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

Similar Structures

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

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Pharmacology

Indication

For management of manifestations of psychotic disorders.

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Associated Conditions

Indication Type	Indication	Combined Product Details	Approval Level	Dose Form
Management of	Chorea		••• •••••
Used in combination to treat	Depression	Combination Product in combination with: Nortriptyline (DB00540)	••••••••••••	••••••• ••••••
Management of	Psychotic disorders		••••••••••••
Management of	Tourette syndrome		••• •••••

Associated Therapies

Sedation

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.

Target	Actions	Organism
ADopamine D2 receptor	antagonist	Humans
ADopamine D1 receptor	antagonist	Humans
UCalmodulin	inhibitor	Humans
UAndrogen receptor	Not Available	Humans
U5-hydroxytryptamine receptor 2A	Not Available	Humans
U5-hydroxytryptamine receptor 2C	Not Available	Humans

Absorption

Not Available

Volume of distribution

Not Available

Protein binding

Not Available

Metabolism

Hover over products below to view reaction partners

Fluphenazine
- Fluphenazine sulfoxide

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 Browse all" title="About SNP Mediated Effects/ADRs" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">

Not Available

Interactions

Drug Interactions Learn More" title="About Drug Interactions" 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 Fluphenazine is combined with 1,2-Benzodiazepine.
Acebutolol	The serum concentration of Acebutolol can be increased when it is combined with Fluphenazine.
Acetaminophen	Fluphenazine may increase the hepatotoxic activities of Acetaminophen.
Acetazolamide	The risk or severity of CNS depression can be increased when Fluphenazine is combined with Acetazolamide.
Acetohexamide	The 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

Ingredient	UNII	CAS	InChI Key
Fluphenazine decanoate	FMU62K1L3C	5002-47-1	VIQCGTZFEYDQMR-UHFFFAOYSA-N
Fluphenazine enanthate	QSB34YF0W9	2746-81-8	LRWSFOSWNAQHHW-UHFFFAOYSA-N
Fluphenazine hydrochloride	ZOU145W1XL	146-56-5	MBHNWCYEGXQEIT-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

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End
Fluphenazine	Tablet	5 mg	Oral	Aa Pharma Inc	1977-12-31	Not applicable
Fluphenazine	Tablet	1 mg	Oral	Aa Pharma Inc	1977-12-31	Not applicable
Fluphenazine	Tablet	2 mg	Oral	Aa Pharma Inc	1977-12-31	Not applicable
Fluphenazine 1 Tab 1mg	Tablet	1 mg	Oral	Pro Doc Limitee	1982-12-31	2010-07-13
Fluphenazine 2 Tab 2mg	Tablet	2 mg	Oral	Pro Doc Limitee	1982-12-31	2010-07-13

Generic Prescription Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End
Apo Fluphenazine Tab 2.5mg	Tablet	2.5 mg	Oral	Apotex Corporation	1977-12-31	2019-05-29
Apo-fluphenazine Injectable	Liquid	25 mg / mL	Intramuscular; Subcutaneous	Apotex Corporation	2001-10-05	2013-08-02
Fluphenazine decanoate	Injection	25 mg/1mL	Intramuscular; Subcutaneous	Teva Parenteral Medicines, Inc.	1996-09-10	2005-08-29
Fluphenazine Decanoate	Injection, solution	25 mg/1mL	Intramuscular; Subcutaneous	Fresenius Kabi USA, LLC	2010-12-15	Not applicable
Fluphenazine Decanoate	Injection, solution	25 mg/1mL	Intramuscular; Subcutaneous	Sagent Pharmaceuticals	2023-08-01	Not applicable

Mixture Products

Name	Ingredients	Dosage	Route	Labeller	Marketing Start	Marketing End	Region	Image
เซตาวอล	Fluphenazine (0.5 MG) + Nortriptyline (10 MG)	Tablet, sugar coated	Oral	บริษัท ฟาร์มาสันต์ แล็บบอราตอรี่ส์ จำกัด จำกัด	1996-08-12	Not applicable

