Identification
- Summary
Trifluoperazine is a phenothiazine used to treat depression, anxiety, and agitation.
- Generic Name
- Trifluoperazine
- DrugBank Accession Number
- DB00831
- Background
A phenothiazine with actions similar to chlorpromazine. It is used as an antipsychotic and an antiemetic.
- Type
- Small Molecule
- Groups
- Approved, Investigational
- Structure
Structure for Trifluoperazine (DB00831)
- Weight
- Average: 407.496
Monoisotopic: 407.164303088 - Chemical Formula
- C21H24F3N3S
- Synonyms
- 10-[3-(4-methyl-1-piperazinyl)propyl]-2-(trifluoromethyl)-10H-phenothiazine
- Trifluoperazina
- Trifluoperazine
- Trifluopérazine
- Trifluoperazinum
- trifluoromethyl-10-(3'-(1-methyl-4-piperazinyl)propyl)phenothiazine
- Trifluoroperazine
- Trifluperazine
- External IDs
- NSC-17474
- RP-7623
Pharmacology
- Indication
For the treatment of anxiety disorders, depressive symptoms secondary to anxiety and agitation.
Reduce drug development failure ratesBuild, train, & validate machine-learning modelswith evidence-based and structured datasets.Build, train, & validate predictive machine-learning models with structured datasets.- Associated Conditions
Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Management of Agitation ••• ••••• Management of Psychosis ••• ••••• Management of Schizophrenia •••••••••••• Management of Acute non-psychotic anxiety •••••••••••• - Contraindications & Blackbox Warnings
Prevent Adverse Drug Events TodayTap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events with our Clinical API- Pharmacodynamics
Trifluoperazine is a trifluoro-methyl phenothiazine derivative intended for the management of schizophrenia and other psychotic disorders. Trifluoperazine has not been shown effective in the management of behaviorial complications in patients with mental retardation.
- Mechanism of action
Trifluoperazine 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 antagonistHumans ANeuron-specific vesicular protein calcyon antagonistHumans AAlpha-1A adrenergic receptor antagonistHumans UCalmodulin inhibitorHumans UTroponin C, slow skeletal and cardiac muscles Not Available Humans UProtein S100-A4 inhibitorHumans - Absorption
Not Available
- Volume of distribution
Not Available
- Protein binding
Not Available
- Metabolism
Hepatic.
- Route of elimination
Not Available
- Half-life
10-20 hours
- Clearance
Not Available
- Adverse Effects
Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates. View sample adverse effects data in our new Data Library!Improve decision support & research outcomes with our structured adverse effects data.- Toxicity
Symptoms of overdose include agitation, coma, convulsions, difficulty breathing, difficulty swallowing, dry mouth, extreme sleepiness, fever, intestinal blockage, irregular heart rate, low blood pressure, and restlessness.
- 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 Integrate drug-drug
interactions in your software1,2-Benzodiazepine The risk or severity of CNS depression can be increased when Trifluoperazine is combined with 1,2-Benzodiazepine. Abametapir The serum concentration of Trifluoperazine can be increased when it is combined with Abametapir. Abatacept The metabolism of Trifluoperazine can be increased when combined with Abatacept. Abiraterone The serum concentration of Trifluoperazine can be increased when it is combined with Abiraterone. Acebutolol The serum concentration of Acebutolol can be increased when it is combined with Trifluoperazine. - Food Interactions
- Avoid excessive or chronic alcohol consumption. Ingesting alcohol may potentiate the sedative and CNS depressant effects of trifluoperazine.
