Identification

Name
Mibefradil
Accession Number
DB01388
Type
Small Molecule
Groups
Investigational, Withdrawn
Description

Mibefradil was withdrawn from the market in 1998 because of potentially harmful interactions with other drugs.

Structure
Thumb
Synonyms
Not Available
International/Other Brands
Posicor
Categories
UNII
27B90X776A
CAS number
116644-53-2
Weight
Average: 495.6287
Monoisotopic: 495.289720302
Chemical Formula
C29H38FN3O3
InChI Key
HBNPJJILLOYFJU-VMPREFPWSA-N
InChI
InChI=1S/C29H38FN3O3/c1-20(2)28-23-12-11-22(30)18-21(23)13-14-29(28,36-27(34)19-35-4)15-17-33(3)16-7-10-26-31-24-8-5-6-9-25(24)32-26/h5-6,8-9,11-12,18,20,28H,7,10,13-17,19H2,1-4H3,(H,31,32)/t28-,29-/m0/s1
IUPAC Name
(1S,2S)-2-(2-{[3-(1H-1,3-benzodiazol-2-yl)propyl](methyl)amino}ethyl)-6-fluoro-1-(propan-2-yl)-1,2,3,4-tetrahydronaphthalen-2-yl 2-methoxyacetate
SMILES
COCC(=O)O[[email protected]]1(CCN(C)CCCC2=NC3=CC=CC=C3N2)CCC2=C(C=CC(F)=C2)[[email protected]@H]1C(C)C

Pharmacology

Indication

For the treatment of angina and high blood pressure.

Structured Indications
Not Available
Pharmacodynamics

Mibefradil belongs to a group of medicines called calcium channel blocking agents, or, more commonly, calcium channel blockers. Calcium channel blocking agents affect the movement of calcium into the cells of the heart and blood vessels. As a result, they relax blood vessels and increase the supply of blood and oxygen to the heart while reducing its workload. Mibefradil is a benzimidazoyl-substituted tetraline that selectively binds and inhibits T-type calcium channels.

Mechanism of action

Mibefradil is a tetralol calcium channel blocking agent that inhibits the influx of calcium ions across both the T (low-voltage) and L (high-voltage) calcium channels of cardiac and vascular smooth muscle, with a greater selectivity for T channels. Vasodilation occurs in vascular smooth muscle, causing a decrease in peripheral vascular resistance and a resulting decrease in blood pressure. Mibefradil causes a slight increase in cardiac output during chronic dosing. Mibefradil slows sinus and atrioventricular (AV) node conduction, producing a slight reduction in heart rate and a slight increase in the PR interval. It has also been shown to slightly lengthen the corrected sinus node recovery time and AH interval and to raise the Wenckebach point. The mechanism by which mibefradil reduces angina is not known, but is thought to be attributed to a reduction in heart rate, total peripheral resistance (afterload), and the heart rate–systolic blood pressure product at any given level of exercise. The result of these effects is a decrease in cardiac workload and myocardial oxygen demand.

TargetActionsOrganism
AVoltage-dependent T-type calcium channel subunit alpha-1G
inhibitor
Human
AVoltage-dependent T-type calcium channel subunit alpha-1H
inhibitor
Human
AVoltage-dependent L-type calcium channel subunit alpha-1C
inhibitor
Human
AVoltage-dependent L-type calcium channel subunit alpha-1D
inhibitor
Human
AVoltage-dependent L-type calcium channel subunit alpha-1F
inhibitor
Human
AVoltage-dependent T-type calcium channel subunit alpha-1I
inhibitor
Human
AVoltage-dependent L-type calcium channel subunit alpha-1S
inhibitor
Human
AVoltage-dependent L-type calcium channel subunit beta-1
inhibitor
Human
AVoltage-dependent L-type calcium channel subunit beta-2
inhibitor
Human
AVoltage-dependent L-type calcium channel subunit beta-3
inhibitor
Human
AVoltage-dependent L-type calcium channel subunit beta-4
inhibitor
Human
Absorption

Bioavailability after a single dose is 70%. After multiple dosing, the proportion of mibefradil undergoing first-pass metabolism is reduced, resulting in a steady state bioavailability of approximately 90%. Food does not affect the rate or extent of absorption of mibefradil.

Volume of distribution
Not Available
Protein binding

≥ 99%, primarily to alpha 1-acid glycoprotein.

Metabolism

The two metabolic pathways that mibefradil undergoes are esterase-catalyzed hydrolysis of the ester side chain (producing an alcohol metabolite) and cytochrome P450 3A4-catalyzed oxidation (that becomes less important during chronic dosing). The pharmacologic effect of the metabolite is approximately 10% of that of the parent mibefradil.

Route of elimination
Not Available
Half life

17 to 25 hours at steady state.

