You are using an unsupported browser. Please upgrade your browser to a newer version to get the best experience on DrugBank.
Identification
NameQuinacrine
Accession NumberDB01103  (APRD00317)
TypeSmall Molecule
GroupsApproved
DescriptionAn acridine derivative formerly widely used as an antimalarial but superseded by chloroquine in recent years. It has also been used as an anthelmintic and in the treatment of giardiasis and malignant effusions. It is used in cell biological experiments as an inhibitor of phospholipase A2. [PubChem]
Structure
Thumb
Synonyms
2-Methoxy-6-chloro-9-diethylaminopentylaminoacridine
3-chloro-7-Methoxy-9-(1-methyl-4-diethylaminobutylamino)acridine
6-chloro-9-((4-(Diethylamino)-1-methylbutyl)amino)-2-methoxyacridine
Mepacrine
N(4)-(6-chloro-2-Methoxy-9-acridinyl)-N(1),N(1)-diethyl-1,4-pentanediamine
Quinacrine
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
AtabrineNot Available
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Quinacrine Dihydrochloride
Thumb
  • InChI Key: UDKVBVICMUEIKS-UHFFFAOYNA-N
  • Monoisotopic Mass: 471.161095782
  • Average Mass: 472.879
DBSALT000420
Categories
UNIIH0C805XYDE
CAS number83-89-6
WeightAverage: 399.957
Monoisotopic: 399.207740304
Chemical FormulaC23H30ClN3O
InChI KeyGPKJTRJOBQGKQK-UHFFFAOYSA-N
InChI
InChI=1S/C23H30ClN3O/c1-5-27(6-2)13-7-8-16(3)25-23-19-11-9-17(24)14-22(19)26-21-12-10-18(28-4)15-20(21)23/h9-12,14-16H,5-8,13H2,1-4H3,(H,25,26)
IUPAC Name
6-chloro-N-[5-(diethylamino)pentan-2-yl]-2-methoxyacridin-9-amine
SMILES
CCN(CC)CCCC(C)NC1=C2C=C(OC)C=CC2=NC2=C1C=CC(Cl)=C2
Pharmacology
IndicationFor the treatment of giardiasis and cutaneous leishmaniasis and the management of malignant effusions.
Structured Indications Not Available
PharmacodynamicsQuinacrine has been used as an antimalarial drug and as an antibiotic. It is used to treat giardiasis, a protozoal infection of the intestinal tract, and certain types of lupus erythematosus, an inflammatory disease that affects the joints, tendons, and other connective tissues and organs. Quinacrine may be injected into the space surrounding the lungs to prevent reoccurrence of pneumothorax. The exact way in which quinacrine works is unknown. It appears to interfere with the parasite's metabolism.
Mechanism of actionThe exact mechanism of antiparasitic action is unknown; however, quinacrine binds to deoxyribonucleic acid (DNA) in vitro by intercalation between adjacent base pairs, inhibiting transcription and translation to ribonucleic acid (RNA). Quinacrine does not appear to localize to the nucleus of Giaridia trophozoites, suggesting that DNA binding may not be the primary mechanism of its antimicrobial action. Fluorescence studies using Giardia suggest that the outer membranes may be involved. Quinacrine inhibits succinate oxidation and interferes with electron transport. In addition, by binding to nucleoproteins, quinacrine suppress the lupus erythematous cell factor and acts as a strong inhibitor of cholinesterase.
TargetKindPharmacological actionActionsOrganismUniProt ID
DNANucleotideyes
intercalation
Humannot applicabledetails
85/88 kDa calcium-independent phospholipase A2Proteinyes
inhibitor
HumanO60733 details
Cytosolic phospholipase A2Proteinyes
inhibitor
HumanP47712 details
Inactive phospholipase C-like protein 1Proteinyes
inhibitor
HumanQ15111 details
Related Articles
AbsorptionAbsorbed rapidly from the gastrointestinal tract following oral administration.
Volume of distributionNot Available
Protein binding80-90%
MetabolismNot Available
Route of eliminationNot Available
Half life5 to 14 days
ClearanceNot Available
ToxicityOral, rat: LD50 = 900 mg/kg; Oral, mouse: LD50 = 1000 mg/kg. Symptoms of overdose include seizures, hypotension, cardiac arrhythmias, and cardiovascular collapse.
