You are using an unsupported browser. Please upgrade your browser to a newer version to get the best experience on DrugBank.
Identification
NamePhenoxybenzamine
Accession NumberDB00925  (APRD00651)
TypeSmall Molecule
GroupsApproved
DescriptionAn alpha-adrenergic antagonist with long duration of action. It has been used to treat hypertension and as a peripheral vasodilator. [PubChem]
Structure
Thumb
Synonyms
Dibenzyline
Fenossibenzamina
Fenoxibenzamina
Phenoxybenzamine
Phenoxybenzaminum
POB
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
DibenzylineCapsule10 mg/1OralWell Spring Pharmaceutical Corporation1999-10-01Not applicableUs
DibenzylineCapsule10 mg/1OralConcordia Pharmaceuticals Inc.1953-01-26Not applicableUs
Phenoxybenzamine HydrochlorideCapsule10 mg/1OralPrasco Laboratories2015-08-11Not applicableUs
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Phenoxybenzamine HydrochlorideCapsule10 mg/1OralWest Ward Pharmaceuticals Corp.2015-08-10Not applicableUs
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Phenoxybenzamine Hydrochloride
63-92-3
Thumb
  • InChI Key: VBCPVIWPDJVHAN-UHFFFAOYNA-N
  • Monoisotopic Mass: 339.115669777
  • Average Mass: 340.287
DBSALT000480
Categories
UNII0TTZ664R7Z
CAS number59-96-1
WeightAverage: 303.826
Monoisotopic: 303.138992038
Chemical FormulaC18H22ClNO
InChI KeyQZVCTJOXCFMACW-UHFFFAOYSA-N
InChI
InChI=1S/C18H22ClNO/c1-16(15-21-18-10-6-3-7-11-18)20(13-12-19)14-17-8-4-2-5-9-17/h2-11,16H,12-15H2,1H3
IUPAC Name
benzyl(2-chloroethyl)(1-phenoxypropan-2-yl)amine
SMILES
CC(COC1=CC=CC=C1)N(CCCl)CC1=CC=CC=C1
Pharmacology
IndicationFor the treatment of phaeochromocytoma (malignant), benign prostatic hypertrophy and malignant essential hypertension.
Structured Indications
PharmacodynamicsPhenoxybenzamine is indicated for the control of episodes of hypertension and sweating that occur with a disease called pheochromocytoma. If tachycardia is excessive, it may be necessary to use a beta-blocking agent concomitantly. Phenoxybenzamine is a long-acting, adrenergic, alpha-receptor blocking agent which can produce and maintain "chemical sympathectomy" by oral administration. It increases blood flow to the skin, mucosa and abdominal viscera, and lowers both supine and erect blood pressures. It has no effect on the parasympathetic system. Phenoxybenzamine works by blocking alpha receptors in certain parts of the body. Alpha receptors are present in the muscle that lines the walls of blood vessels. When the receptors are blocked by Phenoxybenzamine, the muscle relaxes and the blood vessels widen. This widening of the blood vessels results in a lowering of blood pressure.
Mechanism of actionPhenoxybenzamine produces its therapeutic actions by blocking alpha receptors, leading to a muscle relaxation and a widening of the blood vessels. This widening of the blood vessels results in a lowering of blood pressure.
TargetKindPharmacological actionActionsOrganismUniProt ID
Alpha-1A adrenergic receptorProteinyes
antagonist
HumanP35348 details
Alpha-2A adrenergic receptorProteinyes
antagonist
HumanP08913 details
Alpha-2C adrenergic receptorProteinunknown
antagonist
HumanP18825 details
Alpha-2B adrenergic receptorProteinunknown
antagonist
HumanP18089 details
CalmodulinProteinunknown
inhibitor
HumanP62158 details
Beta-2 adrenergic receptorProteinunknownNot AvailableHumanP07550 details
Alpha-1B adrenergic receptorProteinunknown
antagonist
HumanP35368 details
Alpha-1D adrenergic receptorProteinunknown
antagonist
HumanP25100 details
Related Articles
AbsorptionTwenty to 30 percent of orally administered phenoxybenzamine appears to be absorbed in the active form.
Volume of distributionNot Available
Protein bindingNot Available
MetabolismNot Available
Route of eliminationNot Available
Half life24 hours
ClearanceNot Available
ToxicitySymptoms of overdose are largely the result of block of the sympathetic nervous system and of the circulating epinephrine. They may include postural hypotension resulting in dizziness or fainting, tachycardia, particularly postural, vomiting; lethargy, and shock.
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
Interactions
Drug Interactions
DrugInteractionDrug group
7,8-DICHLORO-1,2,3,4-TETRAHYDROISOQUINOLINE7,8-DICHLORO-1,2,3,4-TETRAHYDROISOQUINOLINE may increase the hypotensive activities of Phenoxybenzamine.Experimental
AcebutololPhenoxybenzamine may increase the hypotensive activities of Acebutolol.Approved
AcetazolamideThe risk or severity of adverse effects can be increased when Phenoxybenzamine is combined with Acetazolamide.Approved, Vet Approved
AldesleukinThe risk or severity of adverse effects can be increased when Aldesleukin is combined with Phenoxybenzamine.Approved
AlfuzosinAlfuzosin may increase the hypotensive activities of Phenoxybenzamine.Approved, Investigational
AliskirenPhenoxybenzamine may increase the hypotensive activities of Aliskiren.Approved, Investigational
AlprenololAlprenolol may increase the hypotensive activities of Phenoxybenzamine.Approved, Withdrawn
AmbrisentanPhenoxybenzamine may increase the hypotensive activities of Ambrisentan.Approved, Investigational
AmifostinePhenoxybenzamine may increase the hypotensive activities of Amifostine.Approved, Investigational
AmilorideThe risk or severity of adverse effects can be increased when Amiloride is combined with Phenoxybenzamine.Approved
AmiodaroneThe metabolism of Phenoxybenzamine can be decreased when combined with Amiodarone.Approved, Investigational
AmlodipineAmlodipine may increase the hypotensive activities of Phenoxybenzamine.Approved
AmobarbitalAmobarbital may increase the hypotensive activities of Phenoxybenzamine.Approved, Illicit
Amphotericin BThe risk or severity of adverse effects can be increased when Amphotericin B is combined with Phenoxybenzamine.Approved, Investigational
Amyl NitriteThe risk or severity of adverse effects can be increased when Amyl Nitrite is combined with Phenoxybenzamine.Approved
ApomorphineThe risk or severity of adverse effects can be increased when Apomorphine is combined with Phenoxybenzamine.Approved, Investigational
ApraclonidineThe risk or severity of adverse effects can be increased when Apraclonidine is combined with Phenoxybenzamine.Approved
AprepitantThe serum concentration of Phenoxybenzamine can be increased when it is combined with Aprepitant.Approved, Investigational
AripiprazoleAripiprazole may increase the hypotensive activities of Phenoxybenzamine.Approved, Investigational
ArotinololThe risk or severity of adverse effects can be increased when Arotinolol is combined with Phenoxybenzamine.Approved
Arsenic trioxideThe risk or severity of adverse effects can be increased when Arsenic trioxide is combined with Phenoxybenzamine.Approved, Investigational
AtazanavirThe metabolism of Phenoxybenzamine can be decreased when combined with Atazanavir.Approved, Investigational
AtenololAtenolol may increase the hypotensive activities of Phenoxybenzamine.Approved
