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Identification
NameFlunarizine
Accession NumberDB04841
TypeSmall Molecule
GroupsApproved
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.

Structure
Thumb
Synonyms
1-[bis(4-fluorophenyl)methyl]-4-[(2E)-3-phenylprop-2-en-1-yl]piperazine
Flunarizina
Flunarizinum
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Flunarizinecapsule5 mgoralAa Pharma Inc2002-08-08Not applicableCanada
Novo-flunarizine - Cap 5mgcapsule5 mgoralNovopharm Limited1998-04-302015-10-26Canada
Sibelium Cap 5mgcapsule5 mgoralPharmascience Inc1990-12-312009-01-29Canada
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
FlugeralItalfarmaco
FluxartenGlaxoSmithKline
GradientPolifarma
SibeliumJanssen
ZinasenAtralCipan
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Flunarizine dihydrochloride
Thumb
  • InChI Key: RXKMOPXNWTYEHI-RDRKJGRWSA-N
  • Monoisotopic Mass: 476.15976073
  • Average Mass: 477.417
DBSALT000382
Categories
UNIIR7PLA2DM0J
CAS number52468-60-7
WeightAverage: 404.4948
Monoisotopic: 404.206405252
Chemical FormulaC26H26F2N2
InChI KeyInChIKey=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
Taxonomy
DescriptionThis 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.
KingdomOrganic compounds
Super ClassBenzenoids
ClassBenzene and substituted derivatives
Sub ClassDiphenylmethanes
Direct ParentDiphenylmethanes
Alternative Parents
Substituents
  • Diphenylmethane
  • Phenylpropene
  • Styrene
  • Aralkylamine
  • N-alkylpiperazine
  • Halobenzene
  • Fluorobenzene
  • Piperazine
  • 1,4-diazinane
  • Aryl halide
  • Aryl fluoride
  • Tertiary aliphatic amine
  • Tertiary amine
  • Azacycle
  • Organoheterocyclic compound
  • Hydrocarbon derivative
  • Organonitrogen compound
  • Organofluoride
  • Organohalogen compound
  • Amine
  • Aromatic heteromonocyclic compound
Molecular FrameworkAromatic heteromonocyclic compounds
External DescriptorsNot Available
Pharmacology
IndicationUsed in the prophylaxis of migraine, occlusive peripheral vascular disease, vertigo of central and peripheral origin, and as an adjuvant in the therapy of epilepsy.
PharmacodynamicsFlunarizine is a selective calcium entry blocker with calmodulin binding properties and histamine H1 blocking activity.
Mechanism of actionFlunarizine 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.
Related Articles
Absorption85% following oral administration.
Volume of distributionNot Available
Protein binding99% bound to plasma proteins
Metabolism