Products
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- Product Ingredients
Ingredient UNII CAS InChI Key Trifluoperazine hydrochloride 6P1Y2SNF5V 440-17-5 BXDAOUXDMHXPDI-UHFFFAOYSA-N - Product Images
- International/Other Brands
- Eskazine / Eskazinyl / Jatroneural / Modalina / Stelazine / Terfluzine / Trifluoperaz / Triftazin
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Stelazine Tab 10mg Tablet 10 mg / tab Oral Smithkline Beecham Pharma Division Of Smithkline Beecham Inc 1993-12-31 2000-11-30 Canada 
Stelazine Tab 1mg Tablet 1 mg / tab Oral Smithkline Beecham Pharma Division Of Smithkline Beecham Inc 1993-12-31 2000-11-30 Canada Stelazine Tab 2mg Tablet 2 mg / tab Oral Smithkline Beecham Pharma Division Of Smithkline Beecham Inc 1992-12-31 2000-10-18 Canada Stelazine Tab 5mg Tablet 5 mg / tab Oral Smithkline Beecham Pharma Division Of Smithkline Beecham Inc 1993-12-31 2000-09-28 Canada Terfluzine Concentrate Syrup 10 mg / mL Oral Valeant Canada Lp Valeant Canada S.E.C. 1974-12-31 2011-08-03 Canada - Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Novo-flurazine Tab 1mg Tablet 1.18 mg / tab Oral Novopharm Limited 1971-12-31 1996-09-10 Canada Novo-flurazine Tab 20mg Tablet 23.6 mg / tab Oral Novopharm Limited 1971-12-31 1996-09-10 Canada Novo-trifluzine - Tab 10mg Tablet 11.8 mg Oral Novopharm Limited 1971-12-31 2013-06-03 Canada Novo-trifluzine - Tab 2mg Tablet 2.36 mg Oral Novopharm Limited 1971-12-31 2013-06-03 Canada Novo-trifluzine - Tab 5mg Tablet 5.9 mg Oral Novopharm Limited 1971-12-31 2013-06-03 Canada - Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image CUAIT - D COMPRIMIDOS. Trifluoperazine hydrochloride (0.5 mg) + Amitriptyline hydrochloride (5 mg) Tablet Oral BLISTECO S.A.S. 2006-11-10 2023-09-27 Colombia 
Stelabid Forte Trifluoperazine hydrochloride (2 mg) + Isopropamide iodide (7.5 mg) Tablet Oral Glaxosmithkline Inc 1993-12-31 2002-07-31 Canada Stelabid No 1 Trifluoperazine hydrochloride (1 mg) + Isopropamide iodide (5 mg) Tablet Oral Glaxosmithkline Inc 1993-12-31 2002-01-29 Canada Stelabid No 2 Trifluoperazine hydrochloride (2 mg) + Isopropamide iodide (5 mg) Tablet Oral Glaxosmithkline Inc 1993-12-31 2002-01-29 Canada
Categories
- ATC Codes
- N05AB06 — Trifluoperazine
- Drug Categories
- Adrenergic alpha-1 Receptor Antagonists
- Adrenergic alpha-Antagonists
- Adrenergic Antagonists
- Agents that produce hypertension
- Antiemetics
- Antipsychotic Agents
- Antipsychotic Agents (First Generation [Typical])
- Autonomic Agents
- Central Nervous System Agents
- Central Nervous System Depressants
- Cytochrome P-450 CYP1A2 Substrates
- Cytochrome P-450 Substrates
- Dopamine Agents
- Dopamine Antagonists
- Dopamine D2 Receptor Antagonists
- Drugs causing inadvertant photosensitivity
- Gastrointestinal Agents
- Heterocyclic Compounds, Fused-Ring
- Nervous System
- Neurotoxic agents