Affected organisms
  • Parasitic protozoa and helminths
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
Interactions
Drug Interactions
DrugInteractionDrug group
AcebutololThe serum concentration of Acebutolol can be increased when it is combined with Quinacrine.Approved
AcepromazineThe serum concentration of Acepromazine can be increased when it is combined with Quinacrine.Approved, Vet Approved
AceprometazineThe serum concentration of Aceprometazine can be increased when it is combined with Quinacrine.Approved
AcetaminophenThe serum concentration of Acetaminophen can be increased when it is combined with Quinacrine.Approved
AcetyldigitoxinAcetyldigitoxin may decrease the cardiotoxic activities of Quinacrine.Approved
Acetylsalicylic acidThe serum concentration of Acetylsalicylic acid can be increased when it is combined with Quinacrine.Approved, Vet Approved
AfatinibThe serum concentration of Afatinib can be increased when it is combined with Quinacrine.Approved
AldosteroneThe serum concentration of Aldosterone can be increased when it is combined with Quinacrine.Experimental
AlimemazineThe serum concentration of Alimemazine can be increased when it is combined with Quinacrine.Approved, Vet Approved
AlitretinoinThe serum concentration of Alitretinoin can be increased when it is combined with Quinacrine.Approved, Investigational
AmbrisentanThe serum concentration of Ambrisentan can be increased when it is combined with Quinacrine.Approved, Investigational
AmiodaroneThe metabolism of Quinacrine can be decreased when combined with Amiodarone.Approved, Investigational
AmitriptylineThe serum concentration of Amitriptyline can be increased when it is combined with Quinacrine.Approved
AmodiaquineThe serum concentration of Quinacrine can be decreased when it is combined with Amodiaquine.Approved
AnvirzelAnvirzel may decrease the cardiotoxic activities of Quinacrine.Investigational
ApixabanThe serum concentration of Apixaban can be increased when it is combined with Quinacrine.Approved
AprepitantThe serum concentration of Quinacrine can be increased when it is combined with Aprepitant.Approved, Investigational
Arsenic trioxideThe serum concentration of Arsenic trioxide can be increased when it is combined with Quinacrine.Approved, Investigational
ArtemetherThe risk or severity of adverse effects can be increased when Artemether is combined with Quinacrine.Approved
AtazanavirThe metabolism of Quinacrine can be decreased when combined with Atazanavir.Approved, Investigational
AtenololThe serum concentration of Atenolol can be increased when it is combined with Quinacrine.Approved
AtomoxetineThe metabolism of Quinacrine can be decreased when combined with Atomoxetine.Approved
AxitinibThe serum concentration of Axitinib can be increased when it is combined with Quinacrine.Approved, Investigational
BetamethasoneThe serum concentration of Betamethasone can be increased when it is combined with Quinacrine.Approved, Vet Approved
BevacizumabBevacizumab may increase the cardiotoxic activities of Quinacrine.Approved, Investigational
BexaroteneThe serum concentration of Quinacrine can be decreased when it is combined with Bexarotene.Approved, Investigational
BL-1020The serum concentration of BL-1020 can be increased when it is combined with Quinacrine.Investigational
BoceprevirThe metabolism of Quinacrine can be decreased when combined with Boceprevir.Approved
BortezomibThe metabolism of Quinacrine can be decreased when combined with Bortezomib.Approved, Investigational
BosentanThe serum concentration of Quinacrine can be decreased when it is combined with Bosentan.Approved, Investigational
BosutinibThe serum concentration of Bosutinib can be increased when it is combined with Quinacrine.Approved
Brentuximab vedotinThe serum concentration of Brentuximab vedotin can be increased when it is combined with Quinacrine.Approved
BromocriptineThe serum concentration of Bromocriptine can be increased when it is combined with Quinacrine.Approved, Investigational
CabazitaxelThe risk or severity of adverse effects can be increased when Cabazitaxel is combined with Quinacrine.Approved
CaffeineThe serum concentration of Caffeine can be increased when it is combined with Quinacrine.Approved
CamptothecinThe serum concentration of Camptothecin can be increased when it is combined with Quinacrine.Experimental
CanagliflozinThe serum concentration of Canagliflozin can be increased when it is combined with Quinacrine.Approved
CarbamazepineThe metabolism of Quinacrine can be increased when combined with Carbamazepine.Approved, Investigational
CarfilzomibThe serum concentration of Carfilzomib can be increased when it is combined with Quinacrine.Approved
CeritinibThe serum concentration of Quinacrine can be increased when it is combined with Ceritinib.Approved
CerivastatinThe serum concentration of Cerivastatin can be increased when it is combined with Quinacrine.Withdrawn
ChloroquineThe serum concentration of Quinacrine can be decreased when it is combined with Chloroquine.Approved, Vet Approved
ChlorpromazineThe serum concentration of Chlorpromazine can be increased when it is combined with Quinacrine.Approved, Vet Approved
CimetidineThe serum concentration of Cimetidine can be increased when it is combined with Quinacrine.Approved
CiprofloxacinThe serum concentration of Ciprofloxacin can be increased when it is combined with Quinacrine.Approved, Investigational
CisplatinThe serum concentration of Cisplatin can be increased when it is combined with Quinacrine.Approved
CitalopramThe serum concentration of Citalopram can be increased when it is combined with Quinacrine.Approved
ClarithromycinThe metabolism of Quinacrine can be decreased when combined with Clarithromycin.Approved
ClemastineThe metabolism of Quinacrine can be decreased when combined with Clemastine.Approved
ClobazamThe serum concentration of Clobazam can be increased when it is combined with Quinacrine.Approved, Illicit
ClomifeneThe serum concentration of Clomifene can be increased when it is combined with Quinacrine.Approved, Investigational
ClonidineThe serum concentration of Clonidine can be increased when it is combined with Quinacrine.Approved
ClopidogrelThe serum concentration of Clopidogrel can be increased when it is combined with Quinacrine.Approved, Nutraceutical
ClotrimazoleThe metabolism of Quinacrine can be decreased when combined with Clotrimazole.Approved, Vet Approved