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

SubstrateEnzymesProduct
Flunarizine
Flunarizine metabolite M1Details
Flunarizine
Flunarizine metabolite M2Details
Flunarizine
Flunarizine metabolite M3Details
Route of eliminationNot Available
Half life18 days
ClearanceNot Available
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
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
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 )
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage forms
FormRouteStrength
Capsuleoral5 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.
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point251.5Janssen, 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 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
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 ReferencesNot Available
External Links
ATC CodesN07CA03
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelNot Available
MSDSNot Available
Interactions
Drug Interactions
Drug
AcetaminophenThe metabolism of Flunarizine can be increased when combined with Acetaminophen.
AmobarbitalThe metabolism of Flunarizine can be increased when combined with Amobarbital.
Atracurium besylateFlunarizine may increase the neuromuscular blocking activities of Atracurium besylate.
AzelastineFlunarizine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
BaclofenThe risk or severity of adverse effects can be increased when Baclofen is combined with Flunarizine.
BrimonidineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Flunarizine.
BuprenorphineFlunarizine may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
ButabarbitalThe metabolism of Flunarizine can be increased when combined with Butabarbital.
ButalbitalThe metabolism of Flunarizine can be increased when combined with Butalbital.
CaffeineThe metabolism of Flunarizine can be increased when combined with Caffeine.
Calcium AcetateThe therapeutic efficacy of Flunarizine can be decreased when used in combination with Calcium Acetate.
Calcium carbonateThe therapeutic efficacy of Flunarizine can be decreased when used in combination with Calcium carbonate.
Calcium ChlorideThe therapeutic efficacy of Flunarizine can be decreased when used in combination with Calcium Chloride.
Calcium citrateThe therapeutic efficacy of Flunarizine can be decreased when used in combination with Calcium citrate.
Calcium gluconateThe therapeutic efficacy of Flunarizine can be decreased when used in combination with Calcium gluconate.
CarbamazepineThe serum concentration of Flunarizine can be decreased when it is combined with Carbamazepine.
CimetidineThe serum concentration of Flunarizine can be increased when it is combined with Cimetidine.
Cisatracurium besylateFlunarizine may increase the neuromuscular blocking activities of Cisatracurium besylate.
ClarithromycinThe metabolism of Flunarizine can be decreased when combined with Clarithromycin.
ClopidogrelThe therapeutic efficacy of Clopidogrel can be decreased when used in combination with Flunarizine.
DoxazosinDoxazosin may increase the hypotensive activities of Flunarizine.
DoxylamineDoxylamine may increase the central nervous system depressant (CNS depressant) activities of Flunarizine.
DronabinolDronabinol may increase the central nervous system depressant (CNS depressant) activities of Flunarizine.
DroperidolDroperidol may increase the central nervous system depressant (CNS depressant) activities of Flunarizine.
EfavirenzThe serum concentration of Flunarizine can be decreased when it is combined with Efavirenz.
ErythromycinThe metabolism of Flunarizine can be decreased when combined with Erythromycin.
EthanolFlunarizine may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
FluconazoleThe serum concentration of Flunarizine can be increased when it is combined with Fluconazole.
FosphenytoinThe serum concentration of Flunarizine can be decreased when it is combined with Fosphenytoin.
HydrocodoneFlunarizine may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
HydroxyzineHydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Flunarizine.
ItraconazoleThe risk or severity of adverse effects can be increased when Itraconazole is combined with Flunarizine.
KetoconazoleThe risk or severity of adverse effects can be increased when Ketoconazole is combined with Flunarizine.
LorazepamThe risk or severity of adverse effects can be increased when Lorazepam is combined with Flunarizine.
Magnesium chlorideThe risk or severity of adverse effects can be increased when Flunarizine is combined with Magnesium chloride.
Magnesium citrateThe risk or severity of adverse effects can be increased when Flunarizine is combined with Magnesium citrate.
Magnesium hydroxideThe risk or severity of adverse effects can be increased when Flunarizine is combined with Magnesium hydroxide.
Magnesium oxideThe risk or severity of adverse effects can be increased when Flunarizine is combined with Magnesium oxide.
Magnesium salicylateThe risk or severity of adverse effects can be increased when Flunarizine is combined with Magnesium salicylate.
Magnesium SulfateMagnesium Sulfate may increase the central nervous system depressant (CNS depressant) activities of Flunarizine.
MefloquineThe therapeutic efficacy of Flunarizine can be decreased when used in combination with Mefloquine.
MethohexitalThe metabolism of Flunarizine can be increased when combined with Methohexital.
MethotrimeprazineFlunarizine may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
MetyrosineFlunarizine may increase the sedative activities of Metyrosine.
MinocyclineMinocycline may increase the central nervous system depressant (CNS depressant) activities of Flunarizine.
MirtazapineFlunarizine may increase the central nervous system depressant (CNS depressant) activities of Mirtazapine.
NabiloneNabilone may increase the central nervous system depressant (CNS depressant) activities of Flunarizine.
NafcillinThe metabolism of Flunarizine can be increased when combined with Nafcillin.
NitroprussideFlunarizine may increase the hypotensive activities of Nitroprusside.
OrlistatThe serum concentration of Flunarizine can be decreased when it is combined with Orlistat.
OrphenadrineFlunarizine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
PancuroniumFlunarizine may increase the neuromuscular blocking activities of Pancuronium.
ParaldehydeFlunarizine may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.
ParoxetineThe risk or severity of adverse effects can be increased when Flunarizine is combined with Paroxetine.
PentobarbitalThe metabolism of Flunarizine can be increased when combined with Pentobarbital.
PerampanelPerampanel may increase the central nervous system depressant (CNS depressant) activities of Flunarizine.
PhenobarbitalThe metabolism of Flunarizine can be increased when combined with Phenobarbital.
PhenoxybenzaminePhenoxybenzamine may increase the hypotensive activities of Flunarizine.
PhentolaminePhentolamine may increase the hypotensive activities of Flunarizine.
PhenytoinThe serum concentration of Flunarizine can be decreased when it is combined with Phenytoin.
PosaconazoleThe risk or severity of adverse effects can be increased when Posaconazole is combined with Flunarizine.
PramipexoleFlunarizine may increase the sedative activities of Pramipexole.
PrazosinPrazosin may increase the hypotensive activities of Flunarizine.
RifabutinThe serum concentration of Flunarizine can be decreased when it is combined with Rifabutin.
RifampicinThe serum concentration of Flunarizine can be decreased when it is combined with Rifampicin.
RifapentineThe serum concentration of Flunarizine can be decreased when it is combined with Rifapentine.
RocuroniumFlunarizine may increase the neuromuscular blocking activities of Rocuronium.
RopiniroleFlunarizine may increase the sedative activities of Ropinirole.
RotigotineFlunarizine may increase the sedative activities of Rotigotine.
RufinamideThe risk or severity of adverse effects can be increased when Rufinamide is combined with Flunarizine.
SecobarbitalThe metabolism of Flunarizine can be increased when combined with Secobarbital.
SilodosinSilodosin may increase the hypotensive activities of Flunarizine.
Sodium oxybateSodium oxybate may increase the central nervous system depressant (CNS depressant) activities of Flunarizine.
SulfisoxazoleThe metabolism of Flunarizine can be decreased when combined with Sulfisoxazole.
SuvorexantFlunarizine may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
TamsulosinTamsulosin may increase the hypotensive activities of Flunarizine.
TapentadolTapentadol may increase the central nervous system depressant (CNS depressant) activities of Flunarizine.
TelithromycinThe metabolism of Flunarizine can be decreased when combined with Telithromycin.
TerazosinTerazosin may increase the hypotensive activities of Flunarizine.
ThalidomideFlunarizine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
VecuroniumFlunarizine may increase the neuromuscular blocking activities of Vecuronium.
VoriconazoleThe risk or severity of adverse effects can be increased when Voriconazole is combined with Flunarizine.
ZolpidemFlunarizine may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Food Interactions
  • Avoid alcohol.
  • Take without regard to meals.

