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Identification
NameDebrisoquin
Accession NumberDB04840
TypeSmall Molecule
GroupsApproved
DescriptionAn adrenergic neuron-blocking drug similar in effects to guanethidine. It is also noteworthy in being a substrate for a polymorphic cytochrome P-450 enzyme. Persons with certain isoforms of this enzyme are unable to properly metabolize this and many other clinically important drugs. They are commonly referred to as having a debrisoquin 4-hydroxylase polymorphism. [PubChem]
Structure
Thumb
Synonyms
Debrisochinum
Debrisoquin
Debrisoquina
Debrisoquine
Debrisoquinum
Isocaramidine
External Identifiers Not Available
Approved Prescription ProductsNot Available
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
Bonipresslkapharm
DeclinaxRoche
TendorChinoin
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Debrisoquin sulfate
581-88-4
Thumb
  • InChI Key: CAYGYVYWRIHZCQ-UHFFFAOYSA-N
  • Monoisotopic Mass: 448.189274104
  • Average Mass: 448.539
DBSALT000370
Categories
UNIIX31CDK040E
CAS number1131-64-2
WeightAverage: 175.2303
Monoisotopic: 175.110947431
Chemical FormulaC10H13N3
InChI KeyJWPGJSVJDAJRLW-UHFFFAOYSA-N
InChI
InChI=1S/C10H13N3/c11-10(12)13-6-5-8-3-1-2-4-9(8)7-13/h1-4H,5-7H2,(H3,11,12)
IUPAC Name
1,2,3,4-tetrahydroisoquinoline-2-carboximidamide
SMILES
NC(=N)N1CCC2=CC=CC=C2C1
Pharmacology
IndicationFor the treatment of moderate and severe hypertension, either alone or as an adjunct, and for the treatment of renal hypertension.
Structured Indications Not Available
PharmacodynamicsDebrisoquin is an adrenergic neuron-blocking drug similar in effects to guanethidine. It is a substrate for a polymorphic cytochrome P-450 enzyme. Persons with certain isoforms of this enzyme are unable to properly metabolize this and many other clinically important drugs. They are commonly referred to as having a debrisoquin 4-hydroxylase polymorphism.
Mechanism of actionDebrisoquin acts at the sympathetic neuroeffector junction by inhibiting or interfering with the release and/or distribution of norepinephrine, rather than acting at the effector cell by inhibiting the association of norepinephrine with its receptors. It is taken up by norepinephrine transporters. It becomes concentrated in NE transmitter vesicles, replacing NE in these vesicles. This leads to a gradual depletion of NE stores in the nerve endings. Once inside the terminal it blocks the release of noradrenaline in response to arrival of an action potential. In contrast to ganglionic blocking agents, debrisoquin suppresses equally the responses mediated by alpha-and beta-adrenergic receptors but does not produce parasympathetic blockade. Since sympathetic blockade results in modest decreases in peripheral resistance and cardiac output, debrisoquin lowers blood pressure in the supine position. It further reduces blood pressure by decreasing the degree of vasoconstriction that normally results from reflex sympathetic nervous activity upon assumption of the upright posture, thus reducing venous return and cardiac output more.
TargetKindPharmacological actionActionsOrganismUniProt ID
Sodium-dependent noradrenaline transporterProteinyes
inducer
HumanP23975 details
Related Articles
AbsorptionNot Available
Volume of distributionNot Available
Protein bindingNot Available
Metabolism

Hepatic.

Route of eliminationNot Available
Half lifeNot Available
ClearanceNot Available
ToxicityNot Available
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 Debrisoquin.Experimental
AbirateroneThe serum concentration of Debrisoquin can be increased when it is combined with Abiraterone.Approved
AcebutololAcebutolol may increase the hypotensive activities of Debrisoquin.Approved
AcetaminophenThe serum concentration of Debrisoquin can be increased when it is combined with Acetaminophen.Approved
AfatinibThe serum concentration of Debrisoquin can be increased when it is combined with Afatinib.Approved
AlbendazoleThe serum concentration of Debrisoquin can be increased when it is combined with Albendazole.Approved, Vet Approved
AldosteroneThe serum concentration of Debrisoquin can be decreased when it is combined with Aldosterone.Experimental
AlectinibThe serum concentration of Debrisoquin can be increased when it is combined with Alectinib.Approved
AlfentanilThe serum concentration of Debrisoquin can be increased when it is combined with Alfentanil.Approved, Illicit
AlfuzosinAlfuzosin may increase the hypotensive activities of Debrisoquin.Approved, Investigational
AliskirenDebrisoquin may increase the hypotensive activities of Aliskiren.Approved, Investigational
AlprenololAlprenolol may increase the hypotensive activities of Debrisoquin.Approved, Withdrawn
AmantadineThe serum concentration of Debrisoquin can be increased when it is combined with Amantadine.Approved
AmbrisentanDebrisoquin may increase the hypotensive activities of Ambrisentan.Approved, Investigational
AmifostineDebrisoquin may increase the hypotensive activities of Amifostine.Approved, Investigational
Aminohippuric acidThe serum concentration of Debrisoquin can be increased when it is combined with Aminohippuric acid.Approved
AmiodaroneThe metabolism of Debrisoquin can be decreased when combined with Amiodarone.Approved, Investigational
AmitriptylineThe serum concentration of Debrisoquin can be increased when it is combined with Amitriptyline.Approved
AmlodipineThe serum concentration of Debrisoquin can be increased when it is combined with Amlodipine.Approved
AmprenavirThe serum concentration of Debrisoquin can be decreased when it is combined with Amprenavir.Approved
AmsacrineThe serum concentration of Debrisoquin can be increased when it is combined with Amsacrine.Approved
ArtemetherThe metabolism of Debrisoquin can be decreased when combined with Artemether.Approved
AstemizoleThe serum concentration of Debrisoquin can be increased when it is combined with Astemizole.Approved, Withdrawn
AtazanavirThe serum concentration of Debrisoquin can be increased when it is combined with Atazanavir.Approved, Investigational
AtenololThe serum concentration of Debrisoquin can be increased when it is combined with Atenolol.Approved
AtomoxetineThe metabolism of Debrisoquin can be decreased when combined with Atomoxetine.Approved
AtorvastatinThe serum concentration of Debrisoquin can be increased when it is combined with Atorvastatin.Approved
AzelastineThe serum concentration of Debrisoquin can be increased when it is combined with Azelastine.Approved
AzithromycinThe serum concentration of Debrisoquin can be increased when it is combined with Azithromycin.Approved
BenazeprilBenazepril may increase the hypotensive activities of Debrisoquin.Approved, Investigational
