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Identification
NameDomperidone
Accession NumberDB01184  (APRD00418)
TypeSmall Molecule
GroupsApproved, Investigational, Vet Approved
Description

A specific blocker of dopamine receptors. It speeds gastrointestinal peristalsis, causes prolactin release, and is used as antiemetic and tool in the study of dopaminergic mechanisms. [PubChem]

Structure
Thumb
Synonyms
1-(3-(4-(5-chloro-2-oxo-2,3-Dihydrobenzo[D]imidazol-1-yl)piperidin-1-yl)propyl)-1H-benzo[D]imidazol-2(3H)-one
5-chloro-1-(1-(3-(2-oxo-1-Benzimidazolinyl)propyl)-4-piperidyl)-2-benzimidazolinone
5-chloro-1-(1-(3-(2-oxo-2,3-Dihydrobenzo[D]imidazol-1-yl)propyl)piperidin-4-yl)-1H-benzo[D]imidazol-2(3H)-one
5-chloro-1-{1-[3-(2-oxo-2,3-dihydro-benzoimidazol-1-yl)-propyl]-piperidin-4-yl}-1,3-dihydro-benzoimidazol-2-one
Domperidona
Domperidonum
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Ava-domperidonetablet10 mgoralAvanstra Inc2011-09-152014-08-21Canada
Bio-domperidonetablet10 mgoralBiomed PharmaNot applicableNot applicableCanada
Dom-domperidonetablet10 mgoralDominion Pharmacal1998-09-17Not applicableCanada
Domperidonetablet10 mgoralRanbaxy Pharmaceuticals Canada Inc.Not applicableNot applicableCanada
Domperidonetablet10 mgoralSanis Health Inc2010-05-12Not applicableCanada
Domperidonetablet10 mgoralSivem Pharmaceuticals Ulc1998-09-03Not applicableCanada
Domperidone-10tablet10 mgoralPro Doc Limitee1998-07-13Not applicableCanada
Ftp-domperidone Maleatetablet10 mgoralGmd Distribution Inc.1998-10-092005-08-05Canada
Ipg-domperidonetablet10 mgoralMarcan Pharmaceuticals IncNot applicableNot applicableCanada
Jamp-domperidonetablet10 mgoralJamp Pharma Corporation2011-10-07Not applicableCanada
Mar-domperidonetablet10 mgoralMarcan Pharmaceuticals Inc2014-01-02Not applicableCanada
Motilidonetablet10 mgoralTechnilab Pharma Inc.1997-09-172005-08-05Canada
Motilium Tab 10mgtablet10 mgoralJanssen Inc1990-12-312002-01-07Canada
Mylan-domperidonetablet10 mgoralMylan Pharmaceuticals Ulc2006-03-20Not applicableCanada
Nu-domperidone 10 Mg Tabletstablet10 mgoralNu Pharm Inc1998-03-182012-09-04Canada
PMS-domperidonetablet10 mgoralPharmascience Inc1997-11-13Not applicableCanada
Priva-domperidonetablet10 mgoralPharmapar IncNot applicableNot applicableCanada
Ran-domperidonetablet10 mgoralRanbaxy Pharmaceuticals Canada Inc.2005-07-05Not applicableCanada
Ratio-domperidonetablet10 mgoralTeva Canada Limited1993-12-31Not applicableCanada
Teva-domperidonetablet10 mgoralTeva Canada Limited1997-09-17Not applicableCanada
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo-domperidone - Tab 10mgtablet10 mgoralApotex Inc1997-09-17Not applicableCanada
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
EucitonRoux-Ocefa
MoperidonaSidus
MotiliumJanssen
NauzelinKyowa Hakko Kirin
Brand mixturesNot Available
SaltsNot Available
Categories
UNII5587267Z69
CAS number57808-66-9
WeightAverage: 425.911
Monoisotopic: 425.161852744
Chemical FormulaC22H24ClN5O2
InChI KeyInChIKey=FGXWKSZFVQUSTL-UHFFFAOYSA-N
InChI
InChI=1S/C22H24ClN5O2/c23-15-6-7-20-18(14-15)25-22(30)28(20)16-8-12-26(13-9-16)10-3-11-27-19-5-2-1-4-17(19)24-21(27)29/h1-2,4-7,14,16H,3,8-13H2,(H,24,29)(H,25,30)
IUPAC Name
5-chloro-1-{1-[3-(2-oxo-2,3-dihydro-1H-1,3-benzodiazol-1-yl)propyl]piperidin-4-yl}-2,3-dihydro-1H-1,3-benzodiazol-2-one
SMILES
ClC1=CC2=C(C=C1)N(C1CCN(CCCN3C(=O)NC4=CC=CC=C34)CC1)C(=O)N2
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as benzimidazoles. These are organic compounds containing a benzene ring fused to an imidazole ring (five member ring containing a nitrogen atom, 4 carbon atoms, and two double bonds).
