Identification

Name
Fluphenazine
Accession Number
DB00623  (APRD00633)
Type
Small Molecule
Groups
Approved
Description

A phenothiazine used in the treatment of psychoses. Its properties and uses are generally similar to those of chlorpromazine. [PubChem]

Structure
Thumb
Synonyms
  • 1-(2-Hydroxyethyl)-4-(3-(trifluoromethyl-10-phenothiazinyl)propyl)-piperazine
  • 10-(3-(2-Hydroxyethyl)piperazinopropyl)-2-(trifluoromethyl)phenothiazine
  • 10-(3'-(4''-(beta-hydroxyethyl)-1''-piperazinyl)-propyl)-3-trifluoromethylphenothiazine
  • 2-(4-(3-[2-(Trifluoromethyl)-10H-phenothiazin-10-yl]propyl)-1-piperazinyl)ethanol
  • 2-(Trifluoromethyl)-10-(3-(1-(beta-hydroxyethyl)-4-piperazinyl)propyl)phenothiazine
  • 4-(3-(-Trifluoromethyl-10-phenothiazyl)-propyl)-1-piperazineethanol
  • 4-(3-(2-(Trifluoromethyl)-10H-phenothiazin-10-yl)propyl)-1-piperazineethanol
  • 4-(3-(2-Trifluoromethyl-10-phenothiazyl)-propyl)-1-piperazineethanol
  • Flufenazina
  • Fluorfenazine
  • Fluorophenazine
  • Fluorphenazine
  • Fluphenazin
  • Fluphénazine
  • Fluphenazinum
  • Triflumethazine
External IDs
SQ 10733 / Squibb 16144
Product Ingredients
IngredientUNIICASInChI Key
Fluphenazine decanoateFMU62K1L3C5002-47-1VIQCGTZFEYDQMR-UHFFFAOYSA-N
Fluphenazine dihydrochlorideZOU145W1XL146-56-5MBHNWCYEGXQEIT-UHFFFAOYSA-N
Fluphenazine enanthateQSB34YF0W92746-81-8LRWSFOSWNAQHHW-UHFFFAOYSA-N
Fluphenazine hydrochlorideNot AvailableNot AvailableNot applicable
Product Images
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo Fluphenazine Tab 2.5mgTablet2.5 mgOralApotex Corporation1977-12-31Not applicableCanada
FluphenazineTablet5 mgOralAa Pharma Inc1977-12-31Not applicableCanada
FluphenazineTablet1 mgOralAa Pharma Inc1977-12-31Not applicableCanada
FluphenazineTablet2 mgOralAa Pharma Inc1977-12-31Not applicableCanada
Fluphenazine 1 Tab 1mgTablet1 mgOralPro Doc Limitee1982-12-312010-07-13Canada
Fluphenazine 2 Tab 2mgTablet2 mgOralPro Doc Limitee1982-12-312010-07-13Canada
Fluphenazine 5 Tab 5mgTablet5 mgOralPro Doc Limitee1982-12-312010-07-13Canada
Fluphenazine Decanoate Injection B.P.Liquid25 mgIntramuscular; SubcutaneousHospira, Inc.Not applicableNot applicableCanada
Fluphenazine Decanoate Injection B.P.Liquid100 mgIntramuscular; SubcutaneousHospira, Inc.Not applicableNot applicableCanada
Fluphenazine Decanoate Injection, USPSolution25 mgIntramuscular; SubcutaneousMylan PharmaceuticalsNot applicableNot applicableCanada
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo-fluphenazine InjectableLiquid25 mgIntramuscular; SubcutaneousApotex Corporation2001-10-052013-08-02Canada
Fluphenazine DecanoateInjection, solution25 mg/1mLIntramuscular; SubcutaneousTYA Pharmaceuticals2010-12-15Not applicableUs
Fluphenazine DecanoateInjection, solution25 mg/1mLIntramuscular; SubcutaneousMylan Institutional LLC2018-09-28Not applicableUs
Fluphenazine DecanoateInjection25 mg/1mLIntramuscular; SubcutaneousWest-Ward Pharmaceuticals Corp1996-08-30Not applicableUs
Fluphenazine DecanoateInjection, solution125 mg/5mLIntramuscular; SubcutaneousAuro Medics Pharma Llc2017-10-17Not applicableUs
Fluphenazine decanoateInjection25 mg/1mLIntramuscular; SubcutaneousTeva Parenteral Medicines, Inc.1996-09-102005-08-29Us
Fluphenazine DecanoateInjection, solution25 mg/1mLIntramuscular; SubcutaneousFresenius Kabi2010-12-15Not applicableUs
Fluphenazine DecanoateInjection, solution25 mg/1mLIntramuscular; SubcutaneousPar Pharmaceutical2018-06-26Not applicableUs
Fluphenazine DecanoateInjection25 mg/1mLIntramuscular; SubcutaneousBedford Pharmaceuticals1996-08-302009-11-30Us
Fluphenazine HydrochlorideTablet1 mg/1OralRemedy Repack2011-08-022012-08-03Us
International/Other Brands
Anatensol (Bristol-Myers Squibb) / Dapotum D / Fludecasin (Tanabe Mitsubishi Pharma) / Fludecate (Rafa) / Flumezin (Tanabe Mitsubishi Pharma) / Funazine (Johnson) / Lyogen (Lundbeck) / Lyogen Depot (Lundbeck) / Lyogen Retard (Lundbeck) / Metoten (Hemofarm) / Modecate (Bristol-Myers Squibb) / Moditen (Bristol-Myers Squibb) / Moditen Depo (Krka) / Permitil / Prolixin (Bristol-Myers Squibb)
Categories
UNII
S79426A41Z
CAS number
69-23-8
Weight
Average: 437.522
Monoisotopic: 437.174867774
Chemical Formula
C22H26F3N3OS
InChI Key
PLDUPXSUYLZYBN-UHFFFAOYSA-N
InChI
InChI=1S/C22H26F3N3OS/c23-22(24,25)17-6-7-21-19(16-17)28(18-4-1-2-5-20(18)30-21)9-3-8-26-10-12-27(13-11-26)14-15-29/h1-2,4-7,16,29H,3,8-15H2
IUPAC Name
2-(4-{3-[2-(trifluoromethyl)-10H-phenothiazin-10-yl]propyl}piperazin-1-yl)ethan-1-ol
SMILES
OCCN1CCN(CCCN2C3=CC=CC=C3SC3=C2C=C(C=C3)C(F)(F)F)CC1