BendroflumethiazideBendroflumethiazide may increase the hypotensive activities of Debrisoquin.Approved
BenmoxinBenmoxin may increase the hypotensive activities of Debrisoquin.Withdrawn
BenzocaineThe serum concentration of Debrisoquin can be increased when it is combined with Benzocaine.Approved
BepridilThe serum concentration of Debrisoquin can be increased when it is combined with Bepridil.Approved, Withdrawn
BetaxololThe metabolism of Debrisoquin can be decreased when combined with Betaxolol.Approved
BethanidineBethanidine may increase the hypotensive activities of Debrisoquin.Approved
BimatoprostBimatoprost may increase the hypotensive activities of Debrisoquin.Approved, Investigational
BiperidenThe serum concentration of Debrisoquin can be increased when it is combined with Biperiden.Approved
BisoprololBisoprolol may increase the hypotensive activities of Debrisoquin.Approved
BosentanBosentan may increase the hypotensive activities of Debrisoquin.Approved, Investigational
BosutinibThe serum concentration of Debrisoquin can be increased when it is combined with Bosutinib.Approved
BretyliumBretylium may increase the hypotensive activities of Debrisoquin.Approved
BrimonidineBrimonidine may increase the hypotensive activities of Debrisoquin.Approved
BrimonidineBrimonidine may increase the antihypertensive activities of Debrisoquin.Approved
BromocriptineThe serum concentration of Debrisoquin can be increased when it is combined with Bromocriptine.Approved, Investigational
BupranololDebrisoquin may increase the hypotensive activities of Bupranolol.Approved
BuprenorphineThe serum concentration of Debrisoquin can be increased when it is combined with Buprenorphine.Approved, Illicit, Investigational, Vet Approved
BupropionThe metabolism of Debrisoquin can be decreased when combined with Bupropion.Approved
BuspironeThe serum concentration of Debrisoquin can be increased when it is combined with Buspirone.Approved, Investigational
CabazitaxelThe serum concentration of Debrisoquin can be increased when it is combined with Cabazitaxel.Approved
CaffeineThe serum concentration of Debrisoquin can be increased when it is combined with Caffeine.Approved
CanagliflozinThe serum concentration of Debrisoquin can be increased when it is combined with Canagliflozin.Approved
CandesartanThe serum concentration of Debrisoquin can be increased when it is combined with Candesartan.Approved
CandoxatrilCandoxatril may increase the hypotensive activities of Debrisoquin.Experimental
CaptoprilThe serum concentration of Debrisoquin can be increased when it is combined with Captopril.Approved
CarbamazepineThe serum concentration of Debrisoquin can be decreased when it is combined with Carbamazepine.Approved, Investigational
CaroxazoneCaroxazone may increase the hypotensive activities of Debrisoquin.Withdrawn
CarteololCarteolol may increase the hypotensive activities of Debrisoquin.Approved
CarvedilolThe serum concentration of Debrisoquin can be increased when it is combined with Carvedilol.Approved, Investigational
CaspofunginThe serum concentration of Debrisoquin can be increased when it is combined with Caspofungin.Approved
CelecoxibThe metabolism of Debrisoquin can be decreased when combined with Celecoxib.Approved, Investigational
CeliprololDebrisoquin may increase the hypotensive activities of Celiprolol.Approved, Investigational
ChloroquineThe serum concentration of Debrisoquin can be increased when it is combined with Chloroquine.Approved, Vet Approved
ChlorothiazideChlorothiazide may increase the hypotensive activities of Debrisoquin.Approved, Vet Approved
ChlorpromazineThe serum concentration of Debrisoquin can be increased when it is combined with Chlorpromazine.Approved, Vet Approved
ChlorpropamideThe serum concentration of Debrisoquin can be increased when it is combined with Chlorpropamide.Approved
ChlorprothixeneThe serum concentration of Debrisoquin can be increased when it is combined with Chlorprothixene.Approved, Withdrawn
ChlorthalidoneChlorthalidone may increase the hypotensive activities of Debrisoquin.Approved
CholecalciferolThe metabolism of Debrisoquin can be decreased when combined with Cholecalciferol.Approved, Nutraceutical
CholesterolThe serum concentration of Debrisoquin can be increased when it is combined with Cholesterol.Experimental
Cholic AcidThe serum concentration of Debrisoquin can be decreased when it is combined with Cholic Acid.Approved
CilazaprilThe serum concentration of Debrisoquin can be increased when it is combined with Cilazapril.Approved
CimetidineThe serum concentration of Debrisoquin can be decreased when it is combined with Cimetidine.Approved
CinacalcetThe metabolism of Debrisoquin can be decreased when combined with Cinacalcet.Approved
CiprofloxacinThe serum concentration of Debrisoquin can be increased when it is combined with Ciprofloxacin.Approved, Investigational
CitalopramThe serum concentration of Debrisoquin can be increased when it is combined with Citalopram.Approved
ClarithromycinThe serum concentration of Debrisoquin can be increased when it is combined with Clarithromycin.Approved
ClemastineThe metabolism of Debrisoquin can be decreased when combined with Clemastine.Approved
ClobazamThe metabolism of Debrisoquin can be decreased when combined with Clobazam.Approved, Illicit
ClofazimineThe serum concentration of Debrisoquin can be increased when it is combined with Clofazimine.Approved, Investigational
ClomipramineThe serum concentration of Debrisoquin can be increased when it is combined with Clomipramine.Approved, Vet Approved
ClonidineClonidine may increase the hypotensive activities of Debrisoquin.Approved
ClotrimazoleThe serum concentration of Debrisoquin can be decreased when it is combined with Clotrimazole.Approved, Vet Approved
ClozapineThe metabolism of Debrisoquin can be decreased when combined with Clozapine.Approved
CobicistatThe serum concentration of Debrisoquin can be increased when it is combined with Cobicistat.Approved
CocaineThe metabolism of Debrisoquin can be decreased when combined with Cocaine.Approved, Illicit
ColchicineThe serum concentration of Debrisoquin can be increased when it is combined with Colchicine.Approved
ColforsinThe serum concentration of Debrisoquin can be increased when it is combined with Colforsin.Experimental
CrizotinibThe serum concentration of Debrisoquin can be increased when it is combined with Crizotinib.Approved
CryptenamineCryptenamine may increase the hypotensive activities of Debrisoquin.Approved
CyclophosphamideThe serum concentration of Debrisoquin can be increased when it is combined with Cyclophosphamide.Approved, Investigational
CyclosporineThe serum concentration of Debrisoquin can be decreased when it is combined with Cyclosporine.Approved, Investigational, Vet Approved