ClozapineThe serum concentration of Clozapine can be increased when it is combined with Quinacrine.Approved
CobicistatThe metabolism of Quinacrine can be decreased when combined with Cobicistat.Approved
CobimetinibThe serum concentration of Cobimetinib can be increased when it is combined with Quinacrine.Approved
ColchicineThe serum concentration of Colchicine can be increased when it is combined with Quinacrine.Approved
ConivaptanThe serum concentration of Quinacrine can be increased when it is combined with Conivaptan.Approved, Investigational
Conjugated Equine EstrogensThe serum concentration of Conjugated Equine Estrogens can be increased when it is combined with Quinacrine.Approved
CrizotinibThe metabolism of Quinacrine can be decreased when combined with Crizotinib.Approved
CyclophosphamideCyclophosphamide may increase the cardiotoxic activities of Quinacrine.Approved, Investigational
CyclosporineThe metabolism of Quinacrine can be decreased when combined with Cyclosporine.Approved, Investigational, Vet Approved
Dabigatran etexilateThe serum concentration of the active metabolites of Dabigatran etexilate can be increased when Dabigatran etexilate is used in combination with Quinacrine.Approved
DabrafenibThe serum concentration of Quinacrine can be decreased when it is combined with Dabrafenib.Approved
DactinomycinThe serum concentration of Dactinomycin can be increased when it is combined with Quinacrine.Approved
DapagliflozinThe serum concentration of Dapagliflozin can be increased when it is combined with Quinacrine.Approved
DapsoneThe risk or severity of adverse effects can be increased when Quinacrine is combined with Dapsone.Approved, Investigational
DarunavirThe metabolism of Quinacrine can be decreased when combined with Darunavir.Approved
DasatinibThe serum concentration of Quinacrine can be increased when it is combined with Dasatinib.Approved, Investigational
DaunorubicinThe serum concentration of Daunorubicin can be increased when it is combined with Quinacrine.Approved
DebrisoquinThe serum concentration of Debrisoquin can be increased when it is combined with Quinacrine.Approved
DeferasiroxThe serum concentration of Quinacrine can be decreased when it is combined with Deferasirox.Approved, Investigational
DelavirdineThe metabolism of Quinacrine can be decreased when combined with Delavirdine.Approved
DeslanosideDeslanoside may decrease the cardiotoxic activities of Quinacrine.Approved
DexamethasoneThe serum concentration of Quinacrine can be decreased when it is combined with Dexamethasone.Approved, Investigational, Vet Approved
DiazepamThe serum concentration of Diazepam can be increased when it is combined with Quinacrine.Approved, Illicit, Vet Approved
DiethylstilbestrolThe serum concentration of Diethylstilbestrol can be increased when it is combined with Quinacrine.Approved
DigitoxinDigitoxin may decrease the cardiotoxic activities of Quinacrine.Approved
DigoxinDigoxin may decrease the cardiotoxic activities of Quinacrine.Approved
DihydroergotamineThe metabolism of Quinacrine can be decreased when combined with Dihydroergotamine.Approved
DihydrotestosteroneThe serum concentration of Dihydrotestosterone can be increased when it is combined with Quinacrine.Illicit
DiltiazemThe metabolism of Quinacrine can be decreased when combined with Diltiazem.Approved
DipyridamoleThe serum concentration of Dipyridamole can be increased when it is combined with Quinacrine.Approved
DocetaxelThe risk or severity of adverse effects can be increased when Docetaxel is combined with Quinacrine.Approved, Investigational
DomperidoneThe serum concentration of Domperidone can be increased when it is combined with Quinacrine.Approved, Investigational, Vet Approved
DoxorubicinThe serum concentration of Doxorubicin can be increased when it is combined with Quinacrine.Approved, Investigational
DoxycyclineThe metabolism of Quinacrine can be decreased when combined with Doxycycline.Approved, Investigational, Vet Approved
DronedaroneThe metabolism of Quinacrine can be decreased when combined with Dronedarone.Approved
EdoxabanThe serum concentration of Edoxaban can be increased when it is combined with Quinacrine.Approved
EfavirenzThe serum concentration of Quinacrine can be decreased when it is combined with Efavirenz.Approved, Investigational
EletriptanThe serum concentration of Eletriptan can be increased when it is combined with Quinacrine.Approved, Investigational
EnzalutamideThe serum concentration of Quinacrine can be decreased when it is combined with Enzalutamide.Approved
EpinastineThe serum concentration of Epinastine can be increased when it is combined with Quinacrine.Approved, Investigational
ErlotinibThe serum concentration of Erlotinib can be increased when it is combined with Quinacrine.Approved, Investigational
ErythromycinThe metabolism of Quinacrine can be decreased when combined with Erythromycin.Approved, Vet Approved
Eslicarbazepine acetateThe serum concentration of Quinacrine can be decreased when it is combined with Eslicarbazepine acetate.Approved
EstradiolThe serum concentration of Estradiol can be increased when it is combined with Quinacrine.Approved, Investigational, Vet Approved
EstriolThe serum concentration of Estriol can be increased when it is combined with Quinacrine.Approved, Vet Approved
EstroneThe serum concentration of Estrone can be increased when it is combined with Quinacrine.Approved
Ethinyl EstradiolThe serum concentration of Ethinyl Estradiol can be increased when it is combined with Quinacrine.Approved
EtoposideThe serum concentration of Etoposide can be increased when it is combined with Quinacrine.Approved
EtravirineThe serum concentration of Quinacrine can be decreased when it is combined with Etravirine.Approved
EverolimusThe serum concentration of Everolimus can be increased when it is combined with Quinacrine.Approved
EzetimibeThe serum concentration of Ezetimibe can be increased when it is combined with Quinacrine.Approved
FesoterodineThe serum concentration of Fesoterodine can be increased when it is combined with Quinacrine.Approved
FexofenadineThe serum concentration of Fexofenadine can be increased when it is combined with Quinacrine.Approved
FidaxomicinThe serum concentration of Fidaxomicin can be increased when it is combined with Quinacrine.Approved
FluconazoleThe metabolism of Quinacrine can be decreased when combined with Fluconazole.Approved
