Trifluoperazine
Explore a selection of our essential drug information below, or:
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
- 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 AD(2) dopamine receptor antagonistHumans ACalmodulin-1 inhibitorHumans ACalmodulin-3 inhibitorHumans ACalmodulin-2 inhibitorHumans ANeuron-specific vesicular protein calcyon antagonistHumans AAlpha-1A adrenergic receptor antagonistHumans UTroponin C, slow skeletal and cardiac muscles Not Available Humans UProtein S100-A4 inhibitorHumans UCalmodulin 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
- 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.
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
Clinical Trial & Rare Diseases Add-on Data Package
Explore 4,000+ rare diseases, orphan drugs & condition pairs, clinical trial why stopped data, & more. Preview package Phase Status Purpose Conditions Count Start Date Why Stopped 100+ additional columns Unlock 175K+ rows when you subscribe.View sample dataNot Available Completed Not Available Bipolar Disorder (BD) / Psychosis / Schizoaffective Disorders / Schizophrenia / Type 2 Diabetes Mellitus 1 somestatus stop reason just information to hide Not Available Completed Not Available Schizophrenia 1 somestatus stop reason just information to hide 3 Unknown Status Treatment Psychosis Nos/Other 1 somestatus stop reason just information to hide 1, 2 Terminated Treatment Congenital Hypoplastic Anemia / Pure Red Cell Aplasia 1 somestatus stop reason just information to hide
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 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, 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
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antagonist
- General Function
- Dopamine receptor whose activity is mediated by G proteins which inhibit adenylyl cyclase (PubMed:21645528). Positively regulates postnatal regression of retinal hyaloid vessels via suppression of VEGFR2/KDR activity, downstream of OPN5 (By similarity)
- Specific Function
- dopamine binding
- 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
- Inhibitor
- General Function
- Calmodulin acts as part of a calcium signal transduction pathway by mediating the control of a large number of enzymes, ion channels, aquaporins and other proteins through calcium-binding (PubMed:16760425, PubMed:23893133, PubMed:26969752, PubMed:27165696, PubMed:28890335, PubMed:31454269, PubMed:35568036). Calcium-binding is required for the activation of calmodulin (PubMed:16760425, PubMed:23893133, PubMed:26969752, PubMed:27165696, PubMed:28890335, PubMed:31454269, PubMed:35568036). Among the enzymes to be stimulated by the calmodulin-calcium complex are a number of protein kinases, such as myosin light-chain kinases and calmodulin-dependent protein kinase type II (CaMK2), and phosphatases (PubMed:16760425, PubMed:23893133, PubMed:26969752, PubMed:27165696, PubMed:28890335, PubMed:31454269, PubMed:35568036). Together with CCP110 and centrin, is involved in a genetic pathway that regulates the centrosome cycle and progression through cytokinesis (PubMed:16760425). Is a regulator of voltage-dependent L-type calcium channels (PubMed:31454269). Mediates calcium-dependent inactivation of CACNA1C (PubMed:26969752). Positively regulates calcium-activated potassium channel activity of KCNN2 (PubMed:27165696). Forms a potassium channel complex with KCNQ1 and regulates electrophysiological activity of the channel via calcium-binding (PubMed:25441029). Acts as a sensor to modulate the endoplasmic reticulum contacts with other organelles mediated by VMP1:ATP2A2 (PubMed:28890335)
- Specific Function
- adenylate cyclase activator activity
- Gene Name
- CALM1
- Uniprot ID
- P0DP23
- Uniprot Name
- Calmodulin-1
- Molecular Weight
- 16837.47 Da
References
- Zhou Y, Zhang Y, Zhao D, Yu X, Shen X, Zhou Y, Wang S, Qiu Y, Chen Y, Zhu F: TTD: Therapeutic Target Database describing target druggability information. Nucleic Acids Res. 2024 Jan 5;52(D1):D1465-D1477. doi: 10.1093/nar/gkad751. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- Calmodulin acts as part of a calcium signal transduction pathway by mediating the control of a large number of enzymes, ion channels, aquaporins and other proteins through calcium-binding (PubMed:16760425, PubMed:31454269). Calcium-binding is required for the activation of calmodulin (PubMed:16760425, PubMed:31454269, PubMed:35568036). Among the enzymes to be stimulated by the calmodulin-calcium complex are a number of protein kinases, such as myosin light-chain kinases and calmodulin-dependent protein kinase type II (CaMK2), and phosphatases (PubMed:16760425, PubMed:35568036). Together with CCP110 and centrin, is involved in a genetic pathway that regulates the centrosome cycle and progression through cytokinesis (PubMed:16760425)
