Identification
- Summary
Propofol is a medication used in general anesthesia and for sedation.
- Brand Names
- Diprivan
- Generic Name
- Propofol
- DrugBank Accession Number
- DB00818
- Background
Propofol is an intravenous anaesthetic agent used for induction and maintenance of general anaesthesia. IV administration of propfol is used to induce unconsciousness after which anaesthesia may be maintained using a combination of medications. Recovery from propofol-induced anaesthesia is generally rapid and associated with less frequent side effects (e.g. drowsiness, nausea, vomiting) than with thiopental, methohexital, and etomidate. Propofol may be used prior to diagnostic procedures requiring anaesthesia, in the management of refractory status epilepticus, and for induction and/or maintenance of anaesthesia prior to and during surgeries.
- Type
- Small Molecule
- Groups
- Approved, Investigational, Vet approved
- Structure
Structure for Propofol (DB00818)
- Weight
- Average: 178.2707
Monoisotopic: 178.135765198 - Chemical Formula
- C12H18O
- Synonyms
- 2,6-bis(1-methylethyl)phenol
- 2,6-Diisopropylphenol
- Propofol
- Propofolum
- External IDs
- ICI 35-868
- ICI 35,868
- ICI 35868
- ICI-35868
- ICI35,868
Pharmacology
- Indication
Used for induction and/or maintenance of anaesthesia and for management of refractory status epilepticus.
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- 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
Propofol is a sedative-hypnotic agent for use in the induction and maintenance of anesthesia or sedation. Intravenous injection of a therapeutic dose of propofol produces hypnosis rapidly with minimal excitation, usually within 40 seconds from the start of an injection (the time for one arm-brain circulation).
- Mechanism of action
The action of propofol involves a positive modulation of the inhibitory function of the neurotransmitter gama-aminobutyric acid (GABA) through GABA-A receptors.
Target Actions Organism AGamma-aminobutyric acid receptor subunit beta-2 potentiatorHumans AGamma-aminobutyric acid receptor subunit beta-3 potentiatorHumans AGABA(A) Receptor positive allosteric modulatorHumans USodium channel protein type 4 subunit alpha inhibitorHumans USodium channel protein type 2 subunit alpha inhibitorHumans - Absorption
Rapid - time to onset of unconsciousness is 15-30 seconds, due to rapid distribution from plasma to the CNS. Distribution is so rapid that peak plasma concentrations cannot be readily measured. Duration of action is 5-10 minutes.
- Volume of distribution
- 60 L/kg [healthy adults]
- Protein binding
95 to 99%, primarily to serum albumin and hemoglobin
- Metabolism
Hepatically metabolized mainly by glucuronidation at the C1-hydroxyl. Hydroxylation of the benzene ring to 4-hydroxypropofol may also occur via CYP2B6 and 2C9 with subsequent conjugation to sulfuric and/or glucuronic acid. Hydroxypropofol has approximately 1/3 of hypnotic activity of propofol.
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- Route of elimination
It is chiefly eliminated by hepatic conjugation to inactive metabolites which are excreted by the kidney.
- Half-life
Initial distribution phase t1/2α=1.8-9.5 minutes. Second redistirubtion phase t1/2β=21-70 minutes. Terminal elimination phase t1/2γ=1.5-31 hours.
- Clearance
- 23 - 50 mL/kg/min
- 1.6 - 3.4 L/min [70 Kg adults]
- Adverse Effects
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Overdosage may increase pharmacologic and adverse effects or cause death.
IV LD50=53 mg/kg (mice), 42 mg/kg (rats). Oral LD50 (as a solution in soybean oil)=1230 mg/kg (mice), 600 mg/kg (rats)
- 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 Propofol is combined with 1,2-Benzodiazepine. Abacavir The metabolism of Abacavir can be decreased when combined with Propofol. Abaloparatide The risk or severity of adverse effects can be increased when Propofol is combined with Abaloparatide. Abametapir The serum concentration of Propofol can be increased when it is combined with Abametapir. Abatacept The metabolism of Propofol can be increased when combined with Abatacept. - Food Interactions
- No interactions found.