Pharmacology

Indication

For management of manifestations of psychotic disorders.

Associated Conditions
Pharmacodynamics

Fluphenazine is a trifluoro-methyl phenothiazine derivative intended for the management of schizophrenia and other psychotic disorders. Fluphenazine has not been shown effective in the management of behaviorial complications in patients with mental retardation.

Mechanism of action

Fluphenazine blocks postsynaptic mesolimbic dopaminergic D1 and D2 receptors in the brain; depresses the release of hypothalamic and hypophyseal hormones and is believed to depress the reticular activating system thus affecting basal metabolism, body temperature, wakefulness, vasomotor tone, and emesis.

TargetActionsOrganism
AD(2) dopamine receptor
antagonist
Human
AD(1A) dopamine receptor
antagonist
Human
UCalmodulin
inhibitor
Human
UAndrogen receptorNot AvailableHuman
U5-hydroxytryptamine receptor 2ANot AvailableHuman
U5-hydroxytryptamine receptor 2CNot AvailableHuman
Absorption
Not Available
Volume of distribution
Not Available
Protein binding
Not Available
Metabolism
Route of elimination
Not Available
Half life
Not Available
Clearance
Not Available
Toxicity
Not Available
Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteraction
2,5-Dimethoxy-4-ethylamphetamineFluphenazine may decrease the stimulatory activities of 2,5-Dimethoxy-4-ethylamphetamine.
2,5-Dimethoxy-4-ethylthioamphetamineThe risk or severity of adverse effects can be increased when Fluphenazine is combined with 2,5-Dimethoxy-4-ethylthioamphetamine.
3,4-MethylenedioxyamphetamineFluphenazine may decrease the stimulatory activities of 3,4-Methylenedioxyamphetamine.
3,5-DinitrocatecholThe therapeutic efficacy of 3,5-Dinitrocatechol can be decreased when used in combination with Fluphenazine.
4-Bromo-2,5-dimethoxyamphetamineThe risk or severity of adverse effects can be increased when Fluphenazine is combined with 4-Bromo-2,5-dimethoxyamphetamine.
4-MethoxyamphetamineThe risk or severity of adverse effects can be increased when Fluphenazine is combined with 4-Methoxyamphetamine.
5-methoxy-N,N-dimethyltryptamineThe risk or severity of adverse effects can be increased when Fluphenazine is combined with 5-methoxy-N,N-dimethyltryptamine.
7-NitroindazoleThe risk or severity of adverse effects can be increased when Fluphenazine is combined with 7-Nitroindazole.
7,8-Dichloro-1,2,3,4-tetrahydroisoquinolineThe risk or severity of adverse effects can be increased when Fluphenazine is combined with 7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline.
AbemaciclibThe serum concentration of Abemaciclib can be increased when it is combined with Fluphenazine.
Food Interactions
  • Avoid alcohol.
  • Take with food to reduce irritation.