- Specific Function
- adenylate cyclase activator activity
- Gene Name
- CALM3
- Uniprot ID
- P0DP25
- Uniprot Name
- Calmodulin-3
- Molecular Weight
- 16837.47 Da
References
- Zhou Y, Zhang Y, Zhao D, Yu X, Shen X, Zhou Y, Wang S, Qiu Y, Chen Y, Zhu F: TTD: Therapeutic Target Database describing target druggability information. Nucleic Acids Res. 2024 Jan 5;52(D1):D1465-D1477. doi: 10.1093/nar/gkad751. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- Calmodulin acts as part of a calcium signal transduction pathway by mediating the control of a large number of enzymes, ion channels, aquaporins and other proteins through calcium-binding (PubMed:16760425, PubMed:26969752, PubMed:27165696). Calcium-binding is required for the activation of calmodulin (PubMed:16760425, PubMed:26969752, PubMed:27165696, PubMed:35568036). Among the enzymes to be stimulated by the calmodulin-calcium complex are a number of protein kinases, such as myosin light-chain kinases and calmodulin-dependent protein kinase type II (CaMK2), and phosphatases (PubMed:16760425, PubMed:26969752, PubMed:27165696, PubMed:35568036). Together with CCP110 and centrin, is involved in a genetic pathway that regulates the centrosome cycle and progression through cytokinesis (PubMed:16760425). Mediates calcium-dependent inactivation of CACNA1C (PubMed:26969752). Positively regulates calcium-activated potassium channel activity of KCNN2 (PubMed:27165696)
- Specific Function
- adenylate cyclase activator activity
- Gene Name
- CALM2
- Uniprot ID
- P0DP24
- Uniprot Name
- Calmodulin-2
- Molecular Weight
- 16837.47 Da
References
- Zhou Y, Zhang Y, Zhao D, Yu X, Shen X, Zhou Y, Wang S, Qiu Y, Chen Y, Zhu F: TTD: Therapeutic Target Database describing target druggability information. Nucleic Acids Res. 2024 Jan 5;52(D1):D1465-D1477. doi: 10.1093/nar/gkad751. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antagonist
- General Function
- Interacts with clathrin light chain A and stimulates clathrin self-assembly and clathrin-mediated endocytosis
- Specific Function
- clathrin light chain binding
- 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
- 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) proteins. Nuclear ADRA1A-ADRA1B heterooligomers regulate phenylephrine(PE)-stimulated ERK signaling in cardiac myocytes
- Specific Function
- alpha1-adrenergic receptor activity
- 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
- General 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 for tropomyosin and Tn-C. The binding of calcium to Tn-C abolishes the inhibitory action of Tn on actin filaments
- Specific Function
- actin filament binding
- 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
- Calcium-binding protein that plays a role in various cellular processes including motility, angiogenesis, cell differentiation, apoptosis, and autophagy (PubMed:16707441, PubMed:23752197, PubMed:30713770). Increases cell motility and invasiveness by interacting with non-muscle myosin heavy chain (NMMHC) IIA/MYH9 (PubMed:16707441). Mechanistically, promotes filament depolymerization and increases the amount of soluble myosin-IIA, resulting in the formation of stable protrusions facilitating chemotaxis (By similarity). Modulates also the pro-apoptotic function of TP53 by binding to its C-terminal transactivation domain within the nucleus and reducing its protein levels (PubMed:23752197). Within the extracellular space, stimulates cytokine production including granulocyte colony-stimulating factor and CCL24 from T-lymphocytes (By similarity). In addition, stimulates T-lymphocyte chemotaxis by acting as a chemoattractant complex with PGLYRP1 that promotes lymphocyte migration via CCR5 and CXCR3 receptors (PubMed:26654597, PubMed:30713770)
- Specific Function
- actin binding
- 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]
- Kind
- Protein group
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Calmodulin acts as part of a calcium signal transduction pathway by mediating the control of a large number of enzymes, ion channels, aquaporins and other proteins through calcium-binding (PubMed:16760425, PubMed:23893133, PubMed:26969752, PubMed:27165696, PubMed:28890335, PubMed:31454269, PubMed:35568036). Calcium-binding is required for the activation of calmodulin (PubMed:16760425, PubMed:23893133, PubMed:26969752, PubMed:27165696, PubMed:28890335, PubMed:31454269, PubMed:35568036). Among the enzymes to be stimulated by the calmodulin-calcium complex are a number of protein kinases, such as myosin light-chain kinases and calmodulin-dependent protein kinase type II (CaMK2), and phosphatases (PubMed:16760425, PubMed:23893133, PubMed:26969752, PubMed:27165696, PubMed:28890335, PubMed:31454269, PubMed:35568036). Together with CCP110 and centrin, is involved in a genetic pathway that regulates the centrosome cycle and progression through cytokinesis (PubMed:16760425). Is a regulator of voltage-dependent L-type calcium channels (PubMed:31454269). Mediates calcium-dependent inactivation of CACNA1C (PubMed:26969752). Positively regulates calcium-activated potassium channel activity of KCNN2 (PubMed:27165696). Forms a potassium channel complex with KCNQ1 and regulates electrophysiological activity of the channel via calcium-binding (PubMed:25441029). Acts as a sensor to modulate the endoplasmic reticulum contacts with other organelles mediated by VMP1:ATP2A2 (PubMed:28890335)
