NAV

Flunarizine

Targets (5)Enzymes (6)

Identification

Name
Flunarizine
Accession Number
DB04841
Description

Flunarizine is a selective calcium entry blocker with calmodulin binding properties and histamine H1 blocking activity. It is effective in the prophylaxis of migraine, occlusive peripheral vascular disease, vertigo of central and peripheral origin, and as an adjuvant in the therapy of epilepsy.

Type
Small Molecule
Groups
Approved
Structure
Thumb
3D
Similar Structures
Weight
Average: 404.4948
Monoisotopic: 404.206405252
Chemical Formula
C26H26F2N2
Synonyms
  • 1-[bis(4-fluorophenyl)methyl]-4-[(2E)-3-phenylprop-2-en-1-yl]piperazine
  • Flunarizina
  • Flunarizine
  • Flunarizinum

Pharmacology

Indication

Used in the prophylaxis of migraine, occlusive peripheral vascular disease, vertigo of central and peripheral origin, and as an adjuvant in the therapy of epilepsy.

Associated Conditions
Contraindications & Blackbox Warnings
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Pharmacodynamics

Flunarizine is a selective calcium entry blocker with calmodulin binding properties and histamine H1 blocking activity.

Mechanism of action

Flunarizine inhibits the influx of extracellular calcium through myocardial and vascular membrane pores by physically plugging the channel. The decrease in intracellular calcium inhibits the contractile processes of smooth muscle cells, causing dilation of the coronary and systemic arteries, increased oxygen delivery to the myocardial tissue, decreased total peripheral resistance, decreased systemic blood pressure, and decreased afterload.

TargetActionsOrganism
AVoltage-dependent T-type calcium channel subunit alpha-1G
inhibitor
Humans
AVoltage-dependent T-type calcium channel subunit alpha-1H
inhibitor
Humans
AVoltage-dependent T-type calcium channel subunit alpha-1I
inhibitor
Humans
UHistamine H1 receptor
antagonist
Humans
ACalmodulin
antagonist
Humans
Absorption

85% following oral administration.

Volume of distribution
Not Available
Protein binding

99% bound to plasma proteins

Metabolism

Hepatic, to two metabolites via N-dealylation and hydroxylation.

Hover over products below to view reaction partners

Route of elimination
Not Available
Half-life

18 days

Clearance
Not Available
Adverse Effects
Learn about our commercial Adverse Effects data.
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Toxicity

-Flunarizine should be used with care in patients with depression or those being prescribed other agents, such as phenothiazines, concurrently, which may cause extrapyramidal side-effects. -Acute overdosage has been reported and the observed symptoms were sedation, agitation and tachycardia. -Treatment of acute overdosage consists of charcoal administration, induction of emesis or gastric lavage, and supportive measures. No specific antidote is known.

Affected organisms
  • Humans and other mammals
Pathways
PathwayCategory
Flunarizine H1-Antihistamine ActionDrug action
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
DrugInteraction
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AbametapirThe serum concentration of Flunarizine can be increased when it is combined with Abametapir.
AbataceptThe metabolism of Flunarizine can be increased when combined with Abatacept.
AbirateroneThe serum concentration of Flunarizine can be increased when it is combined with Abiraterone.
AcarboseThe risk or severity of hypoglycemia can be increased when Flunarizine is combined with Acarbose.
AcebutololThe risk or severity of bradycardia can be increased when Flunarizine is combined with Acebutolol.
AceclofenacThe risk or severity of hyperkalemia can be increased when Flunarizine is combined with Aceclofenac.
AcemetacinThe risk or severity of hyperkalemia can be increased when Flunarizine is combined with Acemetacin.
AcenocoumarolThe metabolism of Acenocoumarol can be decreased when combined with Flunarizine.
AcetaminophenThe metabolism of Flunarizine can be decreased when combined with Acetaminophen.
AcetazolamideThe risk or severity of adverse effects can be increased when Acetazolamide is combined with Flunarizine.
Additional Data Available
  • Extended Description
    Extended Description
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    Extended description of the mechanism of action and particular properties of each drug interaction.

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  • Severity
    Severity
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    A severity rating for each drug interaction, from minor to major.

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  • Evidence Level
    Evidence Level
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    A rating for the strength of the evidence supporting each drug interaction.

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  • Action
    Action
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    An effect category for each drug interaction. Know how this interaction affects the subject drug.

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Food Interactions
  • Avoid alcohol.
  • Take with or without food. The absorption is unaffected by food.