AtomoxetineThe metabolism of Phenoxybenzamine can be decreased when combined with Atomoxetine.Approved
Azilsartan medoxomilThe risk or severity of adverse effects can be increased when Azilsartan medoxomil is combined with Phenoxybenzamine.Approved
BarbexacloneBarbexaclone may increase the hypotensive activities of Phenoxybenzamine.Experimental
BarbitalBarbital may increase the hypotensive activities of Phenoxybenzamine.Illicit
BarnidipineThe risk or severity of adverse effects can be increased when Barnidipine is combined with Phenoxybenzamine.Approved
BenazeprilBenazepril may increase the hypotensive activities of Phenoxybenzamine.Approved, Investigational
BendroflumethiazideBendroflumethiazide may increase the hypotensive activities of Phenoxybenzamine.Approved
BenmoxinBenmoxin may increase the hypotensive activities of Phenoxybenzamine.Withdrawn
BepridilPhenoxybenzamine may increase the hypotensive activities of Bepridil.Approved, Withdrawn
BetaxololBetaxolol may increase the hypotensive activities of Phenoxybenzamine.Approved
BethanidineBethanidine may increase the hypotensive activities of Phenoxybenzamine.Approved
BexaroteneThe serum concentration of Phenoxybenzamine can be decreased when it is combined with Bexarotene.Approved, Investigational
BimatoprostBimatoprost may increase the hypotensive activities of Phenoxybenzamine.Approved, Investigational
BisoprololBisoprolol may increase the hypotensive activities of Phenoxybenzamine.Approved
BoceprevirThe metabolism of Phenoxybenzamine can be decreased when combined with Boceprevir.Approved
BortezomibThe metabolism of Phenoxybenzamine can be decreased when combined with Bortezomib.Approved, Investigational
BosentanThe serum concentration of Phenoxybenzamine can be decreased when it is combined with Bosentan.Approved, Investigational
BretyliumPhenoxybenzamine may increase the hypotensive activities of Bretylium.Approved
BrimonidineBrimonidine may increase the hypotensive activities of Phenoxybenzamine.Approved
BrimonidineBrimonidine may increase the antihypertensive activities of Phenoxybenzamine.Approved
BromocriptineThe risk or severity of adverse effects can be increased when Bromocriptine is combined with Phenoxybenzamine.Approved, Investigational
BumetanideThe risk or severity of adverse effects can be increased when Bumetanide is combined with Phenoxybenzamine.Approved
BupivacaineThe risk or severity of adverse effects can be increased when Bupivacaine is combined with Phenoxybenzamine.Approved, Investigational
BupranololPhenoxybenzamine may increase the hypotensive activities of Bupranolol.Approved
CanagliflozinThe risk or severity of adverse effects can be increased when Canagliflozin is combined with Phenoxybenzamine.Approved
CandesartanCandesartan may increase the hypotensive activities of Phenoxybenzamine.Approved
CandoxatrilCandoxatril may increase the hypotensive activities of Phenoxybenzamine.Experimental
CaptoprilPhenoxybenzamine may increase the hypotensive activities of Captopril.Approved
CarbamazepineThe metabolism of Phenoxybenzamine can be increased when combined with Carbamazepine.Approved, Investigational
CarbetocinThe risk or severity of adverse effects can be increased when Carbetocin is combined with Phenoxybenzamine.Approved
CaroxazoneCaroxazone may increase the hypotensive activities of Phenoxybenzamine.Withdrawn
CarteololCarteolol may increase the hypotensive activities of Phenoxybenzamine.Approved
CarvedilolPhenoxybenzamine may increase the hypotensive activities of Carvedilol.Approved, Investigational
CeliprololPhenoxybenzamine may increase the hypotensive activities of Celiprolol.Approved, Investigational
CeritinibThe serum concentration of Phenoxybenzamine can be increased when it is combined with Ceritinib.Approved
ChlorothiazideChlorothiazide may increase the hypotensive activities of Phenoxybenzamine.Approved, Vet Approved
ChlorpromazineThe risk or severity of adverse effects can be increased when Chlorpromazine is combined with Phenoxybenzamine.Approved, Vet Approved
ChlorthalidoneChlorthalidone may increase the hypotensive activities of Phenoxybenzamine.Approved
CilazaprilPhenoxybenzamine may increase the hypotensive activities of Cilazapril.Approved
CilnidipineThe risk or severity of adverse effects can be increased when Cilnidipine is combined with Phenoxybenzamine.Approved
ClarithromycinThe metabolism of Phenoxybenzamine can be decreased when combined with Clarithromycin.Approved
ClemastineThe metabolism of Phenoxybenzamine can be decreased when combined with Clemastine.Approved
ClevidipineThe risk or severity of adverse effects can be increased when Clevidipine is combined with Phenoxybenzamine.Approved
ClofarabineThe risk or severity of adverse effects can be increased when Clofarabine is combined with Phenoxybenzamine.Approved, Investigational
ClomipramineThe risk or severity of adverse effects can be increased when Clomipramine is combined with Phenoxybenzamine.Approved, Vet Approved
ClonidineClonidine may increase the hypotensive activities of Phenoxybenzamine.Approved
ClotrimazoleThe metabolism of Phenoxybenzamine can be decreased when combined with Clotrimazole.Approved, Vet Approved
ClozapineThe risk or severity of adverse effects can be increased when Clozapine is combined with Phenoxybenzamine.Approved
CobicistatThe metabolism of Phenoxybenzamine can be decreased when combined with Cobicistat.Approved
ConivaptanThe serum concentration of Phenoxybenzamine can be increased when it is combined with Conivaptan.Approved, Investigational
CrizotinibThe metabolism of Phenoxybenzamine can be decreased when combined with Crizotinib.Approved
CryptenamineCryptenamine may increase the hypotensive activities of Phenoxybenzamine.Approved
CyclosporineThe metabolism of Phenoxybenzamine can be decreased when combined with Cyclosporine.Approved, Investigational, Vet Approved
CyclothiazideCyclothiazide may increase the hypotensive activities of Phenoxybenzamine.Approved
DabrafenibThe serum concentration of Phenoxybenzamine can be decreased when it is combined with Dabrafenib.Approved
DapagliflozinThe risk or severity of adverse effects can be increased when Dapagliflozin is combined with Phenoxybenzamine.Approved
DarunavirThe metabolism of Phenoxybenzamine can be decreased when combined with Darunavir.Approved
DasatinibThe serum concentration of Phenoxybenzamine can be increased when it is combined with Dasatinib.Approved, Investigational
DebrisoquinPhenoxybenzamine may increase the hypotensive activities of Debrisoquin.Approved
DeferasiroxThe serum concentration of Phenoxybenzamine can be decreased when it is combined with Deferasirox.Approved, Investigational
DelavirdineThe metabolism of Phenoxybenzamine can be decreased when combined with Delavirdine.Approved
DeserpidinePhenoxybenzamine may increase the hypotensive activities of Deserpidine.Approved
DesfluraneThe risk or severity of adverse effects can be increased when Desflurane is combined with Phenoxybenzamine.Approved