CyclothiazideCyclothiazide may increase the hypotensive activities of Debrisoquin.Approved
DaclatasvirThe serum concentration of Debrisoquin can be increased when it is combined with Daclatasvir.Approved
DactinomycinThe serum concentration of Debrisoquin can be increased when it is combined with Dactinomycin.Approved
DarifenacinThe metabolism of Debrisoquin can be decreased when combined with Darifenacin.Approved, Investigational
DarunavirThe serum concentration of Debrisoquin can be increased when it is combined with Darunavir.Approved
DasatinibThe serum concentration of Debrisoquin can be increased when it is combined with Dasatinib.Approved, Investigational
DaunorubicinThe serum concentration of Debrisoquin can be decreased when it is combined with Daunorubicin.Approved
DelavirdineThe metabolism of Debrisoquin can be decreased when combined with Delavirdine.Approved
DeserpidineDebrisoquin may increase the hypotensive activities of Deserpidine.Approved
DesipramineThe serum concentration of Debrisoquin can be increased when it is combined with Desipramine.Approved
DesloratadineThe serum concentration of Debrisoquin can be increased when it is combined with Desloratadine.Approved, Investigational
DexamethasoneThe serum concentration of Debrisoquin can be decreased when it is combined with Dexamethasone.Approved, Investigational, Vet Approved
DextromethorphanThe serum concentration of Debrisoquin can be increased when it is combined with Dextromethorphan.Approved
DiazoxideDiazoxide may increase the hypotensive activities of Debrisoquin.Approved
DiclofenacThe serum concentration of Debrisoquin can be increased when it is combined with Diclofenac.Approved, Vet Approved
DigoxinThe serum concentration of Debrisoquin can be decreased when it is combined with Digoxin.Approved
DihydralazineDebrisoquin may increase the hypotensive activities of Dihydralazine.Investigational
DihydroergotamineThe serum concentration of Debrisoquin can be increased when it is combined with Dihydroergotamine.Approved
DiltiazemThe serum concentration of Debrisoquin can be increased when it is combined with Diltiazem.Approved
DiphenhydramineThe metabolism of Debrisoquin can be decreased when combined with Diphenhydramine.Approved
DipyridamoleThe serum concentration of Debrisoquin can be increased when it is combined with Dipyridamole.Approved
DorzolamideDorzolamide may increase the hypotensive activities of Debrisoquin.Approved
DoxazosinThe serum concentration of Debrisoquin can be increased when it is combined with Doxazosin.Approved
DoxepinThe serum concentration of Debrisoquin can be increased when it is combined with Doxepin.Approved
DoxorubicinThe serum concentration of Debrisoquin can be decreased when it is combined with Doxorubicin.Approved, Investigational
DronabinolThe serum concentration of Debrisoquin can be increased when it is combined with Dronabinol.Approved, Illicit
DronedaroneThe serum concentration of Debrisoquin can be increased when it is combined with Dronedarone.Approved
DuloxetineThe metabolism of Debrisoquin can be decreased when combined with Duloxetine.Approved
EfonidipineDebrisoquin may increase the hypotensive activities of Efonidipine.Approved
ElbasvirThe serum concentration of Debrisoquin can be increased when it is combined with Elbasvir.Approved
EliglustatThe metabolism of Debrisoquin can be decreased when combined with Eliglustat.Approved
EnalaprilThe serum concentration of Debrisoquin can be increased when it is combined with Enalapril.Approved, Vet Approved
EnalaprilatDebrisoquin may increase the hypotensive activities of Enalaprilat.Approved
EnzalutamideThe serum concentration of Debrisoquin can be increased when it is combined with Enzalutamide.Approved
EpoprostenolEpoprostenol may increase the hypotensive activities of Debrisoquin.Approved
EprosartanEprosartan may increase the hypotensive activities of Debrisoquin.Approved
ErgonovineThe serum concentration of Debrisoquin can be increased when it is combined with Ergonovine.Approved
ErgotamineThe serum concentration of Debrisoquin can be increased when it is combined with Ergotamine.Approved
ErythromycinThe serum concentration of Debrisoquin can be decreased when it is combined with Erythromycin.Approved, Vet Approved
EstramustineThe serum concentration of Debrisoquin can be increased when it is combined with Estramustine.Approved
EstriolThe serum concentration of Debrisoquin can be decreased when it is combined with Estriol.Approved, Vet Approved
EstroneThe serum concentration of Debrisoquin can be decreased when it is combined with Estrone.Approved
EtoposideThe serum concentration of Debrisoquin can be increased when it is combined with Etoposide.Approved
EtravirineThe serum concentration of Debrisoquin can be increased when it is combined with Etravirine.Approved
FelodipineThe serum concentration of Debrisoquin can be increased when it is combined with Felodipine.Approved, Investigational
FenoldopamFenoldopam may increase the hypotensive activities of Debrisoquin.Approved
FentanylThe serum concentration of Debrisoquin can be increased when it is combined with Fentanyl.Approved, Illicit, Investigational, Vet Approved
FexofenadineThe serum concentration of Debrisoquin can be increased when it is combined with Fexofenadine.Approved
FidaxomicinThe serum concentration of Debrisoquin can be increased when it is combined with Fidaxomicin.Approved
FluconazoleThe serum concentration of Debrisoquin can be increased when it is combined with Fluconazole.Approved
FluoxetineThe metabolism of Debrisoquin can be decreased when combined with Fluoxetine.Approved, Vet Approved
FlupentixolThe serum concentration of Debrisoquin can be increased when it is combined with Flupentixol.Approved, Withdrawn
FluphenazineThe serum concentration of Debrisoquin can be increased when it is combined with Fluphenazine.Approved
FlurazepamThe serum concentration of Debrisoquin can be increased when it is combined with Flurazepam.Approved, Illicit
FluvoxamineThe serum concentration of Debrisoquin can be increased when it is combined with Fluvoxamine.Approved, Investigational
FosinoprilFosinopril may increase the hypotensive activities of Debrisoquin.Approved
FurazolidoneFurazolidone may increase the hypotensive activities of Debrisoquin.Approved, Vet Approved
GefitinibThe serum concentration of Debrisoquin can be increased when it is combined with Gefitinib.Approved, Investigational
GenisteinThe serum concentration of Debrisoquin can be increased when it is combined with Genistein.Investigational
GlyburideThe serum concentration of Debrisoquin can be increased when it is combined with Glyburide.Approved
GlycerolThe serum concentration of Debrisoquin can be increased when it is combined with Glycerol.Experimental