Products

Product Ingredients
IngredientUNIICASInChI Key
Flunarizine dihydrochlorideC11102TO5330484-77-6RXKMOPXNWTYEHI-RDRKJGRWSA-N
International/Other Brands
Flugeral (Italfarmaco) / Fluxarten (GlaxoSmithKline) / Gradient (Polifarma) / Sibelium (Janssen) / Zinasen (AtralCipan)
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
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FlunarizineCapsuleOralAa Pharma Inc2002-08-08Not applicableCanada flag
Sibelium Cap 5mgCapsuleOralPharmascience Inc1990-12-312009-01-29Canada flag
Additional Data Available
  • Application Number
    Application Number
    Available for Purchase

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

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  • Product Code
    Product Code
    Available for Purchase

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

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Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Unlock Additional Data
Novo-flunarizine - Cap 5mgCapsuleOralNovopharm Limited1998-04-302015-10-26Canada flag
Additional Data Available
  • Application Number
    Application Number
    Available for Purchase

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

    Learn more
  • Product Code
    Product Code
    Available for Purchase

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

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Categories

ATC Codes
N07CA03 — Flunarizine
Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
This compound belongs to the class of organic compounds known as diphenylmethanes. These are compounds containing a diphenylmethane moiety, which consists of a methane wherein two hydrogen atoms are replaced by two phenyl groups.
Kingdom
Organic compounds
Super Class
Benzenoids
Class
Benzene and substituted derivatives
Sub Class
Diphenylmethanes
Direct Parent
Diphenylmethanes
Alternative Parents
Styrenes / N-alkylpiperazines / Fluorobenzenes / Aralkylamines / Aryl fluorides / Trialkylamines / Azacyclic compounds / Organopnictogen compounds / Organofluorides / Hydrocarbon derivatives
Substituents
1,4-diazinane / Amine / Aralkylamine / Aromatic heteromonocyclic compound / Aryl fluoride / Aryl halide / Azacycle / Diphenylmethane / Fluorobenzene / Halobenzene
Molecular Framework
Aromatic heteromonocyclic compounds
External Descriptors
Not Available

Chemical Identifiers

UNII
R7PLA2DM0J
CAS number
52468-60-7
InChI Key
SMANXXCATUTDDT-QPJJXVBHSA-N
InChI
InChI=1S/C26H26F2N2/c27-24-12-8-22(9-13-24)26(23-10-14-25(28)15-11-23)30-19-17-29(18-20-30)16-4-7-21-5-2-1-3-6-21/h1-15,26H,16-20H2/b7-4+
IUPAC Name
1-[bis(4-fluorophenyl)methyl]-4-[(2E)-3-phenylprop-2-en-1-yl]piperazine
SMILES
FC1=CC=C(C=C1)C(N1CCN(C\C=C\C2=CC=CC=C2)CC1)C1=CC=C(F)C=C1

References

Synthesis Reference

Matthew Peterson, Julius Remenar, Carlos Sanrame, "NOVEL FLUNARIZINE SALT FORMS AND METHODS OF MAKING AND USING THE SAME." U.S. Patent US20080200474, issued August 21, 2008.

US20080200474
General References
Not Available
Human Metabolome Database
HMDB0015589
KEGG Drug
D01303
PubChem Compound
941361
PubChem Substance
46507129
ChemSpider
819216
BindingDB
50017702
RxNav
4459
ChEBI
135652
ChEMBL
CHEMBL30008
ZINC
ZINC000019360739
Therapeutic Targets Database
DAP000142
PharmGKB
PA164776636
Drugs.com
Drugs.com Drug Page
Wikipedia
Flunarizine
AHFS Codes
  • 28:32.92 — Antimigraine Agents, Miscellaneous
  • 04:04.16 — Piperazine Derivatives

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4CompletedBasic ScienceChronic Migraine / Fibromyalgia / Pain, Chronic1
4CompletedPreventionTraumas / Wounds and Injuries1
4CompletedTreatmentChronic Migraine1
4CompletedTreatmentSchizophrenia1
4Not Yet RecruitingTreatmentMigraine1
4RecruitingPreventionAdolescent Migraine1
4RecruitingTreatmentSevere Sepsis or Septic Shock1
3CompletedPreventionPost-Dural Puncture Headache1
3CompletedTreatmentAnemia / Cardiovascular Disease (CVD) / Cerebrovascular Accident / Hematologic Diseases / Myocardial Infarction / Pneumonia / Thromboembolism1
3CompletedTreatmentCardiac Output, Low / Coronary Heart Disease (CHD)1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
TabletOral11.8 Mg
TabletOral5.9 MG
CapsuleOral
CapsuleOral5 MG
CapsuleOral10 MG
TabletOral11.4 mg
Capsule, coatedOral5 mg
Tablet, coatedOral5 mg
TabletOral10 mg
TabletOral5 mg
Capsule, extended releaseOral5 mg
Tablet, film coatedOral10 MG
Capsule, coatedOral10 mg
Tablet, film coatedOral5 MG
Prices
Unit descriptionCostUnit
Apo-Flunarizine 5 mg Capsule0.75USD capsule
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Not Available

