NAV

Fluphenazine

Identification

Summary

Fluphenazineis 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
 3D
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

Pharmacology

Indication

For management of manifestations of psychotic disorders.

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Associated Conditions
Associated Therapies
禁忌症& 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

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/ADRsBrowse all" title="" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">
Not Available

Interactions

Drug InteractionsLearn More" title="" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction
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interactions in your software
1,2-Benzodiazepine 不利影响的风险或严重性可以公司reased 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 不利影响的风险或严重性可以公司reased when Fluphenazine is combined with Acetazolamide.
Acetohexamide The therapeutic efficacy of Acetohexamide can be decreased when used in combination with Fluphenazine.
Acetophenazine 不利影响的风险或严重性可以公司reased when Fluphenazine is combined with Acetophenazine.
Agomelatine 不利影响的风险或严重性可以公司reased when Fluphenazine is combined with Agomelatine.
Alfentanil The risk or severity of hypotension and CNS depression can be increased when Fluphenazine is combined with Alfentanil.
Alimemazine 不利影响的风险或严重性可以公司reased when Fluphenazine is combined with Alimemazine.
Almasilate Almasilate can cause a decrease in the absorption of Fluphenazine resulting in a reduced serum concentration and potentially a decrease in efficacy.
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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
名字 Dosage Strength Route Labeller Marketing Start Marketing End Region Image
Fluphenazine Tablet 1 mg Oral Aa Pharma Inc 1977-12-31 Not applicable Canada flag
Fluphenazine Tablet 2 mg Oral Aa Pharma Inc 1977-12-31 Not applicable Canada flag
Fluphenazine Tablet 5 mg Oral Aa Pharma Inc 1977-12-31 Not applicable Canada flag
Fluphenazine 1 Tab 1mg Tablet 1 mg Oral Pro Doc Limitee 1982-12-31 2010-07-13 Canada flag
Fluphenazine 2 Tab 2mg Tablet 2 mg Oral Pro Doc Limitee 1982-12-31 2010-07-13 Canada flag
Fluphenazine 5 Tab 5mg Tablet 5 mg Oral Pro Doc Limitee 1982-12-31 2010-07-13 Canada flag
Fluphenazine Decanoate Injection B.P. Liquid 25 mg / mL Intramuscular; Subcutaneous Hospira医疗城市 Not applicable Not applicable Canada flag
Fluphenazine Decanoate Injection B.P. Liquid 100 mg / mL Intramuscular; Subcutaneous Hospira医疗城市 Not applicable Not applicable Canada flag
Fluphenazine Decanoate Injection, USP Solution 25 mg / mL Intramuscular; Subcutaneous Mylan Pharmaceuticals Not applicable Not applicable Canada flag
Fluphenazine Hydrochloride Tablet 2.5 mg/1 Oral REMEDYREPACK INC. 2009-08-27 2009-09-30 US flag
Generic Prescription Products
名字 Dosage Strength Route Labeller Marketing Start Marketing End Region Image
Apo Fluphenazine Tab 2.5mg Tablet 2.5 mg Oral Apotex Corporation 1977-12-31 2019-05-29 Canada flag
Apo-fluphenazine Injectable Liquid 25 mg / mL Intramuscular; Subcutaneous Apotex Corporation 2001-10-05 2013-08-02 Canada flag
Fluphenazine Decanoate Injection 25 mg/1mL Intramuscular; Subcutaneous Bedford Pharmaceuticals 1996-08-30 2009-11-30 US flag
Fluphenazine Decanoate Injection, solution 125 mg/5mL Intramuscular; Subcutaneous AuroMedics Pharma LLC 2017-10-17 Not applicable US flag
Fluphenazine Decanoate Injection, solution 25 mg/1mL Intramuscular; Subcutaneous Par Pharmaceutical 2018-06-26 Not applicable US flag
Fluphenazine Decanoate Injection, solution 25 mg/1mL Intramuscular; Subcutaneous TYA Pharmaceuticals 2010-12-15 Not applicable US flag
Fluphenazine Decanoate Injection 25 mg/1mL Intramuscular; Subcutaneous Hikma Pharmaceuticals USA Inc. 1996-08-30 Not applicable US flag
Fluphenazine decanoate Injection 25 mg/1mL Intramuscular; Subcutaneous Teva Parenteral Medicines, Inc. 1996-09-10 2005-08-29 US flag
Fluphenazine Decanoate Injection, solution 25 mg/1mL Intramuscular; Subcutaneous Fresenius Kabi USA, LLC 2010-12-15 Not applicable US flag
Fluphenazine Decanoate Injection, solution 25 mg/1mL Intramuscular; Subcutaneous Mylan Institutional LLC 2018-09-28 Not applicable US flag
Mixture Products
名字 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 Thailand flag

Categories

ATC Codes
N05AB02 — Fluphenazine
Drug Categories
Chemical TaxonomyProvided byClassyfire
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 TrialsLearn More" title="" 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
2 Completed Treatment Psoriasis (PsO) 1
2 Terminated Treatment Psoriasis (PsO) 1
1 Unknown Status Treatment Multiple Myeloma (MM) 1
1, 2 Completed Treatment Multiple Myeloma and Plasma Cell Neoplasm 1
Not Available Completed Not Available Bipolar Disorder (BD)/Psychosis/Schizoaffective Disorders/Schizophrenia/Type 2 Diabetes Mellitus 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(盐) 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 没有准备好可生物降解 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 usingadmetSAR, 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 Not Available
GC-MS Spectrum - EI-B GC-MS splash10-0bu4-9430100000-8ccf208ff236ff33462c
Mass Spectrum (Electron Ionization) MS splash10-001i-2391100000-6928faa0b341426b2c11
Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS Not Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS Not Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS Not Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS Not Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS Not Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS Not Available
质/女士Spectrum - LC-ESI-qTof , Positive 质/女士 Not Available
MS/MS Spectrum - , positive 质/女士 splash10-000i-0310900000-a2a4be9e30f6506c9359
MS/MS Spectrum - , positive 质/女士 splash10-014i-0190000000-cf20413d597a3759305d

Targets

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Use our structured and evidence-based datasets tounlock new
insights and accelerate drug research.
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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
分子量
50618.91 Da
References
  1. Seeman P:非典型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
分子量
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:非典型antipsychotics: mechanism of action. Can J Psychiatry. 2002 Feb;47(1):27-38. [Article]
Details 3.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
分子量
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]
Details 4.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
分子量
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]
Details 5.5-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
分子量
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]
Details 6.5-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
分子量
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

Details 1.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
分子量
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]
Details 2.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
分子量
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
分子量
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 24, 2023 20:20