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassBenzimidazoles
Sub ClassNot Available
Direct ParentBenzimidazoles
Alternative Parents
Substituents
  • Benzimidazole
  • Chlorobenzene
  • 4-aminopiperidine
  • Benzenoid
  • Piperidine
  • N-substituted imidazole
  • Aryl halide
  • Aryl chloride
  • Heteroaromatic compound
  • Imidazole
  • Azole
  • Urea
  • Tertiary aliphatic amine
  • Tertiary amine
  • Azacycle
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Organochloride
  • Organohalogen compound
  • Amine
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External Descriptors
Pharmacology
IndicationFor management of dyspepsia, heartburn, epigastric pain, nausea, and vomiting.
PharmacodynamicsDomperidone is a specific blocker of dopamine receptors. It speeds gastrointestinal peristalsis, causes prolactin release, and is used as antiemetic and tool in the study of dopaminergic mechanisms.
Mechanism of actionDomperidone acts as a gastrointestinal emptying (delayed) adjunct and peristaltic stimulant. The gastroprokinetic properties of domperidone are related to its peripheral dopamine receptor blocking properties. Domperidone facilitates gastric emptying and decreases small bowel transit time by increasing esophageal and gastric peristalsis and by lowering esophageal sphincter pressure. Antiemetic: The antiemetic properties of domperidone are related to its dopamine receptor blocking activity at both the chemoreceptor trigger zone and at the gastric level. It has strong affinities for the D2 and D3 dopamine receptors, which are found in the chemoreceptor trigger zone, located just outside the blood brain barrier, which - among others - regulates nausea and vomiting
Related Articles
AbsorptionFast
Volume of distributionNot Available
Protein binding91%-93%
Metabolism
SubstrateEnzymesProduct
Domperidone
5-Chloro-1,3-dihydro-1-(4-piperidinyl)-2H-benzimidazol-2-oneDetails
Route of eliminationNot Available
Half life7 hours
ClearanceNot Available
ToxicitySide effects include galactorrhea, gynecomastia, or menstrual irregularities.
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9967
Blood Brain Barrier+0.8686
Caco-2 permeable-0.8957
P-glycoprotein substrateSubstrate0.7029
P-glycoprotein inhibitor IInhibitor0.7244
P-glycoprotein inhibitor IIInhibitor0.628
Renal organic cation transporterInhibitor0.6546
CYP450 2C9 substrateNon-substrate0.7974
CYP450 2D6 substrateNon-substrate0.9117
CYP450 3A4 substrateSubstrate0.6392
CYP450 1A2 substrateInhibitor0.8737
CYP450 2C9 inhibitorNon-inhibitor0.9071
CYP450 2D6 inhibitorInhibitor0.8933
CYP450 2C19 inhibitorNon-inhibitor0.9025
CYP450 3A4 inhibitorInhibitor0.5577
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.8695
Ames testNon AMES toxic0.6608
CarcinogenicityNon-carcinogens0.922
BiodegradationNot ready biodegradable1.0
Rat acute toxicity1.9828 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Strong inhibitor0.7527
hERG inhibition (predictor II)Inhibitor0.917
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
Packagers
  • Professional Co.