Gramicidin DThe serum concentration of Debrisoquin can be increased when it is combined with Gramicidin D.Approved
GrepafloxacinThe serum concentration of Debrisoquin can be increased when it is combined with Grepafloxacin.Withdrawn
GuanabenzGuanabenz may increase the hypotensive activities of Debrisoquin.Approved
GuanadrelGuanadrel may increase the hypotensive activities of Debrisoquin.Approved
GuanethidineGuanethidine may increase the hypotensive activities of Debrisoquin.Approved
GuanfacineGuanfacine may increase the hypotensive activities of Debrisoquin.Approved, Investigational
HaloperidolThe serum concentration of Debrisoquin can be increased when it is combined with Haloperidol.Approved
HexamethoniumDebrisoquin may increase the hypotensive activities of Hexamethonium.Experimental
HydracarbazineHydracarbazine may increase the hypotensive activities of Debrisoquin.Approved
HydralazineHydralazine may increase the hypotensive activities of Debrisoquin.Approved
HydrochlorothiazideHydrochlorothiazide may increase the hypotensive activities of Debrisoquin.Approved, Vet Approved
HydrocortisoneThe serum concentration of Debrisoquin can be increased when it is combined with Hydrocortisone.Approved, Vet Approved
HydroflumethiazideHydroflumethiazide may increase the hypotensive activities of Debrisoquin.Approved
IdelalisibThe serum concentration of Debrisoquin can be increased when it is combined with Idelalisib.Approved
IloprostIloprost may increase the hypotensive activities of Debrisoquin.Approved, Investigational
ImatinibThe serum concentration of Debrisoquin can be increased when it is combined with Imatinib.Approved
ImidaprilDebrisoquin may increase the hypotensive activities of Imidapril.Investigational
ImipramineThe serum concentration of Debrisoquin can be increased when it is combined with Imipramine.Approved
IndapamideIndapamide may increase the hypotensive activities of Debrisoquin.Approved
IndenololDebrisoquin may increase the hypotensive activities of Indenolol.Withdrawn
IndinavirThe serum concentration of Debrisoquin can be decreased when it is combined with Indinavir.Approved
IndomethacinThe serum concentration of Debrisoquin can be increased when it is combined with Indomethacin.Approved, Investigational
IndoraminDebrisoquin may increase the hypotensive activities of Indoramin.Withdrawn
IproclozideIproclozide may increase the hypotensive activities of Debrisoquin.Withdrawn
IproniazidIproniazid may increase the hypotensive activities of Debrisoquin.Withdrawn
IrbesartanIrbesartan may increase the hypotensive activities of Debrisoquin.Approved, Investigational
IsavuconazoniumThe serum concentration of Debrisoquin can be increased when it is combined with Isavuconazonium.Approved, Investigational
IsocarboxazidIsocarboxazid may increase the hypotensive activities of Debrisoquin.Approved
IsoniazidThe metabolism of Debrisoquin can be decreased when combined with Isoniazid.Approved
IsradipineIsradipine may increase the hypotensive activities of Debrisoquin.Approved
ItraconazoleThe serum concentration of Debrisoquin can be increased when it is combined with Itraconazole.Approved, Investigational
IvacaftorThe serum concentration of Debrisoquin can be increased when it is combined with Ivacaftor.Approved
IvermectinThe serum concentration of Debrisoquin can be increased when it is combined with Ivermectin.Approved, Vet Approved
KetamineThe serum concentration of Debrisoquin can be increased when it is combined with Ketamine.Approved, Vet Approved
KetanserinDebrisoquin may increase the hypotensive activities of Ketanserin.Investigational
KetoconazoleThe serum concentration of Debrisoquin can be increased when it is combined with Ketoconazole.Approved, Investigational
LabetalolLabetalol may increase the hypotensive activities of Debrisoquin.Approved
LacidipineDebrisoquin may increase the hypotensive activities of Lacidipine.Approved
LansoprazoleThe serum concentration of Debrisoquin can be increased when it is combined with Lansoprazole.Approved, Investigational
LapatinibThe serum concentration of Debrisoquin can be increased when it is combined with Lapatinib.Approved, Investigational
LatanoprostLatanoprost may increase the hypotensive activities of Debrisoquin.Approved, Investigational
LercanidipineLercanidipine may increase the hypotensive activities of Debrisoquin.Approved, Investigational
LevofloxacinThe serum concentration of Debrisoquin can be increased when it is combined with Levofloxacin.Approved, Investigational
LevothyroxineThe serum concentration of Debrisoquin can be decreased when it is combined with Levothyroxine.Approved
LidocaineThe serum concentration of Debrisoquin can be increased when it is combined with Lidocaine.Approved, Vet Approved
LiothyronineThe serum concentration of Debrisoquin can be decreased when it is combined with Liothyronine.Approved, Vet Approved
LiotrixThe serum concentration of Debrisoquin can be decreased when it is combined with Liotrix.Approved
LisinoprilThe serum concentration of Debrisoquin can be increased when it is combined with Lisinopril.Approved, Investigational
LofexidineDebrisoquin may increase the hypotensive activities of Lofexidine.Approved, Investigational
LomitapideThe serum concentration of Debrisoquin can be increased when it is combined with Lomitapide.Approved
LoperamideThe serum concentration of Debrisoquin can be increased when it is combined with Loperamide.Approved
LopinavirThe metabolism of Debrisoquin can be decreased when combined with Lopinavir.Approved
LoratadineThe serum concentration of Debrisoquin can be increased when it is combined with Loratadine.Approved
LorcaserinThe metabolism of Debrisoquin can be decreased when combined with Lorcaserin.Approved
LosartanThe serum concentration of Debrisoquin can be increased when it is combined with Losartan.Approved
LovastatinThe serum concentration of Debrisoquin can be increased when it is combined with Lovastatin.Approved, Investigational
LumacaftorThe serum concentration of Debrisoquin can be decreased when it is combined with Lumacaftor.Approved
LumefantrineThe metabolism of Debrisoquin can be decreased when combined with Lumefantrine.Approved
MacitentanDebrisoquin may increase the hypotensive activities of Macitentan.Approved
ManidipineDebrisoquin may increase the hypotensive activities of Manidipine.Approved
MaprotilineThe serum concentration of Debrisoquin can be increased when it is combined with Maprotiline.Approved
MebanazineMebanazine may increase the hypotensive activities of Debrisoquin.Withdrawn
MebendazoleThe serum concentration of Debrisoquin can be increased when it is combined with Mebendazole.Approved, Vet Approved