FluphenazineThe serum concentration of Fluphenazine can be increased when it is combined with Quinacrine.Approved
Fluticasone furoateThe serum concentration of Fluticasone furoate can be increased when it is combined with Quinacrine.Approved
FluvoxamineThe metabolism of Quinacrine can be decreased when combined with Fluvoxamine.Approved, Investigational
FosamprenavirThe metabolism of Quinacrine can be decreased when combined with Fosamprenavir.Approved
FosaprepitantThe serum concentration of Quinacrine can be increased when it is combined with Fosaprepitant.Approved
FosphenytoinThe metabolism of Quinacrine can be increased when combined with Fosphenytoin.Approved
Fusidic AcidThe serum concentration of Quinacrine can be increased when it is combined with Fusidic Acid.Approved
GefitinibThe serum concentration of Gefitinib can be increased when it is combined with Quinacrine.Approved, Investigational
GemcitabineThe serum concentration of Gemcitabine can be increased when it is combined with Quinacrine.Approved
GrazoprevirThe serum concentration of Grazoprevir can be increased when it is combined with Quinacrine.Approved
GrepafloxacinThe serum concentration of Grepafloxacin can be increased when it is combined with Quinacrine.Withdrawn
HaloperidolThe serum concentration of Haloperidol can be increased when it is combined with Quinacrine.Approved
HydrocortisoneThe serum concentration of Hydrocortisone can be increased when it is combined with Quinacrine.Approved, Vet Approved
HydroxychloroquineThe serum concentration of Quinacrine can be decreased when it is combined with Hydroxychloroquine.Approved
IbuprofenThe serum concentration of Ibuprofen can be increased when it is combined with Quinacrine.Approved
IdelalisibThe serum concentration of Quinacrine can be increased when it is combined with Idelalisib.Approved
ImatinibThe metabolism of Quinacrine can be decreased when combined with Imatinib.Approved
ImipramineThe serum concentration of Imipramine can be increased when it is combined with Quinacrine.Approved
IndacaterolThe serum concentration of Indacaterol can be increased when it is combined with Quinacrine.Approved
IndinavirThe metabolism of Quinacrine can be decreased when combined with Indinavir.Approved
IndomethacinThe serum concentration of Indomethacin can be increased when it is combined with Quinacrine.Approved, Investigational
IrinotecanThe serum concentration of Irinotecan can be increased when it is combined with Quinacrine.Approved, Investigational
IsavuconazoniumThe metabolism of Quinacrine can be decreased when combined with Isavuconazonium.Approved, Investigational
IsradipineThe metabolism of Quinacrine can be decreased when combined with Isradipine.Approved
ItraconazoleThe metabolism of Quinacrine can be decreased when combined with Itraconazole.Approved, Investigational
IvacaftorThe serum concentration of Quinacrine can be increased when it is combined with Ivacaftor.Approved
IvermectinThe serum concentration of Ivermectin can be increased when it is combined with Quinacrine.Approved, Vet Approved
KetazolamThe serum concentration of Ketazolam can be increased when it is combined with Quinacrine.Approved
KetoconazoleThe metabolism of Quinacrine can be decreased when combined with Ketoconazole.Approved, Investigational
LamivudineThe serum concentration of Lamivudine can be increased when it is combined with Quinacrine.Approved, Investigational
LamotrigineThe serum concentration of Lamotrigine can be increased when it is combined with Quinacrine.Approved, Investigational
LansoprazoleThe serum concentration of Lansoprazole can be increased when it is combined with Quinacrine.Approved, Investigational
LedipasvirThe serum concentration of Ledipasvir can be increased when it is combined with Quinacrine.Approved
LenalidomideThe serum concentration of Lenalidomide can be increased when it is combined with Quinacrine.Approved
LenvatinibThe serum concentration of Lenvatinib can be increased when it is combined with Quinacrine.Approved
LevetiracetamThe serum concentration of Levetiracetam can be increased when it is combined with Quinacrine.Approved, Investigational
LevofloxacinThe serum concentration of Levofloxacin can be increased when it is combined with Quinacrine.Approved, Investigational
LevomilnacipranThe serum concentration of Levomilnacipran can be increased when it is combined with Quinacrine.Approved
LinagliptinThe serum concentration of Linagliptin can be increased when it is combined with Quinacrine.Approved
LoperamideThe serum concentration of Loperamide can be increased when it is combined with Quinacrine.Approved
LopinavirThe metabolism of Quinacrine can be decreased when combined with Lopinavir.Approved
LosartanThe serum concentration of Losartan can be increased when it is combined with Quinacrine.Approved
LovastatinThe metabolism of Quinacrine can be decreased when combined with Lovastatin.Approved, Investigational
LuliconazoleThe serum concentration of Quinacrine can be increased when it is combined with Luliconazole.Approved
LumacaftorThe metabolism of Quinacrine can be increased when combined with Lumacaftor.Approved
LumefantrineThe risk or severity of adverse effects can be increased when Quinacrine is combined with Lumefantrine.Approved
MannitolThe serum concentration of Mannitol can be increased when it is combined with Quinacrine.Approved, Investigational
MesoridazineThe serum concentration of Mesoridazine can be increased when it is combined with Quinacrine.Approved
MethotrexateThe serum concentration of Methotrexate can be increased when it is combined with Quinacrine.Approved
MethotrimeprazineThe serum concentration of Methotrimeprazine can be increased when it is combined with Quinacrine.Approved
Methylene blueThe serum concentration of Methylene blue can be increased when it is combined with Quinacrine.Investigational
MethylprednisoloneThe serum concentration of Methylprednisolone can be increased when it is combined with Quinacrine.Approved, Vet Approved
MetoprololThe serum concentration of Metoprolol can be increased when it is combined with Quinacrine.Approved, Investigational
MidazolamThe serum concentration of Midazolam can be increased when it is combined with Quinacrine.Approved, Illicit
MifepristoneThe serum concentration of Quinacrine can be increased when it is combined with Mifepristone.Approved, Investigational
MirabegronThe serum concentration of Mirabegron can be increased when it is combined with Quinacrine.Approved