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)251.5Janssen, P.A.J.; U.S. Patent 3,773,939; November 20, 1973; assigned to Janssen Pharmaceutica N.V.
logP5.78BIOBYTE (1995)
Predicted Properties
PropertyValueSource
Water Solubility0.00168 mg/mLALOGPS
logP5.3ALOGPS
logP6.17ChemAxon
logS-5.4ALOGPS
pKa (Strongest Basic)7.6ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count2ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area6.48 Å2ChemAxon
Rotatable Bond Count6ChemAxon
Refractivity120.3 m3·mol-1ChemAxon
Polarizability44.2 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
Rule of FiveNoChemAxon
Ghose FilterNoChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Predicted ADMET Features
PropertyValueProbability
Human Intestinal Absorption+0.9574
Blood Brain Barrier+0.9789
Caco-2 permeable+0.5893
P-glycoprotein substrateSubstrate0.7209
P-glycoprotein inhibitor IInhibitor0.9266
P-glycoprotein inhibitor IINon-inhibitor0.6563
Renal organic cation transporterInhibitor0.7605
CYP450 2C9 substrateNon-substrate0.8855
CYP450 2D6 substrateSubstrate0.8918
CYP450 3A4 substrateNon-substrate0.7208
CYP450 1A2 substrateInhibitor0.9107
CYP450 2C9 inhibitorNon-inhibitor0.9229
CYP450 2D6 inhibitorInhibitor0.9323
CYP450 2C19 inhibitorNon-inhibitor0.9025
CYP450 3A4 inhibitorNon-inhibitor0.9034
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.7304
Ames testNon AMES toxic0.8902
CarcinogenicityNon-carcinogens0.9422
BiodegradationNot ready biodegradable1.0
Rat acute toxicity2.3271 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Strong inhibitor0.5261
hERG inhibition (predictor II)Inhibitor0.7549
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-0udi-0090100000-cef5de63fdba54327f14