DexamethasoneThe serum concentration of Phenoxybenzamine can be decreased when it is combined with Dexamethasone.Approved, Investigational, Vet Approved
DexmedetomidineThe risk or severity of adverse effects can be increased when Dexmedetomidine is combined with Phenoxybenzamine.Approved, Vet Approved
DiazoxideDiazoxide may increase the hypotensive activities of Phenoxybenzamine.Approved
DiclofenamideThe risk or severity of adverse effects can be increased when Diclofenamide is combined with Phenoxybenzamine.Approved
DihydralazinePhenoxybenzamine may increase the hypotensive activities of Dihydralazine.Investigational
DihydroergotamineThe metabolism of Phenoxybenzamine can be decreased when combined with Dihydroergotamine.Approved
DiltiazemThe metabolism of Phenoxybenzamine can be decreased when combined with Diltiazem.Approved
DinutuximabThe risk or severity of adverse effects can be increased when Dinutuximab is combined with Phenoxybenzamine.Approved
DipyridamoleThe risk or severity of adverse effects can be increased when Dipyridamole is combined with Phenoxybenzamine.Approved
DorzolamideDorzolamide may increase the hypotensive activities of Phenoxybenzamine.Approved
DoxazosinDoxazosin may increase the hypotensive activities of Phenoxybenzamine.Approved
DoxycyclineThe metabolism of Phenoxybenzamine can be decreased when combined with Doxycycline.Approved, Investigational, Vet Approved
DronedaroneThe metabolism of Phenoxybenzamine can be decreased when combined with Dronedarone.Approved
DuloxetinePhenoxybenzamine may increase the orthostatic hypotensive activities of Duloxetine.Approved
EfavirenzThe serum concentration of Phenoxybenzamine can be decreased when it is combined with Efavirenz.Approved, Investigational
EfonidipinePhenoxybenzamine may increase the hypotensive activities of Efonidipine.Approved
EmpagliflozinThe risk or severity of adverse effects can be increased when Empagliflozin is combined with Phenoxybenzamine.Approved
EnalaprilEnalapril may increase the hypotensive activities of Phenoxybenzamine.Approved, Vet Approved
EnalaprilatPhenoxybenzamine may increase the hypotensive activities of Enalaprilat.Approved
EnzalutamideThe serum concentration of Phenoxybenzamine can be decreased when it is combined with Enzalutamide.Approved
EplerenoneThe risk or severity of adverse effects can be increased when Eplerenone is combined with Phenoxybenzamine.Approved
EpoprostenolPhenoxybenzamine may increase the hypotensive activities of Epoprostenol.Approved
EprosartanEprosartan may increase the hypotensive activities of Phenoxybenzamine.Approved
ErythromycinThe metabolism of Phenoxybenzamine can be decreased when combined with Erythromycin.Approved, Vet Approved
Eslicarbazepine acetateThe serum concentration of Phenoxybenzamine can be decreased when it is combined with Eslicarbazepine acetate.Approved
EsmololThe risk or severity of adverse effects can be increased when Esmolol is combined with Phenoxybenzamine.Approved
Etacrynic acidThe risk or severity of adverse effects can be increased when Etacrynic acid is combined with Phenoxybenzamine.Approved
EtravirineThe serum concentration of Phenoxybenzamine can be decreased when it is combined with Etravirine.Approved
FelodipinePhenoxybenzamine may increase the hypotensive activities of Felodipine.Approved, Investigational
FenoldopamFenoldopam may increase the hypotensive activities of Phenoxybenzamine.Approved
FimasartanThe risk or severity of adverse effects can be increased when Fimasartan is combined with Phenoxybenzamine.Approved
FluconazoleThe metabolism of Phenoxybenzamine can be decreased when combined with Fluconazole.Approved
FluvoxamineThe metabolism of Phenoxybenzamine can be decreased when combined with Fluvoxamine.Approved, Investigational
FosamprenavirThe metabolism of Phenoxybenzamine can be decreased when combined with Fosamprenavir.Approved
FosaprepitantThe serum concentration of Phenoxybenzamine can be increased when it is combined with Fosaprepitant.Approved
FosinoprilFosinopril may increase the hypotensive activities of Phenoxybenzamine.Approved
FosphenytoinThe metabolism of Phenoxybenzamine can be increased when combined with Fosphenytoin.Approved
FurazolidoneFurazolidone may increase the hypotensive activities of Phenoxybenzamine.Approved, Vet Approved
FurosemideThe risk or severity of adverse effects can be increased when Furosemide is combined with Phenoxybenzamine.Approved, Vet Approved
Fusidic AcidThe serum concentration of Phenoxybenzamine can be increased when it is combined with Fusidic Acid.Approved
GuanabenzGuanabenz may increase the hypotensive activities of Phenoxybenzamine.Approved
GuanadrelGuanadrel may increase the hypotensive activities of Phenoxybenzamine.Approved
GuanethidinePhenoxybenzamine may increase the hypotensive activities of Guanethidine.Approved
GuanfacinePhenoxybenzamine may increase the hypotensive activities of Guanfacine.Approved, Investigational
HalothaneThe risk or severity of adverse effects can be increased when Halothane is combined with Phenoxybenzamine.Approved, Vet Approved
HexamethoniumPhenoxybenzamine may increase the hypotensive activities of Hexamethonium.Experimental
HexobarbitalHexobarbital may increase the hypotensive activities of Phenoxybenzamine.Approved
HydracarbazineHydracarbazine may increase the hypotensive activities of Phenoxybenzamine.Approved
HydralazinePhenoxybenzamine may increase the hypotensive activities of Hydralazine.Approved
HydrochlorothiazidePhenoxybenzamine may increase the hypotensive activities of Hydrochlorothiazide.Approved, Vet Approved
HydroflumethiazideHydroflumethiazide may increase the hypotensive activities of Phenoxybenzamine.Approved
IdelalisibThe serum concentration of Phenoxybenzamine can be increased when it is combined with Idelalisib.Approved
IloprostIloprost may increase the hypotensive activities of Phenoxybenzamine.Approved, Investigational
ImatinibThe metabolism of Phenoxybenzamine can be decreased when combined with Imatinib.Approved
ImidaprilThe risk or severity of adverse effects can be increased when Imidapril is combined with Phenoxybenzamine.Investigational
ImipramineThe risk or severity of adverse effects can be increased when Imipramine is combined with Phenoxybenzamine.Approved
IndapamideIndapamide may increase the hypotensive activities of Phenoxybenzamine.Approved
IndenololPhenoxybenzamine may increase the hypotensive activities of Indenolol.Withdrawn
IndinavirThe metabolism of Phenoxybenzamine can be decreased when combined with Indinavir.Approved
IndoraminPhenoxybenzamine may increase the hypotensive activities of Indoramin.Withdrawn
IproclozideIproclozide may increase the hypotensive activities of Phenoxybenzamine.Withdrawn
IproniazidIproniazid may increase the hypotensive activities of Phenoxybenzamine.Withdrawn
IrbesartanPhenoxybenzamine may increase the hypotensive activities of Irbesartan.Approved, Investigational