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

External Links

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 Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">

Phase	Status	Purpose	Conditions	Count
4	Completed	Treatment	Schizoaffective Disorders / Schizophrenia / Schizophrenia and Disorders With Psychotic Features	1
4	Completed	Treatment	Schizophrenia	1
3	Completed	Treatment	Schizophrenia	1
3	Terminated	Treatment	Anxiety Disorders / Dementia / Depression / Psychosomatic Disorders / Schizophrenia	1
2	Completed	Diagnostic	Pathological Gambling Disorder	1

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

Form	Route	Strength
Tablet, coated
Tablet	Oral	2.5 mg
Liquid	Intramuscular; Subcutaneous	25 mg / mL
Injection, solution	Parenteral	100 mg
Injection, solution	Parenteral	12.5 mg
Injection, solution	Parenteral	25 mg
Injection, solution	Parenteral	250 mg
Injection, solution	Parenteral	50 mg
Tablet	Oral	1 mg
Tablet	Oral	2 mg
Injection	Intramuscular; Subcutaneous	25 mg/1mL
Injection, solution	Intramuscular; Subcutaneous	125 mg/5mL
Injection, solution	Intramuscular; Subcutaneous	25 mg/1mL
Injection, solution	Intramuscular	2.5 mg/1mL
Tablet	Oral	1 mg/1
Tablet	Oral	10 mg/1
Tablet	Oral	2.5 mg/1
Tablet	Oral	2.50 mg/1
Tablet	Oral	5 mg/1
Tablet, film coated	Oral	1 mg/1
Tablet, film coated	Oral	10 mg/1
Tablet, film coated	Oral	2.5 mg/1
Tablet, film coated	Oral	5 mg/1
Liquid	Intramuscular; Subcutaneous	100 mg / mL
Injection, solution	Intramuscular	25 mg/1ml
Injection, suspension, extended release	Intramuscular	25 MG/1ML
Liquid	Intramuscular	25 mg / mL
Tablet	Oral	10 mg
Injection	Intramuscular	25 mg/ml
Tablet	Oral	5 mg
Elixir	Oral	.5 mg / mL
Elixir	Oral	0.5 mg/1mL
Solution, concentrate	Oral	5 mg/1mL
Injection	Intramuscular; Subcutaneous	25 mg/ml
Solution	Intramuscular; Subcutaneous	25 mg / mL
Solution	Intramuscular; Subcutaneous	100 mg / mL
Injection	Intramuscular; Subcutaneous
Tablet, sugar coated	Oral	0.5 mg
Tablet, sugar coated	Oral	2.5 mg
Tablet, sugar coated	Oral	5 mg
Tablet, sugar coated	Oral
Solution	Intramuscular; Subcutaneous	25 mg/1ml

Prices

Unit description	Cost	Unit
Fluphenazine Omega 100 mg/ml	31.2USD	ml
Modecate Concentrate 100 mg/ml	31.2USD	ml
Pms-Fluphenazine Decanoate 100 mg/ml	31.2USD	ml
Fluphenazine Decanoate 25 mg/ml Solution	14.0USD	ml
Fluphenazine 2.5 mg/ml vial	7.82USD	ml
Fluphenazine Omega 25 mg/ml	5.22USD	ml
Prolixin 10 mg tablet	3.1USD	tablet
Prolixin 5 mg tablet	2.38USD	tablet
Fluphenazine dec 25 mg/ml vial	1.92USD	ml
Prolixin 2.5 mg tablet	1.63USD	tablet
Fluphenazine 10 mg tablet	1.25USD	tablet
Fluphenazine HCl 10 mg tablet	1.19USD	tablet
Fluphenazine 5 mg tablet	0.97USD	tablet
Fluphenazine HCl 5 mg tablet	0.94USD	tablet
Fluphenazine 2.5 mg tablet	0.84USD	tablet
Fluphenazine HCl 2.5 mg tablet	0.79USD	tablet
Fluphenazine 1 mg tablet	0.55USD	tablet
Fluphenazine HCl 1 mg tablet	0.52USD	tablet
Apo-Fluphenazine 2 mg Tablet	0.24USD	tablet
Apo-Fluphenazine 1 mg Tablet	0.18USD	tablet
Apo-Fluphenazine 5 mg Tablet	0.18USD	tablet

DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.