MitotaneThe serum concentration of Quinacrine can be decreased when it is combined with Mitotane.Approved
MitoxantroneThe serum concentration of Mitoxantrone can be increased when it is combined with Quinacrine.Approved, Investigational
ModafinilThe serum concentration of Quinacrine can be decreased when it is combined with Modafinil.Approved, Investigational
MoricizineThe serum concentration of Moricizine can be increased when it is combined with Quinacrine.Approved, Withdrawn
MorphineThe serum concentration of Morphine can be increased when it is combined with Quinacrine.Approved, Investigational
Mycophenolate mofetilThe serum concentration of Mycophenolate mofetil can be increased when it is combined with Quinacrine.Approved, Investigational
NadololThe serum concentration of Nadolol can be increased when it is combined with Quinacrine.Approved
NafcillinThe serum concentration of Quinacrine can be decreased when it is combined with Nafcillin.Approved
NaloxegolThe serum concentration of Naloxegol can be increased when it is combined with Quinacrine.Approved
NaloxoneThe serum concentration of Naloxone can be increased when it is combined with Quinacrine.Approved, Vet Approved
NefazodoneThe metabolism of Quinacrine can be decreased when combined with Nefazodone.Approved, Withdrawn
NelfinavirThe metabolism of Quinacrine can be decreased when combined with Nelfinavir.Approved
NetupitantThe serum concentration of Quinacrine can be increased when it is combined with Netupitant.Approved
NevirapineThe metabolism of Quinacrine can be increased when combined with Nevirapine.Approved
NicardipineThe serum concentration of Nicardipine can be increased when it is combined with Quinacrine.Approved
NifedipineThe serum concentration of Nifedipine can be increased when it is combined with Quinacrine.Approved
NilotinibThe metabolism of Quinacrine can be decreased when combined with Nilotinib.Approved, Investigational
NintedanibThe serum concentration of Nintedanib can be increased when it is combined with Quinacrine.Approved
NizatidineThe serum concentration of Nizatidine can be increased when it is combined with Quinacrine.Approved
OlanzapineThe serum concentration of Olanzapine can be increased when it is combined with Quinacrine.Approved, Investigational
OlaparibThe metabolism of Quinacrine can be decreased when combined with Olaparib.Approved
OmbitasvirThe serum concentration of Ombitasvir can be increased when it is combined with Quinacrine.Approved
OsimertinibThe serum concentration of Quinacrine can be increased when it is combined with Osimertinib.Approved
OuabainOuabain may decrease the cardiotoxic activities of Quinacrine.Approved
PaclitaxelThe risk or severity of adverse effects can be increased when Paclitaxel is combined with Quinacrine.Approved, Vet Approved
PalbociclibThe serum concentration of Quinacrine can be increased when it is combined with Palbociclib.Approved
PanobinostatThe serum concentration of Panobinostat can be increased when it is combined with Quinacrine.Approved, Investigational
PazopanibThe serum concentration of Pazopanib can be increased when it is combined with Quinacrine.Approved
PentobarbitalThe metabolism of Quinacrine can be increased when combined with Pentobarbital.Approved, Vet Approved
PerazineThe serum concentration of Perazine can be increased when it is combined with Quinacrine.Investigational
PerphenazineThe serum concentration of Perphenazine can be increased when it is combined with Quinacrine.Approved
PhenobarbitalThe metabolism of Quinacrine can be increased when combined with Phenobarbital.Approved
PhenytoinThe metabolism of Quinacrine can be increased when combined with Phenytoin.Approved, Vet Approved
PitavastatinThe serum concentration of Pitavastatin can be increased when it is combined with Quinacrine.Approved
PomalidomideThe serum concentration of Pomalidomide can be increased when it is combined with Quinacrine.Approved
PonatinibThe serum concentration of Ponatinib can be increased when it is combined with Quinacrine.Approved
PosaconazoleThe metabolism of Quinacrine can be decreased when combined with Posaconazole.Approved, Investigational, Vet Approved
PravastatinThe serum concentration of Pravastatin can be increased when it is combined with Quinacrine.Approved
PrazosinThe serum concentration of Prazosin can be increased when it is combined with Quinacrine.Approved
PrednisoloneThe serum concentration of Prednisolone can be increased when it is combined with Quinacrine.Approved, Vet Approved
PrednisoneThe serum concentration of Prednisone can be increased when it is combined with Quinacrine.Approved, Vet Approved
PrimaquineThe serum concentration of Quinacrine can be decreased when it is combined with Primaquine.Approved
PrimidoneThe metabolism of Quinacrine can be increased when combined with Primidone.Approved, Vet Approved
ProchlorperazineThe serum concentration of Prochlorperazine can be increased when it is combined with Quinacrine.Approved, Vet Approved
ProgesteroneThe serum concentration of Progesterone can be increased when it is combined with Quinacrine.Approved, Vet Approved
PromazineThe serum concentration of Promazine can be increased when it is combined with Quinacrine.Approved, Vet Approved
PromethazineThe serum concentration of Promethazine can be increased when it is combined with Quinacrine.Approved
PropiopromazineThe serum concentration of Propiopromazine can be increased when it is combined with Quinacrine.Vet Approved
PropranololThe serum concentration of Propranolol can be increased when it is combined with Quinacrine.Approved, Investigational
PrucaloprideThe serum concentration of Prucalopride can be increased when it is combined with Quinacrine.Approved
QuetiapineThe serum concentration of Quetiapine can be increased when it is combined with Quinacrine.Approved
QuinidineThe serum concentration of Quinidine can be increased when it is combined with Quinacrine.Approved
QuinineThe serum concentration of Quinine can be increased when it is combined with Quinacrine.Approved
RanitidineThe serum concentration of Ranitidine can be increased when it is combined with Quinacrine.Approved
RanolazineThe serum concentration of Ranolazine can be increased when it is combined with Quinacrine.Approved, Investigational
ReserpineThe serum concentration of Reserpine can be increased when it is combined with Quinacrine.Approved
RifabutinThe metabolism of Quinacrine can be increased when combined with Rifabutin.Approved