Clearance
Not Available
Toxicity
Not Available
Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteractionDrug group
2-HYDROXY-1,4-NAPHTHOQUINONEThe risk or severity of adverse effects can be increased when 2-HYDROXY-1,4-NAPHTHOQUINONE is combined with Mibefradil.Experimental
2-mercaptobenzothiazoleThe risk or severity of adverse effects can be increased when 2-mercaptobenzothiazole is combined with Mibefradil.Vet Approved
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline may increase the hypotensive activities of Mibefradil.Experimental
AfatinibThe serum concentration of Afatinib can be increased when it is combined with Mibefradil.Approved
AlfuzosinAlfuzosin may increase the hypotensive activities of Mibefradil.Approved, Investigational
AliskirenMibefradil may increase the hypotensive activities of Aliskiren.Approved, Investigational
AlprenololAlprenolol may increase the hypotensive activities of Mibefradil.Approved, Withdrawn
AmifostineMibefradil may increase the hypotensive activities of Amifostine.Approved, Investigational
AmiodaroneThe metabolism of Mibefradil can be decreased when combined with Amiodarone.Approved, Investigational
AmlodipineAmlodipine may increase the hypotensive activities of Mibefradil.Approved
AmobarbitalThe metabolism of Mibefradil can be increased when combined with Amobarbital.Approved, Illicit
AmorolfineThe risk or severity of adverse effects can be increased when Amorolfine is combined with Mibefradil.Approved, Investigational
Amphotericin BThe risk or severity of adverse effects can be increased when Amphotericin B is combined with Mibefradil.Approved, Investigational
AnidulafunginThe risk or severity of adverse effects can be increased when Anidulafungin is combined with Mibefradil.Approved, Investigational
AprepitantThe serum concentration of Mibefradil can be increased when it is combined with Aprepitant.Approved, Investigational
ArtemetherThe risk or severity of adverse effects can be increased when Artemether is combined with Mibefradil.Approved
AtazanavirThe metabolism of Mibefradil can be decreased when combined with Atazanavir.Approved, Investigational
AtomoxetineThe metabolism of Mibefradil can be decreased when combined with Atomoxetine.Approved
AtorvastatinThe risk or severity of adverse effects can be increased when Mibefradil is combined with Atorvastatin.Approved
AtosibanThe risk or severity of adverse effects can be increased when Mibefradil is combined with Atosiban.Approved, Investigational
Atracurium besylateMibefradil may increase the neuromuscular blocking activities of Atracurium besylate.Approved
Bafilomycin A1The risk or severity of adverse effects can be increased when Bafilomycin A1 is combined with Mibefradil.Experimental
BarbexacloneThe metabolism of Mibefradil can be increased when combined with Barbexaclone.Experimental
BarbitalThe metabolism of Mibefradil can be increased when combined with Barbital.Illicit
BenazeprilBenazepril may increase the hypotensive activities of Mibefradil.Approved, Investigational
BendroflumethiazideBendroflumethiazide may increase the hypotensive activities of Mibefradil.Approved
BenmoxinBenmoxin may increase the hypotensive activities of Mibefradil.Withdrawn
Benzoic AcidThe risk or severity of adverse effects can be increased when Benzoic Acid is combined with Mibefradil.Approved
BepridilBepridil may increase the hypotensive activities of Mibefradil.Approved, Withdrawn
BetaxololBetaxolol may increase the hypotensive activities of Mibefradil.Approved
BethanidineBethanidine may increase the hypotensive activities of Mibefradil.Approved
BietaserpineBietaserpine may increase the hypotensive activities of Mibefradil.Experimental
BifonazoleThe risk or severity of adverse effects can be increased when Bifonazole is combined with Mibefradil.Approved, Investigational
BimatoprostBimatoprost may increase the hypotensive activities of Mibefradil.Approved, Investigational
BisoprololBisoprolol may increase the hypotensive activities of Mibefradil.Approved
BoceprevirThe metabolism of Mibefradil can be decreased when combined with Boceprevir.Approved, Withdrawn
BortezomibThe metabolism of Mibefradil can be decreased when combined with Bortezomib.Approved, Investigational
BosentanThe serum concentration of Mibefradil can be decreased when it is combined with Bosentan.Approved, Investigational
BosutinibThe serum concentration of Bosutinib can be increased when it is combined with Mibefradil.Approved
BQ-123Mibefradil may increase the hypotensive activities of BQ-123.Investigational
Brefeldin AThe risk or severity of adverse effects can be increased when 1,6,7,8,9,11A,12,13,14,14A-DECAHYDRO-1,13-DIHYDROXY-6-METHYL-4H-CYCLOPENT[F]OXACYCLOTRIDECIN-4-ONE is combined with Mibefradil.Experimental
Brentuximab vedotinThe serum concentration of Brentuximab vedotin can be increased when it is combined with Mibefradil.Approved
BretyliumBretylium may increase the hypotensive activities of Mibefradil.Approved
BrimonidineBrimonidine may increase the antihypertensive activities of Mibefradil.Approved
BrofaromineBrofaromine may increase the hypotensive activities of Mibefradil.Experimental
BucindololBucindolol may increase the hypotensive activities of Mibefradil.Investigational
BunazosinBunazosin may increase the hypotensive activities of Mibefradil.Investigational
BupranololMibefradil may increase the hypotensive activities of Bupranolol.Approved
ButenafineThe risk or severity of adverse effects can be increased when Butenafine is combined with Mibefradil.Approved
ButoconazoleThe risk or severity of adverse effects can be increased when Butoconazole is combined with Mibefradil.Approved
CabergolineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Mibefradil.Approved
CadralazineCadralazine may increase the hypotensive activities of Mibefradil.Experimental
CafedrineMibefradil may increase the hypotensive activities of Cafedrine.Investigational
CalciumThe therapeutic efficacy of Mibefradil can be decreased when used in combination with Calcium.Approved, Nutraceutical
Calcium AcetateThe therapeutic efficacy of Mibefradil can be decreased when used in combination with Calcium Acetate.Approved
Calcium CarbonateThe therapeutic efficacy of Mibefradil can be decreased when used in combination with Calcium Carbonate.Approved
Calcium CitrateThe therapeutic efficacy of Mibefradil can be decreased when used in combination with Calcium Citrate.Approved
Calcium glubionateThe therapeutic efficacy of Mibefradil can be decreased when used in combination with Calcium glubionate.Approved
Calcium GluceptateThe therapeutic efficacy of Mibefradil can be decreased when used in combination with Calcium Gluceptate.Approved
Calcium gluconateThe therapeutic efficacy of Mibefradil can be decreased when used in combination with Calcium gluconate.Approved, Vet Approved
Calcium lactateThe therapeutic efficacy of Mibefradil can be decreased when used in combination with Calcium lactate.Approved, Experimental, Investigational, Vet Approved
Calcium lactate gluconateThe therapeutic efficacy of Mibefradil can be decreased when used in combination with Calcium lactate gluconate.Experimental
Calcium laevulateThe therapeutic efficacy of Mibefradil can be decreased when used in combination with Calcium laevulate.Experimental
Calcium pangamateThe therapeutic efficacy of Mibefradil can be decreased when used in combination with Calcium pangamate.Experimental
Calcium PhosphateThe therapeutic efficacy of Mibefradil can be decreased when used in combination with Calcium Phosphate.Approved
Candesartan cilexetilCandesartan may increase the hypotensive activities of Mibefradil.Approved
CandicidinThe risk or severity of adverse effects can be increased when Candicidin is combined with Mibefradil.Withdrawn
CandoxatrilCandoxatril may increase the hypotensive activities of Mibefradil.Experimental
Capric acidThe risk or severity of adverse effects can be increased when Capric acid is combined with Mibefradil.Experimental
CaptoprilCaptopril may increase the hypotensive activities of Mibefradil.Approved
CarbamazepineThe metabolism of Mibefradil can be increased when combined with Carbamazepine.Approved, Investigational
CarbomycinThe metabolism of Mibefradil can be decreased when combined with Carbomycin.Vet Approved
CaroxazoneCaroxazone may increase the hypotensive activities of Mibefradil.Withdrawn
CarteololCarteolol may increase the hypotensive activities of Mibefradil.Approved
CarvedilolCarvedilol may increase the hypotensive activities of Mibefradil.Approved, Investigational
CaseinThe therapeutic efficacy of Mibefradil can be decreased when used in combination with Casein.Approved
CaspofunginThe risk or severity of adverse effects can be increased when Caspofungin is combined with Mibefradil.Approved
CeliprololMibefradil may increase the hypotensive activities of Celiprolol.Approved, Investigational
CeritinibThe serum concentration of Mibefradil can be increased when it is combined with Ceritinib.Approved
CeruleninThe risk or severity of adverse effects can be increased when Cerulenin is combined with Mibefradil.Approved
ChlorothiazideChlorothiazide may increase the hypotensive activities of Mibefradil.Approved, Vet Approved
ChloroxineThe risk or severity of adverse effects can be increased when Chloroxine is combined with Mibefradil.Approved
ChlorthalidoneChlorthalidone may increase the hypotensive activities of Mibefradil.Approved
CicletanineMibefradil may increase the hypotensive activities of Cicletanine.Investigational
CiclopiroxThe risk or severity of adverse effects can be increased when Ciclopirox is combined with Mibefradil.Approved, Investigational
CilazaprilCilazapril may increase the hypotensive activities of Mibefradil.Approved
CimetidineThe serum concentration of Mibefradil can be increased when it is combined with Cimetidine.Approved
ClarithromycinThe metabolism of Mibefradil can be decreased when combined with Clarithromycin.Approved
ClemastineThe metabolism of Mibefradil can be decreased when combined with Clemastine.Approved
ClopidogrelThe therapeutic efficacy of Clopidogrel can be decreased when used in combination with Mibefradil.Approved, Nutraceutical
CloranololMibefradil may increase the hypotensive activities of Cloranolol.Experimental
ClotrimazoleThe risk or severity of adverse effects can be increased when Clotrimazole is combined with Mibefradil.Approved, Vet Approved
CobicistatThe metabolism of Mibefradil can be decreased when combined with Cobicistat.Approved
ColchicineThe serum concentration of Colchicine can be increased when it is combined with Mibefradil.Approved
ConivaptanThe serum concentration of Mibefradil can be increased when it is combined with Conivaptan.Approved, Investigational
CordycepinThe risk or severity of adverse effects can be increased when Cordycepin is combined with Mibefradil.Investigational
CrizotinibThe metabolism of Mibefradil can be decreased when combined with Crizotinib.Approved
CryptenamineCryptenamine may increase the hypotensive activities of Mibefradil.Approved