References

Synthesis Reference

Ullyot, G.E.; U.S. Patent 3,058,979; October 16, 1962; assigned to Smith Kline & French Laboratories.

US3058979
General References
Not Available
External Links
Human Metabolome Database
HMDB0014761
KEGG Compound
C07010
PubChem Compound
3372
PubChem Substance
46506645
ChemSpider
3255
BindingDB
78433
ChEBI
5123
ChEMBL
CHEMBL726
Therapeutic Targets Database
DCL000806
PharmGKB
PA449676
IUPHAR
204
Guide to Pharmacology
GtP Drug Page
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Fluphenazine
ATC Codes
N05AB02 — Fluphenazine
AHFS Codes
  • 28:16.08.24 — Phenothiazines

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1Unknown StatusTreatmentMultiple Myeloma (MM)1
1, 2CompletedTreatmentMultiple Myeloma and Plasma Cell Neoplasm1
2CompletedDiagnosticPathological Gambling1
2CompletedTreatmentPsoriasis1
2TerminatedTreatmentPsoriasis1
3CompletedTreatmentSchizophrenic Disorders1
3TerminatedTreatmentAnxiety Disorders / Dementias / Depression / Psychosomatic Disorders / Schizophrenic Disorders1
4CompletedTreatmentSchizoaffective Disorders / Schizophrenia and Disorders With Psychotic Features / Schizophrenic Disorders1
4CompletedTreatmentSchizophrenic Disorders1
Not AvailableCompletedNot AvailableBipolar Disorder (BD) / Psychotic Disorder NOS / Schizoaffective Disorders / Schizophrenic Disorders / Type 2 Diabetes Mellitus1
Not AvailableCompletedNot AvailableSchizophrenic Disorders1