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.- International/Other Brands
- Anepol (Ha Na Pharm) / Anespro (Behrens) / Anesvan (Chi Sheng) / Critifol (Abbott) / Disoprivan (AstraZeneca) / Disoprofol / Dormofol (Actavis) / Fresofol (Boryung) / Gobbifol (Gobbi) / Hipnolam (AC Farma) / Hypro (Celon) / IV-Pro (Claris Lifesciences) / Lipuro (B. Braun Medical) / Oleo-Lax (Fada) / Plofed (Warsaw Pharmaceutical Works) / Profol (Biogalenic) / Profolen (Blausiegel) / Propofabb (Hospira) / Propofil (Alvia) / Propogen (Genepharm) / Propolipid (Fresenius) / Propovan (Bharat Serums) / Propoven (Fresenius) / Provive (AFT) / Rapinovet / Recofol (Bayer) / Safol (Novell) / Trivam (Hana Pharm) / Troypofol (Troikaa) / Unifol (Claris Lifesciences)
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Diprivan Injection, emulsion 10 mg/1mL Intravenous Fresenius Kabi USA, LLC 2009-11-13 Not applicable US 
Diprivan Injection, emulsion 10 mg/1mL Intravenous General Injectables & Vaccines 2010-03-01 Not applicable US Diprivan Injection, emulsion 10 mg/1mL Intravenous Fresenius Kabi USA, LLC 2020-01-13 Not applicable US Diprivan Injection, emulsion 10 mg/1mL Intravenous Astra Zeneca Lp 1996-06-24 2010-10-31 US Diprivan 1% Emulsion 10 mg / mL Intravenous Aspen Pharmacare Canada Inc. 1993-12-31 Not applicable Canada 
- Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Propofol Injection, emulsion 10 mg/1mL Intravenous General Injectables and Vaccines, Inc. 2018-04-11 2019-07-31 US Propofol Injection, emulsion 10 mg/1mL Intravenous Hospira, Inc. 2022-05-22 Not applicable US Propofol Injection, emulsion 10 mg/1mL Intravenous Hikma Pharmaceuticals USA Inc. 2020-05-01 Not applicable US Propofol Injection, emulsion 10 mg/1mL Intravenous REMEDYREPACK INC. 2021-10-25 Not applicable US Propofol Injection, emulsion 10 mg/1mL Intravenous Hospira, Inc. 2006-04-03 Not applicable US - Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image Anesthesia S/I-40 Propofol (10 mg/1mL) + Isopropyl alcohol (0.7 mL/1mL) Injection, emulsion; Kit Intravenous; Topical RX PHARMA-PACK, INC. 2017-08-24 Not applicable US Anesthesia S/I-50 Propofol (10 mg/1mL) + Isopropyl alcohol (0.7 mL/1mL) Injection, emulsion; Kit Intravenous; Topical RX PHARMA-PACK, INC. 2017-06-16 2018-12-14 US Anesthesia S/I-60 Propofol (10 mg/1mL) + Isopropyl alcohol (0.7 mL/1mL) Injection, emulsion; Kit Intravenous; Topical RX PHARMA-PACK, INC. 2017-06-16 Not applicable US - Unapproved/Other Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image Fresenius Propoven 2% Propofol (20 mg/1mL) Emulsion Intravenous Fresenius Kabi Austria GmbH 2020-06-05 Not applicable US Fresenius Propoven 2% Propofol (20 mg/1mL) Emulsion Intravenous Fresenius Kabi USA, LLC 2020-06-05 Not applicable US PROPOFOL % 1 FRESENIUS 10 GR 20 ML AMPUL, 5 ADET Propofol (1 %) Emulsion Intravenous FRESENİUS KABİ İLAÇ SAN. VE TİC. LTD. ŞTİ. 2013-01-29 2022-11-03 Turkey 
Propofol 1% Propofol (10 mg/1mL) Injection, emulsion Intravenous Genixus 2023-03-29 Not applicable US Propofol Lipuro Propofol (10 mg/1mL) Injection, emulsion Intravenous B. Braun Medical Inc. 2021-03-12 Not applicable US
Categories
- ATC Codes