MecamylamineMecamylamine may increase the hypotensive activities of Debrisoquin.Approved
MefloquineThe serum concentration of Debrisoquin can be increased when it is combined with Mefloquine.Approved
Megestrol acetateThe serum concentration of Debrisoquin can be increased when it is combined with Megestrol acetate.Approved, Vet Approved
MeprobamateThe serum concentration of Debrisoquin can be increased when it is combined with Meprobamate.Approved, Illicit
MethadoneThe serum concentration of Debrisoquin can be increased when it is combined with Methadone.Approved
MethotrimeprazineThe metabolism of Debrisoquin can be decreased when combined with Methotrimeprazine.Approved
MethyldopaMethyldopa may increase the hypotensive activities of Debrisoquin.Approved
Methylene blueMethylene blue may increase the hypotensive activities of Debrisoquin.Investigational
MethylphenidateMethylphenidate may decrease the antihypertensive activities of Debrisoquin.Approved, Investigational
MetipranololMetipranolol may increase the hypotensive activities of Debrisoquin.Approved
MetolazoneMetolazone may increase the hypotensive activities of Debrisoquin.Approved
MetoprololThe serum concentration of Debrisoquin can be increased when it is combined with Metoprolol.Approved, Investigational
MetyrosineDebrisoquin may increase the hypotensive activities of Metyrosine.Approved
MibefradilThe serum concentration of Debrisoquin can be increased when it is combined with Mibefradil.Withdrawn
MiconazoleThe serum concentration of Debrisoquin can be increased when it is combined with Miconazole.Approved, Investigational, Vet Approved
MidazolamThe serum concentration of Debrisoquin can be decreased when it is combined with Midazolam.Approved, Illicit
MifepristoneThe serum concentration of Debrisoquin can be decreased when it is combined with Mifepristone.Approved, Investigational
MinaprineMinaprine may increase the hypotensive activities of Debrisoquin.Approved
MinoxidilMinoxidil may increase the hypotensive activities of Debrisoquin.Approved
MirabegronThe metabolism of Debrisoquin can be decreased when combined with Mirabegron.Approved
MitomycinThe serum concentration of Debrisoquin can be increased when it is combined with Mitomycin.Approved
MitoxantroneThe serum concentration of Debrisoquin can be decreased when it is combined with Mitoxantrone.Approved, Investigational
MoclobemideMoclobemide may increase the hypotensive activities of Debrisoquin.Approved
MoexiprilMoexipril may increase the hypotensive activities of Debrisoquin.Approved
MolsidomineMolsidomine may increase the hypotensive activities of Debrisoquin.Approved
MorphineThe serum concentration of Debrisoquin can be increased when it is combined with Morphine.Approved, Investigational
MoxonidineDebrisoquin may increase the hypotensive activities of Moxonidine.Approved
NadololNadolol may increase the hypotensive activities of Debrisoquin.Approved
NaftopidilDebrisoquin may increase the hypotensive activities of Naftopidil.Investigational
NaltrexoneThe serum concentration of Debrisoquin can be increased when it is combined with Naltrexone.Approved, Investigational, Vet Approved
NaringeninThe serum concentration of Debrisoquin can be increased when it is combined with Naringenin.Experimental
NebivololDebrisoquin may increase the hypotensive activities of Nebivolol.Approved, Investigational
NefazodoneThe serum concentration of Debrisoquin can be decreased when it is combined with Nefazodone.Approved, Withdrawn
NelfinavirThe serum concentration of Debrisoquin can be decreased when it is combined with Nelfinavir.Approved
NeostigmineThe serum concentration of Debrisoquin can be increased when it is combined with Neostigmine.Approved, Vet Approved
NevirapineThe metabolism of Debrisoquin can be decreased when combined with Nevirapine.Approved
NialamideNialamide may increase the hypotensive activities of Debrisoquin.Withdrawn
NicardipineThe serum concentration of Debrisoquin can be increased when it is combined with Nicardipine.Approved
NicorandilDebrisoquin may increase the hypotensive activities of Nicorandil.Approved
NifedipineThe serum concentration of Debrisoquin can be decreased when it is combined with Nifedipine.Approved
NiguldipineDebrisoquin may increase the hypotensive activities of Niguldipine.Experimental
NilotinibThe serum concentration of Debrisoquin can be increased when it is combined with Nilotinib.Approved, Investigational
NilvadipineDebrisoquin may increase the hypotensive activities of Nilvadipine.Approved
NimodipineNimodipine may increase the hypotensive activities of Debrisoquin.Approved
NisoldipineThe serum concentration of Debrisoquin can be increased when it is combined with Nisoldipine.Approved
NitrazepamThe serum concentration of Debrisoquin can be increased when it is combined with Nitrazepam.Approved
NitrendipineThe serum concentration of Debrisoquin can be increased when it is combined with Nitrendipine.Approved
NitroprussideNitroprusside may increase the hypotensive activities of Debrisoquin.Approved
NorethisteroneThe serum concentration of Debrisoquin can be decreased when it is combined with Norethisterone.Approved
ObinutuzumabDebrisoquin may increase the hypotensive activities of Obinutuzumab.Approved
OctamoxinOctamoxin may increase the hypotensive activities of Debrisoquin.Withdrawn
OlmesartanOlmesartan may increase the hypotensive activities of Debrisoquin.Approved, Investigational
OmapatrilatOmapatrilat may increase the hypotensive activities of Debrisoquin.Investigational
OmeprazoleThe serum concentration of Debrisoquin can be increased when it is combined with Omeprazole.Approved, Investigational, Vet Approved
OxprenololOxprenolol may increase the hypotensive activities of Debrisoquin.Approved
P-NitrophenolThe serum concentration of Debrisoquin can be increased when it is combined with P-Nitrophenol.Experimental
PaclitaxelThe serum concentration of Debrisoquin can be increased when it is combined with Paclitaxel.Approved, Vet Approved
Palmitic AcidThe serum concentration of Debrisoquin can be increased when it is combined with Palmitic Acid.Experimental
PanobinostatThe serum concentration of Debrisoquin can be increased when it is combined with Panobinostat.Approved, Investigational
PantoprazoleThe serum concentration of Debrisoquin can be increased when it is combined with Pantoprazole.Approved
PargylinePargyline may increase the hypotensive activities of Debrisoquin.Approved
ParoxetineThe metabolism of Debrisoquin can be decreased when combined with Paroxetine.Approved, Investigational
Peginterferon alfa-2bThe serum concentration of Debrisoquin can be decreased when it is combined with Peginterferon alfa-2b.Approved
PenbutololPenbutolol may increase the hypotensive activities of Debrisoquin.Approved, Investigational
