator (activating)

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

Publications:

Interaction Types & Directionality: partial agonist (activating)

Interaction Info: Mechanism of Interaction GABA-A receptor; benzodiazepine site partial agonist Direct Interaction yes Trial Name NG2-73

Publications:

Interaction Types & Directionality: positive modulator (activating)

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

Publications:

Interaction Types & Directionality: agonist (activating)

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

Publications:

Interaction Types & Directionality: agonist (activating)

Interaction Info: Mechanism of Interaction GABA-A receptor; anion channel agonist Direct Interaction yes

Publications:

Interaction Types & Directionality: agonist (activating)

Interaction Info: Mechanism of Interaction GABA-A receptor; agonist GABA site agonist Direct Interaction yes Trial Name gaboxadol

Publications:

Interaction Types & Directionality: positive modulator (activating)

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

Publications:

Interaction Types & Directionality: positive modulator (activating)

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

Publications:

Interaction Types & Directionality: positive modulator (activating)

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

Publications:

Interaction Types & Directionality: positive modulator (activating)

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

Publications:

Interaction Types & Directionality: positive modulator (activating)

Interaction Info: Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator Direct Interaction yes Trial Name JZP-8

Publications:

Interaction Types & Directionality:

antagonist (inhibitory)

allosteric modulator

Interaction Info:

Novel drug target Established target

Trial Name -

Mechanism of Interaction GABA-A receptor; anion channel allosteric antagonist

Publications:

Clément et al., 2009, Pharmacological alterations of anxious behaviour in mice depending on both strain and the behavioural situation., PLoS ONE

Interaction Types & Directionality:

positive modulator (activating)

potentiator

Interaction Info:

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

Direct Interaction yes

Trial Name -

Publications:

Schove et al., 1994, Molecular determinants of recognition and activation at the cerebellar benzodiazepine receptor site., Bioorg. Med. Chem.

Interaction Types & Directionality:

positive modulator (activating)

allosteric modulator

potentiator

Interaction Info:

Novel drug target Established target

Trial Name ARX-03, sufentanil + triazolam NanoTab

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

Publications:

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

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

Interaction Types & Directionality:

potentiator

allosteric modulator

Interaction Info:

Trial Name -

Novel drug target Established target

Specific Binding Site for Interaction benzodiazepine site

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Novel drug target Established target

Trial Name -

Mechanism of Interaction GABA-A receptor; anion channel agonist

Publications:

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

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

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

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

Direct Interaction yes

Trial Name -

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand None

Interaction Types & Directionality:

positive modulator (activating)

allosteric modulator

Interaction Info:

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

Direct Interaction yes

Trial Name AZ-002, Staccato alprazolam

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

Direct Interaction yes

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

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Binding Site for Interaction GABA site

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

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

Direct Interaction yes

Interaction Types & Directionality:

allosteric modulator

Interaction Info:

Trial Name ocinaplon

Novel drug target Established target

Specific Binding Site for Interaction benzodiazepine site

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

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

Direct Interaction yes

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

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

Direct Interaction yes

Novel drug target Established target

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

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

Direct Interaction yes

Interaction Types & Directionality:

partial agonist (activating)

Interaction Info:

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

Direct Interaction yes

Trial Name NG2-73

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

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

Direct Interaction yes

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Binding Site for Interaction GABA site

Specific Action of the Ligand Full agonist

Endogenous Drug? False

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel agonist

Direct Interaction yes

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

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

Direct Interaction yes

Trial Name gaboxadol

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

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

Direct Interaction yes

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

Trial Name -

Novel drug target Established target

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

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

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

Direct Interaction yes

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

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

Direct Interaction yes

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

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

Direct Interaction yes

Trial Name JZP-8

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

Direct Interaction yes

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

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

Direct Interaction yes

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

Interaction Types & Directionality:

inverse agonist (inhibitory)

Interaction Info:

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

Direct Interaction yes

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Binding Site for Interaction GABA site

Specific Action of the Ligand Full agonist

Endogenous Drug? False

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

Direct Interaction yes

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

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

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

Direct Interaction yes

Interaction Types & Directionality:

allosteric modulator

Interaction Info:

Specific Binding Site for Interaction benzodiazepine site

Specific Action of the Ligand Full agonist

Endogenous Drug? False

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

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

Direct Interaction yes

Interaction Types & Directionality:

allosteric modulator

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

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

Direct Interaction yes

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

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

Direct Interaction yes