RifampicinThe metabolism of Quinacrine can be increased when combined with Rifampicin.Approved
RifapentineThe metabolism of Quinacrine can be increased when combined with Rifapentine.Approved
RifaximinThe serum concentration of Rifaximin can be increased when it is combined with Quinacrine.Approved, Investigational
RisperidoneThe serum concentration of Risperidone can be increased when it is combined with Quinacrine.Approved, Investigational
RitonavirThe metabolism of Quinacrine can be decreased when combined with Ritonavir.Approved, Investigational
RivaroxabanThe serum concentration of Rivaroxaban can be increased when it is combined with Quinacrine.Approved
RomidepsinThe serum concentration of Romidepsin can be increased when it is combined with Quinacrine.Approved, Investigational
Salicylic acidThe serum concentration of Salicylic acid can be increased when it is combined with Quinacrine.Approved, Vet Approved
SaquinavirThe metabolism of Quinacrine can be decreased when combined with Saquinavir.Approved, Investigational
SelexipagThe serum concentration of Selexipag can be increased when it is combined with Quinacrine.Approved
SildenafilThe metabolism of Quinacrine can be decreased when combined with Sildenafil.Approved, Investigational
SilodosinThe serum concentration of Silodosin can be increased when it is combined with Quinacrine.Approved
SiltuximabThe serum concentration of Quinacrine can be decreased when it is combined with Siltuximab.Approved
SimeprevirThe serum concentration of Quinacrine can be increased when it is combined with Simeprevir.Approved
SitagliptinThe serum concentration of Sitagliptin can be increased when it is combined with Quinacrine.Approved, Investigational
SofosbuvirThe serum concentration of Sofosbuvir can be increased when it is combined with Quinacrine.Approved
SorafenibThe serum concentration of Sorafenib can be increased when it is combined with Quinacrine.Approved, Investigational
SparfloxacinThe serum concentration of Sparfloxacin can be increased when it is combined with Quinacrine.Approved
SphingosineThe serum concentration of Sphingosine can be increased when it is combined with Quinacrine.Experimental
St. John's WortThe serum concentration of Quinacrine can be decreased when it is combined with St. John's Wort.Nutraceutical
StiripentolThe serum concentration of Quinacrine can be increased when it is combined with Stiripentol.Approved
SulfisoxazoleThe metabolism of Quinacrine can be decreased when combined with Sulfisoxazole.Approved, Vet Approved
TacrolimusThe serum concentration of Tacrolimus can be increased when it is combined with Quinacrine.Approved, Investigational
TamoxifenThe serum concentration of Tamoxifen can be increased when it is combined with Quinacrine.Approved
Taurocholic AcidThe serum concentration of Taurocholic Acid can be increased when it is combined with Quinacrine.Experimental
Technetium Tc-99m sestamibiThe serum concentration of Technetium Tc-99m sestamibi can be increased when it is combined with Quinacrine.Approved
TelaprevirThe metabolism of Quinacrine can be decreased when combined with Telaprevir.Approved
TelithromycinThe metabolism of Quinacrine can be decreased when combined with Telithromycin.Approved
TemsirolimusThe serum concentration of Temsirolimus can be increased when it is combined with Quinacrine.Approved
ThiethylperazineThe serum concentration of Thiethylperazine can be increased when it is combined with Quinacrine.Withdrawn
ThioridazineThe serum concentration of Thioridazine can be increased when it is combined with Quinacrine.Approved
TicagrelorThe serum concentration of Ticagrelor can be increased when it is combined with Quinacrine.Approved
TiclopidineThe metabolism of Quinacrine can be decreased when combined with Ticlopidine.Approved
TimololThe serum concentration of Timolol can be increased when it is combined with Quinacrine.Approved
TocilizumabThe serum concentration of Quinacrine can be decreased when it is combined with Tocilizumab.Approved
TolvaptanThe serum concentration of Tolvaptan can be increased when it is combined with Quinacrine.Approved
TopotecanThe serum concentration of Topotecan can be increased when it is combined with Quinacrine.Approved, Investigational
ToremifeneThe serum concentration of Toremifene can be increased when it is combined with Quinacrine.Approved, Investigational
TrastuzumabTrastuzumab may increase the cardiotoxic activities of Quinacrine.Approved, Investigational
Trastuzumab emtansineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Quinacrine.Approved
TrifluoperazineThe serum concentration of Trifluoperazine can be increased when it is combined with Quinacrine.Approved
TriflupromazineThe serum concentration of Triflupromazine can be increased when it is combined with Quinacrine.Approved, Vet Approved
UlipristalThe serum concentration of Ulipristal can be increased when it is combined with Quinacrine.Approved
UmeclidiniumThe serum concentration of Umeclidinium can be increased when it is combined with Quinacrine.Approved
VecuroniumThe serum concentration of Vecuronium can be increased when it is combined with Quinacrine.Approved
VenetoclaxThe serum concentration of Venetoclax can be increased when it is combined with Quinacrine.Approved
VenlafaxineThe metabolism of Quinacrine can be decreased when combined with Venlafaxine.Approved
VerapamilThe metabolism of Quinacrine can be decreased when combined with Verapamil.Approved
VinblastineThe serum concentration of Vinblastine can be increased when it is combined with Quinacrine.Approved
VincristineThe serum concentration of Vincristine can be increased when it is combined with Quinacrine.Approved, Investigational
VismodegibThe serum concentration of Vismodegib can be increased when it is combined with Quinacrine.Approved
VoriconazoleThe metabolism of Quinacrine can be decreased when combined with Voriconazole.Approved, Investigational
ZidovudineThe serum concentration of Zidovudine can be increased when it is combined with Quinacrine.Approved
ZiprasidoneThe metabolism of Quinacrine can be decreased when combined with Ziprasidone.Approved
Food InteractionsNot Available
References
Synthesis Reference

DrugSyn.org

US2113357
General References
  1. Canete R, Escobedo AA, Gonzalez ME, Almirall P: Randomized clinical study of five days apostrophe therapy with mebendazole compared to quinacrine in the treatment of symptomatic giardiasis in children. World J Gastroenterol. 2006 Oct 21;12(39):6366-70. [PubMed:17072963 ]
