DGIdb - FLUMAZENIL Drug Record

FLUMAZENIL chembl:CHEMBL407 Approved

Alternate Names:

RO-15-1788
RO-41-8157
RO-151788000
RO-151788
ROMAZICON
MAZICON
FLUMAZEPIL
FLUMAZENIL
RO-1722
ANEXATE
ANEXATE®
FLUMAZENILUM
FLUMAZENILO
RO15-1788
chembl:CHEMBL407
chemidplus:78755-81-4
pubchem.compound:3373
drugbank:01205
rxcui:4457

Drug Info:

FDA Approval	1991
Drug Class	small molecule
Drug Indications	Antidotes, Benzodoazepine Overdose
Drug Class	antidotes, benzodoazepine overdose
Year of Approval	1991
Drug Categories	benzodiazepine antagonist
Drug Categories	compounds used in a research, industrial, or household setting
Drug Categories	drugs that are mainly renally excreted
Drug Categories	heterocyclic compounds, fused-ring
Drug Categories	miscellaneous central nervous system agents

(4 More Sources)

Publications:

Whitwam et al., 1995, Pharmacology of flumazenil., Acta Anaesthesiol Scand Suppl
Wingrove et al., 2002, Mechanism of alpha-subunit selectivity of benzodiazepine pharmacology at gamma-aminobutyric acid type A receptors., Eur. J. Pharmacol.
Imming et al., 2006, Drugs, their targets and the nature and number of drug targets., Nat Rev Drug Discov
Clément et al., 2009, Pharmacological alterations of anxious behaviour in mice depending on both strain and the behavioural situation., PLoS ONE
Padgett et al., 2008, The F-loop of the GABA A receptor gamma2 subunit contributes to benzodiazepine modulation., J. Biol. Chem.

FLUMAZENIL GABRA5

Interaction Score: 0.24

Interaction Types & Directionality:

allosteric modulator

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

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

PMIDs:
19907641

Sources:
TEND TdgClinicalTrial TTD DrugBank GuideToPharmacology ChemblInteractions
FLUMAZENIL GABRG2

Interaction Score: 0.21

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

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

Direct Interaction yes

PMIDs:
17974564 8693922 11864636

Sources:
DrugBank ChemblInteractions

FLUMAZENIL GABRA1

Interaction Score: 0.19

Interaction Types & Directionality:

positive modulator (activating)

allosteric modulator

antagonist (inhibitory)

Interaction Info:

Specific Binding Site for Interaction benzodiazepine site

Details of the Assay for Interaction Affinity measured using α1β3γ2 receptors.

Specific Action of the Ligand Antagonist

PMIDs:
8693922 11864636 17016423

Sources:
TEND TdgClinicalTrial DrugBank GuideToPharmacology ChemblInteractions

FLUMAZENIL GABRA2

Interaction Score: 0.17

Interaction Types & Directionality:

allosteric modulator

Interaction Info:

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

Direct Interaction yes

Specific Binding Site for Interaction benzodiazepine site

PMIDs:
None found

Sources:
TEND TdgClinicalTrial TTD GuideToPharmacology ChemblInteractions
FLUMAZENIL GABRA3

Interaction Score: 0.17

Interaction Types & Directionality:

allosteric modulator

Interaction Info:

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

Direct Interaction yes

Specific Binding Site for Interaction benzodiazepine site

PMIDs:
None found

Sources:
TEND TdgClinicalTrial TTD GuideToPharmacology ChemblInteractions
FLUMAZENIL TSPO

Interaction Score: 0.09

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
FLUMAZENIL GABRG3

Interaction Score: 0.08

Interaction Types & Directionality:

n/a

Interaction Info:

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

Direct Interaction yes

PMIDs:
None found

Sources:
TTD ChemblInteractions

FLUMAZENIL GABRA6

Interaction Score: 0.08

Interaction Types & Directionality:

allosteric modulator

Interaction Info:

Specific Binding Site for Interaction benzodiazepine site

Details of the Assay for Interaction Affinity measured using α6β3γ2 receptors.