Pharmacoeconomics

Manufacturers
  • App pharmaceuticals llc
  • Bedford laboratories div ben venue laboratories inc
  • Claris lifesciences ltd
  • Hospira inc
  • Teva parenteral medicines inc
  • Bristol myers squibb co
  • Apothecon inc div bristol myers squibb
  • Pharmaceutical assoc inc div beach products
  • Teva pharmaceuticals usa
  • Lannett holdings inc
  • Mylan pharmaceuticals inc
  • Sandoz inc
  • Watson laboratories inc
Packagers
  • Amerisource Health Services Corp.
  • Apotex Inc.
  • APP Pharmaceuticals
  • APPD
  • Bedford Labs
  • Ben Venue Laboratories Inc.
  • Comprehensive Consultant Services Inc.
  • Dept Health Central Pharmacy
  • Direct Dispensing Inc.
  • E.R. Squibb and Sons LLC
  • Heartland Repack Services LLC
  • Major Pharmaceuticals
  • Murfreesboro Pharmaceutical Nursing Supply
  • Mylan
  • Novex Pharma
  • Pharmaceutical Association
  • Physicians Total Care Inc.
  • Prepackage Specialists
  • Prepak Systems Inc.
  • Remedy Repack
  • Sandoz
  • Superior Pharmeceuticals
  • Teva Pharmaceutical Industries Ltd.
  • UDL Laboratories
  • United Research Laboratories Inc.
  • Vangard Labs Inc.
Dosage forms
FormRouteStrength
TabletOral2.5 mg
LiquidIntramuscular; Subcutaneous25 mg
TabletOral1 mg
TabletOral2 mg
InjectionIntramuscular; Subcutaneous25 mg/1mL
Injection, solutionIntramuscular; Subcutaneous125 mg/5mL
Injection, solutionIntramuscular; Subcutaneous25 mg/1mL
ElixirOral0.5 mg/1mL
Injection, solutionIntramuscular2.5 mg/1mL
TabletOral1 mg/1
TabletOral10 mg/1
TabletOral2.5 mg/1
TabletOral2.50 mg/1
TabletOral5 mg/1
Tablet, film coatedOral1 mg/1
Tablet, film coatedOral10 mg/1
Tablet, film coatedOral2.5 mg/1
Tablet, film coatedOral5 mg/1
LiquidIntramuscular; Subcutaneous100 mg
LiquidIntramuscular25 mg
TabletOral10 mg
TabletOral5 mg
ElixirOral.5 mg
Solution, concentrateOral5 mg/1mL
SolutionIntramuscular; Subcutaneous25 mg
SolutionIntramuscular; Subcutaneous100 mg
Prices
Unit descriptionCostUnit
Fluphenazine Omega 100 mg/ml31.2USD ml
Modecate Concentrate 100 mg/ml31.2USD ml
Pms-Fluphenazine Decanoate 100 mg/ml31.2USD ml
Fluphenazine Decanoate 25 mg/ml Solution14.0USD ml
Fluphenazine 2.5 mg/ml vial7.82USD ml
Fluphenazine Omega 25 mg/ml5.22USD ml
Prolixin 10 mg tablet3.1USD tablet
Prolixin 5 mg tablet2.38USD tablet
Fluphenazine dec 25 mg/ml vial1.92USD ml
Prolixin 2.5 mg tablet1.63USD tablet
Fluphenazine 10 mg tablet1.25USD tablet
Fluphenazine HCl 10 mg tablet1.19USD tablet
Fluphenazine 5 mg tablet0.97USD tablet
Fluphenazine HCl 5 mg tablet0.94USD tablet
Fluphenazine 2.5 mg tablet0.84USD tablet
Fluphenazine HCl 2.5 mg tablet0.79USD tablet
Fluphenazine 1 mg tablet0.55USD tablet
Fluphenazine HCl 1 mg tablet0.52USD tablet
Apo-Fluphenazine 2 mg Tablet0.24USD tablet
Apo-Fluphenazine 1 mg Tablet0.18USD tablet
Apo-Fluphenazine 5 mg Tablet0.18USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Not Available

Properties

State
Liquid
Experimental Properties
PropertyValueSource
melting point (°C)224-226 (Salt)U.S. Patent 3,058,979
boiling point (°C)268-274 °C at 5.00E-01 mm HgPhysProp
water solubility31.1 mg/L (at 37 °C)YALKOWSKY,SH & DANNENFELSER,RM (1992)
logP4.36HANSCH,C ET AL. (1995)
logS-4.15ADME Research, USCD
pKa7.9EL TAYAR,N ET AL. (1985)
Predicted Properties
PropertyValueSource
Water Solubility0.019 mg/mLALOGPS
logP4.4ALOGPS
logP3.97ChemAxon
logS-4.4ALOGPS
pKa (Strongest Acidic)15.59ChemAxon
pKa (Strongest Basic)8.21ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count4ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area29.95 Å2ChemAxon
Rotatable Bond Count7ChemAxon
Refractivity117.27 m3·mol-1ChemAxon
Polarizability44.92 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9837
Blood Brain Barrier+0.975
Caco-2 permeable-0.5387
P-glycoprotein substrateSubstrate0.7862
P-glycoprotein inhibitor IInhibitor0.923
P-glycoprotein inhibitor IIInhibitor0.8388
Renal organic cation transporterInhibitor0.5
CYP450 2C9 substrateNon-substrate0.7669
CYP450 2D6 substrateSubstrate0.8918
CYP450 3A4 substrateNon-substrate0.7091
CYP450 1A2 substrateInhibitor0.9107
CYP450 2C9 inhibitorNon-inhibitor0.907
CYP450 2D6 inhibitorInhibitor0.8931
CYP450 2C19 inhibitorNon-inhibitor0.937
CYP450 3A4 inhibitorNon-inhibitor0.715
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.7056
Ames testNon AMES toxic0.9132
CarcinogenicityNon-carcinogens0.8828
BiodegradationNot ready biodegradable1.0
Rat acute toxicity2.8990 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9146
hERG inhibition (predictor II)Inhibitor0.8157
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Download (8.44 KB)
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
GC-MS Spectrum - EI-BGC-MSsplash10-0bu4-9430100000-8ccf208ff236ff33462c
Mass Spectrum (Electron Ionization)MSsplash10-001i-2391100000-6928faa0b341426b2c11
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-qTof , PositiveLC-MS/MSNot Available
MS/MS Spectrum - , positiveLC-MS/MSsplash10-000i-0310900000-a2a4be9e30f6506c9359
MS/MS Spectrum - , positiveLC-MS/MSsplash10-014i-0190000000-cf20413d597a3759305d