CyclopenthiazideMibefradil may increase the hypotensive activities of Cyclopenthiazide.Experimental
CyclosporineThe risk or severity of adverse effects can be increased when Cyclosporine is combined with Mibefradil.Approved, Investigational, Vet Approved
CyclothiazideCyclothiazide may increase the hypotensive activities of Mibefradil.Approved
Dabigatran etexilateThe serum concentration of the active metabolites of Dabigatran etexilate can be increased when Dabigatran etexilate is used in combination with Mibefradil.Approved
DabrafenibThe serum concentration of Mibefradil can be decreased when it is combined with Dabrafenib.Approved
DapoxetineDapoxetine may increase the orthostatic hypotensive activities of Mibefradil.Investigational
DarunavirThe metabolism of Mibefradil can be decreased when combined with Darunavir.Approved
DasatinibThe serum concentration of Mibefradil can be increased when it is combined with Dasatinib.Approved, Investigational
DeferasiroxThe serum concentration of Mibefradil can be decreased when it is combined with Deferasirox.Approved, Investigational
DelaprilMibefradil may increase the hypotensive activities of Delapril.Experimental
DelavirdineThe metabolism of Mibefradil can be decreased when combined with Delavirdine.Approved
DeserpidineMibefradil may increase the hypotensive activities of Deserpidine.Approved
DiazoxideDiazoxide may increase the hypotensive activities of Mibefradil.Approved
DichloropheneThe risk or severity of adverse effects can be increased when Dichlorophene is combined with Mibefradil.Vet Approved
diethylnorspermineMibefradil may increase the hypotensive activities of diethylnorspermine.Investigational
DihydralazineDihydralazine may increase the hypotensive activities of Mibefradil.Investigational
DihydroergocornineThe risk or severity of adverse effects can be increased when Dihydroergocornine is combined with Mibefradil.Approved
DihydroergocristineThe risk or severity of adverse effects can be increased when Dihydroergocristine is combined with Mibefradil.Experimental
DihydroergocryptineThe risk or severity of adverse effects can be increased when Dihydroergocryptine is combined with Mibefradil.Experimental
DihydroergotamineThe metabolism of Mibefradil can be decreased when combined with Dihydroergotamine.Approved
DiltiazemThe metabolism of Mibefradil can be decreased when combined with Diltiazem.Approved
DorzolamideDorzolamide may increase the hypotensive activities of Mibefradil.Approved
DoxazosinDoxazosin may increase the hypotensive activities of Mibefradil.Approved
DoxorubicinThe serum concentration of Doxorubicin can be increased when it is combined with Mibefradil.Approved, Investigational
DoxycyclineThe metabolism of Mibefradil can be decreased when combined with Doxycycline.Approved, Investigational, Vet Approved
DronedaroneThe metabolism of Mibefradil can be decreased when combined with Dronedarone.Approved
EconazoleThe risk or severity of adverse effects can be increased when Econazole is combined with Mibefradil.Approved
EdoxabanThe serum concentration of Edoxaban can be increased when it is combined with Mibefradil.Approved
EfavirenzThe serum concentration of Mibefradil can be decreased when it is combined with Efavirenz.Approved, Investigational
EfinaconazoleThe risk or severity of adverse effects can be increased when Efinaconazole is combined with Mibefradil.Approved
EfonidipineMibefradil may increase the hypotensive activities of Efonidipine.Approved
EnalaprilEnalapril may increase the hypotensive activities of Mibefradil.Approved, Vet Approved
EnalaprilatMibefradil may increase the hypotensive activities of Enalaprilat.Approved
EndralazineEndralazine may increase the hypotensive activities of Mibefradil.Experimental
EnzalutamideThe serum concentration of Mibefradil can be decreased when it is combined with Enzalutamide.Approved
EpanololMibefradil may increase the hypotensive activities of Epanolol.Experimental
EpoprostenolEpoprostenol may increase the hypotensive activities of Mibefradil.Approved
EprosartanEprosartan may increase the hypotensive activities of Mibefradil.Approved
ErgonovineThe risk or severity of adverse effects can be increased when Ergonovine is combined with Mibefradil.Approved
ErgotamineThe risk or severity of adverse effects can be increased when Ergotamine is combined with Mibefradil.Approved
ErythromycinThe metabolism of Mibefradil can be decreased when combined with Erythromycin.Approved, Vet Approved
EverolimusThe serum concentration of Everolimus can be increased when it is combined with Mibefradil.Approved
FelodipineFelodipine may increase the hypotensive activities of Mibefradil.Approved, Investigational
FenoldopamFenoldopam may increase the hypotensive activities of Mibefradil.Approved
FenticonazoleThe risk or severity of adverse effects can be increased when Fenticonazole is combined with Mibefradil.Experimental
Ferulic acidMibefradil may increase the hypotensive activities of Ferulic acid.Experimental
FesoterodineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Mibefradil.Approved
FluconazoleThe serum concentration of Mibefradil can be increased when it is combined with Fluconazole.Approved
FlucytosineThe risk or severity of adverse effects can be increased when Flucytosine is combined with Mibefradil.Approved
FlutrimazoleThe risk or severity of adverse effects can be increased when Flutrimazole is combined with Mibefradil.Experimental
FluvastatinThe serum concentration of Fluvastatin can be increased when it is combined with Mibefradil.Approved
FluvoxamineThe metabolism of Mibefradil can be decreased when combined with Fluvoxamine.Approved, Investigational
FosamprenavirThe metabolism of Mibefradil can be decreased when combined with Fosamprenavir.Approved
FosaprepitantThe serum concentration of Mibefradil can be increased when it is combined with Fosaprepitant.Approved
FosinoprilFosinopril may increase the hypotensive activities of Mibefradil.Approved
FosphenytoinThe serum concentration of Fosphenytoin can be increased when it is combined with Mibefradil.Approved
FurazolidoneFurazolidone may increase the hypotensive activities of Mibefradil.Approved, Investigational, Vet Approved
Fusidic AcidThe serum concentration of Mibefradil can be increased when it is combined with Fusidic Acid.Approved
GlyphosateThe risk or severity of adverse effects can be increased when Glyphosate is combined with Mibefradil.Experimental
GriseofulvinThe risk or severity of adverse effects can be increased when Griseofulvin is combined with Mibefradil.Approved, Vet Approved
GuanabenzGuanabenz may increase the hypotensive activities of Mibefradil.Approved, Investigational
GuanadrelGuanadrel may increase the hypotensive activities of Mibefradil.Approved
GuanazodineMibefradil may increase the hypotensive activities of Guanazodine.Experimental
GuanethidineGuanethidine may increase the hypotensive activities of Mibefradil.Approved
GuanfacineGuanfacine may increase the hypotensive activities of Mibefradil.Approved, Investigational
GuanoclorMibefradil may increase the hypotensive activities of Guanoclor.Experimental
GuanoxabenzMibefradil may increase the hypotensive activities of Guanoxabenz.Experimental
GuanoxanMibefradil may increase the hypotensive activities of Guanoxan.Experimental
HachimycinThe risk or severity of adverse effects can be increased when Hachimycin is combined with Mibefradil.Experimental
HaloproginThe risk or severity of adverse effects can be increased when Haloprogin is combined with Mibefradil.Approved, Withdrawn
HarmalineHarmaline may increase the hypotensive activities of Mibefradil.Experimental
HexamethoniumMibefradil may increase the hypotensive activities of Hexamethonium.Experimental
HexetidineThe risk or severity of adverse effects can be increased when Hexetidine is combined with Mibefradil.Approved, Investigational
HexobarbitalThe metabolism of Mibefradil can be increased when combined with Hexobarbital.Approved
HydracarbazineHydracarbazine may increase the hypotensive activities of Mibefradil.Experimental
HydralazineHydralazine may increase the hypotensive activities of Mibefradil.Approved
HydrochlorothiazideHydrochlorothiazide may increase the hypotensive activities of Mibefradil.Approved, Vet Approved
HydroflumethiazideHydroflumethiazide may increase the hypotensive activities of Mibefradil.Approved, Investigational
IdelalisibThe serum concentration of Mibefradil can be increased when it is combined with Idelalisib.Approved
IloprostIloprost may increase the hypotensive activities of Mibefradil.Approved, Investigational
ImatinibThe metabolism of Mibefradil can be decreased when combined with Imatinib.Approved
ImidaprilMibefradil may increase the hypotensive activities of Imidapril.Investigational
IndapamideIndapamide may increase the hypotensive activities of Mibefradil.Approved
IndenololMibefradil may increase the hypotensive activities of Indenolol.Withdrawn
IndinavirThe metabolism of Mibefradil can be decreased when combined with Indinavir.Approved
IndoraminIndoramin may increase the hypotensive activities of Mibefradil.Withdrawn
IproclozideIproclozide may increase the hypotensive activities of Mibefradil.Withdrawn
IproniazidIproniazid may increase the hypotensive activities of Mibefradil.Withdrawn
IrbesartanIrbesartan may increase the hypotensive activities of Mibefradil.Approved, Investigational
IsavuconazoniumThe metabolism of Mibefradil can be decreased when combined with Isavuconazonium.Approved, Investigational
IsocarboxazidIsocarboxazid may increase the hypotensive activities of Mibefradil.Approved
IsoconazoleThe risk or severity of adverse effects can be increased when Isoconazole is combined with Mibefradil.Approved
IsradipineThe metabolism of Mibefradil can be decreased when combined with Isradipine.Approved
ItraconazoleThe metabolism of Mibefradil can be decreased when combined with Itraconazole.Approved, Investigational
IvacaftorThe serum concentration of Mibefradil can be increased when it is combined with Ivacaftor.Approved
JosamycinThe metabolism of Mibefradil can be decreased when combined with Josamycin.Approved, Investigational
KetanserinKetanserin may increase the hypotensive activities of Mibefradil.Investigational
KetoconazoleThe metabolism of Mibefradil can be decreased when combined with Ketoconazole.Approved, Investigational
KitasamycinThe metabolism of Mibefradil can be decreased when combined with Kitasamycin.Experimental
LabetalolLabetalol may increase the hypotensive activities of Mibefradil.Approved
LacidipineMibefradil may increase the hypotensive activities of Lacidipine.Approved, Investigational
LatanoprostLatanoprost may increase the hypotensive activities of Mibefradil.Approved, Investigational
LedipasvirThe serum concentration of Ledipasvir can be increased when it is combined with Mibefradil.Approved
LercanidipineLercanidipine may increase the hypotensive activities of Mibefradil.Approved, Investigational