Dosage forms
FormRouteStrength
Tabletoral10 mg
Prices
Unit descriptionCostUnit
Domperidone bp powder55.2USD g
Ratio-Domperidone Maleate 10 mg Tablet0.16USD tablet
Apo-Domperidone 10 mg Tablet0.16USD tablet
Mylan-Domperidone 10 mg Tablet0.16USD tablet
Novo-Domperidone 10 mg Tablet0.16USD tablet
Nu-Domperidone 10 mg Tablet0.16USD tablet
Pms-Domperidone 10 mg Tablet0.15USD tablet
Ran-Domperidone 10 mg Tablet0.15USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point242.5 °CVanderberk, J., Kennis, L.E.J., Van der Aa, M.J.M.C. and Van Heertum, A.H.M.T.; U.S. Patents 4,066,772; January 3,1978; 4.1 10,333; August 29,1978; 4,126,687; November 21, 1978; 4,126,688; November 21,1978; 4,160,836; July 10,1979 and 4,175,129; November 20,1979; all assigned to Janssen Pharmaceutica NV (Belgium).
water solubility0.986 mg/LNot Available
logP3.90EL TAYER,N ET AL. (1985)
pKa7.9EL TAYAR,N ET AL. (1985)
Predicted Properties
PropertyValueSource
Water Solubility0.0925 mg/mLALOGPS
logP3.7ALOGPS
logP2.9ChemAxon
logS-3.7ALOGPS
pKa (Strongest Acidic)12.52ChemAxon
pKa (Strongest Basic)7.03ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count3ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area67.92 Å2ChemAxon
Rotatable Bond Count5ChemAxon
Refractivity119.37 m3·mol-1ChemAxon
Polarizability45.61 Å3ChemAxon
Number of Rings5ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
References
Synthesis Reference

Vanderberk, J., Kennis, L.E.J., Van der Aa, M.J.M.C. and Van Heertum, A.H.M.T.; U.S. Patents 4,066,772; January 3,1978; 4.1 10,333; August 29,1978; 4,126,687; November 21, 1978; 4,126,688; November 21,1978; 4,160,836; July 10,1979 and 4,175,129; November 20,1979; all assigned to Janssen Pharmaceutica NV (Belgium).

General References
  1. Silvers D, Kipnes M, Broadstone V, Patterson D, Quigley EM, McCallum R, Leidy NK, Farup C, Liu Y, Joslyn A: Domperidone in the management of symptoms of diabetic gastroparesis: efficacy, tolerability, and quality-of-life outcomes in a multicenter controlled trial. DOM-USA-5 Study Group. Clin Ther. 1998 May-Jun;20(3):438-53. [PubMed:9663360 ]
External Links
ATC CodesA03FA03
AHFS Codes
  • 56:32.00
  • 56:92.00
PDB EntriesNot Available
FDA labelNot Available
MSDSDownload (73.8 KB)
Interactions
Drug Interactions
Drug
AprepitantThe serum concentration of Domperidone can be increased when it is combined with Aprepitant.
AtazanavirThe serum concentration of Domperidone can be increased when it is combined with Atazanavir.
BoceprevirThe serum concentration of Domperidone can be increased when it is combined with Boceprevir.
CeritinibThe serum concentration of Domperidone can be increased when it is combined with Ceritinib.
CitalopramCitalopram may increase the QTc-prolonging activities of Domperidone.
ClarithromycinThe serum concentration of Domperidone can be increased when it is combined with Clarithromycin.
CobicistatThe serum concentration of Domperidone can be increased when it is combined with Cobicistat.
ConivaptanThe serum concentration of Domperidone can be increased when it is combined with Conivaptan.
CrizotinibThe serum concentration of Domperidone can be increased when it is combined with Crizotinib.
DarunavirThe serum concentration of Domperidone can be increased when it is combined with Darunavir.
DelavirdineThe serum concentration of Domperidone can be increased when it is combined with Delavirdine.
DiltiazemThe serum concentration of Domperidone can be increased when it is combined with Diltiazem.
DofetilideDofetilide may increase the QTc-prolonging activities of Domperidone.
DronedaroneThe serum concentration of Domperidone can be increased when it is combined with Dronedarone.