Specific Action of the Ligand Partial agonist

PMIDs:
None found

Sources:
GuideToPharmacology ChemblInteractions

FLUMAZENIL GABRQ

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

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

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
FLUMAZENIL GABRE

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

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

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
FLUMAZENIL GABRP

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

Direct Interaction yes

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

PMIDs:
None found

Sources:
ChemblInteractions
FLUMAZENIL GABRD

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

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

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
FLUMAZENIL GABRG1

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

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

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
FLUMAZENIL GABRB1

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

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

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
FLUMAZENIL GABRB3

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

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

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
FLUMAZENIL GABRB2

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

Direct Interaction yes

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

PMIDs:
None found

Sources:
ChemblInteractions
FLUMAZENIL GABRA4

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

Direct Interaction yes

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

PMIDs:
None found

Sources:
ChemblInteractions
FLUMAZENIL CYP2C19

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
FLUMAZENIL NFE2L2

Interaction Score: 0.0

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC

DrugBank: DB01205

Version: 5.1.7

Alternate Names:

FLUMAZENIL DrugBank Drug Name

78755-81-4 CAS Number

Anexate Drug Brand

Drug Info:

Drug Type small molecule

Drug Groups approved

Drug Categories antidotes

Publications:

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

Whitwam et al., 1995, Pharmacology of flumazenil., Acta Anaesthesiol Scand Suppl

Wingrove et al., 2002, Mechanism of alpha-subunit selectivity of benzodiazepine pharmacology at gamma-aminobutyric acid type A receptors., Eur. J. Pharmacol.

TEND: FLUMAZENIL
- Version: 01-August-2011
Alternate Names:

FLUMAZENIL Primary Drug Name

Drug Info:

Year of Approval 1991

Drug Class antidotes, benzodoazepine overdose

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

Drug Info:

Drug Indications Antidotes, Benzodoazepine Overdose

Drug Class small molecule

FDA Approval 1991

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

CHEMBL407 ChEMBL Drug ID

Drug Info:

Publications:
TTD: Flumazenil
- Version: 2020.06.01
Alternate Names:

D0D5GD TTD Drug ID

Drug Info:

Publications:
GuideToPharmacology: 178101009
- Version: 29-September-2020
Alternate Names:

FLUMAZENIL GuideToPharmacology Ligand Name

Drug Info:

Publications:
ChemblDrugs: chembl:CHEMBL407
- Version: ChEMBL_27
Alternate Names:

Drug Info:

Publications:
ChemblInteractions: CHEMBL407
- Version: chembl_23
Alternate Names:

Drug Info:

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 allosteric antagonist
Direct Interaction	yes

Specific Binding Site for Interaction	benzodiazepine site
Details of the Assay for Interaction	Affinity measured using α1β3γ2 receptors.
Specific Action of the Ligand	Antagonist

FLUMAZENIL	DrugBank Drug Name
78755-81-4	CAS Number
Anexate	Drug Brand

Drug Type	small molecule
Drug Groups	approved
Drug Categories	antidotes

FLUMAZENIL Drug Record

FLUMAZENIL chembl:CHEMBL407 Approved

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality: allosteric modulator antagonist (inhibitory)

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

PMIDs: 19907641

Sources: TEND TdgClinicalTrial TTD DrugBank GuideToPharmacology ChemblInteractions

Interaction Types & Directionality: antagonist (inhibitory)

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

PMIDs: 17974564 8693922 11864636

Sources: DrugBank ChemblInteractions

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

Interaction Info: Specific Binding Site for Interaction benzodiazepine site Details of the Assay for Interaction Affinity measured using &alpha;1&beta;3&gamma;2 receptors. Specific Action of the Ligand Antagonist

PMIDs: 8693922 11864636 17016423

Sources: TEND TdgClinicalTrial DrugBank GuideToPharmacology ChemblInteractions

Interaction Types & Directionality: allosteric modulator

Interaction Info: Mechanism of Interaction GABA-A receptor; anion channel allosteric antagonist Direct Interaction yes Specific Binding Site for Interaction benzodiazepine site