Patents

Not Available

Properties

State

Liquid

Experimental Properties

Property	Value	Source
melting point (°C)	224-226 (Salt)	U.S. Patent 3,058,979
boiling point (°C)	268-274 °C at 5.00E-01 mm Hg	PhysProp
water solubility	31.1 mg/L (at 37 °C)	YALKOWSKY,SH & DANNENFELSER,RM (1992)
logP	4.36	HANSCH,C ET AL. (1995)
logS	-4.15	ADME Research, USCD
pKa	7.9	EL TAYAR,N ET AL. (1985)

Predicted Properties

Property	Value	Source
Water Solubility	0.019 mg/mL	ALOGPS
logP	4.4	ALOGPS
logP	3.97	Chemaxon
logS	-4.4	ALOGPS
pKa (Strongest Acidic)	15.59	Chemaxon
pKa (Strongest Basic)	7.81	Chemaxon
Physiological Charge	1	Chemaxon
Hydrogen Acceptor Count	4	Chemaxon
Hydrogen Donor Count	1	Chemaxon
Polar Surface Area	29.95 Å²	Chemaxon
Rotatable Bond Count	7	Chemaxon
Refractivity	117.27 m³·mol^-1	Chemaxon
Polarizability	44.92 Å³	Chemaxon
Number of Rings	4	Chemaxon
Bioavailability	1	Chemaxon
Rule of Five	Yes	Chemaxon
Ghose Filter	Yes	Chemaxon
Veber's Rule	Yes	Chemaxon
MDDR-like Rule	Yes	Chemaxon

Predicted ADMET Features

Property	Value	Probability
Human Intestinal Absorption	+	0.9837
Blood Brain Barrier	+	0.975
Caco-2 permeable	-	0.5387
P-glycoprotein substrate	Substrate	0.7862
P-glycoprotein inhibitor I	Inhibitor	0.923
P-glycoprotein inhibitor II	Inhibitor	0.8388
Renal organic cation transporter	Inhibitor	0.5
CYP450 2C9 substrate	Non-substrate	0.7669
CYP450 2D6 substrate	Substrate	0.8918
CYP450 3A4 substrate	Non-substrate	0.7091
CYP450 1A2 substrate	Inhibitor	0.9107
CYP450 2C9 inhibitor	Non-inhibitor	0.907
CYP450 2D6 inhibitor	Inhibitor	0.8931
CYP450 2C19 inhibitor	Non-inhibitor	0.937
CYP450 3A4 inhibitor	Non-inhibitor	0.715
CYP450 inhibitory promiscuity	High CYP Inhibitory Promiscuity	0.7056
Ames test	Non AMES toxic	0.9132
Carcinogenicity	Non-carcinogens	0.8828
Biodegradation	Not ready biodegradable	1.0
Rat acute toxicity	2.8990 LD50, mol/kg	Not applicable
hERG inhibition (predictor I)	Weak inhibitor	0.9146
hERG inhibition (predictor II)	Inhibitor	0.8157

ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)

Download (8.44 KB)