Targets

Details1. Voltage-dependent T-type calcium channel subunit alpha-1G
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Inhibitor
General Function
Scaffold protein binding
Specific Function
Voltage-sensitive calcium channels (VSCC) mediate the entry of calcium ions into excitable cells and are also involved in a variety of calcium-dependent processes, including muscle contraction, hor...
Gene Name
CACNA1G
Uniprot ID
O43497
Uniprot Name
Voltage-dependent T-type calcium channel subunit alpha-1G
Molecular Weight
262468.62 Da
References
  1. 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. Uebele VN, Nuss CE, Fox SV, Garson SL, Cristescu R, Doran SM, Kraus RL, Santarelli VP, Li Y, Barrow JC, Yang ZQ, Schlegel KA, Rittle KE, Reger TS, Bednar RA, Lemaire W, Mullen FA, Ballard JE, Tang C, Dai G, McManus OB, Koblan KS, Renger JJ: Positive allosteric interaction of structurally diverse T-type calcium channel antagonists. Cell Biochem Biophys. 2009;55(2):81-93. doi: 10.1007/s12013-009-9057-4. Epub 2009 Jul 7. [PubMed:19582593]
  4. Santi CM, Cayabyab FS, Sutton KG, McRory JE, Mezeyova J, Hamming KS, Parker D, Stea A, Snutch TP: Differential inhibition of T-type calcium channels by neuroleptics. J Neurosci. 2002 Jan 15;22(2):396-403. [PubMed:11784784]
Details2. Voltage-dependent T-type calcium channel subunit alpha-1H
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Inhibitor
General Function
Scaffold protein binding
Specific Function
Voltage-sensitive calcium channels (VSCC) mediate the entry of calcium ions into excitable cells and are also involved in a variety of calcium-dependent processes, including muscle contraction, hor...
Gene Name
CACNA1H
Uniprot ID
O95180
Uniprot Name
Voltage-dependent T-type calcium channel subunit alpha-1H
Molecular Weight
259160.2 Da
References
  1. 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. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
  4. Uebele VN, Nuss CE, Fox SV, Garson SL, Cristescu R, Doran SM, Kraus RL, Santarelli VP, Li Y, Barrow JC, Yang ZQ, Schlegel KA, Rittle KE, Reger TS, Bednar RA, Lemaire W, Mullen FA, Ballard JE, Tang C, Dai G, McManus OB, Koblan KS, Renger JJ: Positive allosteric interaction of structurally diverse T-type calcium channel antagonists. Cell Biochem Biophys. 2009;55(2):81-93. doi: 10.1007/s12013-009-9057-4. Epub 2009 Jul 7. [PubMed:19582593]
  5. Santi CM, Cayabyab FS, Sutton KG, McRory JE, Mezeyova J, Hamming KS, Parker D, Stea A, Snutch TP: Differential inhibition of T-type calcium channels by neuroleptics. J Neurosci. 2002 Jan 15;22(2):396-403. [PubMed:11784784]
Details3. Voltage-dependent T-type calcium channel subunit alpha-1I
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Inhibitor
General Function
Voltage-gated calcium channel activity
Specific Function
Voltage-sensitive calcium channels (VSCC) mediate the entry of calcium ions into excitable cells and are also involved in a variety of calcium-dependent processes, including muscle contraction, hor...
Gene Name
CACNA1I
Uniprot ID
Q9P0X4
Uniprot Name
Voltage-dependent T-type calcium channel subunit alpha-1I
Molecular Weight
245100.8 Da
References
  1. 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. Uebele VN, Nuss CE, Fox SV, Garson SL, Cristescu R, Doran SM, Kraus RL, Santarelli VP, Li Y, Barrow JC, Yang ZQ, Schlegel KA, Rittle KE, Reger TS, Bednar RA, Lemaire W, Mullen FA, Ballard JE, Tang C, Dai G, McManus OB, Koblan KS, Renger JJ: Positive allosteric interaction of structurally diverse T-type calcium channel antagonists. Cell Biochem Biophys. 2009;55(2):81-93. doi: 10.1007/s12013-009-9057-4. Epub 2009 Jul 7. [PubMed:19582593]
  4. Santi CM, Cayabyab FS, Sutton KG, McRory JE, Mezeyova J, Hamming KS, Parker D, Stea A, Snutch TP: Differential inhibition of T-type calcium channels by neuroleptics. J Neurosci. 2002 Jan 15;22(2):396-403. [PubMed:11784784]
Details4. Histamine H1 receptor
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Antagonist
General Function
Histamine receptor activity
Specific Function
In peripheral tissues, the H1 subclass of histamine receptors mediates the contraction of smooth muscles, increase in capillary permeability due to contraction of terminal venules, and catecholamin...
Gene Name
HRH1
Uniprot ID
P35367
Uniprot Name
Histamine H1 receptor
Molecular Weight
55783.61 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. Taylor JE, Defeudis FV: Interactions of verapamil, D 600, flunarizine and nifedipine with cerebral histamine-receptors. Neurochem Int. 1986;9(3):379-81. [PubMed:20493137]
Details5. Calmodulin
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Antagonist
General Function
Titin binding
Specific Function
Calmodulin mediates the control of a large number of enzymes, ion channels, aquaporins and other proteins by Ca(2+). Among the enzymes to be stimulated by the calmodulin-Ca(2+) complex are a number...
Gene Name
CALM1
Uniprot ID
P0DP23
Uniprot Name
Calmodulin
Molecular Weight
16837.47 Da
References
  1. Gajdus M, Szadujkis-Szadurski L, Szadujkis-Szadurski R, Glaza I, Zalewska M, Szadujkis-Szadurska K, Gurtowska N: Role of calcium and calmodulin in reaction of gastric fundus contraction. Postepy Hig Med Dosw (Online). 2011 Sep 5;65:569-73. doi: 10.5604/17322693.958061. [PubMed:21918260]
  2. Castellino SM, Friedman HS, Elion GB, Ong ET, Marcelli SL, Page R, Bigner DD, Dewhirst MW: Flunarizine enhancement of melphalan activity against drug-sensitive/resistant rhabdomyosarcoma. Br J Cancer. 1995 Jun;71(6):1181-7. doi: 10.1038/bjc.1995.230. [PubMed:7779708]
  3. Kavanagh BD, Coffey BE, Needham D, Hochmuth RM, Dewhirst MW: The effect of flunarizine on erythrocyte suspension viscosity under conditions of extreme hypoxia, low pH, and lactate treatment. Br J Cancer. 1993 Apr;67(4):734-41. doi: 10.1038/bjc.1993.134. [PubMed:8471430]

