NAV

Flunarizine

Identification

Summary

Flunarizineis a selective calcium-entry blocker used as migraine prophylaxis in patients with severe and frequent episodes who have not responded adequately to more common treatments.

Generic Name
Flunarizine
DrugBank Accession Number
DB04841
Background

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
 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.

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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.

Target Actions Organism
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
ACalmodulin
antagonist
 Humans
UHistamine H1 receptor
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
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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.

Pathways
Pathway Category
Flunarizine H1-Antihistamine Action Drug action
Pharmacogenomic Effects/ADRsBrowse all" title="" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">
Not Available

Interactions

Drug InteractionsLearn More" title="" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
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.
Drug Interaction
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1,2-Benzodiazepine The risk or severity of CNS depression can be increased when Flunarizine is combined with 1,2-Benzodiazepine.
Abametapir 可以增加血清氟桂利嗪的浓度eased when it is combined with Abametapir.
Abatacept The metabolism of Flunarizine can be increased when combined with Abatacept.
Abiraterone 可以增加血清氟桂利嗪的浓度eased when it is combined with Abiraterone.
Abrocitinib The metabolism of Abrocitinib can be decreased when combined with Flunarizine.
Acarbose The risk or severity of hypoglycemia can be increased when Flunarizine is combined with Acarbose.
Acebutolol Acebutolol may increase the arrhythmogenic activities of Flunarizine.
Aceclofenac The risk or severity of hyperkalemia can be increased when Flunarizine is combined with Aceclofenac.
Acemetacin The risk or severity of hyperkalemia can be increased when Flunarizine is combined with Acemetacin.
Acenocoumarol The metabolism of Flunarizine can be decreased when combined with Acenocoumarol.
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Food Interactions
  • Avoid alcohol.
  • Take with or without food. The absorption is unaffected by food.

Products

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Product Ingredients
Ingredient UNII CAS InChI Key
Flunarizine dihydrochloride C11102TO53 30484-77-6 RXKMOPXNWTYEHI-RDRKJGRWSA-N
International/Other Brands
Flugeral (Italfarmaco)/Fluxarten (GlaxoSmithKline)/Gradient (Polifarma)/Sibelium (Janssen)/Zinasen (AtralCipan)
Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image
Flunarizine Capsule 5 mg Oral Aa Pharma Inc 2002-08-08 Not applicable Canada flag
Sibelium Cap 5mg Capsule 5 mg Oral Pharmascience Inc 1990-12-31 2009-01-29 Canada flag
Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image
Novo-flunarizine - Cap 5mg Capsule 5 mg Oral Novopharm Limited 1998-04-30 2015-10-26 Canada flag
Over the Counter Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image
FORKNOW TABLET 10 mg Tablet 10 mg Oral YUNG SHIN PHARMACEUTICAL (SINGAPORE) PTE LTD 1995-04-07 Not applicable
POLI-FLUNARIN CAPSULE 5 mg Capsule 5 mg Oral MD PHARMACEUTICALS PTE. LTD. 1997-07-23 Not applicable

Categories

ATC Codes
N07CA03 — Flunarizine
Drug Categories
Chemical TaxonomyProvided byClassyfire
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
二苯基甲烷s
Direct Parent
二苯基甲烷s
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/二苯基甲烷/Fluorobenzene/Halobenzene
Molecular Framework
Aromatic heteromonocyclic compounds
External Descriptors
Not Available
Affected organisms
  • Humans and other mammals

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

Clinical Trials

Clinical TrialsLearn More" title="" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
Phase Status Purpose Conditions Count
4 Completed Basic Science Chronic Migraine/Fibromyalgia/Pain, Chronic 1
4 Completed Treatment Chronic Migraine 1
4 Completed Treatment Schizophrenia 1
4 Recruiting Prevention Migraine in Adolescents 1
4 Recruiting Treatment Migraine 1
1 Completed Treatment Human Volunteers/Migraine 1
Not Available Completed Treatment Migraine 2

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
Form Route Strength
Capsule Oral 10 MG
Tablet Oral 11.4 mg
Capsule, coated Oral 5 mg
Tablet Oral 11.8 MG
Tablet Oral 10 MG
Capsule Oral
Tablet Oral
Tablet, film coated Oral
Tablet, film coated Oral 5 MG
Tablet Oral 5 MG
Capsule, coated Oral 10 mg
Tablet, coated Oral 5 mg
Capsule Oral 5 mg
Capsule, extended release 5 mg
Prices
Unit description Cost Unit
Apo-Flunarizine 5 mg Capsule 0.75USD capsule
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Not Available