PMIDs: None found

Sources: TEND TdgClinicalTrial TTD GuideToPharmacology ChemblInteractions

Interaction Types & Directionality: allosteric modulator

Interaction Info: Mechanism of Interaction GABA-A receptor; anion channel allosteric antagonist Direct Interaction yes Specific Binding Site for Interaction benzodiazepine site

PMIDs: None found

Sources: TEND TdgClinicalTrial TTD GuideToPharmacology ChemblInteractions

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: TTD

Interaction Types & Directionality: n/a

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

PMIDs: None found

Sources: TTD ChemblInteractions

Interaction Types & Directionality: allosteric modulator

Interaction Info: Specific Binding Site for Interaction benzodiazepine site Details of the Assay for Interaction Affinity measured using &alpha;6&beta;3&gamma;2 receptors. Specific Action of the Ligand Partial agonist

PMIDs: None found

Sources: GuideToPharmacology ChemblInteractions

Interaction Types & Directionality: n/a

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

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: n/a

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

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: n/a

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

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: n/a

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

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: n/a

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

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: n/a

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

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: n/a

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

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: n/a

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

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: n/a

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

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Interaction Types & Directionality:

allosteric modulator

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

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

PMIDs:
19907641

Sources:
TEND TdgClinicalTrial TTD DrugBank GuideToPharmacology ChemblInteractions

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

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

Direct Interaction yes

PMIDs:
17974564 8693922 11864636

Sources:
DrugBank ChemblInteractions

Interaction Types & Directionality:

positive modulator (activating)

allosteric modulator

antagonist (inhibitory)

Interaction Info:

Specific Binding Site for Interaction benzodiazepine site

Details of the Assay for Interaction Affinity measured using α1β3γ2 receptors.

Specific Action of the Ligand Antagonist

PMIDs:
8693922 11864636 17016423

Sources:
TEND TdgClinicalTrial DrugBank GuideToPharmacology ChemblInteractions

Interaction Types & Directionality:

allosteric modulator

Interaction Info:

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

Direct Interaction yes

Specific Binding Site for Interaction benzodiazepine site

PMIDs:
None found

Sources:
TEND TdgClinicalTrial TTD GuideToPharmacology ChemblInteractions

Interaction Types & Directionality:

allosteric modulator

Interaction Info:

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

Direct Interaction yes

Specific Binding Site for Interaction benzodiazepine site

PMIDs:
None found

Sources:
TEND TdgClinicalTrial TTD GuideToPharmacology ChemblInteractions

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

n/a

Interaction Info:

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

Direct Interaction yes

PMIDs:
None found

Sources:
TTD ChemblInteractions

Interaction Types & Directionality:

allosteric modulator

Interaction Info:

Specific Binding Site for Interaction benzodiazepine site

Details of the Assay for Interaction Affinity measured using α6β3γ2 receptors.

Specific Action of the Ligand Partial agonist

PMIDs:
None found

Sources:
GuideToPharmacology ChemblInteractions

Interaction Types & Directionality:

n/a

Interaction Info:

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

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

n/a

Interaction Info:

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

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

n/a

Interaction Info:

Direct Interaction yes

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

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

n/a

Interaction Info:

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

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

n/a

Interaction Info:

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

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

n/a

Interaction Info:

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

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

n/a

Interaction Info:

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

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

n/a

Interaction Info:

Direct Interaction yes

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

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

n/a

Interaction Info:

Direct Interaction yes

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

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Alternate Names:

FLUMAZENIL DrugBank Drug Name

78755-81-4 CAS Number

Anexate Drug Brand

Drug Info:

Drug Type small molecule

Drug Groups approved

Drug Categories antidotes

Alternate Names:

FLUMAZENIL Primary Drug Name

Drug Info:

Year of Approval 1991

Drug Class antidotes, benzodoazepine overdose

Drug Info:

Drug Indications Antidotes, Benzodoazepine Overdose

Drug Class small molecule

FDA Approval 1991

Alternate Names:

CHEMBL407 ChEMBL Drug ID

Alternate Names:

D0D5GD TTD Drug ID