IsavuconazoniumThe metabolism of Phenoxybenzamine can be decreased when combined with Isavuconazonium.Approved, Investigational
IsocarboxazidIsocarboxazid may increase the hypotensive activities of Phenoxybenzamine.Approved
IsofluraneThe risk or severity of adverse effects can be increased when Isoflurane is combined with Phenoxybenzamine.Approved, Vet Approved
Isosorbide DinitrateThe risk or severity of adverse effects can be increased when Isosorbide Dinitrate is combined with Phenoxybenzamine.Approved
Isosorbide MononitrateThe risk or severity of adverse effects can be increased when Isosorbide Mononitrate is combined with Phenoxybenzamine.Approved
IsoxsuprineThe risk or severity of adverse effects can be increased when Isoxsuprine is combined with Phenoxybenzamine.Approved, Withdrawn
IsradipineThe metabolism of Phenoxybenzamine can be decreased when combined with Isradipine.Approved
ItraconazoleThe metabolism of Phenoxybenzamine can be decreased when combined with Itraconazole.Approved, Investigational
IvacaftorThe serum concentration of Phenoxybenzamine can be increased when it is combined with Ivacaftor.Approved
KetanserinPhenoxybenzamine may increase the hypotensive activities of Ketanserin.Investigational
KetoconazoleThe metabolism of Phenoxybenzamine can be decreased when combined with Ketoconazole.Approved, Investigational
LabetalolLabetalol may increase the hypotensive activities of Phenoxybenzamine.Approved
LacidipinePhenoxybenzamine may increase the hypotensive activities of Lacidipine.Approved
LatanoprostLatanoprost may increase the hypotensive activities of Phenoxybenzamine.Approved, Investigational
LercanidipineLercanidipine may increase the hypotensive activities of Phenoxybenzamine.Approved, Investigational
LevobunololThe risk or severity of adverse effects can be increased when Levobunolol is combined with Phenoxybenzamine.Approved
LevobupivacaineThe risk or severity of adverse effects can be increased when Levobupivacaine is combined with Phenoxybenzamine.Approved
LevodopaPhenoxybenzamine may increase the orthostatic hypotensive activities of Levodopa.Approved
LevosimendanThe risk or severity of adverse effects can be increased when Levosimendan is combined with Phenoxybenzamine.Approved, Investigational
LisinoprilLisinopril may increase the hypotensive activities of Phenoxybenzamine.Approved, Investigational
LofexidinePhenoxybenzamine may increase the hypotensive activities of Lofexidine.Approved, Investigational
LopinavirThe metabolism of Phenoxybenzamine can be decreased when combined with Lopinavir.Approved
LosartanLosartan may increase the hypotensive activities of Phenoxybenzamine.Approved
LovastatinThe metabolism of Phenoxybenzamine can be decreased when combined with Lovastatin.Approved, Investigational
LuliconazoleThe serum concentration of Phenoxybenzamine can be increased when it is combined with Luliconazole.Approved
LumacaftorThe metabolism of Phenoxybenzamine can be increased when combined with Lumacaftor.Approved
MacitentanPhenoxybenzamine may increase the hypotensive activities of Macitentan.Approved
ManidipinePhenoxybenzamine may increase the hypotensive activities of Manidipine.Approved
MannitolThe risk or severity of adverse effects can be increased when Mannitol is combined with Phenoxybenzamine.Approved, Investigational
MebanazineMebanazine may increase the hypotensive activities of Phenoxybenzamine.Withdrawn
MecamylamineMecamylamine may increase the hypotensive activities of Phenoxybenzamine.Approved
MethazolamideThe risk or severity of adverse effects can be increased when Methazolamide is combined with Phenoxybenzamine.Approved
MethohexitalMethohexital may increase the hypotensive activities of Phenoxybenzamine.Approved
MethyclothiazideThe risk or severity of adverse effects can be increased when Methyclothiazide is combined with Phenoxybenzamine.Approved
MethyldopaPhenoxybenzamine may increase the hypotensive activities of Methyldopa.Approved
Methylene blueMethylene blue may increase the hypotensive activities of Phenoxybenzamine.Investigational
MethylphenidateMethylphenidate may decrease the antihypertensive activities of Phenoxybenzamine.Approved, Investigational
MethylphenobarbitalMethylphenobarbital may increase the hypotensive activities of Phenoxybenzamine.Approved
MetipranololPhenoxybenzamine may increase the hypotensive activities of Metipranolol.Approved
MetolazoneMetolazone may increase the hypotensive activities of Phenoxybenzamine.Approved
MetoprololMetoprolol may increase the hypotensive activities of Phenoxybenzamine.Approved, Investigational
MetyrosinePhenoxybenzamine may increase the hypotensive activities of Metyrosine.Approved
MibefradilPhenoxybenzamine may increase the hypotensive activities of Mibefradil.Withdrawn
MifepristoneThe serum concentration of Phenoxybenzamine can be increased when it is combined with Mifepristone.Approved, Investigational
MinaprineMinaprine may increase the hypotensive activities of Phenoxybenzamine.Approved
MinoxidilMinoxidil may increase the hypotensive activities of Phenoxybenzamine.Approved
MitotaneThe serum concentration of Phenoxybenzamine can be decreased when it is combined with Mitotane.Approved
MoclobemideMoclobemide may increase the hypotensive activities of Phenoxybenzamine.Approved
ModafinilThe serum concentration of Phenoxybenzamine can be decreased when it is combined with Modafinil.Approved, Investigational
MoexiprilMoexipril may increase the hypotensive activities of Phenoxybenzamine.Approved
MolsidomineMolsidomine may increase the hypotensive activities of Phenoxybenzamine.Approved
MorphineThe risk or severity of adverse effects can be increased when Morphine is combined with Phenoxybenzamine.Approved, Investigational
MoxonidinePhenoxybenzamine may increase the hypotensive activities of Moxonidine.Approved
NabiloneThe risk or severity of adverse effects can be increased when Nabilone is combined with Phenoxybenzamine.Approved, Investigational
NadololPhenoxybenzamine may increase the hypotensive activities of Nadolol.Approved
NafcillinThe serum concentration of Phenoxybenzamine can be decreased when it is combined with Nafcillin.Approved
NaftopidilPhenoxybenzamine may increase the hypotensive activities of Naftopidil.Investigational
NebivololPhenoxybenzamine may increase the hypotensive activities of Nebivolol.Approved, Investigational
NefazodoneThe metabolism of Phenoxybenzamine can be decreased when combined with Nefazodone.Approved, Withdrawn
NelfinavirThe metabolism of Phenoxybenzamine can be decreased when combined with Nelfinavir.Approved
NesiritideThe risk or severity of adverse effects can be increased when Nesiritide is combined with Phenoxybenzamine.Approved, Investigational
NetupitantThe serum concentration of Phenoxybenzamine can be increased when it is combined with Netupitant.Approved
NevirapineThe metabolism of Phenoxybenzamine can be increased when combined with Nevirapine.Approved