- Neurotransmitter Agents
- P-glycoprotein inhibitors
- P-glycoprotein substrates
- Peripheral Nervous System Agents
- Phenothiazines
- Phenothiazines With Piperazine Structure
- Photosensitizing Agents
- Psycholeptics
- Psychotropic Drugs
- Sulfur Compounds
- Tranquilizing Agents
- UGT1A4 substrates
- 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-methylpiperazines / Benzenoids / 1,4-thiazines / Trialkylamines / Azacyclic compounds / Organopnictogen compounds / Organofluorides / Hydrocarbon derivatives show 1 more
- Substituents
- 1,4-diazinane / Alkyl fluoride / Alkyl halide / Alkyldiarylamine / Amine / Aromatic heteropolycyclic compound / Aryl thioether / Azacycle / Benzenoid / Diarylthioether show 15 more
- Molecular Framework
- Aromatic heteropolycyclic compounds
- External Descriptors
- phenothiazines, organofluorine compound, N-alkylpiperazine, N-methylpiperazine (CHEBI:45951)
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- 214IZI85K3
- CAS number
- 117-89-5
- InChI Key
- ZEWQUBUPAILYHI-UHFFFAOYSA-N
- InChI
- InChI=1S/C21H24F3N3S/c1-25-11-13-26(14-12-25)9-4-10-27-17-5-2-3-6-19(17)28-20-8-7-16(15-18(20)27)21(22,23)24/h2-3,5-8,15H,4,9-14H2,1H3
- IUPAC Name
- 10-[3-(4-methylpiperazin-1-yl)propyl]-2-(trifluoromethyl)-10H-phenothiazine
- SMILES
- CN1CCN(CCCN2C3=CC=CC=C3SC3=C2C=C(C=C3)C(F)(F)F)CC1
References
- General References
- Not Available
- External Links
- Human Metabolome Database
- HMDB0014969
- KEGG Drug
- D08636
- KEGG Compound
- C07168
- PubChem Compound
- 5566
- PubChem Substance
- 46507961
- ChemSpider
- 5365
- BindingDB
- 79181
- 10800
- ChEBI
- 45951
- ChEMBL
- CHEMBL422
- ZINC
- ZINC000019418959
- Therapeutic Targets Database
- DAP000034
- PharmGKB
- PA451771
- Guide to Pharmacology
- GtP Drug Page
- PDBe Ligand
- TFP
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- PDRhealth
- PDRhealth Drug Page
- Wikipedia
- Trifluoperazine
- PDB Entries
- 1a29 / 1ctr / 1lin / 1wrk / 1wrl / 3ko0 / 4rjd
- MSDS
- Download (73.8 KB)
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 3 Unknown Status Treatment Psychosis Nos/Other 1 1, 2 Terminated Treatment Congenital Hypoplastic Anemia / Pure Red Cell Aplasia 1 Not Available Completed Not Available Bipolar Disorder (BD) / Psychosis / Schizoaffective Disorders / Schizophrenia / Type 2 Diabetes Mellitus 1 Not Available Completed Not Available Schizophrenia 1
Pharmacoeconomics
- Manufacturers
- Glaxosmithkline
- Sandoz inc
- Wockhardt eu operations (swiss) ag
- Duramed pharmaceuticals inc sub barr laboratories inc
- Ivax pharmaceuticals inc
- Mylan pharmaceuticals inc
- Watson laboratories inc
- Packagers
- Apotheca Inc.
- Comprehensive Consultant Services Inc.
- Heartland Repack Services LLC
- Murfreesboro Pharmaceutical Nursing Supply
- Mylan
- Nucare Pharmaceuticals Inc.
- Physicians Total Care Inc.
- Remedy Repack
- Sandhills Packaging Inc.