ErythromycinThe serum concentration of Domperidone can be increased when it is combined with Erythromycin.
FluconazoleThe serum concentration of Domperidone can be increased when it is combined with Fluconazole.
FosamprenavirThe serum concentration of Domperidone can be increased when it is combined with Fosamprenavir.
FosaprepitantThe serum concentration of Domperidone can be increased when it is combined with Fosaprepitant.
Fusidic AcidThe serum concentration of Domperidone can be increased when it is combined with Fusidic Acid.
GoserelinGoserelin may increase the QTc-prolonging activities of Domperidone.
IdelalisibThe serum concentration of Domperidone can be increased when it is combined with Idelalisib.
ImatinibThe serum concentration of Domperidone can be increased when it is combined with Imatinib.
IndinavirThe serum concentration of Domperidone can be increased when it is combined with Indinavir.
IsavuconazoniumThe serum concentration of Domperidone can be increased when it is combined with Isavuconazonium.
IsocarboxazidThe risk or severity of adverse effects can be increased when Isocarboxazid is combined with Domperidone.
ItraconazoleThe serum concentration of Domperidone can be increased when it is combined with Itraconazole.
IvabradineIvabradine may increase the QTc-prolonging activities of Domperidone.
IvacaftorThe serum concentration of Domperidone can be increased when it is combined with Ivacaftor.
KetoconazoleThe serum concentration of Domperidone can be increased when it is combined with Ketoconazole.
LeuprolideLeuprolide may increase the QTc-prolonging activities of Domperidone.
LinezolidThe risk or severity of adverse effects can be increased when Linezolid is combined with Domperidone.
LuliconazoleThe serum concentration of Domperidone can be increased when it is combined with Luliconazole.
MifepristoneThe serum concentration of Domperidone can be increased when it is combined with Mifepristone.
MoclobemideThe risk or severity of adverse effects can be increased when Moclobemide is combined with Domperidone.
NefazodoneThe serum concentration of Domperidone can be increased when it is combined with Nefazodone.
NelfinavirThe serum concentration of Domperidone can be increased when it is combined with Nelfinavir.
NilotinibThe serum concentration of Domperidone can be increased when it is combined with Nilotinib.
OctreotideOctreotide may increase the QTc-prolonging activities of Domperidone.
PalbociclibThe serum concentration of Domperidone can be increased when it is combined with Palbociclib.
PhenelzineThe risk or severity of adverse effects can be increased when Phenelzine is combined with Domperidone.
PosaconazoleThe serum concentration of Domperidone can be increased when it is combined with Posaconazole.
ProcarbazineThe risk or severity of adverse effects can be increased when Procarbazine is combined with Domperidone.
RasagilineThe risk or severity of adverse effects can be increased when Rasagiline is combined with Domperidone.
RitonavirThe serum concentration of Domperidone can be increased when it is combined with Ritonavir.
SaquinavirThe serum concentration of Domperidone can be increased when it is combined with Saquinavir.
SelegilineThe risk or severity of adverse effects can be increased when Selegiline is combined with Domperidone.
SimeprevirThe serum concentration of Domperidone can be increased when it is combined with Simeprevir.
StiripentolThe serum concentration of Domperidone can be increased when it is combined with Stiripentol.
Tedizolid PhosphateThe risk or severity of adverse effects can be increased when Tedizolid Phosphate is combined with Domperidone.
TelaprevirThe serum concentration of Domperidone can be increased when it is combined with Telaprevir.
TelithromycinThe serum concentration of Domperidone can be increased when it is combined with Telithromycin.
TranylcypromineThe risk or severity of adverse effects can be increased when Tranylcypromine is combined with Domperidone.
VerapamilThe serum concentration of Domperidone can be increased when it is combined with Verapamil.
VoriconazoleThe serum concentration of Domperidone can be increased when it is combined with Voriconazole.
Food Interactions
  • Take 15 to 30 minutes before meals.

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
antagonist
General Function:
Potassium channel regulator activity
Specific Function:
Dopamine receptor whose activity is mediated by G proteins which inhibit adenylyl cyclase.