Properties

State
Solid
Experimental Properties
Property Value Source
melting point (°C) 251.5 Janssen, P.A.J.; U.S. Patent 3,773,939; November 20, 1973; assigned to Janssen Pharmaceutica N.V.
logP 5.78 BIOBYTE (1995)
Predicted Properties
Property Value Source
Water Solubility 0.00168 mg/mL ALOGPS
logP 5.3 ALOGPS
logP 6.17 Chemaxon
logS -5.4 ALOGPS
pKa (Strongest Basic) 7.22 Chemaxon
Physiological Charge 1 Chemaxon
Hydrogen Acceptor Count 2 Chemaxon
Hydrogen Donor Count 0 Chemaxon
Polar Surface Area 6.48 Å2 Chemaxon
Rotatable Bond Count 6 Chemaxon
Refractivity 120.3 m3·mol-1 Chemaxon
Polarizability 44.2 Å3 Chemaxon
Number of Rings 4 Chemaxon
Bioavailability 1 Chemaxon
Rule of Five No Chemaxon
Ghose Filter No Chemaxon
Veber's Rule Yes Chemaxon
MDDR-like Rule Yes Chemaxon
Predicted ADMET Features
Property Value Probability
Human Intestinal Absorption + 0.9574
Blood Brain Barrier + 0.9789
Caco-2 permeable + 0.5893
P-glycoprotein substrate Substrate 0.7209
P-glycoprotein inhibitor I Inhibitor 0.9266
P-glycoprotein inhibitor II Non-inhibitor 0.6563
Renal organic cation transporter Inhibitor 0.7605
CYP450 2C9 substrate Non-substrate 0.8855
CYP450 2D6 substrate Substrate 0.8918
CYP450 3A4 substrate Non-substrate 0.7208
CYP450 1A2 substrate Inhibitor 0.9107
CYP450 2C9 inhibitor Non-inhibitor 0.9229
CYP450 2D6 inhibitor Inhibitor 0.9323
CYP450 2C19 inhibitor Non-inhibitor 0.9025
CYP450 3A4 inhibitor Non-inhibitor 0.9034
CYP450 inhibitory promiscuity High CYP Inhibitory Promiscuity 0.7304
Ames test Non AMES toxic 0.8902
Carcinogenicity Non-carcinogens 0.9422
Biodegradation Not ready biodegradable 1.0
Rat acute toxicity 2.3271 LD50, mol/kg Not applicable
hERG inhibition (predictor I) Strong inhibitor 0.5261
hERG inhibition (predictor II) Inhibitor 0.7549
ADMET data is predicted usingadmetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
Spectrum Spectrum Type Splash Key
Predicted GC-MS Spectrum - GC-MS Predicted GC-MS Not Available
Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS Not Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS Not Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS Not Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS Not Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS Not Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS Not Available
LC-MS/MS Spectrum - LC-ESI-ITFT , positive LC-MS/MS splash10-0udi-0090100000-cef5de63fdba54327f14

Targets

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insights and accelerate drug research.
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Details 1.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
分子量
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. [Article]
  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. [Article]
  3. Uebele VN主犯CE,福克斯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. [Article]
  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. [Article]
Details 2.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
分子量
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. [Article]
  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. [Article]
  3. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
  4. Uebele VN主犯CE,福克斯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. [Article]
  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. [Article]
Details 3.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
分子量
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. [Article]
  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. [Article]
  3. Uebele VN主犯CE,福克斯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. [Article]
  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. [Article]
Details 4.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
分子量
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. [Article]
  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. [Article]
  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. [Article]
Details 5.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
分子量
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. [Article]
  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. [Article]
  3. Taylor JE, Defeudis FV: Interactions of verapamil, D 600, flunarizine and nifedipine with cerebral histamine-receptors. Neurochem Int. 1986;9(3):379-81. [Article]

Enzymes

Details 1.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
分子量
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. [Article]
Details 2.Cytochrome P450 2D6
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Steroid hydroxylase activity
Specific Function
负责许多药物的代谢和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
分子量
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. [Article]
  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. [Article]
  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. [Article]
Details 3.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
分子量
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. [Article]
  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. [Article]
  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. [Article]
Details 4.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
分子量
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. [Article]
Details 5.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
分子量
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. [Article]
Details 6.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
分子量
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. [Article]
  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. [Article]

Drug created at September 27, 2007 13:47 / Updated at April 30, 2023 03:04