LinsidomineMibefradil may increase the hypotensive activities of Linsidomine.Experimental
LisinoprilLisinopril may increase the hypotensive activities of Mibefradil.Approved, Investigational
LisurideThe risk or severity of adverse effects can be increased when Lisuride is combined with Mibefradil.Approved, Investigational
LofexidineMibefradil may increase the hypotensive activities of Lofexidine.Approved, Investigational
LopinavirThe metabolism of Mibefradil can be decreased when combined with Lopinavir.Approved
LovastatinThe metabolism of Mibefradil can be decreased when combined with Lovastatin.Approved, Investigational
LuliconazoleThe serum concentration of Mibefradil can be increased when it is combined with Luliconazole.Approved
LumacaftorThe metabolism of Mibefradil can be increased when combined with Lumacaftor.Approved
Lysergic Acid DiethylamideThe risk or severity of adverse effects can be increased when Lysergic Acid Diethylamide is combined with Mibefradil.Illicit, Investigational, Withdrawn
MacitentanMibefradil may increase the hypotensive activities of Macitentan.Approved
Magnesium HydroxideThe risk or severity of adverse effects can be increased when Mibefradil is combined with Magnesium Hydroxide.Approved
Magnesium oxideThe risk or severity of adverse effects can be increased when Mibefradil is combined with Magnesium oxide.Approved
Magnesium salicylateThe risk or severity of adverse effects can be increased when Mibefradil is combined with Magnesium salicylate.Approved
Magnesium SulfateThe risk or severity of adverse effects can be increased when Mibefradil is combined with Magnesium Sulfate.Approved, Vet Approved
ManidipineMibefradil may increase the hypotensive activities of Manidipine.Approved, Investigational
MebanazineMebanazine may increase the hypotensive activities of Mibefradil.Withdrawn
MecamylamineMecamylamine may increase the hypotensive activities of Mibefradil.Approved
MepartricinThe risk or severity of adverse effects can be increased when Mepartricin is combined with Mibefradil.Experimental
MetergolineThe risk or severity of adverse effects can be increased when Metergoline is combined with Mibefradil.Experimental
MethohexitalThe metabolism of Mibefradil can be increased when combined with Methohexital.Approved
MethoserpidineMibefradil may increase the hypotensive activities of Methoserpidine.Experimental
MethyldopaMethyldopa may increase the hypotensive activities of Mibefradil.Approved
Methylene blueMethylene blue may increase the hypotensive activities of Mibefradil.Approved, Investigational
MethylergometrineThe risk or severity of adverse effects can be increased when Methylergometrine is combined with Mibefradil.Approved
MethylphenidateMethylphenidate may decrease the antihypertensive activities of Mibefradil.Approved, Investigational
MethylphenobarbitalThe metabolism of Mibefradil can be increased when combined with Methylphenobarbital.Approved
MethysergideThe risk or severity of adverse effects can be increased when Methysergide is combined with Mibefradil.Approved
MetipranololMetipranolol may increase the hypotensive activities of Mibefradil.Approved
MetolazoneMetolazone may increase the hypotensive activities of Mibefradil.Approved
MetoprololThe serum concentration of Metoprolol can be increased when it is combined with Mibefradil.Approved, Investigational
MetyrosineMibefradil may increase the hypotensive activities of Metyrosine.Approved
MevastatinThe risk or severity of adverse effects can be increased when Mevastatin is combined with Mibefradil.Experimental
MicafunginThe risk or severity of adverse effects can be increased when Micafungin is combined with Mibefradil.Approved, Investigational
MiconazoleThe risk or severity of adverse effects can be increased when Miconazole is combined with Mibefradil.Approved, Investigational, Vet Approved
MifepristoneThe serum concentration of Mibefradil can be increased when it is combined with Mifepristone.Approved, Investigational
MiltefosineThe risk or severity of adverse effects can be increased when Miltefosine is combined with Mibefradil.Approved
MinaprineMinaprine may increase the hypotensive activities of Mibefradil.Approved
MinoxidilMinoxidil may increase the hypotensive activities of Mibefradil.Approved
MirodenafilMirodenafil may increase the antihypertensive activities of Mibefradil.Investigational
MitotaneThe serum concentration of Mibefradil can be decreased when it is combined with Mitotane.Approved
MivacuriumMibefradil may increase the neuromuscular blocking activities of Mivacurium.Approved
MoclobemideMoclobemide may increase the hypotensive activities of Mibefradil.Approved
MoexiprilMoexipril may increase the hypotensive activities of Mibefradil.Approved
MolsidomineMolsidomine may increase the hypotensive activities of Mibefradil.Approved, Investigational
MonensinThe risk or severity of adverse effects can be increased when Monensin is combined with Mibefradil.Vet Approved
MoxonidineMoxonidine may increase the hypotensive activities of Mibefradil.Approved, Investigational
MuzolimineMibefradil may increase the hypotensive activities of Muzolimine.Experimental
MyxothiazolThe risk or severity of adverse effects can be increased when Myxothiazol is combined with Mibefradil.Experimental
NafcillinThe metabolism of Mibefradil can be increased when combined with Nafcillin.Approved
NaftifineThe risk or severity of adverse effects can be increased when Naftifine is combined with Mibefradil.Approved
NaftopidilMibefradil may increase the hypotensive activities of Naftopidil.Investigational
NaloxegolThe serum concentration of Naloxegol can be increased when it is combined with Mibefradil.Approved
NatamycinThe risk or severity of adverse effects can be increased when Natamycin is combined with Mibefradil.Approved
NebivololMibefradil may increase the hypotensive activities of Nebivolol.Approved, Investigational
NefazodoneThe metabolism of Mibefradil can be decreased when combined with Nefazodone.Approved, Withdrawn
NelfinavirThe metabolism of Mibefradil can be decreased when combined with Nelfinavir.Approved
NetupitantThe serum concentration of Mibefradil can be increased when it is combined with Netupitant.Approved
NevirapineThe metabolism of Mibefradil can be increased when combined with Nevirapine.Approved
NialamideNialamide may increase the hypotensive activities of Mibefradil.Withdrawn
NicergolineThe risk or severity of adverse effects can be increased when Nicergoline is combined with Mibefradil.Approved, Investigational
NicorandilMibefradil may increase the hypotensive activities of Nicorandil.Approved, Investigational
NifuratelThe risk or severity of adverse effects can be increased when Nifuratel is combined with Mibefradil.Experimental
NiguldipineMibefradil may increase the hypotensive activities of Niguldipine.Experimental
Nikkomycin ZThe risk or severity of adverse effects can be increased when Nikkomycin Z is combined with Mibefradil.Investigational
NilotinibThe metabolism of Mibefradil can be decreased when combined with Nilotinib.Approved, Investigational
NilvadipineMibefradil may increase the hypotensive activities of Nilvadipine.Approved, Investigational
NimodipineNimodipine may increase the hypotensive activities of Mibefradil.Approved
NintedanibThe serum concentration of Nintedanib can be increased when it is combined with Mibefradil.Approved
NisoldipineNisoldipine may increase the hypotensive activities of Mibefradil.Approved
NitrendipineNitrendipine may increase the hypotensive activities of Mibefradil.Approved, Investigational
NitroprussideMibefradil may increase the hypotensive activities of Nitroprusside.Approved
NitroxolineThe risk or severity of adverse effects can be increased when Nitroxoline is combined with Mibefradil.Approved
NystatinThe risk or severity of adverse effects can be increased when Nystatin is combined with Mibefradil.Approved, Vet Approved
ObinutuzumabMibefradil may increase the hypotensive activities of Obinutuzumab.Approved
OctamoxinOctamoxin may increase the hypotensive activities of Mibefradil.Withdrawn
OlaparibThe metabolism of Mibefradil can be decreased when combined with Olaparib.Approved
OleandomycinThe metabolism of Mibefradil can be decreased when combined with Oleandomycin.Vet Approved
OlmesartanOlmesartan may increase the hypotensive activities of Mibefradil.Approved, Investigational
OmapatrilatOmapatrilat may increase the hypotensive activities of Mibefradil.Investigational
OmoconazoleThe risk or severity of adverse effects can be increased when Omoconazole is combined with Mibefradil.Experimental
OsimertinibThe serum concentration of Mibefradil can be increased when it is combined with Osimertinib.Approved
OxiconazoleThe risk or severity of adverse effects can be increased when Oxiconazole is combined with Mibefradil.Approved
OxprenololMibefradil may increase the hypotensive activities of Oxprenolol.Approved
pafuramidineThe risk or severity of adverse effects can be increased when pafuramidine is combined with Mibefradil.Investigational
PalbociclibThe serum concentration of Mibefradil can be increased when it is combined with Palbociclib.Approved
PargylinePargyline may increase the hypotensive activities of Mibefradil.Approved
PazopanibThe serum concentration of Pazopanib can be increased when it is combined with Mibefradil.Approved
PenbutololPenbutolol may increase the hypotensive activities of Mibefradil.Approved, Investigational
PentamidineThe risk or severity of adverse effects can be increased when Pentamidine is combined with Mibefradil.Approved
PentobarbitalThe metabolism of Mibefradil can be increased when combined with Pentobarbital.Approved, Vet Approved
PentoliniumPentolinium may increase the hypotensive activities of Mibefradil.Approved
PentoxifyllinePentoxifylline may increase the hypotensive activities of Mibefradil.Approved, Investigational
PergolideThe risk or severity of adverse effects can be increased when Pergolide is combined with Mibefradil.Approved, Investigational, Vet Approved, Withdrawn
PerindoprilPerindopril may increase the hypotensive activities of Mibefradil.Approved
PhenelzinePhenelzine may increase the hypotensive activities of Mibefradil.Approved
PheniprazinePheniprazine may increase the hypotensive activities of Mibefradil.Withdrawn
PhenobarbitalThe metabolism of Mibefradil can be increased when combined with Phenobarbital.Approved
PhenoxybenzaminePhenoxybenzamine may increase the hypotensive activities of Mibefradil.Approved
PhenoxypropazinePhenoxypropazine may increase the hypotensive activities of Mibefradil.Withdrawn
PhentolaminePhentolamine may increase the hypotensive activities of Mibefradil.Approved
PhenytoinThe serum concentration of Phenytoin can be increased when it is combined with Mibefradil.Approved, Vet Approved
PinacidilPinacidil may increase the hypotensive activities of Mibefradil.Withdrawn
PindololPindolol may increase the hypotensive activities of Mibefradil.Approved
PirlindolePirlindole may increase the hypotensive activities of Mibefradil.Approved