- Sandoz
- Stat Rx Usa
- UDL Laboratories
- Dosage Forms
Form Route Strength Tablet Oral Tablet Oral 5 MG Pill 1 MG Pill 2 MG Pill 5 MG Suppository 4 MG Tablet, coated Oral 1 MG Tablet, coated Oral 2 MG Tablet Oral 1.2 mg Tablet Oral 1.18 mg / tab Tablet Oral 23.6 mg / tab Tablet Oral 11.8 mg Tablet Oral 2.36 mg Tablet Oral 5.9 mg Tablet Oral 1 mg / tab Tablet Oral 20 mg / tab Syrup Oral 1 mg / mL Tablet Oral Tablet, film coated Oral Tablet Oral 10 mg / tab Tablet Oral 2 mg / tab Tablet Oral 5 mg / tab Tablet, coated Oral 5 mg Injection, solution Intramuscular 1 mg Syrup Oral 10 mg / mL Tablet Oral 1 mg Tablet Oral 10 mg Tablet Oral 2 mg Tablet Oral 20 mg Tablet, film coated Oral 2 mg/1 Tablet Oral 1 mg/1 Tablet, film coated Oral 1 mg/1 Tablet, film coated Oral 10 mg/1 Tablet, film coated Oral 5 mg/1 Tablet, sugar coated Oral Tablet, coated Oral 10 mg Tablet, sugar coated Oral 10 mg Tablet, film coated Oral 1 mg Tablet, film coated Oral 5 mg Tablet, sugar coated Oral 5 mg - Prices
Unit description Cost Unit Trifluoperazine HCl 10 mg tablet 1.7USD tablet Trifluoperazine 10 mg tablet 1.63USD tablet Trifluoperazine HCl 5 mg tablet 1.09USD tablet Trifluoperazine 5 mg tablet 1.08USD tablet Trifluoperazine HCl 2 mg tablet 0.89USD tablet Trifluoperazine 2 mg tablet 0.86USD tablet Trifluoperazine HCl 1 mg tablet 0.59USD tablet Trifluoperazine 1 mg tablet 0.58USD tablet Apo-Trifluoperazine 20 mg Tablet 0.58USD tablet Apo-Trifluoperazine 10 mg Tablet 0.29USD tablet Apo-Trifluoperazine 5 mg Tablet 0.24USD tablet Apo-Trifluoperazine 2 mg Tablet 0.18USD tablet Apo-Trifluoperazine 1 mg Tablet 0.14USD tablet DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
Property Value Source water solubility 12.2 mg/L (at 24 °C) YALKOWSKY,SH & DANNENFELSER,RM (1992) logP 5.03 HANSCH,C ET AL. (1995) logS -4.52 ADME Research, USCD - Predicted Properties
Property Value Source Water Solubility 0.00876 mg/mL ALOGPS logP 4.87 ALOGPS logP 4.66 Chemaxon logS -4.7 ALOGPS pKa (Strongest Basic) 7.99 Chemaxon Physiological Charge 1 Chemaxon Hydrogen Acceptor Count 3 Chemaxon Hydrogen Donor Count 0 Chemaxon Polar Surface Area 9.72 Å2 Chemaxon Rotatable Bond Count 5 Chemaxon Refractivity 110.98 m3·mol-1 Chemaxon Polarizability 41.94 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 No Chemaxon - Predicted ADMET Features
Property Value Probability Human Intestinal Absorption + 0.9946 Blood Brain Barrier + 0.9814 Caco-2 permeable + 0.6856 P-glycoprotein substrate Substrate 0.8529 P-glycoprotein inhibitor I Inhibitor 0.9058 P-glycoprotein inhibitor II Inhibitor 0.9089 Renal organic cation transporter Inhibitor 0.6842 CYP450 2C9 substrate Non-substrate 0.7898 CYP450 2D6 substrate Non-substrate 0.9109 CYP450 3A4 substrate Non-substrate 0.594 CYP450 1A2 substrate Inhibitor 0.9106 CYP450 2C9 inhibitor Non-inhibitor 0.9144 CYP450 2D6 inhibitor Inhibitor 0.8931 CYP450 2C19 inhibitor Inhibitor 0.8995 CYP450 3A4 inhibitor Non-inhibitor 0.5618 CYP450 inhibitory promiscuity High CYP Inhibitory Promiscuity 0.8247 Ames test Non AMES toxic 0.8944 Carcinogenicity Non-carcinogens 0.9446 Biodegradation Not ready biodegradable 1.0 Rat acute toxicity 2.8411 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.9327 hERG inhibition (predictor II) Inhibitor 0.8556
Spectra
- Mass Spec (NIST)
- Download (10.1 KB)
- Spectra
- Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 199.4083836 predictedDarkChem Lite v0.1.0 [M-H]- 192.13991 predictedDeepCCS 1.0 (2019) [M+H]+ 199.6042836 predictedDarkChem Lite v0.1.0 [M+H]+ 194.63963 predictedDeepCCS 1.0 (2019) [M+Na]+ 199.2972836 predictedDarkChem Lite v0.1.0 [M+Na]+ 202.05873 predictedDeepCCS 1.0 (2019)
Targets
Build, predict & validate machine-learning models
Use our structured and evidence-based datasets to unlock newinsights and accelerate drug research.