Gene Name:
DRD2
Uniprot ID:
P14416
Molecular Weight:
50618.91 Da
References
  1. Cavallotti C, Nuti F, Bruzzone P, Mancone M: Age-related changes in dopamine D2 receptors in rat heart and coronary vessels. Clin Exp Pharmacol Physiol. 2002 May-Jun;29(5-6):412-8. [PubMed:12010185 ]
  2. Osinski MA, Uchic ME, Seifert T, Shaughnessy TK, Miller LN, Nakane M, Cox BF, Brioni JD, Moreland RB: Dopamine D2, but not D4, receptor agonists are emetogenic in ferrets. Pharmacol Biochem Behav. 2005 May;81(1):211-9. [PubMed:15894081 ]
  3. de Mey C, Enterling D, Meineke I, Yeulet S: Interactions between domperidone and ropinirole, a novel dopamine D2-receptor agonist. Br J Clin Pharmacol. 1991 Oct;32(4):483-8. [PubMed:1683559 ]
  4. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
  5. Ali I, Gupta VK, Singh P, Pant HV: Screening of domperidone in wastewater by high performance liquid chromatography and solid phase extraction methods. Talanta. 2006 Jan 15;68(3):928-31. doi: 10.1016/j.talanta.2005.06.027. Epub 2005 Jul 22. [PubMed:18970411 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
antagonist
General Function:
G-protein coupled amine receptor activity
Specific Function:
Dopamine receptor whose activity is mediated by G proteins which inhibit adenylyl cyclase. Promotes cell proliferation.
Gene Name:
DRD3
Uniprot ID:
P35462
Molecular Weight:
44224.335 Da
References
  1. Freedman SB, Patel S, Marwood R, Emms F, Seabrook GR, Knowles MR, McAllister G: Expression and pharmacological characterization of the human D3 dopamine receptor. J Pharmacol Exp Ther. 1994 Jan;268(1):417-26. [PubMed:8301582 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Vitamin d3 25-hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
Molecular Weight:
57342.67 Da
References
  1. Chang SY, Fancher RM, Zhang H, Gan J: Mechanism-based inhibition of human cytochrome P4503A4 by domperidone. Xenobiotica. 2010 Feb;40(2):138-45. doi: 10.3109/00498250903406762. [PubMed:20082577 ]
  2. 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 ]
  3. Simard C, Michaud V, Gibbs B, Masse R, Lessard E, Turgeon J: Identification of the cytochrome P450 enzymes involved in the metabolism of domperidone. Xenobiotica. 2004 Nov-Dec;34(11-12):1013-23. [PubMed:15801545 ]
  4. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
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. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
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:
CYP3A7
Uniprot ID:
P24462
Molecular Weight:
57525.03 Da
References
  1. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. Most active in catalyzing 2-hydroxylation. Caffeine is metabolized primarily by cytochrome CYP1A2 in the liver through an initial N...
Gene Name:
CYP1A2
Uniprot ID:
P05177
Molecular Weight:
58293.76 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Steroid 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. Acts as a 1,4-cineole 2-exo-monooxygenase.
Gene Name:
CYP2B6
Uniprot ID:
P20813
Molecular Weight:
56277.81 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:
Steroid 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. In the epoxidation of arachidonic acid it generates only 14,15- and 11,12-cis-epoxyeicosatrienoic acids. It is the principal enzyme...
Gene Name:
CYP2C8
Uniprot ID:
P10632
Molecular Weight:
55824.275 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:
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 ]

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. Faassen F, Vogel G, Spanings H, Vromans H: Caco-2 permeability, P-glycoprotein transport ratios and brain penetration of heterocyclic drugs. Int J Pharm. 2003 Sep 16;263(1-2):113-22. [PubMed:12954186 ]
  2. Schinkel AH, Wagenaar E, Mol CA, van Deemter L: P-glycoprotein in the blood-brain barrier of mice influences the brain penetration and pharmacological activity of many drugs. J Clin Invest. 1996 Jun 1;97(11):2517-24. [PubMed:8647944 ]
Comments
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Drug created on June 13, 2005 07:24 / Updated on April 15, 2014 14:42