Taxonomy

Description
This compound belongs to the class of organic compounds known as phenothiazines. These are polycyclic aromatic compounds containing a phenothiazine moiety, which is a linear tricyclic system that consists of a two benzene rings joined by a para-thiazine ring.
Kingdom
Organic compounds
Super Class
Organoheterocyclic compounds
Class
Benzothiazines
Sub Class
Phenothiazines
Direct Parent
Phenothiazines
Alternative Parents
Alkyldiarylamines / Diarylthioethers / N-alkylpiperazines / Benzenoids / 1,4-thiazines / Trialkylamines / 1,2-aminoalcohols / Azacyclic compounds / Primary alcohols / Organopnictogen compounds
show 3 more
Substituents
Phenothiazine / Alkyldiarylamine / Diarylthioether / Aryl thioether / Tertiary aliphatic/aromatic amine / N-alkylpiperazine / Para-thiazine / 1,4-diazinane / Benzenoid / Piperazine
show 20 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
phenothiazines, organofluorine compound, N-alkylpiperazine (CHEBI:5123)

Targets

Details
1. D(2) dopamine receptor
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
Uniprot Name
D(2) dopamine receptor
Molecular Weight
50618.91 Da
References
  1. Seeman P: Atypical antipsychotics: mechanism of action. Can J Psychiatry. 2002 Feb;47(1):27-38. [PubMed:11873706]
  2. Hoyberg OJ, Fensbo C, Remvig J, Lingjaerde O, Sloth-Nielsen M, Salvesen I: Risperidone versus perphenazine in the treatment of chronic schizophrenic patients with acute exacerbations. Acta Psychiatr Scand. 1993 Dec;88(6):395-402. [PubMed:7508675]
  3. Qin ZH, Weiss B: Dopamine receptor blockade increases dopamine D2 receptor and glutamic acid decarboxylase mRNAs in mouse substantia nigra. Eur J Pharmacol. 1994 Sep 15;269(1):25-33. [PubMed:7828655]
  4. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
Details
2. D(1A) dopamine receptor
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 activate adenylyl cyclase.
Gene Name
DRD1
Uniprot ID
P21728
Uniprot Name
D(1A) dopamine receptor
Molecular Weight
49292.765 Da
References
  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
  2. Van Kampen JM, Stoessl AJ: Dopamine D(1A) receptor function in a rodent model of tardive dyskinesia. Neuroscience. 2000;101(3):629-35. [PubMed:11113312]
  3. Cai G, Gurdal H, Smith C, Wang HY, Friedman E: Inverse agonist properties of dopaminergic antagonists at the D(1A) dopamine receptor: uncoupling of the D(1A) dopamine receptor from G(s) protein. Mol Pharmacol. 1999 Nov;56(5):989-96. [PubMed:10531405]
  4. Seeman P: Atypical antipsychotics: mechanism of action. Can J Psychiatry. 2002 Feb;47(1):27-38. [PubMed:11873706]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
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. Mongin AA, Cai Z, Kimelberg HK: Volume-dependent taurine release from cultured astrocytes requires permissive [Ca(2+)](i) and calmodulin. Am J Physiol. 1999 Oct;277(4 Pt 1):C823-32. [PubMed:10516112]
  2. Kawai M, Nakashima A, Ueno M, Ushimaru T, Aiba K, Doi H, Uritani M: Fission yeast tor1 functions in response to various stresses including nitrogen starvation, high osmolarity, and high temperature. Curr Genet. 2001 May;39(3):166-74. [PubMed:11409178]
  3. Edlind T, Smith L, Henry K, Katiyar S, Nickels J: Antifungal activity in Saccharomyces cerevisiae is modulated by calcium signalling. Mol Microbiol. 2002 Oct;46(1):257-68. [PubMed:12366848]
  4. Nakabayashi H, Komada H, Yoshida T, Takanari H, Izutsu K: Lymphocyte calmodulin and its participation in the stimulation of T lymphocytes by mitogenic lectins. Biol Cell. 1992;75(1):55-9. [PubMed:1515867]