NialamideNialamide may increase the hypotensive activities of Phenoxybenzamine.Withdrawn
NicardipineNicardipine may increase the hypotensive activities of Phenoxybenzamine.Approved
NicorandilNicorandil may increase the hypotensive activities of Phenoxybenzamine.Approved
NifedipineThe risk or severity of adverse effects can be increased when Nifedipine is combined with Phenoxybenzamine.Approved
NiguldipinePhenoxybenzamine may increase the hypotensive activities of Niguldipine.Experimental
NilotinibThe metabolism of Phenoxybenzamine can be decreased when combined with Nilotinib.Approved, Investigational
NilvadipinePhenoxybenzamine may increase the hypotensive activities of Nilvadipine.Approved
NimodipineNimodipine may increase the hypotensive activities of Phenoxybenzamine.Approved
NisoldipineNisoldipine may increase the hypotensive activities of Phenoxybenzamine.Approved
NitrendipinePhenoxybenzamine may increase the hypotensive activities of Nitrendipine.Approved
Nitric OxideThe risk or severity of adverse effects can be increased when Nitric Oxide is combined with Phenoxybenzamine.Approved
NitroglycerinThe risk or severity of adverse effects can be increased when Nitroglycerin is combined with Phenoxybenzamine.Approved, Investigational
NitroprussideNitroprusside may increase the hypotensive activities of Phenoxybenzamine.Approved
ObinutuzumabPhenoxybenzamine may increase the hypotensive activities of Obinutuzumab.Approved
OctamoxinOctamoxin may increase the hypotensive activities of Phenoxybenzamine.Withdrawn
OlaparibThe metabolism of Phenoxybenzamine can be decreased when combined with Olaparib.Approved
OlmesartanOlmesartan may increase the hypotensive activities of Phenoxybenzamine.Approved, Investigational
OmapatrilatOmapatrilat may increase the hypotensive activities of Phenoxybenzamine.Investigational
OsimertinibThe serum concentration of Phenoxybenzamine can be increased when it is combined with Osimertinib.Approved
OxprenololPhenoxybenzamine may increase the hypotensive activities of Oxprenolol.Approved
PaclitaxelThe risk or severity of adverse effects can be increased when Paclitaxel is combined with Phenoxybenzamine.Approved, Vet Approved
PalbociclibThe serum concentration of Phenoxybenzamine can be increased when it is combined with Palbociclib.Approved
PapaverineThe risk or severity of adverse effects can be increased when Papaverine is combined with Phenoxybenzamine.Approved
PargylinePargyline may increase the hypotensive activities of Phenoxybenzamine.Approved
PenbutololPhenoxybenzamine may increase the hypotensive activities of Penbutolol.Approved, Investigational
PentobarbitalThe metabolism of Phenoxybenzamine can be increased when combined with Pentobarbital.Approved, Vet Approved
PentoliniumPhenoxybenzamine may increase the hypotensive activities of Pentolinium.Approved
PentoxifyllinePentoxifylline may increase the hypotensive activities of Phenoxybenzamine.Approved, Investigational
PerindoprilPerindopril may increase the hypotensive activities of Phenoxybenzamine.Approved
PhenelzinePhenelzine may increase the hypotensive activities of Phenoxybenzamine.Approved
PheniprazinePheniprazine may increase the hypotensive activities of Phenoxybenzamine.Withdrawn
PhenobarbitalThe metabolism of Phenoxybenzamine can be increased when combined with Phenobarbital.Approved
PhenoxypropazinePhenoxypropazine may increase the hypotensive activities of Phenoxybenzamine.Withdrawn
PhentolaminePhentolamine may increase the hypotensive activities of Phenoxybenzamine.Approved
PhenytoinThe metabolism of Phenoxybenzamine can be increased when combined with Phenytoin.Approved, Vet Approved
PinacidilPhenoxybenzamine may increase the hypotensive activities of Pinacidil.Withdrawn
PindololPhenoxybenzamine may increase the hypotensive activities of Pindolol.Approved
PipamperoneThe risk or severity of adverse effects can be increased when Phenoxybenzamine is combined with Pipamperone.Approved
PirlindolePirlindole may increase the hypotensive activities of Phenoxybenzamine.Approved
PivhydrazinePivhydrazine may increase the hypotensive activities of Phenoxybenzamine.Withdrawn
PolythiazidePhenoxybenzamine may increase the hypotensive activities of Polythiazide.Approved
PosaconazoleThe metabolism of Phenoxybenzamine can be decreased when combined with Posaconazole.Approved, Investigational, Vet Approved
PramipexoleThe risk or severity of adverse effects can be increased when Phenoxybenzamine is combined with Pramipexole.Approved, Investigational
PrazosinPrazosin may increase the hypotensive activities of Phenoxybenzamine.Approved
PrimidoneThe metabolism of Phenoxybenzamine can be increased when combined with Primidone.Approved, Vet Approved
PropofolThe risk or severity of adverse effects can be increased when Phenoxybenzamine is combined with Propofol.Approved, Investigational, Vet Approved
PropranololPropranolol may increase the hypotensive activities of Phenoxybenzamine.Approved, Investigational
QuetiapineThe risk or severity of adverse effects can be increased when Quetiapine is combined with Phenoxybenzamine.Approved
QuinaprilQuinapril may increase the hypotensive activities of Phenoxybenzamine.Approved, Investigational
QuinineQuinine may increase the hypotensive activities of Phenoxybenzamine.Approved
RamiprilRamipril may increase the hypotensive activities of Phenoxybenzamine.Approved
RanolazineThe metabolism of Phenoxybenzamine can be decreased when combined with Ranolazine.Approved, Investigational
RasagilineRasagiline may increase the hypotensive activities of Phenoxybenzamine.Approved
RemifentanilThe risk or severity of adverse effects can be increased when Phenoxybenzamine is combined with Remifentanil.Approved
RemikirenRemikiren may increase the hypotensive activities of Phenoxybenzamine.Approved
RescinnaminePhenoxybenzamine may increase the hypotensive activities of Rescinnamine.Approved
ReserpineReserpine may increase the hypotensive activities of Phenoxybenzamine.Approved
RifabutinThe metabolism of Phenoxybenzamine can be increased when combined with Rifabutin.Approved
RifampicinThe metabolism of Phenoxybenzamine can be increased when combined with Rifampicin.Approved
RifapentineThe metabolism of Phenoxybenzamine can be increased when combined with Rifapentine.Approved
RilmenidinePhenoxybenzamine may increase the hypotensive activities of Rilmenidine.Investigational
RiociguatPhenoxybenzamine may increase the hypotensive activities of Riociguat.Approved
RisperidonePhenoxybenzamine may increase the hypotensive activities of Risperidone.Approved, Investigational
RitonavirThe metabolism of Phenoxybenzamine can be decreased when combined with Ritonavir.Approved, Investigational
RituximabPhenoxybenzamine may increase the hypotensive activities of Rituximab.Approved
RopiniroleThe risk or severity of adverse effects can be increased when Phenoxybenzamine is combined with Ropinirole.Approved, Investigational