PentoliniumPentolinium may increase the hypotensive activities of Debrisoquin.Approved
PentoxifyllinePentoxifylline may increase the hypotensive activities of Debrisoquin.Approved, Investigational
PerindoprilThe serum concentration of Debrisoquin can be increased when it is combined with Perindopril.Approved
PhenelzinePhenelzine may increase the hypotensive activities of Debrisoquin.Approved
PheniprazinePheniprazine may increase the hypotensive activities of Debrisoquin.Withdrawn
PhenobarbitalThe serum concentration of Debrisoquin can be decreased when it is combined with Phenobarbital.Approved
PhenoxybenzaminePhenoxybenzamine may increase the hypotensive activities of Debrisoquin.Approved
PhenoxypropazinePhenoxypropazine may increase the hypotensive activities of Debrisoquin.Withdrawn
PhentolaminePhentolamine may increase the hypotensive activities of Debrisoquin.Approved
PimozideThe serum concentration of Debrisoquin can be increased when it is combined with Pimozide.Approved
PinacidilDebrisoquin may increase the hypotensive activities of Pinacidil.Withdrawn
PindololPindolol may increase the hypotensive activities of Debrisoquin.Approved
PirlindolePirlindole may increase the hypotensive activities of Debrisoquin.Approved
PivhydrazinePivhydrazine may increase the hypotensive activities of Debrisoquin.Withdrawn
Platelet Activating FactorThe serum concentration of Debrisoquin can be decreased when it is combined with Platelet Activating Factor.Experimental
PolythiazidePolythiazide may increase the hypotensive activities of Debrisoquin.Approved
PonatinibThe serum concentration of Debrisoquin can be increased when it is combined with Ponatinib.Approved
PosaconazoleThe serum concentration of Debrisoquin can be increased when it is combined with Posaconazole.Approved, Investigational, Vet Approved
PravastatinThe serum concentration of Debrisoquin can be increased when it is combined with Pravastatin.Approved
PrazosinThe serum concentration of Debrisoquin can be increased when it is combined with Prazosin.Approved
PrednisoneThe serum concentration of Debrisoquin can be increased when it is combined with Prednisone.Approved, Vet Approved
ProbenecidThe serum concentration of Debrisoquin can be increased when it is combined with Probenecid.Approved
ProgesteroneThe serum concentration of Debrisoquin can be decreased when it is combined with Progesterone.Approved, Vet Approved
PromazineThe metabolism of Debrisoquin can be decreased when combined with Promazine.Approved, Vet Approved
PromethazineThe serum concentration of Debrisoquin can be increased when it is combined with Promethazine.Approved
PropafenoneThe serum concentration of Debrisoquin can be increased when it is combined with Propafenone.Approved
PropranololThe serum concentration of Debrisoquin can be increased when it is combined with Propranolol.Approved, Investigational
ProtriptylineThe serum concentration of Debrisoquin can be increased when it is combined with Protriptyline.Approved
QuercetinThe serum concentration of Debrisoquin can be increased when it is combined with Quercetin.Experimental
QuinacrineThe serum concentration of Debrisoquin can be increased when it is combined with Quinacrine.Approved
QuinaprilQuinapril may increase the hypotensive activities of Debrisoquin.Approved, Investigational
QuinidineThe metabolism of Debrisoquin can be decreased when combined with Quinidine.Approved
QuinineQuinine may increase the hypotensive activities of Debrisoquin.Approved
RamiprilRamipril may increase the hypotensive activities of Debrisoquin.Approved
RanitidineThe serum concentration of Debrisoquin can be increased when it is combined with Ranitidine.Approved
RanolazineThe serum concentration of Debrisoquin can be increased when it is combined with Ranolazine.Approved, Investigational
RasagilineRasagiline may increase the hypotensive activities of Debrisoquin.Approved
ReboxetineThe serum concentration of Debrisoquin can be increased when it is combined with Reboxetine.Approved, Investigational
RegorafenibThe serum concentration of Debrisoquin can be increased when it is combined with Regorafenib.Approved
RemikirenRemikiren may increase the hypotensive activities of Debrisoquin.Approved
RescinnamineDebrisoquin may increase the hypotensive activities of Rescinnamine.Approved
ReserpineThe serum concentration of Debrisoquin can be decreased when it is combined with Reserpine.Approved
RifampicinThe serum concentration of Debrisoquin can be decreased when it is combined with Rifampicin.Approved
RilmenidineDebrisoquin may increase the hypotensive activities of Rilmenidine.Investigational
RilpivirineThe serum concentration of Debrisoquin can be increased when it is combined with Rilpivirine.Approved
RiociguatDebrisoquin may increase the hypotensive activities of Riociguat.Approved
RitonavirThe metabolism of Debrisoquin can be decreased when combined with Ritonavir.Approved, Investigational
RituximabDebrisoquin may increase the hypotensive activities of Rituximab.Approved
RolapitantThe serum concentration of Debrisoquin can be increased when it is combined with Rolapitant.Approved
RopiniroleThe metabolism of Debrisoquin can be decreased when combined with Ropinirole.Approved, Investigational
SafrazineSafrazine may increase the hypotensive activities of Debrisoquin.Withdrawn
SaprisartanSaprisartan may increase the hypotensive activities of Debrisoquin.Experimental
SaquinavirThe serum concentration of Debrisoquin can be decreased when it is combined with Saquinavir.Approved, Investigational
ScopolamineThe serum concentration of Debrisoquin can be increased when it is combined with Scopolamine.Approved
SelegilineThe serum concentration of Debrisoquin can be increased when it is combined with Selegiline.Approved, Investigational, Vet Approved
SelexipagDebrisoquin may increase the hypotensive activities of Selexipag.Approved
SertralineThe serum concentration of Debrisoquin can be increased when it is combined with Sertraline.Approved
SildenafilSildenafil may increase the antihypertensive activities of Debrisoquin.Approved, Investigational
SimeprevirThe serum concentration of Debrisoquin can be increased when it is combined with Simeprevir.Approved
SimvastatinThe serum concentration of Debrisoquin can be increased when it is combined with Simvastatin.Approved
SirolimusThe serum concentration of Debrisoquin can be decreased when it is combined with Sirolimus.Approved, Investigational
SitaxentanDebrisoquin may increase the hypotensive activities of Sitaxentan.Approved, Investigational, Withdrawn
SorafenibThe serum concentration of Debrisoquin can be increased when it is combined with Sorafenib.Approved, Investigational
SpiraprilSpirapril may increase the hypotensive activities of Debrisoquin.Approved