- Specific Function
- adenylate cyclase activator activity
Components:
Name | UniProt ID |
---|---|
Calmodulin-1 | P0DP23 |
Calmodulin-2 | P0DP24 |
Calmodulin-3 | P0DP25 |
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]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Modulator
- General 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. Has also low oxidase activity towards aldehydes (in vitro)
- Specific Function
- 2 iron, 2 sulfur cluster binding
- 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
- UDP-glucuronosyltransferase (UGT) that catalyzes phase II biotransformation reactions in which lipophilic substrates are conjugated with glucuronic acid to increase the metabolite's water solubility, thereby facilitating excretion into either the urine or bile (PubMed:18177842, PubMed:24641623). Essential for the elimination and detoxification of drugs, xenobiotics and endogenous compounds (PubMed:18177842). Involved in the glucuronidation of calcidiol, which is the major circulating form of vitamin D3 essential for the regulation of calcium and phosphate homeostasis (PubMed:24641623). Also glucuronidates the biologically active form of vitamin D3, calcitriol, probably leading to its biliary transport and intestinal reabsorption (PubMed:18177842)
- Specific Function
- enzyme binding
- Gene Name
- UGT1A4
- Uniprot ID
- P22310
- Uniprot Name
- UDP-glucuronosyltransferase 1A4
- 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
- A cytochrome P450 monooxygenase involved in the metabolism of various endogenous substrates, including fatty acids, steroid hormones and vitamins (PubMed:10681376, PubMed:11555828, PubMed:12865317, PubMed:19965576, PubMed:9435160). Mechanistically, uses molecular oxygen inserting one oxygen atom into a substrate, and reducing the second into a water molecule, with two electrons provided by NADPH via cytochrome P450 reductase (NADPH--hemoprotein reductase) (PubMed:10681376, PubMed:11555828, PubMed:12865317, PubMed:19965576, PubMed:9435160). Catalyzes the hydroxylation of carbon-hydrogen bonds (PubMed:11555828, PubMed:12865317). Exhibits high catalytic activity for the formation of hydroxyestrogens from estrone (E1) and 17beta-estradiol (E2), namely 2-hydroxy E1 and E2 (PubMed:11555828, PubMed:12865317). Metabolizes cholesterol toward 25-hydroxycholesterol, a physiological regulator of cellular cholesterol homeostasis (PubMed:21576599). May act as a major enzyme for all-trans retinoic acid biosynthesis in the liver. Catalyzes two successive oxidative transformation of all-trans retinol to all-trans retinal and then to the active form all-trans retinoic acid (PubMed:10681376). Primarily catalyzes stereoselective epoxidation of the last double bond of polyunsaturated fatty acids (PUFA), displaying a strong preference for the (R,S) stereoisomer (PubMed:19965576). Catalyzes bisallylic hydroxylation and omega-1 hydroxylation of PUFA (PubMed:9435160). May also participate in eicosanoids metabolism by converting hydroperoxide species into oxo metabolites (lipoxygenase-like reaction, NADPH-independent) (PubMed:21068195). Plays a role in the oxidative metabolism of xenobiotics. Catalyzes the N-hydroxylation of heterocyclic amines and the O-deethylation of phenacetin (PubMed:14725854). Metabolizes caffeine via N3-demethylation (Probable)
- Specific Function
- aromatase activity
- Gene Name
- CYP1A2
- Uniprot ID
- P05177
- Uniprot Name
- Cytochrome P450 1A2
- Molecular Weight
- 58406.915 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
- Translocates drugs and phospholipids across the membrane (PubMed:2897240, PubMed:35970996, PubMed:8898203, PubMed:9038218). Catalyzes the flop of phospholipids from the cytoplasmic to the exoplasmic leaflet of the apical membrane. Participates mainly to the flop of phosphatidylcholine, phosphatidylethanolamine, beta-D-glucosylceramides and sphingomyelins (PubMed:8898203). Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells (PubMed:2897240, PubMed:35970996, PubMed:9038218)
- Specific Function
- ABC-type xenobiotic transporter activity
- Gene Name
- ABCB1
- Uniprot ID
- P08183
- Uniprot Name
- ATP-dependent translocase ABCB1
- 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 October 21, 2024 12:53