Use our structured and evidence-based datasets to unlock new insights and accelerate drug research.
- 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
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
- Seeman P: Atypical antipsychotics: mechanism of action. Can J Psychiatry. 2002 Feb;47(1):27-38. [Article]
- Lahti RA, Evans DL, Stratman NC, Figur LM: Dopamine D4 versus D2 receptor selectivity of dopamine receptor antagonists: possible therapeutic implications. Eur J Pharmacol. 1993 Jun 4;236(3):483-6. [Article]
- Schmidt MH, Lee T: Investigation of striatal dopamine D2 receptor acquisition following prenatal neuroleptic exposure. Psychiatry Res. 1991 Mar;36(3):319-28. [Article]
- Cahir M, King DJ: Antipsychotics lack alpha 1A/B adrenoceptor subtype selectivity in the rat. Eur Neuropsychopharmacol. 2005 Mar;15(2):231-4. [Article]
- Seeman P, Lee T, Chau-Wong M, Wong K: Antipsychotic drug doses and neuroleptic/dopamine receptors. Nature. 1976 Jun 24;261(5562):717-9. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antagonist
- General Function
- Clathrin light chain binding
- Specific Function
- Interacts with clathrin light chain A and stimulates clathrin self-assembly and clathrin-mediated endocytosis.
- Gene Name
- CALY
- Uniprot ID
- Q9NYX4
- Uniprot Name
- Neuron-specific vesicular protein calcyon
- Molecular Weight
- 23433.49 Da
References
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
- Seeman P, Lee T, Chau-Wong M, Wong K: Antipsychotic drug doses and neuroleptic/dopamine receptors. Nature. 1976 Jun 24;261(5562):717-9. [Article]
- Madrid PB, Polgar WE, Toll L, Tanga MJ: Synthesis and antitubercular activity of phenothiazines with reduced binding to dopamine and serotonin receptors. Bioorg Med Chem Lett. 2007 Jun 1;17(11):3014-7. Epub 2007 Mar 24. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antagonist
- General Function
- Protein heterodimerization activity
- Specific Function
- This alpha-adrenergic receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. Its effect is mediated by G(q) and G(11) prot...
- Gene Name
- ADRA1A
- Uniprot ID
- P35348
- Uniprot Name
- Alpha-1A adrenergic receptor
- Molecular Weight
- 51486.005 Da
References
- Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [Article]
- Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [Article]
- Fujinaga M, Hoffman BB, Baden JM: Receptor subtype and intracellular signal transduction pathway associated with situs inversus induced by alpha 1 adrenergic stimulation in rat embryos. Dev Biol. 1994 Apr;162(2):558-67. [Article]
- Huerta-Bahena J, Villalobos-Molina R, Garcia-Sainz JA: Trifluoperazine and chlorpromazine antagonize alpha 1- but not alpha2- adrenergic effects. Mol Pharmacol. 1983 Jan;23(1):67-70. [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
- Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. [Article]
- Torres-Piedra M, Figueroa M, Hernandez-Abreu O, Ibarra-Barajas M, Navarrete-Vazquez G, Estrada-Soto S: Vasorelaxant effect of flavonoids through calmodulin inhibition: Ex vivo, in vitro, and in silico approaches. Bioorg Med Chem. 2011 Jan 1;19(1):542-6. doi: 10.1016/j.bmc.2010.10.063. Epub 2010 Nov 4. [Article]
- Bohr V, Mansbridge J, Hanawalt P: Comparative effects of growth inhibitors on DNA replication, DNA repair, and protein synthesis in human epidermal keratinocytes. Cancer Res. 1986 Jun;46(6):2929-35. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- Troponin t binding
- Specific Function
- Troponin is the central regulatory protein of striated muscle contraction. Tn consists of three components: Tn-I which is the inhibitor of actomyosin ATPase, Tn-T which contains the binding site fo...