  2. Toubi E, Kessel A, Rosner I, Rozenbaum M, Paran D, Shoenfeld Y: The reduction of serum B-lymphocyte activating factor levels following quinacrine add-on therapy in systemic lupus erythematosus. Scand J Immunol. 2006 Apr;63(4):299-303. [PubMed:16623930 ]
  3. Zipper J, Cole LP, Goldsmith A, Wheeler R, Rivera M: Quinacrine hydrochloride pellets: preliminary data on a nonsurgical method of female sterilization. Int J Gynaecol Obstet. 1980;18(4):275-9. [PubMed:6109672 ]
  4. Bhatt RV: Camp laparoscopic sterilization deaths in Gujarat State, India, 1978-1980. Asia Oceania J Obstet Gynaecol. 1991 Dec;17(4):297-301. [PubMed:1839351 ]
  5. Peterson HB, Lubell I, DeStefano F, Ory HW: The safety and efficacy of tubal sterilization: an international overview. Int J Gynaecol Obstet. 1983 Apr;21(2):139-44. [PubMed:6136433 ]
External Links
ATC CodesP01AX05
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelNot Available
MSDSDownload (73.8 KB)
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9952
Blood Brain Barrier+0.9253
Caco-2 permeable+0.596
P-glycoprotein substrateSubstrate0.8401
P-glycoprotein inhibitor IInhibitor0.7537
P-glycoprotein inhibitor IIInhibitor0.8526
Renal organic cation transporterInhibitor0.6497
CYP450 2C9 substrateNon-substrate0.8442
CYP450 2D6 substrateNon-substrate0.9116
CYP450 3A4 substrateSubstrate0.701
CYP450 1A2 substrateInhibitor0.9107
CYP450 2C9 inhibitorNon-inhibitor0.9185
CYP450 2D6 inhibitorInhibitor0.8932
CYP450 2C19 inhibitorNon-inhibitor0.9025
CYP450 3A4 inhibitorNon-inhibitor0.9063
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.5494
Ames testAMES toxic0.9107
CarcinogenicityNon-carcinogens0.8806
BiodegradationNot ready biodegradable1.0
Rat acute toxicity2.8888 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Strong inhibitor0.585
hERG inhibition (predictor II)Inhibitor0.8622
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
Packagers
Dosage formsNot Available
Prices
Unit descriptionCostUnit
Quinacrine hcl powder8.11USD g
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point248-250 °CNot Available
water solubilitySlightNot Available
logP5.5Not Available
pKa10.3Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.00239 mg/mLALOGPS
logP6.13ALOGPS
logP5.15ChemAxon
logS-5.2ALOGPS
pKa (Strongest Basic)10.33ChemAxon
Physiological Charge2ChemAxon
Hydrogen Acceptor Count4ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area37.39 Å2ChemAxon
Rotatable Bond Count9ChemAxon
Refractivity118.96 m3·mol-1ChemAxon
Polarizability46.32 Å3ChemAxon
Number of Rings3ChemAxon
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 acridines. These are organic compounds containing the acridine moiety, a linear tricyclic heterocycle which consists of two benzene rings joined by a pyridine ring.
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassQuinolines and derivatives
Sub ClassBenzoquinolines
Direct ParentAcridines
Alternative Parents
Substituents
  • Acridine
  • Chloroquinoline
  • Hydroxyquinoline
  • Aminoquinoline
  • Anisole
  • Secondary aliphatic/aromatic amine
  • Chlorobenzene
  • Aminopyridine
  • Alkyl aryl ether
  • Benzenoid
  • Pyridine
  • Aryl halide
  • Aryl chloride
  • Heteroaromatic compound
  • Tertiary aliphatic amine
  • Tertiary amine
  • Azacycle
  • Secondary amine
  • Ether
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Organochloride
  • Organohalogen compound
  • Amine
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External DescriptorsNot Available

Targets

1. DNA
Kind
Nucleotide
Organism
Human
Pharmacological action
yes
Actions
intercalation
General Function:
Used for biological information storage.
Specific Function:
DNA contains the instructions needed for an organism to develop, survive and reproduce.
Molecular Weight:
2.15 x 1012 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284 ]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423 ]
  3. Hossain M, Giri P, Kumar GS: DNA intercalation by quinacrine and methylene blue: a comparative binding and thermodynamic characterization study. DNA Cell Biol. 2008 Feb;27(2):81-90. [PubMed:17924822 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Phospholipase a2 activity
Specific Function:
Catalyzes the release of fatty acids from phospholipids. It has been implicated in normal phospholipid remodeling, nitric oxide-induced or vasopressin-induced arachidonic acid release and in leukotriene and prostaglandin production. May participate in fas mediated apoptosis and in regulating transmembrane ion flux in glucose-stimulated B-cells. Has a role in cardiolipin (CL) deacylation. Requir...
Gene Name:
PLA2G6
Uniprot ID:
O60733
Molecular Weight:
89902.295 Da
References
  1. Nuttle LC, Ligon AL, Farrell KR, Hester RL: Inhibition of phospholipase A2 attenuates functional hyperemia in the hamster cremaster muscle. Am J Physiol. 1999 Apr;276(4 Pt 2):H1289-94. [PubMed:10199854 ]
  2. Sastry BV, Hemontolor ME, Vidaver PS, Sastry WS, Janson VE: Influence of halothane on phospholipase A2 and enzymatic methylations in the rat retinal membranes. J Ocul Pharmacol Ther. 1999 Apr;15(2):165-78. [PubMed:10229494 ]
  3. Lohmann CH, Sagun R Jr, Sylvia VL, Cochran DL, Dean DD, Boyan BD, Schwartz Z: Surface roughness modulates the response of MG63 osteoblast-like cells to 1,25-(OH)(2)D(3) through regulation of phospholipase A(2) activity and activation of protein kinase A. J Biomed Mater Res. 1999 Nov;47(2):139-51. [PubMed:10449625 ]
  4. Schwartz Z, Sylvia VL, Del Toro F, Hardin RR, Dean DD, Boyan BD: 24R,25-(OH)(2)D(3) mediates its membrane receptor-dependent effects on protein kinase C and alkaline phosphatase via phospholipase A(2) and cyclooxygenase-1 but not cyclooxygenase-2 in growth plate chondrocytes. J Cell Physiol. 2000 Mar;182(3):390-401. [PubMed:10653606 ]
  5. Sylvia VL, Del Toro F, Dean DD, Hardin RR, Schwartz Z, Boyan BD: Effects of 1alpha,25-(OH)(2)D(3) on rat growth zone chondrocytes are mediated via cyclooxygenase-1 and phospholipase A(2). J Cell Biochem Suppl. 2001;Suppl 36:32-45. [PubMed:11455568 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Phospholipase a2 activity
Specific Function:
Selectively hydrolyzes arachidonyl phospholipids in the sn-2 position releasing arachidonic acid. Together with its lysophospholipid activity, it is implicated in the initiation of the inflammatory response.