PivhydrazinePivhydrazine may increase the hypotensive activities of Mibefradil.Withdrawn
PolythiazidePolythiazide may increase the hypotensive activities of Mibefradil.Approved
PosaconazoleThe metabolism of Mibefradil can be decreased when combined with Posaconazole.Approved, Investigational, Vet Approved
PrimidoneThe metabolism of Mibefradil can be increased when combined with Primidone.Approved, Vet Approved
PrucaloprideThe serum concentration of Prucalopride can be increased when it is combined with Mibefradil.Approved
PyrrolnitrinThe risk or severity of adverse effects can be increased when Pyrrolnitrin is combined with Mibefradil.Experimental
QuinaprilQuinapril may increase the hypotensive activities of Mibefradil.Approved, Investigational
QuinineQuinine may increase the hypotensive activities of Mibefradil.Approved
RadicicolThe risk or severity of adverse effects can be increased when Radicicol is combined with Mibefradil.Experimental
RamiprilRamipril may increase the hypotensive activities of Mibefradil.Approved
RanolazineThe serum concentration of Ranolazine can be increased when it is combined with Mibefradil.Approved, Investigational
RapacuroniumMibefradil may increase the neuromuscular blocking activities of Rapacuronium.Withdrawn
RasagilineRasagiline may increase the hypotensive activities of Mibefradil.Approved
RemikirenRemikiren may increase the hypotensive activities of Mibefradil.Approved
RescinnamineMibefradil may increase the hypotensive activities of Rescinnamine.Approved
RifabutinThe metabolism of Mibefradil can be increased when combined with Rifabutin.Approved
RifampicinThe metabolism of Mibefradil can be increased when combined with Rifampicin.Approved
RifapentineThe metabolism of Mibefradil can be increased when combined with Rifapentine.Approved
RifaximinThe serum concentration of Rifaximin can be increased when it is combined with Mibefradil.Approved, Investigational
RilmenidineRilmenidine may increase the hypotensive activities of Mibefradil.Investigational
RiociguatMibefradil may increase the hypotensive activities of Riociguat.Approved
RitonavirThe metabolism of Mibefradil can be decreased when combined with Ritonavir.Approved, Investigational
RituximabMibefradil may increase the hypotensive activities of Rituximab.Approved
RosuvastatinThe serum concentration of Rosuvastatin can be increased when it is combined with Mibefradil.Approved
SafrazineSafrazine may increase the hypotensive activities of Mibefradil.Withdrawn
Salicylhydroxamic AcidThe risk or severity of adverse effects can be increased when Salicylhydroxamic Acid is combined with Mibefradil.Experimental
Salicylic acidThe risk or severity of adverse effects can be increased when Salicylic acid is combined with Mibefradil.Approved, Vet Approved
SaprisartanSaprisartan may increase the hypotensive activities of Mibefradil.Experimental
SaquinavirThe metabolism of Mibefradil can be decreased when combined with Saquinavir.Approved, Investigational
SecobarbitalThe metabolism of Mibefradil can be increased when combined with Secobarbital.Approved, Vet Approved
SelegilineSelegiline may increase the hypotensive activities of Mibefradil.Approved, Investigational, Vet Approved
SertaconazoleThe risk or severity of adverse effects can be increased when Sertaconazole is combined with Mibefradil.Approved
SildenafilSildenafil may increase the antihypertensive activities of Mibefradil.Approved, Investigational
SilodosinThe serum concentration of Silodosin can be increased when it is combined with Mibefradil.Approved
SiltuximabThe serum concentration of Mibefradil can be decreased when it is combined with Siltuximab.Approved
SimeprevirThe serum concentration of Mibefradil can be increased when it is combined with Simeprevir.Approved
SimvastatinThe serum concentration of Simvastatin can be increased when it is combined with Mibefradil.Approved
SinefunginThe risk or severity of adverse effects can be increased when Sinefungin is combined with Mibefradil.Experimental
SirolimusThe risk or severity of adverse effects can be increased when Sirolimus is combined with Mibefradil.Approved, Investigational
SitaxentanMibefradil may increase the hypotensive activities of Sitaxentan.Approved, Investigational, Withdrawn
SolithromycinThe metabolism of Mibefradil can be decreased when combined with Solithromycin.Investigational
SpiraprilSpirapril may increase the hypotensive activities of Mibefradil.Approved
St. John's WortThe serum concentration of Mibefradil can be decreased when it is combined with St. John's Wort.Investigational, Nutraceutical
StiripentolThe serum concentration of Mibefradil can be increased when it is combined with Stiripentol.Approved
SulconazoleThe risk or severity of adverse effects can be increased when Sulconazole is combined with Mibefradil.Approved
SulfisoxazoleThe metabolism of Mibefradil can be decreased when combined with Sulfisoxazole.Approved, Vet Approved
TadalafilTadalafil may increase the antihypertensive activities of Mibefradil.Approved, Investigational
TalinololMibefradil may increase the hypotensive activities of Talinolol.Investigational
TamsulosinTamsulosin may increase the hypotensive activities of Mibefradil.Approved, Investigational
TavaboroleThe risk or severity of adverse effects can be increased when Tavaborole is combined with Mibefradil.Approved
TelaprevirThe metabolism of Mibefradil can be decreased when combined with Telaprevir.Approved, Withdrawn
TelithromycinThe metabolism of Mibefradil can be decreased when combined with Telithromycin.Approved
TelmisartanTelmisartan may increase the hypotensive activities of Mibefradil.Approved, Investigational
TemocaprilMibefradil may increase the hypotensive activities of Temocapril.Experimental, Investigational
TerazosinTerazosin may increase the hypotensive activities of Mibefradil.Approved
TerbinafineThe risk or severity of adverse effects can be increased when Terbinafine is combined with Mibefradil.Approved, Investigational, Vet Approved
TerconazoleThe risk or severity of adverse effects can be increased when Terconazole is combined with Mibefradil.Approved
TergurideThe risk or severity of adverse effects can be increased when Terguride is combined with Mibefradil.Experimental
TerlipressinMibefradil may increase the hypotensive activities of Terlipressin.Approved, Investigational
TetrahydropalmatineMibefradil may increase the hypotensive activities of Tetrahydropalmatine.Investigational
TheodrenalineMibefradil may increase the hypotensive activities of Theodrenaline.Investigational
ThiamylalThe metabolism of Mibefradil can be increased when combined with Thiamylal.Approved, Vet Approved
ThiopentalThe metabolism of Mibefradil can be increased when combined with Thiopental.Approved, Vet Approved
ThioridazineThe serum concentration of Thioridazine can be increased when it is combined with Mibefradil.Approved, Withdrawn
ThymolThe risk or severity of adverse effects can be increased when Thymol is combined with Mibefradil.Approved
TiboloneMibefradil may increase the hypotensive activities of Tibolone.Approved, Investigational
TiclopidineThe metabolism of Mibefradil can be decreased when combined with Ticlopidine.Approved
TicrynafenMibefradil may increase the hypotensive activities of Ticrynafen.Withdrawn
TioconazoleThe risk or severity of adverse effects can be increased when Tioconazole is combined with Mibefradil.Approved
TocilizumabThe serum concentration of Mibefradil can be decreased when it is combined with Tocilizumab.Approved
TolazolineTolazoline may increase the hypotensive activities of Mibefradil.Approved, Vet Approved
TolciclateThe risk or severity of adverse effects can be increased when Tolciclate is combined with Mibefradil.Experimental
TolnaftateThe risk or severity of adverse effects can be increased when Tolnaftate is combined with Mibefradil.Approved, Vet Approved
TolonidineMibefradil may increase the hypotensive activities of Tolonidine.Experimental
ToloxatoneToloxatone may increase the hypotensive activities of Mibefradil.Approved
TopotecanThe serum concentration of Topotecan can be increased when it is combined with Mibefradil.Approved, Investigational
TorasemideTorasemide may increase the hypotensive activities of Mibefradil.Approved
TrandolaprilTrandolapril may increase the hypotensive activities of Mibefradil.Approved
Trans-2-PhenylcyclopropylamineTrans-2-Phenylcyclopropylamine may increase the hypotensive activities of Mibefradil.Experimental
TranylcypromineTranylcypromine may increase the hypotensive activities of Mibefradil.Approved
TravoprostTravoprost may increase the hypotensive activities of Mibefradil.Approved
TreprostinilTreprostinil may increase the hypotensive activities of Mibefradil.Approved, Investigational
TrichlormethiazideTrichlormethiazide may increase the hypotensive activities of Mibefradil.Approved, Vet Approved
TrimazosinTrimazosin may increase the hypotensive activities of Mibefradil.Experimental
TrimethaphanTrimethaphan may increase the hypotensive activities of Mibefradil.Approved, Investigational
TrimetrexateThe risk or severity of adverse effects can be increased when Trimetrexate is combined with Mibefradil.Approved, Investigational
TylosinThe metabolism of Mibefradil can be decreased when combined with Tylosin.Vet Approved
UbidecarenoneThe serum concentration of Ubidecarenone can be increased when it is combined with Mibefradil.Approved, Experimental
UdenafilUdenafil may increase the antihypertensive activities of Mibefradil.Approved, Investigational
UnoprostoneMibefradil may increase the hypotensive activities of Unoprostone.Approved
UrapidilUrapidil may increase the hypotensive activities of Mibefradil.Investigational
ValsartanValsartan may increase the hypotensive activities of Mibefradil.Approved, Investigational
VardenafilVardenafil may increase the antihypertensive activities of Mibefradil.Approved
VenlafaxineThe metabolism of Mibefradil can be decreased when combined with Venlafaxine.Approved
VerapamilThe metabolism of Mibefradil can be decreased when combined with Verapamil.Approved
VincamineMibefradil may increase the hypotensive activities of Vincamine.Experimental
VincristineThe serum concentration of Vincristine can be increased when it is combined with Mibefradil.Approved, Investigational
VinpocetineMibefradil may increase the hypotensive activities of Vinpocetine.Investigational
VoriconazoleThe metabolism of Mibefradil can be decreased when combined with Voriconazole.Approved, Investigational
XipamideMibefradil may increase the hypotensive activities of Xipamide.Experimental
XylometazolineMibefradil may increase the hypotensive activities of Xylometazoline.Approved
YohimbineYohimbine may decrease the antihypertensive activities of Mibefradil.Approved, Vet Approved
ZiprasidoneThe metabolism of Mibefradil can be decreased when combined with Ziprasidone.Approved
ZofenoprilMibefradil may increase the hypotensive activities of Zofenopril.Experimental
Food Interactions
Not Available