SpironolactoneThe serum concentration of Debrisoquin can be increased when it is combined with Spironolactone.Approved
St. John's WortThe serum concentration of Debrisoquin can be decreased when it is combined with St. John's Wort.Nutraceutical
StaurosporineThe serum concentration of Debrisoquin can be increased when it is combined with Staurosporine.Experimental
StiripentolThe metabolism of Debrisoquin can be decreased when combined with Stiripentol.Approved
StreptozocinThe serum concentration of Debrisoquin can be decreased when it is combined with Streptozocin.Approved
SulfinpyrazoneThe serum concentration of Debrisoquin can be increased when it is combined with Sulfinpyrazone.Approved
SumatriptanThe serum concentration of Debrisoquin can be increased when it is combined with Sumatriptan.Approved, Investigational
SunitinibThe serum concentration of Debrisoquin can be increased when it is combined with Sunitinib.Approved, Investigational
TacrineThe serum concentration of Debrisoquin can be increased when it is combined with Tacrine.Withdrawn
TacrolimusThe serum concentration of Debrisoquin can be decreased when it is combined with Tacrolimus.Approved, Investigational
TadalafilTadalafil may increase the antihypertensive activities of Debrisoquin.Approved, Investigational
TamoxifenThe serum concentration of Debrisoquin can be decreased when it is combined with Tamoxifen.Approved
Taurocholic AcidThe serum concentration of Debrisoquin can be increased when it is combined with Taurocholic Acid.Experimental
TelmisartanThe serum concentration of Debrisoquin can be increased when it is combined with Telmisartan.Approved, Investigational
TemocaprilDebrisoquin may increase the hypotensive activities of Temocapril.Experimental, Investigational
TemsirolimusThe serum concentration of Debrisoquin can be increased when it is combined with Temsirolimus.Approved
TerazosinThe serum concentration of Debrisoquin can be increased when it is combined with Terazosin.Approved
TerbinafineThe metabolism of Debrisoquin can be decreased when combined with Terbinafine.Approved, Investigational, Vet Approved
TerfenadineThe serum concentration of Debrisoquin can be increased when it is combined with Terfenadine.Withdrawn
TerlipressinTerlipressin may increase the hypotensive activities of Debrisoquin.Approved, Investigational
TesmilifeneThe serum concentration of Debrisoquin can be decreased when it is combined with Tesmilifene.Investigational
TestosteroneThe serum concentration of Debrisoquin can be increased when it is combined with Testosterone.Approved, Investigational
ThioridazineThe metabolism of Debrisoquin can be decreased when combined with Thioridazine.Approved
TiboloneDebrisoquin may increase the hypotensive activities of Tibolone.Approved
TicagrelorThe serum concentration of Debrisoquin can be increased when it is combined with Ticagrelor.Approved
TiclopidineThe metabolism of Debrisoquin can be decreased when combined with Ticlopidine.Approved
TicrynafenTicrynafen may increase the hypotensive activities of Debrisoquin.Withdrawn
TimololTimolol may increase the hypotensive activities of Debrisoquin.Approved
TipranavirThe metabolism of Debrisoquin can be decreased when combined with Tipranavir.Approved, Investigational
TolazolineTolazoline may increase the hypotensive activities of Debrisoquin.Approved, Vet Approved
ToloxatoneToloxatone may increase the hypotensive activities of Debrisoquin.Approved
TolvaptanThe serum concentration of Debrisoquin can be increased when it is combined with Tolvaptan.Approved
TorasemideTorasemide may increase the hypotensive activities of Debrisoquin.Approved
TrandolaprilTrandolapril may increase the hypotensive activities of Debrisoquin.Approved
Trans-2-PhenylcyclopropylamineTrans-2-Phenylcyclopropylamine may increase the hypotensive activities of Debrisoquin.Experimental
TranylcypromineThe metabolism of Debrisoquin can be decreased when combined with Tranylcypromine.Approved
TravoprostTravoprost may increase the hypotensive activities of Debrisoquin.Approved
TrazodoneThe serum concentration of Debrisoquin can be decreased when it is combined with Trazodone.Approved, Investigational
TreprostinilTreprostinil may increase the hypotensive activities of Debrisoquin.Approved, Investigational
TrichlormethiazideTrichlormethiazide may increase the hypotensive activities of Debrisoquin.Approved, Vet Approved
TrifluoperazineThe serum concentration of Debrisoquin can be increased when it is combined with Trifluoperazine.Approved
TriflupromazineThe serum concentration of Debrisoquin can be increased when it is combined with Triflupromazine.Approved, Vet Approved
TrimazosinDebrisoquin may increase the hypotensive activities of Trimazosin.Experimental
TrimethaphanTrimethaphan may increase the hypotensive activities of Debrisoquin.Approved
TrimethoprimThe serum concentration of Debrisoquin can be decreased when it is combined with Trimethoprim.Approved, Vet Approved
TrimipramineThe serum concentration of Debrisoquin can be increased when it is combined with Trimipramine.Approved
TroleandomycinThe serum concentration of Debrisoquin can be increased when it is combined with Troleandomycin.Approved
UdenafilUdenafil may increase the antihypertensive activities of Debrisoquin.Approved, Investigational
UnoprostoneDebrisoquin may increase the hypotensive activities of Unoprostone.Approved
ValsartanValsartan may increase the hypotensive activities of Debrisoquin.Approved, Investigational
VardenafilVardenafil may increase the antihypertensive activities of Debrisoquin.Approved
VenlafaxineThe serum concentration of Debrisoquin can be increased when it is combined with Venlafaxine.Approved
VerapamilThe serum concentration of Debrisoquin can be decreased when it is combined with Verapamil.Approved
VinblastineThe serum concentration of Debrisoquin can be decreased when it is combined with Vinblastine.Approved
VincristineThe serum concentration of Debrisoquin can be decreased when it is combined with Vincristine.Approved, Investigational
VinorelbineThe serum concentration of Debrisoquin can be increased when it is combined with Vinorelbine.Approved, Investigational
VinpocetineDebrisoquin may increase the hypotensive activities of Vinpocetine.Investigational
XylometazolineDebrisoquin may increase the hypotensive activities of Xylometazoline.Approved
YohimbineYohimbine may decrease the antihypertensive activities of Debrisoquin.Approved, Vet Approved
ZimelidineThe serum concentration of Debrisoquin can be increased when it is combined with Zimelidine.Withdrawn
ZiprasidoneThe metabolism of Debrisoquin can be decreased when combined with Ziprasidone.Approved
Food Interactions
  • Take without regard to meals.