Gene Name:
PLA2G4A
Uniprot ID:
P47712
Molecular Weight:
85238.2 Da
References
  1. Hellstrand M, Eriksson E, Nilsson CL: Dopamine D(2) receptor-induced COX-2-mediated production of prostaglandin E(2) in D(2)-transfected Chinese hamster ovary cells without simultaneous administration of a Ca(2+)-mobilizing agent. Biochem Pharmacol. 2002 Jun 15;63(12):2151-8. [PubMed:12110374 ]
  2. Ong WY, Lu XR, Ong BK, Horrocks LA, Farooqui AA, Lim SK: Quinacrine abolishes increases in cytoplasmic phospholipase A2 mRNA levels in the rat hippocampus after kainate-induced neuronal injury. Exp Brain Res. 2003 Feb;148(4):521-4. Epub 2002 Dec 11. [PubMed:12582837 ]
  3. Kim BC, Kim JH: Exogenous C2-ceramide activates c-fos serum response element via Rac-dependent signalling pathway. Biochem J. 1998 Mar 1;330 ( Pt 2):1009-14. [PubMed:9480923 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Signal transducer activity
Specific Function:
Involved in an inositol phospholipid-based intracellular signaling cascade. Shows no PLC activity to phosphatidylinositol 4,5-bisphosphate and phosphatidylinositol. Component in the phospho-dependent endocytosis process of GABA A receptor (By similarity). Regulates the turnover of receptors and thus contributes to the maintenance of GABA-mediated synaptic inhibition. Its aberrant expression cou...
Gene Name:
PLCL1
Uniprot ID:
Q15111
Molecular Weight:
122726.98 Da
References
  1. Biondi C, Pavan B, Ferretti ME, Corradini FG, Neri LM, Vesce F: Formyl-methionyl-leucyl-phenylalanine induces prostaglandin E2 release from human amnion-derived WISH cells by phospholipase C-mediated [Ca+]i rise. Biol Reprod. 2001 Mar;64(3):865-70. [PubMed:11207202 ]
  2. Takuwa N, Kumada M, Yamashita K, Takuwa Y: Mechanisms of bombesin-induced arachidonate mobilization in Swiss 3T3 fibroblasts. J Biol Chem. 1991 Aug 5;266(22):14237-43. [PubMed:1860838 ]
  3. Otamiri T: Phospholipase C-mediated intestinal mucosal damage is ameliorated by quinacrine. Food Chem Toxicol. 1989 Jun;27(6):399-402. [PubMed:2551803 ]
  4. Noveral JP, Grunstein MM: Tachykinin regulation of airway smooth muscle cell proliferation. Am J Physiol. 1995 Sep;269(3 Pt 1):L339-43. [PubMed:7573467 ]
  5. Bjoro T, Englund K, Torjesen PA, Haug E: Inhibitors of the arachidonic acid metabolism attenuate the thyroliberin (TRH) stimulated prolactin production without modifying the production of inositolphosphates in GH4C1 pituitary cells. Scand J Clin Lab Invest. 1993 Apr;53(2):111-6. [PubMed:8469910 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Histamine n-methyltransferase activity
Specific Function:
Inactivates histamine by N-methylation. Plays an important role in degrading histamine and in regulating the airway response to histamine.
Gene Name:
HNMT
Uniprot ID:
P50135
Molecular Weight:
33294.765 Da
References
  1. Grassmann S, Apelt J, Sippl W, Ligneau X, Pertz HH, Zhao YH, Arrang JM, Ganellin CR, Schwartz JC, Schunack W, Stark H: Imidazole derivatives as a novel class of hybrid compounds with inhibitory histamine N-methyltransferase potencies and histamine hH3 receptor affinities. Bioorg Med Chem. 2003 May 15;11(10):2163-74. [PubMed:12713826 ]
  2. Hui JY, Taylor SL: Inhibition of in vivo histamine metabolism in rats by foodborne and pharmacologic inhibitors of diamine oxidase, histamine N-methyltransferase, and monoamine oxidase. Toxicol Appl Pharmacol. 1985 Nov;81(2):241-9. [PubMed:3933141 ]
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 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Oxygen binding
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics.
Gene Name:
CYP3A5
Uniprot ID:
P20815
Molecular Weight:
57108.065 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]

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. Sweet DH, Pritchard JB: rOCT2 is a basolateral potential-driven carrier, not an organic cation/proton exchanger. Am J Physiol. 1999 Dec;277(6 Pt 2):F890-8. [PubMed:10600936 ]
  2. Dohgu S, Yamauchi A, Takata F, Sawada Y, Higuchi S, Naito M, Tsuruo T, Shirabe S, Niwa M, Katamine S, Kataoka Y: Uptake and efflux of quinacrine, a candidate for the treatment of prion diseases, at the blood-brain barrier. Cell Mol Neurobiol. 2004 Apr;24(2):205-17. [PubMed:15176436 ]
  3. Beck WT, Cirtain MC, Glover CJ, Felsted RL, Safa AR: Effects of indole alkaloids on multidrug resistance and labeling of P-glycoprotein by a photoaffinity analog of vinblastine. Biochem Biophys Res Commun. 1988 Jun 30;153(3):959-66. [PubMed:2898941 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Xenobiotic-transporting atpase activity
Specific Function:
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name:
ABCB1
Uniprot ID:
P08183
Molecular Weight:
141477.255 Da
References
  1. Tiberghien F, Loor F: Ranking of P-glycoprotein substrates and inhibitors by a calcein-AM fluorometry screening assay. Anticancer Drugs. 1996 Jul;7(5):568-78. [PubMed:8862725 ]
Comments
comments powered by Disqus
Drug created on June 13, 2005 07:24 / Updated on August 17, 2016 12:23