Fluphenazine

Identification

Summary

Fluphenazine is a phenothiazine used to treat patients requiring long-term neuroleptic therapy.

Brand Names
Modecate
Generic Name
Fluphenazine
DrugBank Accession Number
DB00623
Background

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

Type
Small Molecule
Groups
Approved
Structure
Weight
Average: 437.522
Monoisotopic: 437.174867774
Chemical Formula
C22H26F3N3OS
Synonyms
  • 1-(2-hydroxyethyl)-4-(3-(trifluoromethyl-10-phenothiazinyl)propyl)-piperazine
  • 10-(3-(2-hydroxyethyl)piperazinopropyl)-2-(trifluoromethyl)phenothiazine
  • 10-(3'-(4''-(β-hydroxyethyl)-1''-piperazinyl)-propyl)-3-trifluoromethylphenothiazine
  • 2-(4-(3-[2-(trifluoromethyl)-10H-phenothiazin-10-yl]propyl)-1-piperazinyl)ethanol
  • 2-(trifluoromethyl)-10-(3-(1-(β-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
  • Fluphenazine
  • Fluphenazinum
  • Triflumethazine
External IDs
  • SQ 10733
  • Squibb 16144

Pharmacology

Indication

For management of manifestations of psychotic disorders.

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Associated Conditions
Indication TypeIndicationCombined Product DetailsApproval LevelAge GroupPatient CharacteristicsDose Form
Management ofChorea••• •••••
Used in combination to treatDepressionCombination Product in combination with: Nortriptyline (DB00540)••••••••••••••••••• ••••••
Management ofPsychotic disorders••••••••••••
Management ofTourette syndrome••• •••••
Associated Therapies
Contraindications & Blackbox Warnings
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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
ADopamine D2 receptor
antagonist
Humans
ADopamine D1 receptor
antagonist
Humans
UCalmodulin
inhibitor
Humans
UAndrogen receptorNot AvailableHumans
U5-hydroxytryptamine receptor 2ANot AvailableHumans
U5-hydroxytryptamine receptor 2CNot AvailableHumans
Absorption

Not Available

Volume of distribution

Not Available

Protein binding

Not Available

Metabolism

Hover over products below to view reaction partners

Route of elimination

Not Available

Half-life

Not Available

Clearance

Not Available

Adverse Effects
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Toxicity

Not Available

Pathways
Not Available
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
1,2-BenzodiazepineThe risk or severity of CNS depression can be increased when Fluphenazine is combined with 1,2-Benzodiazepine.
AcebutololThe serum concentration of Acebutolol can be increased when it is combined with Fluphenazine.
AcetaminophenFluphenazine may increase the hepatotoxic activities of Acetaminophen.
AcetazolamideThe risk or severity of CNS depression can be increased when Fluphenazine is combined with Acetazolamide.
AcetohexamideThe therapeutic efficacy of Acetohexamide can be decreased when used in combination with Fluphenazine.
Food Interactions
  • Avoid alcohol.
  • Take with food. Food reduces irritation.

Products

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Product Ingredients
IngredientUNIICASInChI Key
Fluphenazine decanoateFMU62K1L3C5002-47-1VIQCGTZFEYDQMR-UHFFFAOYSA-N
Fluphenazine enanthateQSB34YF0W92746-81-8LRWSFOSWNAQHHW-UHFFFAOYSA-N
Fluphenazine hydrochlorideZOU145W1XL146-56-5MBHNWCYEGXQEIT-UHFFFAOYSA-N
Product Images
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
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
FluphenazineTablet5 mgOralAa Pharma Inc1977-12-31Not applicableCanada flag
FluphenazineTablet1 mgOralAa Pharma Inc1977-12-31Not applicableCanada flag
FluphenazineTablet2 mgOralAa Pharma Inc1977-12-31Not applicableCanada flag
Fluphenazine 1 Tab 1mgTablet1 mgOralPro Doc Limitee1982-12-312010-07-13Canada flag
Fluphenazine 2 Tab 2mgTablet2 mgOralPro Doc Limitee1982-12-312010-07-13Canada flag
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Apo Fluphenazine Tab 2.5mgTablet2.5 mgOralApotex Corporation1977-12-312019-05-29Canada flag
Apo-fluphenazine InjectableLiquid25 mg / mLIntramuscular; SubcutaneousApotex Corporation2001-10-052013-08-02Canada flag
Fluphenazine DecanoateInjection, solution25 mg/1mLIntramuscular; SubcutaneousMylan Institutional LLC2018-09-28Not applicableUS flag
Fluphenazine DecanoateInjection, solution25 mg/1mLIntramuscular; SubcutaneousFresenius Kabi USA, LLC2010-12-15Not applicableUS flag
Fluphenazine DecanoateInjection, solution25 mg/1mLIntramuscular; SubcutaneousNovadoz Pharmaceuticals Llc2023-11-02Not applicableUS flag
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
เซตาวอลFluphenazine (0.5 MG) + Nortriptyline (10 MG)Tablet, sugar coatedOralบริษัท ฟาร์มาสันต์ แล็บบอราตอรี่ส์ จำกัด จำกัด1996-08-12Not applicableThailand flag

Categories

ATC Codes
N05AB02 — Fluphenazine
Drug Categories
Chemical TaxonomyProvided by Classyfire
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
1,2-aminoalcohol / 1,4-diazinane / Alcohol / Alkanolamine / Alkyl fluoride / Alkyl halide / Alkyldiarylamine / Amine / Aromatic heteropolycyclic compound / Aryl thioether
show 20 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
phenothiazines, organofluorine compound, N-alkylpiperazine (CHEBI:5123)
Affected organisms
  • Humans and other mammals