References

General References
Not Available
External Links
KEGG Compound
C07222
PubChem Compound
60663
PubChem Substance
46504498
ChemSpider
54673
BindingDB
50117922
ChEBI
6920
ChEMBL
CHEMBL45816
Therapeutic Targets Database
DCL000341
PharmGKB
PA450492
Wikipedia
Mibefradil
ATC Codes
C08CX01 — Mibefradil

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1CompletedTreatmentBrain and Central Nervous System Tumors1
1CompletedTreatmentGlioblastoma Multiforme (GBM)1
1CompletedTreatmentNo Condition. Assessment of Healthy Volunteers1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage forms
Not Available
Prices
Not Available
Patents
Not Available

Properties

State
Solid
Experimental Properties
PropertyValueSource
Caco2 permeability-4.87ADME Research, USCD
Predicted Properties
PropertyValueSource
Water Solubility0.00104 mg/mLALOGPS
logP5.34ALOGPS
logP5.16ChemAxon
logS-5.7ALOGPS
pKa (Strongest Acidic)12.54ChemAxon
pKa (Strongest Basic)9.82ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count4ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area67.45 Å2ChemAxon
Rotatable Bond Count12ChemAxon
Refractivity139.73 m3·mol-1ChemAxon
Number of Rings4ChemAxon
Bioavailability0ChemAxon
Rule of FiveNoChemAxon
Ghose FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleYesChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9964
Blood Brain Barrier+0.5
Caco-2 permeable+0.5
P-glycoprotein substrateSubstrate0.9087
P-glycoprotein inhibitor IInhibitor0.8718
P-glycoprotein inhibitor IIInhibitor0.8388
Renal organic cation transporterNon-inhibitor0.549
CYP450 2C9 substrateNon-substrate0.8596
CYP450 2D6 substrateNon-substrate0.9116
CYP450 3A4 substrateSubstrate0.7408
CYP450 1A2 substrateInhibitor0.9107
CYP450 2C9 inhibitorNon-inhibitor0.907
CYP450 2D6 inhibitorInhibitor0.8932
CYP450 2C19 inhibitorNon-inhibitor0.9025
CYP450 3A4 inhibitorInhibitor0.796
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.6921
Ames testNon AMES toxic0.6864
CarcinogenicityNon-carcinogens0.892
BiodegradationNot ready biodegradable1.0
Rat acute toxicity2.8610 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9611
hERG inhibition (predictor II)Inhibitor0.7742
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available

Taxonomy

Description
This compound belongs to the class of organic compounds known as tetralins. These are polycyclic aromatic compounds containing a tetralin moiety, which consists of a benzene fused to a cyclohexane.
Kingdom
Organic compounds
Super Class
Benzenoids
Class
Tetralins
Sub Class
Not Available
Direct Parent
Tetralins
Alternative Parents
Benzimidazoles / Aralkylamines / Aryl fluorides / Heteroaromatic compounds / Imidazoles / Trialkylamines / Amino acids and derivatives / Carboxylic acid esters / Dialkyl ethers / Azacyclic compounds
show 6 more
Substituents
Tetralin / Benzimidazole / Aralkylamine / Aryl fluoride / Aryl halide / Imidazole / Azole / Heteroaromatic compound / Amino acid or derivatives / Carboxylic acid ester
show 20 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
tetralins (CHEBI:6920)