Spectra

Spectrum	Spectrum Type	Splash Key
Predicted GC-MS Spectrum - GC-MS	Predicted GC-MS	splash10-0a4l-5545900000-cdc372e9bc4eddfcf306
GC-MS Spectrum - EI-B	GC-MS	splash10-0bu4-9430100000-8ccf208ff236ff33462c
Mass Spectrum (Electron Ionization)	MS	splash10-001i-2391100000-6928faa0b341426b2c11
LC-MS/MS Spectrum - LC-ESI-qTof , Positive	LC-MS/MS	splash10-014i-0190000000-cf20413d597a3759305d
MS/MS Spectrum - , positive	LC-MS/MS	splash10-000i-0310900000-a2a4be9e30f6506c9359
MS/MS Spectrum - , positive	LC-MS/MS	splash10-014i-0190000000-cf20413d597a3759305d
Predicted MS/MS Spectrum - 10V, Positive (Annotated)	Predicted LC-MS/MS	splash10-000i-0000900000-55a4c75044ab4cd3dec1
Predicted MS/MS Spectrum - 10V, Negative (Annotated)	Predicted LC-MS/MS	splash10-000i-0000900000-2b5284e50831657a99ff
Predicted MS/MS Spectrum - 20V, Positive (Annotated)	Predicted LC-MS/MS	splash10-059i-0526900000-0a6f436b08be1e90b3fd
Predicted MS/MS Spectrum - 20V, Negative (Annotated)	Predicted LC-MS/MS	splash10-05n0-0002900000-1741de348112f3b5560e
Predicted MS/MS Spectrum - 40V, Negative (Annotated)	Predicted LC-MS/MS	splash10-07vi-3269800000-3977326bac371547f2e4
Predicted MS/MS Spectrum - 40V, Positive (Annotated)	Predicted LC-MS/MS	splash10-01rf-0319300000-6bdb74a73b3e9e7b3c1c
Predicted 1H NMR Spectrum	1D NMR	Not Applicable
Predicted 13C NMR Spectrum	1D NMR	Not Applicable

Chromatographic Properties

Collision Cross Sections (CCS)

Adduct	CCS Value (Å²)	Source type	Source
[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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Property	Measurement	pH	Temperature (°C)	References
Ki (nM)	1.44	N/A	N/A	A11189

Details1. 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

Seeman P: Atypical antipsychotics: mechanism of action. Can J Psychiatry. 2002 Feb;47(1):27-38. [Article]
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]
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]
Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]

Property	Measurement	pH	Temperature (°C)	References
Ki (nM)	21	N/A	N/A	A27892
Ki (nM)	7	N/A	N/A	A18178
Ki (nM)	179	N/A	N/A	A11189

Details2. 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

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

Details3. Calmodulin

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

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]
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]
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]
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]
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]

Details4. Androgen receptor

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

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]

Property	Measurement	pH	Temperature (°C)	References
Ki (nM)	80	N/A	N/A	A15616
Ki (nM)	3.2	N/A	N/A	A12818
Ki (nM)	30	N/A	N/A	A27477

Details5. 5-hydroxytryptamine receptor 2A

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

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]

Property	Measurement	pH	Temperature (°C)	References
Ki (nM)	188.67	N/A	N/A	A27490
Ki (nM)	579	N/A	N/A	A10971
Ki (nM)	1386	N/A	N/A	A27477

Details6. 5-hydroxytryptamine receptor 2C

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

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

Details1. Cytochrome P450 2E1

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

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]
Fluphenazine - StatPearls - NCBI Bookshelf [Link]

Details2. Cytochrome P450 2D6

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

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

Property	Measurement	pH	Temperature (°C)	References
IC 50 (nM)	5700	N/A	N/A	A15813
IC 50 (nM)	10400	N/A	N/A	A15813
IC 50 (nM)	6500	N/A	N/A	A15813

Details1. 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

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 February 20, 2024 23:55

Fluphenazine

Identification

Structure for Fluphenazine (DB00623)

Pharmacology

Interactions

Products

Categories

Chemical Identifiers

References

Clinical Trials

Pharmacoeconomics

Properties

Spectra

Collision Cross Sections (CCS)

Targets

References

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Enzymes

References

References

Transporters

References