RopivacaineThe risk or severity of adverse effects can be increased when Phenoxybenzamine is combined with Ropivacaine.Approved
RotigotineThe risk or severity of adverse effects can be increased when Phenoxybenzamine is combined with Rotigotine.Approved
SacubitrilThe risk or severity of adverse effects can be increased when Phenoxybenzamine is combined with Sacubitril.Approved
SafrazineSafrazine may increase the hypotensive activities of Phenoxybenzamine.Withdrawn
SaprisartanPhenoxybenzamine may increase the hypotensive activities of Saprisartan.Experimental
SaquinavirThe metabolism of Phenoxybenzamine can be decreased when combined with Saquinavir.Approved, Investigational
SecobarbitalSecobarbital may increase the hypotensive activities of Phenoxybenzamine.Approved, Vet Approved
SelegilineSelegiline may increase the hypotensive activities of Phenoxybenzamine.Approved, Investigational, Vet Approved
SelexipagPhenoxybenzamine may increase the hypotensive activities of Selexipag.Approved
SevofluraneThe risk or severity of adverse effects can be increased when Phenoxybenzamine is combined with Sevoflurane.Approved, Vet Approved
SildenafilSildenafil may increase the antihypertensive activities of Phenoxybenzamine.Approved, Investigational
SiltuximabThe serum concentration of Phenoxybenzamine can be decreased when it is combined with Siltuximab.Approved
SimeprevirThe serum concentration of Phenoxybenzamine can be increased when it is combined with Simeprevir.Approved
SitaxentanPhenoxybenzamine may increase the hypotensive activities of Sitaxentan.Approved, Investigational, Withdrawn
Sodium NitriteThe risk or severity of adverse effects can be increased when Phenoxybenzamine is combined with Sodium Nitrite.Approved
SotalolThe risk or severity of adverse effects can be increased when Sotalol is combined with Phenoxybenzamine.Approved
SpiraprilPhenoxybenzamine may increase the hypotensive activities of Spirapril.Approved
SpironolactoneThe risk or severity of adverse effects can be increased when Spironolactone is combined with Phenoxybenzamine.Approved
St. John's WortThe serum concentration of Phenoxybenzamine can be decreased when it is combined with St. John's Wort.Nutraceutical
StiripentolThe serum concentration of Phenoxybenzamine can be increased when it is combined with Stiripentol.Approved
StreptokinaseThe risk or severity of adverse effects can be increased when Phenoxybenzamine is combined with Streptokinase.Approved
SufentanilThe risk or severity of adverse effects can be increased when Phenoxybenzamine is combined with Sufentanil.Approved, Investigational
SulfisoxazoleThe metabolism of Phenoxybenzamine can be decreased when combined with Sulfisoxazole.Approved, Vet Approved
TadalafilTadalafil may increase the antihypertensive activities of Phenoxybenzamine.Approved, Investigational
TamsulosinThe risk or severity of adverse effects can be increased when Phenoxybenzamine is combined with Tamsulosin.Approved, Investigational
TelaprevirThe metabolism of Phenoxybenzamine can be decreased when combined with Telaprevir.Approved
TelithromycinThe metabolism of Phenoxybenzamine can be decreased when combined with Telithromycin.Approved
TelmisartanPhenoxybenzamine may increase the hypotensive activities of Telmisartan.Approved, Investigational
TemocaprilPhenoxybenzamine may increase the hypotensive activities of Temocapril.Experimental, Investigational
TerazosinThe risk or severity of adverse effects can be increased when Terazosin is combined with Phenoxybenzamine.Approved
TerlipressinPhenoxybenzamine may increase the hypotensive activities of Terlipressin.Approved, Investigational
ThalidomideThe risk or severity of adverse effects can be increased when Phenoxybenzamine is combined with Thalidomide.Approved, Investigational, Withdrawn
ThiamylalThiamylal may increase the hypotensive activities of Phenoxybenzamine.Approved, Vet Approved
ThiopentalThiopental may increase the hypotensive activities of Phenoxybenzamine.Approved, Vet Approved
ThioridazineThe risk or severity of adverse effects can be increased when Phenoxybenzamine is combined with Thioridazine.Approved
TibolonePhenoxybenzamine may increase the hypotensive activities of Tibolone.Approved
TiclopidineThe metabolism of Phenoxybenzamine can be decreased when combined with Ticlopidine.Approved
TicrynafenPhenoxybenzamine may increase the hypotensive activities of Ticrynafen.Withdrawn
TimololTimolol may increase the hypotensive activities of Phenoxybenzamine.Approved
TizanidineThe risk or severity of adverse effects can be increased when Tizanidine is combined with Phenoxybenzamine.Approved
TocilizumabThe serum concentration of Phenoxybenzamine can be decreased when it is combined with Tocilizumab.Approved
TolazolineTolazoline may increase the hypotensive activities of Phenoxybenzamine.Approved, Vet Approved
TolcaponeThe risk or severity of adverse effects can be increased when Phenoxybenzamine is combined with Tolcapone.Approved, Withdrawn
ToloxatoneToloxatone may increase the hypotensive activities of Phenoxybenzamine.Approved
TorasemideTorasemide may increase the hypotensive activities of Phenoxybenzamine.Approved
TrandolaprilTrandolapril may increase the hypotensive activities of Phenoxybenzamine.Approved
Trans-2-PhenylcyclopropylamineTrans-2-Phenylcyclopropylamine may increase the hypotensive activities of Phenoxybenzamine.Experimental
TranylcypromineTranylcypromine may increase the hypotensive activities of Phenoxybenzamine.Approved
TravoprostTravoprost may increase the hypotensive activities of Phenoxybenzamine.Approved
TreprostinilTreprostinil may increase the hypotensive activities of Phenoxybenzamine.Approved, Investigational
TretinoinThe risk or severity of adverse effects can be increased when Phenoxybenzamine is combined with Tretinoin.Approved, Investigational, Nutraceutical
TriamtereneThe risk or severity of adverse effects can be increased when Triamterene is combined with Phenoxybenzamine.Approved
TrichlormethiazidePhenoxybenzamine may increase the hypotensive activities of Trichlormethiazide.Approved, Vet Approved
TrimazosinPhenoxybenzamine may increase the hypotensive activities of Trimazosin.Experimental
TrimethaphanPhenoxybenzamine may increase the hypotensive activities of Trimethaphan.Approved
UdenafilUdenafil may increase the antihypertensive activities of Phenoxybenzamine.Approved, Investigational
UnoprostonePhenoxybenzamine may increase the hypotensive activities of Unoprostone.Approved
ValsartanValsartan may increase the hypotensive activities of Phenoxybenzamine.Approved, Investigational
VardenafilVardenafil may increase the antihypertensive activities of Phenoxybenzamine.Approved
VenlafaxineThe metabolism of Phenoxybenzamine can be decreased when combined with Venlafaxine.Approved
VerapamilThe metabolism of Phenoxybenzamine can be decreased when combined with Verapamil.Approved
VinpocetinePhenoxybenzamine may increase the hypotensive activities of Vinpocetine.Investigational