Targets

Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Inhibitor
General Function
Scaffold protein binding
Specific Function
Voltage-sensitive calcium channels (VSCC) mediate the entry of calcium ions into excitable cells and are also involved in a variety of calcium-dependent processes, including muscle contraction, hor...
Gene Name
CACNA1G
Uniprot ID
O43497
Uniprot Name
Voltage-dependent T-type calcium channel subunit alpha-1G
Molecular Weight
262468.62 Da
References
  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
  2. Lee TS, Kaku T, Takebayashi S, Uchino T, Miyamoto S, Hadama T, Perez-Reyes E, Ono K: Actions of mibefradil, efonidipine and nifedipine block of recombinant T- and L-type Ca channels with distinct inhibitory mechanisms. Pharmacology. 2006;78(1):11-20. Epub 2006 Aug 7. [PubMed:16899990]
  3. Monteil A, Chemin J, Bourinet E, Mennessier G, Lory P, Nargeot J: Molecular and functional properties of the human alpha(1G) subunit that forms T-type calcium channels. J Biol Chem. 2000 Mar 3;275(9):6090-100. [PubMed:10692398]
  4. Massie BM: Mibefradil: a selective T-type calcium antagonist. Am J Cardiol. 1997 Nov 6;80(9A):23I-32I. [PubMed:9375939]
  5. Clozel JP, Ertel EA, Ertel SI: Discovery and main pharmacological properties of mibefradil (Ro 40-5967), the first selective T-type calcium channel blocker. J Hypertens Suppl. 1997 Dec;15(5):S17-25. [PubMed:9481612]
  6. McNulty MM, Hanck DA: State-dependent mibefradil block of Na+ channels. Mol Pharmacol. 2004 Dec;66(6):1652-61. [PubMed:15562257]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Inhibitor
General Function
Scaffold protein binding
Specific Function
Voltage-sensitive calcium channels (VSCC) mediate the entry of calcium ions into excitable cells and are also involved in a variety of calcium-dependent processes, including muscle contraction, hor...
Gene Name
CACNA1H
Uniprot ID
O95180
Uniprot Name
Voltage-dependent T-type calcium channel subunit alpha-1H
Molecular Weight
259160.2 Da
References
  1. Brueggemann LI, Martin BL, Barakat J, Byron KL, Cribbs LL: Low voltage-activated calcium channels in vascular smooth muscle: T-type channels and AVP-stimulated calcium spiking. Am J Physiol Heart Circ Physiol. 2005 Feb;288(2):H923-35. Epub 2004 Oct 21. [PubMed:15498818]
  2. Coste B, Crest M, Delmas P: 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. 2007 Jan;129(1):57-77. [PubMed:17190903]
  3. Cribbs LL, Lee JH, Yang J, Satin J, Zhang Y, Daud A, Barclay J, Williamson MP, Fox M, Rees M, Perez-Reyes E: Cloning and characterization of alpha1H from human heart, a member of the T-type Ca2+ channel gene family. Circ Res. 1998 Jul 13;83(1):103-9. [PubMed:9670923]
  4. Lee TS, Kaku T, Takebayashi S, Uchino T, Miyamoto S, Hadama T, Perez-Reyes E, Ono K: Actions of mibefradil, efonidipine and nifedipine block of recombinant T- and L-type Ca channels with distinct inhibitory mechanisms. Pharmacology. 2006;78(1):11-20. Epub 2006 Aug 7. [PubMed:16899990]
  5. Perez-Reyes E: Paradoxical role of T-type calcium channels in coronary smooth muscle. Mol Interv. 2004 Feb;4(1):16-8. [PubMed:14993472]
  6. Massie BM: Mibefradil: a selective T-type calcium antagonist. Am J Cardiol. 1997 Nov 6;80(9A):23I-32I. [PubMed:9375939]
  7. Clozel JP, Ertel EA, Ertel SI: Discovery and main pharmacological properties of mibefradil (Ro 40-5967), the first selective T-type calcium channel blocker. J Hypertens Suppl. 1997 Dec;15(5):S17-25. [PubMed:9481612]
  8. McNulty MM, Hanck DA: State-dependent mibefradil block of Na+ channels. Mol Pharmacol. 2004 Dec;66(6):1652-61. [PubMed:15562257]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Inhibitor
General Function
Voltage-gated calcium channel activity
Specific Function
Voltage-sensitive calcium channels (VSCC) mediate the entry of calcium ions into excitable cells and are also involved in a variety of calcium-dependent processes, including muscle contraction, hor...
Gene Name
CACNA1C
Uniprot ID
Q13936
Uniprot Name
Voltage-dependent L-type calcium channel subunit alpha-1C
Molecular Weight
248974.1 Da
References
  1. Moosmang S, Haider N, Bruderl B, Welling A, Hofmann F: Antihypertensive effects of the putative T-type calcium channel antagonist mibefradil are mediated by the L-type calcium channel Cav1.2. Circ Res. 2006 Jan 6;98(1):105-10. Epub 2005 Nov 23. [PubMed:16306443]
  2. Lee TS, Kaku T, Takebayashi S, Uchino T, Miyamoto S, Hadama T, Perez-Reyes E, Ono K: Actions of mibefradil, efonidipine and nifedipine block of recombinant T- and L-type Ca channels with distinct inhibitory mechanisms. Pharmacology. 2006;78(1):11-20. Epub 2006 Aug 7. [PubMed:16899990]
  3. Mocanu MM, Gadgil S, Yellon DM, Baxter GF: Mibefradil, a T-type and L-type calcium channel blocker, limits infarct size through a glibenclamide-sensitive mechanism. Cardiovasc Drugs Ther. 1999 Apr;13(2):115-22. [PubMed:10372226]
  4. Jimenez C, Bourinet E, Leuranguer V, Richard S, Snutch TP, Nargeot J: Determinants of voltage-dependent inactivation affect Mibefradil block of calcium channels. Neuropharmacology. 2000;39(1):1-10. [PubMed:10665814]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Inhibitor
General Function
Voltage-gated calcium channel activity involved sa node cell action potential
Specific Function
Voltage-sensitive calcium channels (VSCC) mediate the entry of calcium ions into excitable cells and are also involved in a variety of calcium-dependent processes, including muscle contraction, hor...
Gene Name
CACNA1D
Uniprot ID
Q01668
Uniprot Name
Voltage-dependent L-type calcium channel subunit alpha-1D
Molecular Weight
245138.75 Da
References
  1. Mocanu MM, Gadgil S, Yellon DM, Baxter GF: Mibefradil, a T-type and L-type calcium channel blocker, limits infarct size through a glibenclamide-sensitive mechanism. Cardiovasc Drugs Ther. 1999 Apr;13(2):115-22. [PubMed:10372226]
  2. Jimenez C, Bourinet E, Leuranguer V, Richard S, Snutch TP, Nargeot J: Determinants of voltage-dependent inactivation affect Mibefradil block of calcium channels. Neuropharmacology. 2000;39(1):1-10. [PubMed:10665814]
  3. Lee TS, Kaku T, Takebayashi S, Uchino T, Miyamoto S, Hadama T, Perez-Reyes E, Ono K: Actions of mibefradil, efonidipine and nifedipine block of recombinant T- and L-type Ca channels with distinct inhibitory mechanisms. Pharmacology. 2006;78(1):11-20. Epub 2006 Aug 7. [PubMed:16899990]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Inhibitor
General Function
Voltage-gated calcium channel activity
Specific Function
Voltage-sensitive calcium channels (VSCC) mediate the entry of calcium ions into excitable cells and are also involved in a variety of calcium-dependent processes, including muscle contraction, hor...
Gene Name
CACNA1F
Uniprot ID
O60840
Uniprot Name
Voltage-dependent L-type calcium channel subunit alpha-1F
Molecular Weight
220675.9 Da
References
  1. Mocanu MM, Gadgil S, Yellon DM, Baxter GF: Mibefradil, a T-type and L-type calcium channel blocker, limits infarct size through a glibenclamide-sensitive mechanism. Cardiovasc Drugs Ther. 1999 Apr;13(2):115-22. [PubMed:10372226]
  2. Jimenez C, Bourinet E, Leuranguer V, Richard S, Snutch TP, Nargeot J: Determinants of voltage-dependent inactivation affect Mibefradil block of calcium channels. Neuropharmacology. 2000;39(1):1-10. [PubMed:10665814]
  3. Lee TS, Kaku T, Takebayashi S, Uchino T, Miyamoto S, Hadama T, Perez-Reyes E, Ono K: Actions of mibefradil, efonidipine and nifedipine block of recombinant T- and L-type Ca channels with distinct inhibitory mechanisms. Pharmacology. 2006;78(1):11-20. Epub 2006 Aug 7. [PubMed:16899990]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Inhibitor
General Function
Voltage-gated calcium channel activity
Specific Function
Voltage-sensitive calcium channels (VSCC) mediate the entry of calcium ions into excitable cells and are also involved in a variety of calcium-dependent processes, including muscle contraction, hor...
Gene Name
CACNA1I
Uniprot ID
Q9P0X4
Uniprot Name
Voltage-dependent T-type calcium channel subunit alpha-1I
Molecular Weight
245100.8 Da
References
  1. Massie BM: Mibefradil: a selective T-type calcium antagonist. Am J Cardiol. 1997 Nov 6;80(9A):23I-32I. [PubMed:9375939]
  2. Clozel JP, Ertel EA, Ertel SI: Discovery and main pharmacological properties of mibefradil (Ro 40-5967), the first selective T-type calcium channel blocker. J Hypertens Suppl. 1997 Dec;15(5):S17-25. [PubMed:9481612]
  3. McNulty MM, Hanck DA: State-dependent mibefradil block of Na+ channels. Mol Pharmacol. 2004 Dec;66(6):1652-61. [PubMed:15562257]
  4. Lee TS, Kaku T, Takebayashi S, Uchino T, Miyamoto S, Hadama T, Perez-Reyes E, Ono K: Actions of mibefradil, efonidipine and nifedipine block of recombinant T- and L-type Ca channels with distinct inhibitory mechanisms. Pharmacology. 2006;78(1):11-20. Epub 2006 Aug 7. [PubMed:16899990]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Inhibitor
General Function
Voltage-gated calcium channel activity
Specific Function
Voltage-sensitive calcium channels (VSCC) mediate the entry of calcium ions into excitable cells and are also involved in a variety of calcium-dependent processes, including muscle contraction, hor...
Gene Name
CACNA1S
Uniprot ID
Q13698
Uniprot Name
Voltage-dependent L-type calcium channel subunit alpha-1S
Molecular Weight
212348.1 Da
References
  1. Mocanu MM, Gadgil S, Yellon DM, Baxter GF: Mibefradil, a T-type and L-type calcium channel blocker, limits infarct size through a glibenclamide-sensitive mechanism. Cardiovasc Drugs Ther. 1999 Apr;13(2):115-22. [PubMed:10372226]
  2. Jimenez C, Bourinet E, Leuranguer V, Richard S, Snutch TP, Nargeot J: Determinants of voltage-dependent inactivation affect Mibefradil block of calcium channels. Neuropharmacology. 2000;39(1):1-10. [PubMed:10665814]
  3. Lee TS, Kaku T, Takebayashi S, Uchino T, Miyamoto S, Hadama T, Perez-Reyes E, Ono K: Actions of mibefradil, efonidipine and nifedipine block of recombinant T- and L-type Ca channels with distinct inhibitory mechanisms. Pharmacology. 2006;78(1):11-20. Epub 2006 Aug 7. [PubMed:16899990]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Inhibitor
General Function
Voltage-gated calcium channel activity
Specific Function
The beta subunit of voltage-dependent calcium channels contributes to the function of the calcium channel by increasing peak calcium current, shifting the voltage dependencies of activation and ina...
Gene Name
CACNB1
Uniprot ID
Q02641
Uniprot Name
Voltage-dependent L-type calcium channel subunit beta-1
Molecular Weight
65712.995 Da
References
  1. Lee TS, Kaku T, Takebayashi S, Uchino T, Miyamoto S, Hadama T, Perez-Reyes E, Ono K: Actions of mibefradil, efonidipine and nifedipine block of recombinant T- and L-type Ca channels with distinct inhibitory mechanisms. Pharmacology. 2006;78(1):11-20. Epub 2006 Aug 7. [PubMed:16899990]
  2. Mocanu MM, Gadgil S, Yellon DM, Baxter GF: Mibefradil, a T-type and L-type calcium channel blocker, limits infarct size through a glibenclamide-sensitive mechanism. Cardiovasc Drugs Ther. 1999 Apr;13(2):115-22. [PubMed:10372226]
  3. Jimenez C, Bourinet E, Leuranguer V, Richard S, Snutch TP, Nargeot J: Determinants of voltage-dependent inactivation affect Mibefradil block of calcium channels. Neuropharmacology. 2000;39(1):1-10. [PubMed:10665814]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Inhibitor
General Function
Voltage-gated calcium channel activity
Specific Function
The beta subunit of voltage-dependent calcium channels contributes to the function of the calcium channel by increasing peak calcium current, shifting the voltage dependencies of activation and ina...
Gene Name
CACNB2
Uniprot ID
Q08289
Uniprot Name
Voltage-dependent L-type calcium channel subunit beta-2
Molecular Weight
73579.925 Da
References
  1. Lee TS, Kaku T, Takebayashi S, Uchino T, Miyamoto S, Hadama T, Perez-Reyes E, Ono K: Actions of mibefradil, efonidipine and nifedipine block of recombinant T- and L-type Ca channels with distinct inhibitory mechanisms. Pharmacology. 2006;78(1):11-20. Epub 2006 Aug 7. [PubMed:16899990]
  2. Mocanu MM, Gadgil S, Yellon DM, Baxter GF: Mibefradil, a T-type and L-type calcium channel blocker, limits infarct size through a glibenclamide-sensitive mechanism. Cardiovasc Drugs Ther. 1999 Apr;13(2):115-22. [PubMed:10372226]
  3. Jimenez C, Bourinet E, Leuranguer V, Richard S, Snutch TP, Nargeot J: Determinants of voltage-dependent inactivation affect Mibefradil block of calcium channels. Neuropharmacology. 2000;39(1):1-10. [PubMed:10665814]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Inhibitor
General Function
Voltage-gated calcium channel activity
Specific Function
The beta subunit of voltage-dependent calcium channels contributes to the function of the calcium channel by increasing peak calcium current, shifting the voltage dependencies of activation and ina...
Gene Name
CACNB3
Uniprot ID
P54284
Uniprot Name
Voltage-dependent L-type calcium channel subunit beta-3
Molecular Weight
54531.425 Da
References
  1. Lee TS, Kaku T, Takebayashi S, Uchino T, Miyamoto S, Hadama T, Perez-Reyes E, Ono K: Actions of mibefradil, efonidipine and nifedipine block of recombinant T- and L-type Ca channels with distinct inhibitory mechanisms. Pharmacology. 2006;78(1):11-20. Epub 2006 Aug 7. [PubMed:16899990]
  2. Mocanu MM, Gadgil S, Yellon DM, Baxter GF: Mibefradil, a T-type and L-type calcium channel blocker, limits infarct size through a glibenclamide-sensitive mechanism. Cardiovasc Drugs Ther. 1999 Apr;13(2):115-22. [PubMed:10372226]
  3. Jimenez C, Bourinet E, Leuranguer V, Richard S, Snutch TP, Nargeot J: Determinants of voltage-dependent inactivation affect Mibefradil block of calcium channels. Neuropharmacology. 2000;39(1):1-10. [PubMed:10665814]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Inhibitor
General Function
Voltage-gated calcium channel activity
Specific Function
The beta subunit of voltage-dependent calcium channels contributes to the function of the calcium channel by increasing peak calcium current, shifting the voltage dependencies of activation and ina...
Gene Name
CACNB4
Uniprot ID
O00305
Uniprot Name
Voltage-dependent L-type calcium channel subunit beta-4
Molecular Weight
58168.625 Da
References
  1. Lee TS, Kaku T, Takebayashi S, Uchino T, Miyamoto S, Hadama T, Perez-Reyes E, Ono K: Actions of mibefradil, efonidipine and nifedipine block of recombinant T- and L-type Ca channels with distinct inhibitory mechanisms. Pharmacology. 2006;78(1):11-20. Epub 2006 Aug 7. [PubMed:16899990]
  2. Mocanu MM, Gadgil S, Yellon DM, Baxter GF: Mibefradil, a T-type and L-type calcium channel blocker, limits infarct size through a glibenclamide-sensitive mechanism. Cardiovasc Drugs Ther. 1999 Apr;13(2):115-22. [PubMed:10372226]
  3. Jimenez C, Bourinet E, Leuranguer V, Richard S, Snutch TP, Nargeot J: Determinants of voltage-dependent inactivation affect Mibefradil block of calcium channels. Neuropharmacology. 2000;39(1):1-10. [PubMed:10665814]