  5. Kauss H: Sensing of volume changes by poterioochromonas involves a ca-regulated system which controls activation of isofloridoside-phosphate synthase. Plant Physiol. 1981 Aug;68(2):420-4. [PubMed:16661928]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Zinc ion binding
Specific Function
Steroid hormone receptors are ligand-activated transcription factors that regulate eukaryotic gene expression and affect cellular proliferation and differentiation in target tissues. Transcription ...
Gene Name
AR
Uniprot ID
P10275
Uniprot Name
Androgen receptor
Molecular Weight
98987.9 Da
References
  1. Bisson WH, Cheltsov AV, Bruey-Sedano N, Lin B, Chen J, Goldberger N, May LT, Christopoulos A, Dalton JT, Sexton PM, Zhang XK, Abagyan R: Discovery of antiandrogen activity of nonsteroidal scaffolds of marketed drugs. Proc Natl Acad Sci U S A. 2007 Jul 17;104(29):11927-32. Epub 2007 Jul 2. [PubMed:17606915]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Virus receptor activity
Specific Function
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances, including mescaline, psilocybin, 1-(2,5-dimethoxy-4-iodop...
Gene Name
HTR2A
Uniprot ID
P28223
Uniprot Name
5-hydroxytryptamine receptor 2A
Molecular Weight
52602.58 Da
References
  1. Bisson WH, Cheltsov AV, Bruey-Sedano N, Lin B, Chen J, Goldberger N, May LT, Christopoulos A, Dalton JT, Sexton PM, Zhang XK, Abagyan R: Discovery of antiandrogen activity of nonsteroidal scaffolds of marketed drugs. Proc Natl Acad Sci U S A. 2007 Jul 17;104(29):11927-32. Epub 2007 Jul 2. [PubMed:17606915]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Serotonin receptor activity
Specific Function
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances, including ergot alkaloid derivatives, 1-2,5,-dimethoxy-4-...
Gene Name
HTR2C
Uniprot ID
P28335
Uniprot Name
5-hydroxytryptamine receptor 2C
Molecular Weight
51820.705 Da
References
  1. Bisson WH, Cheltsov AV, Bruey-Sedano N, Lin B, Chen J, Goldberger N, May LT, Christopoulos A, Dalton JT, Sexton PM, Zhang XK, Abagyan R: Discovery of antiandrogen activity of nonsteroidal scaffolds of marketed drugs. Proc Natl Acad Sci U S A. 2007 Jul 17;104(29):11927-32. Epub 2007 Jul 2. [PubMed:17606915]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
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. 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]
  2. Shin JG, Soukhova N, Flockhart DA: Effect of antipsychotic drugs on human liver cytochrome P-450 (CYP) isoforms in vitro: preferential inhibition of CYP2D6. Drug Metab Dispos. 1999 Sep;27(9):1078-84. [PubMed:10460810]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Steroid hydroxylase activity
Specific Function
Metabolizes several precarcinogens, drugs, and solvents to reactive metabolites. Inactivates a number of drugs and xenobiotics and also bioactivates many xenobiotic substrates to their hepatotoxic ...
Gene Name
CYP2E1
Uniprot ID
P05181
Uniprot Name
Cytochrome P450 2E1
Molecular Weight
56848.42 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]
  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]

Transporters

Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Xenobiotic-transporting atpase activity
Specific Function
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name
ABCB1
Uniprot ID
P08183
Uniprot Name
Multidrug resistance protein 1
Molecular Weight
141477.255 Da
References
  1. Wang EJ, Casciano CN, Clement RP, Johnson WW: Active transport of fluorescent P-glycoprotein substrates: evaluation as markers and interaction with inhibitors. Biochem Biophys Res Commun. 2001 Nov 30;289(2):580-5. [PubMed:11716514]

Drug created on June 13, 2005 07:24 / Updated on November 14, 2018 12:44