DGIdb - MIBEFRADIL Drug Record

MIBEFRADIL chembl:CHEMBL45816

Alternate Names:

POSICOR
MIBEFRADIL
POSICOR 100
POSICOR 50
POSICOR®
RO-405967-001
chemidplus:116644-53-2
drugbank:01388
pubchem.compound:60663
rxcui:83213
chembl:CHEMBL45816

Drug Info:

(1 More Sources)

Publications:

Clozel et al., 1997, Discovery and main pharmacological properties of mibefradil (Ro 40-5967), the first selective T-type calcium channel blocker., J Hypertens Suppl
Lee et al., 2006, Actions of mibefradil, efonidipine and nifedipine block of recombinant T- and L-type Ca channels with distinct inhibitory mechanisms., Pharmacology
McNulty et al., 2004, State-dependent mibefradil block of Na+ channels., Mol. Pharmacol.
Massie, 1997, Mibefradil: a selective T-type calcium antagonist., Am. J. Cardiol.
Monteil et al., 2000, Molecular and functional properties of the human alpha(1G) subunit that forms T-type calcium channels., J. Biol. Chem.
Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
Jiménez et al., 2000, Determinants of voltage-dependent inactivation affect Mibefradil block of calcium channels., Neuropharmacology
Moosmang et al., 2006, Antihypertensive effects of the putative T-type calcium channel antagonist mibefradil are mediated by the L-type calcium channel Cav1.2., Circ. Res.
Mocanu et al., 1999, Mibefradil, a T-type and L-type calcium channel blocker, limits infarct size through a glibenclamide-sensitive mechanism., Cardiovasc Drugs Ther
Fitzgerald PT et al., 2005, Drug-induced torsades de pointes: the evolving role of pharmacogenetics., Heart Rhythm
Coste et al., 2007, Pharmacological dissection and distribution of NaN/Nav1.9, T-type Ca2+ currents, and mechanically activated cation currents in different populations of DRG neurons., J. Gen. Physiol.
Brueggemann et al., 2005, Low voltage-activated calcium channels in vascular smooth muscle: T-type channels and AVP-stimulated calcium spiking., Am. J. Physiol. Heart Circ. Physiol.
Cribbs et al., 1998, Cloning and characterization of alpha1H from human heart, a member of the T-type Ca2+ channel gene family., Circ. Res.
Perez-Reyes, 2004, Paradoxical role of T-type calcium channels in coronary smooth muscle., Mol. Interv.
Foti RS et al., 2011, Mechanism-based inactivation of cytochrome P450 3A4 by mibefradil through heme destruction., Drug Metab Dispos

MIBEFRADIL CACNA1H

Interaction Score: 1.34

Interaction Types & Directionality:

blocker (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? False

PMIDs:
16899990 9481612 17190903 15498818 15562257 9670923 14993472 9375939

Sources:
GuideToPharmacology TTD
MIBEFRADIL CACNA1G

Interaction Score: 1.31

Interaction Types & Directionality:

blocker (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? False

PMIDs:
16899990 10692398 9481612 15562257 11752352 9375939

Sources:
GuideToPharmacology
MIBEFRADIL ANO1

Interaction Score: 1.25

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Specific Action of the Ligand None

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
MIBEFRADIL CATSPER2

Interaction Score: 0.94

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Details of the Assay for Interaction Patch clamp electrophysiology and kinetic rapid mixing fluometry.

Specific Action of the Ligand Inhibition

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
MIBEFRADIL CATSPER1

Interaction Score: 0.94

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Inhibition

PMIDs:
None found

Sources:
GuideToPharmacology
MIBEFRADIL CACNA1I

Interaction Score: 0.94

Interaction Types & Directionality:

blocker (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Antagonist

PMIDs:
9481612 16899990 15562257 9375939

Sources:
GuideToPharmacology
MIBEFRADIL CATSPER3

Interaction Score: 0.94

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Inhibition

PMIDs:
None found

Sources:
GuideToPharmacology
MIBEFRADIL CATSPER4

Interaction Score: 0.94

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Details of the Assay for Interaction Patch clamp electrophysiology, kinetic rapid mixing fluometry.

Specific Action of the Ligand Inhibition

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
MIBEFRADIL CACNA1C

Interaction Score: 0.55

Interaction Types & Directionality:

blocker (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Endogenous Drug? False

Specific Action of the Ligand Antagonist

PMIDs:
16899990 10665814 16306443 10372226

Sources:
GuideToPharmacology
MIBEFRADIL THPO

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
MIBEFRADIL MTOR

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
MIBEFRADIL MAPK1

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
MIBEFRADIL KCNH2

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
16253929

Sources:
PharmGKB
MIBEFRADIL ATXN2

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
MIBEFRADIL ATAD5

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
MIBEFRADIL CYP3A4

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
21447734

Sources:
DTC
MIBEFRADIL CYP2D6

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC

DTC: MIBEFRADIL
- Version: 02-September-2020
Alternate Names:

CHEMBL45816 ChEMBL Drug ID

Drug Info:

Publications:

Foti RS et al., 2011, Mechanism-based inactivation of cytochrome P450 3A4 by mibefradil through heme destruction., Drug Metab Dispos
PharmGKB: mibefradil
- Version: 18-August-2020
Alternate Names:

Drug Info:

Publications:

Fitzgerald PT et al., 2005, Drug-induced torsades de pointes: the evolving role of pharmacogenetics., Heart Rhythm
TTD: Mibefradil
- Version: 2020.06.01
Alternate Names:

D0W8XT TTD Drug ID

Drug Info:

Publications:
GuideToPharmacology: 53801058
- Version: 29-September-2020
Alternate Names:

MIBEFRADIL GuideToPharmacology Ligand Name

Drug Info:

Publications:
ChemblDrugs: chembl:CHEMBL45816
- Version: ChEMBL_27
Alternate Names:

Drug Info:

Publications:

Specific Action of the Ligand	Antagonist
Endogenous Drug?	False
Direct Interaction?	False

Details of the Assay for Interaction	Patch clamp electrophysiology and kinetic rapid mixing fluometry.
Specific Action of the Ligand	Inhibition
Endogenous Drug?	False

Details of the Assay for Interaction	Patch clamp electrophysiology, kinetic rapid mixing fluometry.
Specific Action of the Ligand	Inhibition
Endogenous Drug?	False

blocker (inhibitory)
inhibitor (inhibitory)

blocker (inhibitory)
inhibitor (inhibitory)

blocker (inhibitory)
inhibitor (inhibitory)

blocker (inhibitory)
inhibitor (inhibitory)

MIBEFRADIL Drug Record

MIBEFRADIL chembl:CHEMBL45816

Alternate Names:

Drug Info:

Publications:

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

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

PMIDs: 16899990 9481612 17190903 15498818 15562257 9670923 14993472 9375939

Sources: GuideToPharmacology TTD

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

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

PMIDs: 16899990 10692398 9481612 15562257 11752352 9375939

Sources: GuideToPharmacology

Interaction Types & Directionality: blocker (inhibitory)

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

PMIDs: None found

Sources: GuideToPharmacology

Interaction Types & Directionality: blocker (inhibitory)

Interaction Info: Details of the Assay for Interaction Patch clamp electrophysiology and kinetic rapid mixing fluometry. Specific Action of the Ligand Inhibition Endogenous Drug? False

PMIDs: None found

Sources: GuideToPharmacology

Interaction Types & Directionality: blocker (inhibitory)

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

PMIDs: None found

Sources: GuideToPharmacology

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

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

PMIDs: 9481612 16899990 15562257 9375939

Sources: GuideToPharmacology

Interaction Types & Directionality: blocker (inhibitory)

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

PMIDs: None found

Sources: GuideToPharmacology

Interaction Types & Directionality: blocker (inhibitory)

Interaction Info: Details of the Assay for Interaction Patch clamp electrophysiology, kinetic rapid mixing fluometry. Specific Action of the Ligand Inhibition Endogenous Drug? False

PMIDs: None found

Sources: GuideToPharmacology

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

Interaction Info: Endogenous Drug? False Specific Action of the Ligand Antagonist

PMIDs: 16899990 10665814 16306443 10372226

Sources: GuideToPharmacology

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 16253929

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 21447734

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

DTC: MIBEFRADIL

Alternate Names: CHEMBL45816 ChEMBL Drug ID

Drug Info:

Publications: Foti RS et al., 2011, Mechanism-based inactivation of cytochrome P450 3A4 by mibefradil through heme destruction., Drug Metab Dispos

PharmGKB: mibefradil

Alternate Names:

Drug Info:

Interaction Types & Directionality:

blocker (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? False

PMIDs:
16899990 9481612 17190903 15498818 15562257 9670923 14993472 9375939

Sources:
GuideToPharmacology TTD

Interaction Types & Directionality:

blocker (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? False

PMIDs:
16899990 10692398 9481612 15562257 11752352 9375939

Sources:
GuideToPharmacology

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Specific Action of the Ligand None

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Details of the Assay for Interaction Patch clamp electrophysiology and kinetic rapid mixing fluometry.

Specific Action of the Ligand Inhibition

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Inhibition

PMIDs:
None found

Sources:
GuideToPharmacology

Interaction Types & Directionality:

blocker (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Antagonist

PMIDs:
9481612 16899990 15562257 9375939

Sources:
GuideToPharmacology

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Inhibition

PMIDs:
None found

Sources:
GuideToPharmacology

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Details of the Assay for Interaction Patch clamp electrophysiology, kinetic rapid mixing fluometry.

Specific Action of the Ligand Inhibition

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology

Interaction Types & Directionality:

blocker (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Endogenous Drug? False

Specific Action of the Ligand Antagonist

PMIDs:
16899990 10665814 16306443 10372226

Sources:
GuideToPharmacology

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
16253929

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
21447734

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Alternate Names:

CHEMBL45816 ChEMBL Drug ID

Publications:

Foti RS et al., 2011, Mechanism-based inactivation of cytochrome P450 3A4 by mibefradil through heme destruction., Drug Metab Dispos

Publications:

Fitzgerald PT et al., 2005, Drug-induced torsades de pointes: the evolving role of pharmacogenetics., Heart Rhythm

Alternate Names:

D0W8XT TTD Drug ID

Alternate Names:

MIBEFRADIL GuideToPharmacology Ligand Name