Enzymes

Details
1. Cytochrome P450 3A4
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
General Function
Vitamin d3 25-hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
Molecular Weight
57342.67 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
  2. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP1A2
Uniprot ID
P05177
Uniprot Name
Cytochrome P450 1A2
Molecular Weight
58293.76 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
  2. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Details
3. Cytochrome P450 2D6
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Steroid hydroxylase activity
Specific Function
Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic...
Gene Name
CYP2D6
Uniprot ID
P10635
Uniprot Name
Cytochrome P450 2D6
Molecular Weight
55768.94 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
  2. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Oxygen binding
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP3A5
Uniprot ID
P20815
Uniprot Name
Cytochrome P450 3A5
Molecular Weight
57108.065 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
  2. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Oxygen binding
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP3A7
Uniprot ID
P24462
Uniprot Name
Cytochrome P450 3A7
Molecular Weight
57525.03 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
  2. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Steroid 11-beta-monooxygenase activity
Specific Function
Has steroid 11-beta-hydroxylase activity. In addition to this activity, the 18 or 19-hydroxylation of steroids and the aromatization of androstendione to estrone have also been ascribed to cytochro...
Gene Name
CYP11B1
Uniprot ID
P15538
Uniprot Name
Cytochrome P450 11B1, mitochondrial
Molecular Weight
57572.44 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Steroid 11-beta-monooxygenase activity
Specific Function
Preferentially catalyzes the conversion of 11-deoxycorticosterone to aldosterone via corticosterone and 18-hydroxycorticosterone.
Gene Name
CYP11B2
Uniprot ID
P19099
Uniprot Name
Cytochrome P450 11B2, mitochondrial
Molecular Weight
57559.62 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Vitamin d 24-hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP1A1
Uniprot ID
P04798
Uniprot Name
Cytochrome P450 1A1
Molecular Weight
58164.815 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]

Transporters

Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Xenobiotic-transporting atpase activity
Specific Function
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name
ABCB1
Uniprot ID
P08183
Uniprot Name
Multidrug resistance protein 1
Molecular Weight
141477.255 Da
References
  1. Wandel C, Kim RB, Guengerich FP, Wood AJ: Mibefradil is a P-glycoprotein substrate and a potent inhibitor of both P-glycoprotein and CYP3A in vitro. Drug Metab Dispos. 2000 Aug;28(8):895-8. [PubMed:10901697]
  2. Ekins S, Kim RB, Leake BF, Dantzig AH, Schuetz EG, Lan LB, Yasuda K, Shepard RL, Winter MA, Schuetz JD, Wikel JH, Wrighton SA: Three-dimensional quantitative structure-activity relationships of inhibitors of P-glycoprotein. Mol Pharmacol. 2002 May;61(5):964-73. [PubMed:11961113]
  3. Schwab D, Fischer H, Tabatabaei A, Poli S, Huwyler J: Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery. J Med Chem. 2003 Apr 24;46(9):1716-25. [PubMed:12699389]
  4. Nagy H, Goda K, Fenyvesi F, Bacso Z, Szilasi M, Kappelmayer J, Lustyik G, Cianfriglia M, Szabo G Jr: Distinct groups of multidrug resistance modulating agents are distinguished by competition of P-glycoprotein-specific antibodies. Biochem Biophys Res Commun. 2004 Mar 19;315(4):942-9. [PubMed:14985103]

Drug created on July 06, 2007 14:41 / Updated on November 09, 2017 02:59