References
Synthesis Reference

Wenner,W.; U.S. Patent 3,157,573; November 17,1964; assigned to Hoffmann-LaRoche, Inc.

General ReferencesNot Available
External Links
ATC CodesC02CC04
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelNot Available
MSDSNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9714
Blood Brain Barrier+0.9106
Caco-2 permeable+0.5
P-glycoprotein substrateSubstrate0.8427
P-glycoprotein inhibitor INon-inhibitor0.8781
P-glycoprotein inhibitor IINon-inhibitor0.8382
Renal organic cation transporterInhibitor0.8817
CYP450 2C9 substrateNon-substrate0.8429
CYP450 2D6 substrateSubstrate0.8918
CYP450 3A4 substrateNon-substrate0.7101
CYP450 1A2 substrateNon-inhibitor0.9045
CYP450 2C9 inhibitorNon-inhibitor0.9549
CYP450 2D6 inhibitorNon-inhibitor0.9231
CYP450 2C19 inhibitorNon-inhibitor0.9026
CYP450 3A4 inhibitorNon-inhibitor0.9532
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.9462
Ames testNon AMES toxic0.7018
CarcinogenicityNon-carcinogens0.976
BiodegradationNot ready biodegradable0.9422
Rat acute toxicity2.7479 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.6904
hERG inhibition (predictor II)Inhibitor0.5928
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage formsNot Available
PricesNot Available
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point278-280 °CPhysProp
logP0.75SANGSTER (1994)
Predicted Properties
PropertyValueSource
Water Solubility0.842 mg/mLALOGPS
logP0.58ALOGPS
logP1.07ChemAxon
logS-2.3ALOGPS
pKa (Strongest Basic)12.47ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count3ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area53.11 Å2ChemAxon
Rotatable Bond Count0ChemAxon
Refractivity63.85 m3·mol-1ChemAxon
Polarizability19.48 Å3ChemAxon
Number of Rings2ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as tetrahydroisoquinolines. These are tetrahydrogenated isoquinoline derivatives.
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassTetrahydroisoquinolines
Sub ClassNot Available
Direct ParentTetrahydroisoquinolines
Alternative Parents
Substituents
  • Tetrahydroisoquinoline
  • Benzenoid
  • Tertiary amine
  • Guanidine
  • Azacycle
  • Carboximidamide
  • Hydrocarbon derivative
  • Organonitrogen compound
  • Imine
  • Amine
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External Descriptors

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inducer
General Function:
Norepinephrine:sodium symporter activity
Specific Function:
Amine transporter. Terminates the action of noradrenaline by its high affinity sodium-dependent reuptake into presynaptic terminals.
Gene Name:
SLC6A2
Uniprot ID:
P23975
Molecular Weight:
69331.42 Da
References
  1. Joyce PI, Rizzi D, Calo G, Rowbotham DJ, Lambert DG: The effect of guanethidine and local anesthetics on the electrically stimulated mouse vas deferens. Anesth Analg. 2002 Nov;95(5):1339-43, table of contents. [PubMed:12401623 ]
  2. Bryan-Lluka LJ, Seers H, Sharpe I: Amezinium and debrisoquine are substrates of uptake1 and potent inhibitors of monoamine oxidase in perfused lungs of rats. Naunyn Schmiedebergs Arch Pharmacol. 1996 Apr;353(5):536-44. [PubMed:8740147 ]
  3. Mitchell JR, Cavanaugh JH, Arias L, Oates JA: Guanethidine and related agents. 3. Antagonism by drugs which inhibit the norepinephrine pump in man. J Clin Invest. 1970 Aug;49(8):1596-604. [PubMed:5431666 ]
  4. Yi E, Love JA: Alpha-adrenergic modulation of synaptic transmission in rabbit pancreatic ganglia. Auton Neurosci. 2005 Oct 30;122(1-2):45-57. Epub 2005 Aug 25. [PubMed:16126010 ]
  5. Galli A, Blakely RD, DeFelice LJ: Norepinephrine transporters have channel modes of conduction. Proc Natl Acad Sci U S A. 1996 Aug 6;93(16):8671-6. [PubMed:8710929 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
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 antidepressants.
Gene Name:
CYP2D6
Uniprot ID:
P10635
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
substrate
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 unrelated compounds, including steroids, fatty acids, and xenobiotics.
Gene Name:
CYP1A1
Uniprot ID:
P04798
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
substrate
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
Molecular Weight:
141477.255 Da
References
  1. Kim RB, Wandel C, Leake B, Cvetkovic M, Fromm MF, Dempsey PJ, Roden MM, Belas F, Chaudhary AK, Roden DM, Wood AJ, Wilkinson GR: Interrelationship between substrates and inhibitors of human CYP3A and P-glycoprotein. Pharm Res. 1999 Mar;16(3):408-14. [PubMed:10213372 ]
Comments
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Drug created on September 26, 2007 09:28 / Updated on August 17, 2016 12:24