Targets

Kind
Protein
Organism
Human
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, hormone or neurotransmitter release, gene expression, cell motility, cell division and cell death. The isoform alpha-1G gives rise to T-type calcium currents. T-type calcium channels belong to the "low-v...
Gene Name:
CACNA1G
Uniprot ID:
O43497
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 ]
Kind
Protein
Organism
Human
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, hormone or neurotransmitter release, gene expression, cell motility, cell division and cell death. The isoform alpha-1H gives rise to T-type calcium currents. T-type calcium channels belong to the "low-v...
Gene Name:
CACNA1H
Uniprot ID:
O95180
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 ]
Kind
Protein
Organism
Human
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, hormone or neurotransmitter release, gene expression, cell motility, cell division and cell death. Isoform alpha-1I gives rise to T-type calcium currents. T-type calcium channels belong to the "low-volta...
Gene Name:
CACNA1I
Uniprot ID:
Q9P0X4
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 ]
Kind
Protein
Organism
Human
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 catecholamine release from adrenal medulla, as well as mediating neurotransmission in the central nervous system.
Gene Name:
HRH1
Uniprot ID:
P35367
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 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
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 of protein kinases and phosphatases. Together with CCP110 and centrin, is involved in a genetic pathway that regulates the centrosome cycle and progression through cytokinesis.
Gene Name:
CALM1
Uniprot ID:
P62158
Molecular Weight:
16837.47 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 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Steroid hydroxylase activity
Specific Function:
Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic antidepressants.
Gene Name:
CYP2D6
Uniprot ID:
P10635
Molecular Weight:
55768.94 Da
References
  1. 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. 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. 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 ]
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. This enzyme contributes to the wide pharmacokinetics variability of the metabolism of drugs such as S-warfarin, diclofenac, phenyto...
Gene Name:
CYP2C9
Uniprot ID:
P11712
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. 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:
Vitamin d 24-hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics.
Gene Name:
CYP1A1
Uniprot ID:
P04798
Molecular Weight:
58164.815 Da
References
  1. 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. 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:
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. 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. 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:
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. Constitutes the major nicotine C-oxidase. Acts as a 1,4-cineole 2-exo-monooxygenase. Possesses low phenacetin O-deethylation activity.
Gene Name:
CYP2A6
Uniprot ID:
P11509
Molecular Weight:
56501.005 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. 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 ]
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Drug created on September 27, 2007 07:47 / Updated on August 17, 2016 12:24