VoriconazoleThe metabolism of Phenoxybenzamine can be decreased when combined with Voriconazole.Approved, Investigational
XylometazolinePhenoxybenzamine may increase the hypotensive activities of Xylometazoline.Approved
YohimbineYohimbine may decrease the antihypertensive activities of Phenoxybenzamine.Approved, Vet Approved
ZiprasidoneThe metabolism of Phenoxybenzamine can be decreased when combined with Ziprasidone.Approved
Food InteractionsNot Available
References
Synthesis ReferenceNot Available
General References
  1. Caine M, Perlberg S, Meretyk S: A placebo-controlled double-blind study of the effect of phenoxybenzamine in benign prostatic obstruction. Br J Urol. 1978 Dec;50(7):551-4. [PubMed:88984 ]
  2. Frang H, Cockcroft V, Karskela T, Scheinin M, Marjamaki A: Phenoxybenzamine binding reveals the helical orientation of the third transmembrane domain of adrenergic receptors. J Biol Chem. 2001 Aug 17;276(33):31279-84. Epub 2001 Jun 6. [PubMed:11395517 ]
External Links
ATC CodesC04AX02
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelNot Available
MSDSDownload (73.8 KB)
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+1.0
Blood Brain Barrier+0.9629
Caco-2 permeable+0.7367
P-glycoprotein substrateSubstrate0.6059
P-glycoprotein inhibitor IInhibitor0.6043
P-glycoprotein inhibitor IIInhibitor0.5871
Renal organic cation transporterInhibitor0.7955
CYP450 2C9 substrateNon-substrate0.6666
CYP450 2D6 substrateNon-substrate0.6013
CYP450 3A4 substrateSubstrate0.5937
CYP450 1A2 substrateInhibitor0.9107
CYP450 2C9 inhibitorNon-inhibitor0.7714
CYP450 2D6 inhibitorInhibitor0.8931
CYP450 2C19 inhibitorInhibitor0.8994
CYP450 3A4 inhibitorNon-inhibitor0.8309
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.6682
Ames testAMES toxic0.9107
CarcinogenicityNon-carcinogens0.7565
BiodegradationNot ready biodegradable0.9973
Rat acute toxicity2.1163 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Strong inhibitor0.7145
hERG inhibition (predictor II)Inhibitor0.5874
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Wellspring pharmaceutical corp
Packagers
Dosage forms
FormRouteStrength
CapsuleOral10 mg/1
Prices
Unit descriptionCostUnit
Phenoxybenzamine hcl powd42.35USD g
Dibenzyline 10 mg capsule8.61USD capsule
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point39 °CPhysProp
logP4.7Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.0103 mg/mLALOGPS
logP4.26ALOGPS
logP4.64ChemAxon
logS-4.5ALOGPS
pKa (Strongest Basic)7.97ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count2ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area12.47 Å2ChemAxon
Rotatable Bond Count8ChemAxon
Refractivity88.92 m3·mol-1ChemAxon
Polarizability34.09 Å3ChemAxon
Number of Rings2ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
Spectra
Spectrum TypeDescriptionSplash Key
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, NegativeNot Available
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as phenylmethylamines. These are compounds containing a phenylmethtylamine moiety, which consists of a phenyl group substituted by an methanamine.
KingdomOrganic compounds
Super ClassBenzenoids
ClassBenzene and substituted derivatives
Sub ClassPhenylmethylamines
Direct ParentPhenylmethylamines
Alternative Parents
Substituents
  • Phenylmethylamine
  • Phenol ether
  • Benzylamine
  • Aralkylamine
  • Alkyl aryl ether
  • Tertiary aliphatic amine
  • Tertiary amine
  • Ether
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Organochloride
  • Organohalogen compound
  • Amine
  • Alkyl halide
  • Alkyl chloride
  • Aromatic homomonocyclic compound
Molecular FrameworkAromatic homomonocyclic compounds
External DescriptorsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
antagonist
General Function:
Protein heterodimerization activity
Specific Function:
This alpha-adrenergic receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. Its effect is mediated by G(q) and G(11) proteins. Nuclear ADRA1A-ADRA1B heterooligomers regulate phenylephrine(PE)-stimulated ERK signaling in cardiac myocytes.
Gene Name:
ADRA1A
Uniprot ID:
P35348
Molecular Weight:
51486.005 Da
References
  1. Stam WB, Van der Graaf PH, Saxena PR: Analysis of alpha 1L-adrenoceptor pharmacology in rat small mesenteric artery. Br J Pharmacol. 1999 Jun;127(3):661-70. [PubMed:10401556 ]
  2. Michel MC, Hanft G, Gross G: Functional studies on alpha 1-adrenoceptor subtypes mediating inotropic effects in rat right ventricle. Br J Pharmacol. 1994 Feb;111(2):539-46. [PubMed:7911719 ]
  3. Yu Y, Koss MC: Functional characterization of alpha-adrenoceptors mediating pupillary dilation in rats. Eur J Pharmacol. 2003 Jun 20;471(2):135-40. [PubMed:12818701 ]
  4. Salles J, Gascon S, Badia A: Sustained increase in rat myocardial alpha 1A-adrenoceptors induced by 6-hydroxydopamine treatment involves a decelerated receptor turnover. Naunyn Schmiedebergs Arch Pharmacol. 1996 Mar;353(4):408-16. [PubMed:8935707 ]
  5. Suzuki E, Tsujimoto G, Tamura K, Hashimoto K: Two pharmacologically distinct alpha 1-adrenoceptor subtypes in the contraction of rabbit aorta: each subtype couples with a different Ca2+ signalling mechanism and plays a different physiological role. Mol Pharmacol. 1990 Nov;38(5):725-36. [PubMed:1978244 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
antagonist
General Function:
Thioesterase binding
Specific Function:
Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins. The rank order of potency for agonists of this receptor is oxymetazoline > clonidine > epinephrine > norepinephrine > phenylephrine > dopamine > p-synephrine > p-tyramine > serotonin = p-octopamine. For antagonists, the rank order is yohimbine > phentolamine = mianser...
Gene Name:
ADRA2A
Uniprot ID:
P08913
Molecular Weight:
48956.275 Da
References
  1. Frang H, Cockcroft V, Karskela T, Scheinin M, Marjamaki A: Phenoxybenzamine binding reveals the helical orientation of the third transmembrane domain of adrenergic receptors. J Biol Chem. 2001 Aug 17;276(33):31279-84. Epub 2001 Jun 6. [PubMed:11395517 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Protein homodimerization activity
Specific Function:
Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins.
Gene Name:
ADRA2C
Uniprot ID:
P18825
Molecular Weight:
49521.585 Da
References
  1. Frang H, Cockcroft V, Karskela T, Scheinin M, Marjamaki A: Phenoxybenzamine binding reveals the helical orientation of the third transmembrane domain of adrenergic receptors. J Biol Chem. 2001 Aug 17;276(33):31279-84. Epub 2001 Jun 6. [PubMed:11395517 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Epinephrine binding
Specific Function:
Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins. The rank order of potency for agonists of this receptor is clonidine > norepinephrine > epinephrine = oxymetazoline > dopamine > p-tyramine = phenylephrine > serotonin > p-synephrine / p-octopamine. For antagonists, the rank order is yohimbine > chlorpromazine > phent...