Enzymes

Details1. Cytochrome P450 2D6
Kind
Protein
Organism
Humans
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...
Gene Name
CYP2D6
Uniprot ID
P10635
Uniprot Name
Cytochrome P450 2D6
Molecular Weight
55768.94 Da
References
  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014]
  2. Narimatsu S, Kariya S, Isozaki S, Ohmori S, Kitada M, Hosokawa S, Masubuchi Y, Suzuki T: Involvement of CYP2D6 in oxidative metabolism of cinnarizine and flunarizine in human liver microsomes. Biochem Biophys Res Commun. 1993 Jun 30;193(3):1262-8. doi: 10.1006/bbrc.1993.1761. [PubMed:8323546]
  3. Kariya S, Isozaki S, Uchino K, Suzuki T, Narimatsu S: Oxidative metabolism of flunarizine and cinnarizine by microsomes from B-lymphoblastoid cell lines expressing human cytochrome P450 enzymes. Biol Pharm Bull. 1996 Nov;19(11):1511-4. doi: 10.1248/bpb.19.1511. [PubMed:8951176]
Details2. Cytochrome P450 2C9
Kind
Protein
Organism
Humans
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 un...
Gene Name
CYP2C9
Uniprot ID
P11712
Uniprot Name
Cytochrome P450 2C9
Molecular Weight
55627.365 Da
References
  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014]
  2. Rendic S: Summary of information on human CYP enzymes: human P450 metabolism data. Drug Metab Rev. 2002 Feb-May;34(1-2):83-448. [PubMed:11996015]
  3. Kariya S, Isozaki S, Uchino K, Suzuki T, Narimatsu S: Oxidative metabolism of flunarizine and cinnarizine by microsomes from B-lymphoblastoid cell lines expressing human cytochrome P450 enzymes. Biol Pharm Bull. 1996 Nov;19(11):1511-4. doi: 10.1248/bpb.19.1511. [PubMed:8951176]
Details3. Cytochrome P450 1A1
Kind
Protein
Organism
Humans
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 un...
Gene Name
CYP1A1
Uniprot ID
P04798
Uniprot Name
Cytochrome P450 1A1
Molecular Weight
58164.815 Da
References
  1. Kariya S, Isozaki S, Uchino K, Suzuki T, Narimatsu S: Oxidative metabolism of flunarizine and cinnarizine by microsomes from B-lymphoblastoid cell lines expressing human cytochrome P450 enzymes. Biol Pharm Bull. 1996 Nov;19(11):1511-4. doi: 10.1248/bpb.19.1511. [PubMed:8951176]
Details4. Cytochrome P450 1A2
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
Curator comments
Data is limited to in vitro studies.
General Function
Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP1A2
Uniprot ID
P05177
Uniprot Name
Cytochrome P450 1A2
Molecular Weight
58293.76 Da
References
  1. Kariya S, Isozaki S, Uchino K, Suzuki T, Narimatsu S: Oxidative metabolism of flunarizine and cinnarizine by microsomes from B-lymphoblastoid cell lines expressing human cytochrome P450 enzymes. Biol Pharm Bull. 1996 Nov;19(11):1511-4. doi: 10.1248/bpb.19.1511. [PubMed:8951176]
Details5. Cytochrome P450 2A6
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Steroid hydroxylase activity
Specific Function
Exhibits a high coumarin 7-hydroxylase activity. Can act in the hydroxylation of the anti-cancer drugs cyclophosphamide and ifosphamide. Competent in the metabolic activation of aflatoxin B1. Const...
Gene Name
CYP2A6
Uniprot ID
P11509
Uniprot Name
Cytochrome P450 2A6
Molecular Weight
56501.005 Da
References
  1. Rendic S: Summary of information on human CYP enzymes: human P450 metabolism data. Drug Metab Rev. 2002 Feb-May;34(1-2):83-448. [PubMed:11996015]
  2. Kariya S, Isozaki S, Uchino K, Suzuki T, Narimatsu S: Oxidative metabolism of flunarizine and cinnarizine by microsomes from B-lymphoblastoid cell lines expressing human cytochrome P450 enzymes. Biol Pharm Bull. 1996 Nov;19(11):1511-4. doi: 10.1248/bpb.19.1511. [PubMed:8951176]
Details6. Cytochrome P450 3A4
Kind
Protein
Organism
Humans
Pharmacological action
No
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 react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
Molecular Weight
57342.67 Da
References
  1. Uesawa Y, Takeuchi T, Mohri K: Integrated analysis on the physicochemical properties of dihydropyridine calcium channel blockers in grapefruit juice interactions. Curr Pharm Biotechnol. 2012 Jul;13(9):1705-17. [PubMed:22039822]

Drug created on September 27, 2007 07:47 / Updated on January 25, 2021 22:38