- Gene Name
- TNNC1
- Uniprot ID
- P63316
- Uniprot Name
- Troponin C, slow skeletal and cardiac muscles
- Molecular Weight
- 18402.36 Da
References
- Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. [Article]
- Kleerekoper Q, Liu W, Choi D, Putkey JA: Identification of binding sites for bepridil and trifluoperazine on cardiac troponin C. J Biol Chem. 1998 Apr 3;273(14):8153-60. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Rage receptor binding
- Specific Function
- Not Available
- Gene Name
- S100A4
- Uniprot ID
- P26447
- Uniprot Name
- Protein S100-A4
- Molecular Weight
- 11728.41 Da
References
- Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. [Article]
- Malashkevich VN, Dulyaninova NG, Ramagopal UA, Liriano MA, Varney KM, Knight D, Brenowitz M, Weber DJ, Almo SC, Bresnick AR: Phenothiazines inhibit S100A4 function by inducing protein oligomerization. Proc Natl Acad Sci U S A. 2010 May 11;107(19):8605-10. doi: 10.1073/pnas.0913660107. Epub 2010 Apr 26. [Article]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Modulator
- General Function
- Xanthine oxidase activity
- Specific Function
- Key enzyme in purine degradation. Catalyzes the oxidation of hypoxanthine to xanthine. Catalyzes the oxidation of xanthine to uric acid. Contributes to the generation of reactive oxygen species. Ha...
- Gene Name
- XDH
- Uniprot ID
- P47989
- Uniprot Name
- Xanthine dehydrogenase/oxidase
- Molecular Weight
- 146422.99 Da
References
- Hirata Y, Ishii K, Taguchi T, Suita S, Takeshige K: Conversion of xanthine dehydrogenase to xanthine oxidase during ischemia of the rat small intestine and the effect of trifluoperazine on the conversion. J Pediatr Surg. 1993 Apr;28(4):597-600. [Article]
- Greene EL, Paller MS: Calcium and free radicals in hypoxia/reoxygenation injury of renal epithelial cells. Am J Physiol. 1994 Jan;266(1 Pt 2):F13-20. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Protein homodimerization activity
- Specific Function
- UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds. This isoform glucuronidates bilirubin IX-alpha to form both the...
- Gene Name
- UGT1A4
- Uniprot ID
- P22310
- Uniprot Name
- UDP-glucuronosyltransferase 1-4
- Molecular Weight
- 60024.535 Da
References
- Kerdpin O, Mackenzie PI, Bowalgaha K, Finel M, Miners JO: Influence of N-terminal domain histidine and proline residues on the substrate selectivities of human UDP-glucuronosyltransferase 1A1, 1A6, 1A9, 2B7, and 2B10. Drug Metab Dispos. 2009 Sep;37(9):1948-55. doi: 10.1124/dmd.109.028225. Epub 2009 Jun 1. [Article]
- Fujiwara R, Nakajima M, Yamanaka H, Katoh M, Yokoi T: Interactions between human UGT1A1, UGT1A4, and UGT1A6 affect their enzymatic activities. Drug Metab Dispos. 2007 Oct;35(10):1781-7. Epub 2007 Jul 9. [Article]
- Uchaipichat V, Mackenzie PI, Elliot DJ, Miners JO: Selectivity of substrate (trifluoperazine) and inhibitor (amitriptyline, androsterone, canrenoic acid, hecogenin, phenylbutazone, quinidine, quinine, and sulfinpyrazone) "probes" for human udp-glucuronosyltransferases. Drug Metab Dispos. 2006 Mar;34(3):449-56. Epub 2005 Dec 28. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
- Gene Name
- CYP1A2
- Uniprot ID
- P05177
- Uniprot Name
- Cytochrome P450 1A2
- Molecular Weight
- 58293.76 Da
References
- Psychotropic Medications Metabolized by Cytochromes P450 (CYP) 1A2 Enzyme and Relevant Drug Interactions: Review of Articles [File]
Transporters
- 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