Gene Name:
ADRA2B
Uniprot ID:
P18089
Molecular Weight:
49565.8 Da
References
  1. Frang H, Cockcroft V, Karskela T, Scheinin M, Marjamaki A: Phenoxybenzamine binding reveals the helical orientation of the third transmembrane domain of adrenergic receptors. J Biol Chem. 2001 Aug 17;276(33):31279-84. Epub 2001 Jun 6. [PubMed:11395517 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Titin binding
Specific Function:
Calmodulin mediates the control of a large number of enzymes, ion channels, aquaporins and other proteins by Ca(2+). Among the enzymes to be stimulated by the calmodulin-Ca(2+) complex are a number of protein kinases and phosphatases. Together with CCP110 and centrin, is involved in a genetic pathway that regulates the centrosome cycle and progression through cytokinesis.
Gene Name:
CALM1
Uniprot ID:
P62158
Molecular Weight:
16837.47 Da
References
  1. Cimino M, Weiss B: Characteristics of the binding of phenoxybenzamine to calmodulin. Biochem Pharmacol. 1988 Jul 15;37(14):2739-45. [PubMed:3134891 ]
  2. Suko J, Wyskovsky W, Pidlich J, Hauptner R, Plank B, Hellmann G: Calcium release from calmodulin and its C-terminal or N-terminal halves in the presence of the calmodulin antagonists phenoxybenzamine and melittin measured by stopped-flow fluorescence with Quin 2 and intrinsic tyrosine. Inhibition of calmodulin-dependent protein kinase of cardiac sarcoplasmic reticulum. Eur J Biochem. 1986 Sep 15;159(3):425-34. [PubMed:3758070 ]
  3. Lukas TJ, Marshak DR, Watterson DM: Drug-protein interactions: isolation and characterization of covalent adducts of phenoxybenzamine and calmodulin. Biochemistry. 1985 Jan 1;24(1):151-7. [PubMed:3994963 ]
  4. Earl CQ, Prozialeck WC, Weiss B: Interaction of alpha adrenergic antagonists with calmodulin. Life Sci. 1984 Jul 30;35(5):525-34. [PubMed:6146911 ]
  5. Kuromi H, Yoshihara M, Kidokoro Y: An inhibitory role of calcineurin in endocytosis of synaptic vesicles at nerve terminals of Drosophila larvae. Neurosci Res. 1997 Feb;27(2):101-13. [PubMed:9100252 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Protein homodimerization activity
Specific Function:
Beta-adrenergic receptors mediate the catecholamine-induced activation of adenylate cyclase through the action of G proteins. The beta-2-adrenergic receptor binds epinephrine with an approximately 30-fold greater affinity than it does norepinephrine.
Gene Name:
ADRB2
Uniprot ID:
P07550
Molecular Weight:
46458.32 Da
References
  1. Frang H, Cockcroft V, Karskela T, Scheinin M, Marjamaki A: Phenoxybenzamine binding reveals the helical orientation of the third transmembrane domain of adrenergic receptors. J Biol Chem. 2001 Aug 17;276(33):31279-84. Epub 2001 Jun 6. [PubMed:11395517 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Protein heterodimerization activity
Specific Function:
This alpha-adrenergic receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. Its effect is mediated by G(q) and G(11) proteins. Nuclear ADRA1A-ADRA1B heterooligomers regulate phenylephrine (PE)-stimulated ERK signaling in cardiac myocytes.
Gene Name:
ADRA1B
Uniprot ID:
P35368
Molecular Weight:
56835.375 Da
References
  1. Minneman KP, Theroux TL, Hollinger S, Han C, Esbenshade TA: Selectivity of agonists for cloned alpha 1-adrenergic receptor subtypes. Mol Pharmacol. 1994 Nov;46(5):929-36. [PubMed:7969082 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Alpha1-adrenergic receptor activity
Specific Function:
This alpha-adrenergic receptor mediates its effect through the influx of extracellular calcium.
Gene Name:
ADRA1D
Uniprot ID:
P25100
Molecular Weight:
60462.205 Da
References
  1. Minneman KP, Theroux TL, Hollinger S, Han C, Esbenshade TA: Selectivity of agonists for cloned alpha 1-adrenergic receptor subtypes. Mol Pharmacol. 1994 Nov;46(5):929-36. [PubMed:7969082 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
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 reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
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 ]

Transporters

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Quaternary ammonium group transmembrane transporter activity
Specific Function:
Mediates tubular uptake of organic compounds from circulation. Mediates the influx of agmatine, dopamine, noradrenaline (norepinephrine), serotonin, choline, famotidine, ranitidine, histamin, creatinine, amantadine, memantine, acriflavine, 4-[4-(dimethylamino)-styryl]-N-methylpyridinium ASP, amiloride, metformin, N-1-methylnicotinamide (NMN), tetraethylammonium (TEA), 1-methyl-4-phenylpyridiniu...
Gene Name:
SLC22A2
Uniprot ID:
O15244
Molecular Weight:
62579.99 Da
References
  1. Hayer-Zillgen M, Bruss M, Bonisch H: Expression and pharmacological profile of the human organic cation transporters hOCT1, hOCT2 and hOCT3. Br J Pharmacol. 2002 Jul;136(6):829-36. [PubMed:12110607 ]
  2. Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. [PubMed:10592235 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Secondary active organic cation transmembrane transporter activity
Specific Function:
Translocates a broad array of organic cations with various structures and molecular weights including the model compounds 1-methyl-4-phenylpyridinium (MPP), tetraethylammonium (TEA), N-1-methylnicotinamide (NMN), 4-(4-(dimethylamino)styryl)-N-methylpyridinium (ASP), the endogenous compounds choline, guanidine, histamine, epinephrine, adrenaline, noradrenaline and dopamine, and the drugs quinine...
Gene Name:
SLC22A1
Uniprot ID:
O15245
Molecular Weight:
61153.345 Da
References
  1. Hayer-Zillgen M, Bruss M, Bonisch H: Expression and pharmacological profile of the human organic cation transporters hOCT1, hOCT2 and hOCT3. Br J Pharmacol. 2002 Jul;136(6):829-36. [PubMed:12110607 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Toxin transporter activity
Specific Function:
Mediates potential-dependent transport of a variety of organic cations. May play a significant role in the disposition of cationic neurotoxins and neurotransmitters in the brain.
Gene Name:
SLC22A3
Uniprot ID:
O75751
Molecular Weight:
61279.485 Da
References
  1. Hayer-Zillgen M, Bruss M, Bonisch H: Expression and pharmacological profile of the human organic cation transporters hOCT1, hOCT2 and hOCT3. Br J Pharmacol. 2002 Jul;136(6):829-36. [PubMed:12110607 ]
Comments
comments powered by Disqus
Drug created on June 13, 2005 07:24 / Updated on December 08, 2016 11:11