DGIdb - GABRR1 Gene Record

GABRR1 2569 Druggable Genome

Alternate Names:

2569
GAMMA-AMINOBUTYRIC ACID TYPE A RECEPTOR RHO1 SUBUNIT
GABRR1
137161
4090
ENSG00000146276
OTTHUMG00000015195
P24046
GABRG2
GAMMA-AMINOBUTYRIC-ACID RECEPTOR RHO-1 SUBUNIT PRECURSOR (GABA(A) RECEPTOR). [SOURCE:UNIPROT/SWISSPROT;ACC:P24046]
GBRR1_HUMAN
GAMMA-AMINOBUTYRIC ACID RECEPTOR SUBUNIT RHO-1
gamma-aminobutyric acid type A receptor subunit rho1

Gene Info:

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

(4 More Sources)

Gene Categories: Category Details

ION CHANNEL
DRUGGABLE GENOME

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.
Petersen JG et al., 2014, Synthesis and pharmacological evaluation of 6-aminonicotinic acid analogues as novel GABA(A) receptor agonists., Eur J Med Chem
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
Giersch et al., 2010, Atypical behavioural effects of lorazepam: clues to the design of novel therapies?, Pharmacol. Ther.
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.
Nakatsuka et al., 1985, Benzodiazepines and their metabolites: relationship between binding affinity to the benzodiazepine receptor and pharmacological activity., Life Sci.
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.
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
Richter et al., 2010, Intrinsic activation of GABA(A) receptors suppresses epileptiform activity in the cerebral cortex of immature mice., Epilepsia
Law et al., 2008, Gaba receptor insecticide non-competitive antagonists may bind at allosteric modulator sites., Int. J. Neurosci.
Mandrioli et al., 2008, Benzodiazepine metabolism: an analytical perspective., Curr. Drug Metab.
Schove et al., 1994, Molecular determinants of recognition and activation at the cerebellar benzodiazepine receptor site., Bioorg. Med. Chem.
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
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.

PICROTOXIN GABRR1

Interaction Score: 3.43

Interaction Types & Directionality:

antagonist (inhibitory)

blocker (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
17016423 17139284 20491873 18446586

Sources:
TdgClinicalTrial TEND
ISONIPECOTIC ACID GABRR1

Interaction Score: 1.14

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
25038482

Sources:
DTC
ADINAZOLAM GABRR1

Interaction Score: 0.54

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
6320036 6148400

Sources:
TdgClinicalTrial TEND
QUAZEPAM GABRR1

Interaction Score: 0.46

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
2892106 3017690

Sources:
TdgClinicalTrial TEND
HALAZEPAM GABRR1

Interaction Score: 0.46

Interaction Types & Directionality:

potentiator

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
6738302 2867566

Sources:
TdgClinicalTrial TEND
NITRAZEPAM GABRR1

Interaction Score: 0.44

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
11752090 18384456

Sources:
TdgClinicalTrial TEND
FLURAZEPAM GABRR1

Interaction Score: 0.44

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
11752090 18384456

Sources:
TdgClinicalTrial TEND
TEMAZEPAM GABRR1

Interaction Score: 0.42

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
20138190 18384456

Sources:
TdgClinicalTrial TEND
CLOTIAZEPAM GABRR1

Interaction Score: 0.4

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
18855614

Sources:
TdgClinicalTrial TEND
FLUDIAZEPAM GABRR1

Interaction Score: 0.4

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
2857046

Sources:
TdgClinicalTrial TEND
CINOLAZEPAM GABRR1

Interaction Score: 0.4

Interaction Types & Directionality:

potentiator

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
7849137

Sources:
TdgClinicalTrial TEND
ESTAZOLAM GABRR1

Interaction Score: 0.4

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
639854 2889803

Sources:
TdgClinicalTrial TEND
OXAZEPAM GABRR1

Interaction Score: 0.35

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
11752090 18384456

Sources:
TdgClinicalTrial TEND
BROMAZEPAM GABRR1

Interaction Score: 0.33

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
18384456

Sources:
TdgClinicalTrial TEND
PRAZEPAM GABRR1

Interaction Score: 0.31

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
7773620

Sources:
TdgClinicalTrial TEND
DIAZEPAM GABRR1

Interaction Score: 0.31

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name diazepam rectal gel

Novel drug target Established target

Trial Name NRL-01

PMIDs:
11752090 18384456

Sources:
TdgClinicalTrial TEND
TRIAZOLAM GABRR1

Interaction Score: 0.31

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name ARX-03, sufentanil + triazolam NanoTab

Novel drug target Established target

PMIDs:
11752090 18384456

Sources:
TdgClinicalTrial TEND
MIDAZOLAM GABRR1

Interaction Score: 0.25

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
11752090 18384456

Sources:
TdgClinicalTrial TEND
CLORAZEPIC ACID GABRR1

Interaction Score: 0.23

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial TEND
CHLORDIAZEPOXIDE GABRR1

Interaction Score: 0.22

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial TEND
CLOBAZAM GABRR1

Interaction Score: 0.22

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name Clobazam

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial TEND
LORAZEPAM GABRR1

Interaction Score: 0.21

Interaction Types & Directionality:

n/a

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
None found

Sources:
TdgClinicalTrial TEND
CLONAZEPAM GABRR1

Interaction Score: 0.2

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name JZP-8

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial TEND
OCINAPLON GABRR1

Interaction Score: 0.13

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name ocinaplon

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial
REMIMAZOLAM GABRR1

Interaction Score: 0.13

Interaction Types & Directionality:

n/a

Interaction Info:

Novel drug target Established target

Trial Name CNS-7056

PMIDs:
None found

Sources:
TdgClinicalTrial
ADIPIPLON GABRR1

Interaction Score: 0.12

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name NG2-73

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial
ALPRAZOLAM GABRR1

Interaction Score: 0.08

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name AZ-002, Staccato alprazolam

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial

Ensembl: ENSG00000146276
- Version: 101_38
Alternate Names:

GABRR1 Ensembl Gene Name

Gene Info:

Gene Biotype PROTEIN_CODING

Publications:
TdgClinicalTrial: P24046
- Version: January-2014
Alternate Names:

GABRR1 Gene Symbol

GABRG2 Gene Symbol

Gene Info:

Target Class Receptors

Target Subclass TC:1.A.9

Publications:
TEND: P24046
- Version: 01-August-2011
Alternate Names:

2569 Entrez Gene Id

GBRR1_HUMAN Uniprot Id

ENSG00000146276 Ensembl Gene Id

Gene Info:

Target Main Class Receptors

Target Subclass Ligand_gated_ion_channels

Target Subclass cys-loop

Publications:
HopkinsGroom: P24046
- Version: 11-September-2012
Alternate Names:

GAMMA-AMINOBUTYRIC ACID RECEPTOR SUBUNIT RHO-1 Uniprot Protein Name

GABRR1 Uniprot Gene Name

P24046 Uniprot Accession

Gene Info:

Uniprot Evidence 2: Evidence at transcript level

Interpro Acc IPR006202

Uniprot Status Swiss-Prot

Gene Categories:

ION CHANNEL, DRUGGABLE GENOME

Publications:
RussLampel: ENSG00000146276
- Version: 26-July-2011
Alternate Names:

ENSG00000146276 Ensembl Gene Id

GABRR1 Display Id

GAMMA-AMINOBUTYRIC-ACID RECEPTOR RHO-1 SUBUNIT PRECURSOR (GABA(A) RECEPTOR). [SOURCE:UNIPROT/SWISSPROT;ACC:P24046] Description

Gene Info:

Human Readable Name DRUGGABLE GENOME

Gene Categories:

DRUGGABLE GENOME

Publications:
DTC: GABRR1
- Version: 02-September-2020
Alternate Names:

Gene Info:

Publications:

Petersen JG et al., 2014, Synthesis and pharmacological evaluation of 6-aminonicotinic acid analogues as novel GABA(A) receptor agonists., Eur J Med Chem
HingoraniCasas: ENSG00000146276
- Version: 31-May-2017
Alternate Names:

ENSG00000146276 Gene Symbol

GABRR1 Ensembl Id

Gene Info:

Gene Categories:

DRUGGABLE GENOME

Publications:
Pharos: GABRR1
- Version: 01-February-2022
Alternate Names:

Gamma-aminobutyric acid receptor subunit rho-1 Gene Name

P24046 UniProt ID

Gene Info:

Gene Categories:

ION CHANNEL

Publications:

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

Trial Name	ARX-03, sufentanil + triazolam NanoTab
Novel drug target	Established target

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

2569	Entrez Gene Id
GBRR1_HUMAN	Uniprot Id
ENSG00000146276	Ensembl Gene Id

GAMMA-AMINOBUTYRIC ACID RECEPTOR SUBUNIT RHO-1	Uniprot Protein Name
GABRR1	Uniprot Gene Name
P24046	Uniprot Accession

Gamma-aminobutyric acid receptor subunit rho-1	Gene Name
P24046	UniProt ID

antagonist (inhibitory)
blocker (inhibitory)

GABRR1 Gene Record

GABRR1 2569 Druggable Genome

Alternate Names:

Gene Info:

Gene Categories: Category Details

Publications:

Interaction Types & Directionality: antagonist (inhibitory) blocker (inhibitory)

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 17016423 17139284 20491873 18446586

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 25038482

Sources: DTC

Interaction Types & Directionality: potentiator

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 6320036 6148400

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: potentiator

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 2892106 3017690

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: potentiator

Interaction Info: Novel drug target Established target Trial Name -

PMIDs: 6738302 2867566

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: potentiator

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 11752090 18384456

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: potentiator

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 11752090 18384456

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: potentiator

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 20138190 18384456

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: potentiator

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 18855614

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: potentiator

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 2857046

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: potentiator

Interaction Info: Novel drug target Established target Trial Name -

PMIDs: 7849137

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: potentiator

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 639854 2889803

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: potentiator

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 11752090 18384456

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: potentiator

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 18384456

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: potentiator

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 7773620

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: potentiator

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

PMIDs: 11752090 18384456

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: potentiator

Interaction Info: Trial Name ARX-03, sufentanil + triazolam NanoTab Novel drug target Established target

PMIDs: 11752090 18384456

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: potentiator

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 11752090 18384456

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: n/a

Interaction Info: Trial Name - Novel drug target Established target

Interaction Types & Directionality:

antagonist (inhibitory)

blocker (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
17016423 17139284 20491873 18446586

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

n/a

PMIDs:
25038482

Sources:
DTC

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
6320036 6148400

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
2892106 3017690

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

potentiator

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
6738302 2867566

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
11752090 18384456

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
11752090 18384456

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
20138190 18384456

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
18855614

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
2857046

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

potentiator

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
7849137

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
639854 2889803

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
11752090 18384456

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
18384456

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
7773620

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name diazepam rectal gel

Novel drug target Established target

Trial Name NRL-01

PMIDs:
11752090 18384456

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name ARX-03, sufentanil + triazolam NanoTab

Novel drug target Established target

PMIDs:
11752090 18384456

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

potentiator

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
11752090 18384456

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

n/a