Chemical Identifiers

UNII
S79426A41Z
CAS number
69-23-8
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

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
Human Metabolome Database
HMDB0014761
KEGG Drug
D07977
KEGG Compound
C07010
PubChem Compound
3372
PubChem Substance
46506645
ChemSpider
3255
BindingDB
78433
RxNav
4496
ChEBI
5123
ChEMBL
CHEMBL726
ZINC
ZINC000019203912
Therapeutic Targets Database
DCL000806
PharmGKB
PA449676
Guide to Pharmacology
GtP Drug Page
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Fluphenazine

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4CompletedTreatmentSchizoaffective Disorders / Schizophrenia / Schizophrenia and Disorders With Psychotic Features1
4CompletedTreatmentSchizophrenia1
3CompletedTreatmentSchizophrenia1
3TerminatedTreatmentAnxiety Disorders / Dementia / Depression / Psychosomatic Disorders / Schizophrenia1
2CompletedDiagnosticPathological Gambling Disorder1

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
Tablet, coated
TabletOral2.5 mg
LiquidIntramuscular; Subcutaneous25 mg / mL
Injection, solutionParenteral100 mg
Injection, solutionParenteral12.5 mg
Injection, solutionParenteral25 mg
Injection, solutionParenteral250 mg
Injection, solutionParenteral50 mg
TabletOral1 mg
TabletOral2 mg
InjectionIntramuscular; Subcutaneous25 mg/1mL
Injection, solutionIntramuscular; Subcutaneous125 mg/5mL
Injection, solutionIntramuscular; Subcutaneous25 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 / mL
Injection, solutionIntramuscular25 mg/1ml
Injection, suspension, extended releaseIntramuscular25 MG/1ML
LiquidIntramuscular25 mg / mL
TabletOral10 mg
InjectionIntramuscular25 mg/ml
TabletOral5 mg
ElixirOral.5 mg / mL
ElixirOral0.5 mg/1mL
Solution, concentrateOral5 mg/1mL
InjectionIntramuscular; Subcutaneous25 mg/ml
SolutionIntramuscular; Subcutaneous25 mg / mL
SolutionIntramuscular; Subcutaneous100 mg / mL
InjectionIntramuscular; Subcutaneous
Tablet, sugar coatedOral0.5 mg
Tablet, sugar coatedOral2.5 mg
Tablet, sugar coatedOral5 mg
Tablet, sugar coatedOral
SolutionIntramuscular; Subcutaneous25 mg/1ml
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)7.81Chemaxon
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-MSsplash10-0a4l-5545900000-cdc372e9bc4eddfcf306
GC-MS Spectrum - EI-BGC-MSsplash10-0bu4-9430100000-8ccf208ff236ff33462c
Mass Spectrum (Electron Ionization)MSsplash10-001i-2391100000-6928faa0b341426b2c11
LC-MS/MS Spectrum - LC-ESI-qTof , PositiveLC-MS/MSsplash10-014i-0190000000-cf20413d597a3759305d
MS/MS Spectrum - , positiveLC-MS/MSsplash10-000i-0310900000-a2a4be9e30f6506c9359
MS/MS Spectrum - , positiveLC-MS/MSsplash10-014i-0190000000-cf20413d597a3759305d
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSsplash10-000i-0000900000-55a4c75044ab4cd3dec1
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSsplash10-000i-0000900000-2b5284e50831657a99ff
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSsplash10-059i-0526900000-0a6f436b08be1e90b3fd
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSsplash10-05n0-0002900000-1741de348112f3b5560e
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSsplash10-07vi-3269800000-3977326bac371547f2e4
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSsplash10-01rf-0319300000-6bdb74a73b3e9e7b3c1c
Predicted 1H NMR Spectrum1D NMRNot Applicable
Predicted 13C NMR Spectrum1D NMRNot Applicable
Chromatographic Properties
Collision Cross Sections (CCS)
AdductCCS Value (Å2)Source typeSource
[M-H]-210.6250749
predicted
DarkChem Lite v0.1.0
[M-H]-196.62927
predicted
DeepCCS 1.0 (2019)
[M+H]+210.7222749
predicted
DarkChem Lite v0.1.0
[M+H]+198.98727
predicted
DeepCCS 1.0 (2019)
[M+Na]+211.1263749
predicted
DarkChem Lite v0.1.0
[M+Na]+206.01103
predicted
DeepCCS 1.0 (2019)

Targets

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Details
1. Dopamine D2 receptor
Kind
Protein
Organism
Humans
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. [Article]
  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. [Article]
  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. [Article]
  4. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
Details
2. Dopamine D1 receptor
Kind
Protein
Organism
Humans
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. [Article]
  2. Van Kampen JM, Stoessl AJ: Dopamine D(1A) receptor function in a rodent model of tardive dyskinesia. Neuroscience. 2000;101(3):629-35. [Article]
  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. [Article]
  4. Seeman P: Atypical antipsychotics: mechanism of action. Can J Psychiatry. 2002 Feb;47(1):27-38. [Article]
Kind
Protein
Organism
Humans
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. [Article]
  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. [Article]
  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. [Article]
  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. [Article]
  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. [Article]
Kind
Protein
Organism
Humans
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. [Article]
Kind
Protein
Organism
Humans
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. [Article]
Kind
Protein
Organism
Humans
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. [Article]

Enzymes

Kind
Protein
Organism
Humans
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. 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. Fluphenazine - StatPearls - NCBI Bookshelf [Link]
Kind
Protein
Organism
Humans
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. 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. [Article]

Transporters

Details
1. P-glycoprotein 1
Kind
Protein
Organism
Humans
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. [Article]

Drug created at June 13, 2005 13:24 / Updated at March 18, 2024 16:48