- N01AX10 — Propofol
- Drug Categories
- Agents Causing Muscle Toxicity
- Agents that produce hypertension
- Agents that reduce seizure threshold
- Anesthetics
- Anesthetics, General
- Anesthetics, Intravenous
- Benzene Derivatives
- Central Nervous System Agents
- Central Nervous System Depressants
- Cytochrome P-450 CYP1A2 Inhibitors
- Cytochrome P-450 CYP1A2 Inhibitors (strength unknown)
- Cytochrome P-450 CYP2B6 Substrates
- Cytochrome P-450 CYP2C18 Substrates
- Cytochrome P-450 CYP2C19 Substrates
- Cytochrome P-450 CYP2C8 Substrates
- Cytochrome P-450 CYP2C9 Substrates
- Cytochrome P-450 CYP2E1 Inhibitors
- Cytochrome P-450 CYP2E1 Inhibitors (strength unknown)
- Cytochrome P-450 CYP3A Inhibitors
- Cytochrome P-450 CYP3A4 Inhibitors
- Cytochrome P-450 CYP3A4 Inhibitors (weak)
- Cytochrome P-450 Enzyme Inhibitors
- Cytochrome P-450 Substrates
- Hypnotics and Sedatives
- Hypotensive Agents
- Miscellaneous General Anesthetics
- Nervous System
- P-glycoprotein inducers
- Phenols
- Potential QTc-Prolonging Agents
- QTc Prolonging Agents
- UGT1A1 Inhibitors
- UGT1A1 Substrates
- UGT1A6 substrate
- UGT1A9 Substrates
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as cumenes. These are aromatic compounds containing a prop-2-ylbenzene moiety.
- Kingdom
- Organic compounds
- Super Class
- Benzenoids
- Class
- Benzene and substituted derivatives
- Sub Class
- Cumenes
- Direct Parent
- Cumenes
- Alternative Parents
- Phenylpropanes / 1-hydroxy-4-unsubstituted benzenoids / Organooxygen compounds / Hydrocarbon derivatives
- Substituents
- 1-hydroxy-4-unsubstituted benzenoid / Aromatic homomonocyclic compound / Cumene / Hydrocarbon derivative / Organic oxygen compound / Organooxygen compound / Phenol / Phenylpropane
- Molecular Framework
- Aromatic homomonocyclic compounds
- External Descriptors
- phenols (CHEBI:44915) / a small molecule (CPD-11437)
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- YI7VU623SF
- CAS number
- 2078-54-8
- InChI Key
- OLBCVFGFOZPWHH-UHFFFAOYSA-N
- InChI
- InChI=1S/C12H18O/c1-8(2)10-6-5-7-11(9(3)4)12(10)13/h5-9,13H,1-4H3
- IUPAC Name
- 2,6-bis(propan-2-yl)phenol
- SMILES
- CC(C)C1=CC=CC(C(C)C)=C1O
References
- Synthesis Reference
John R. Carpenter, "Propofol-based anesthetic and method of making same." U.S. Patent US6150423, issued May, 1977.
US6150423- General References
- Vasile B, Rasulo F, Candiani A, Latronico N: The pathophysiology of propofol infusion syndrome: a simple name for a complex syndrome. Intensive Care Med. 2003 Sep;29(9):1417-25. Epub 2003 Aug 6. [Article]
- Ke JJ, Zhan J, Feng XB, Wu Y, Rao Y, Wang YL: A comparison of the effect of total intravenous anaesthesia with propofol and remifentanil and inhalational anaesthesia with isoflurane on the release of pro- and anti-inflammatory cytokines in patients undergoing open cholecystectomy. Anaesth Intensive Care. 2008 Jan;36(1):74-8. [Article]
- Hong JY, Kang YS, Kil HK: Anaesthesia for day case excisional breast biopsy: propofol-remifentanil compared with sevoflurane-nitrous oxide. Eur J Anaesthesiol. 2008 Jun;25(6):460-7. doi: 10.1017/S026502150800375X. Epub 2008 Feb 26. [Article]
- FDA Approved Drug Products: DIPRIVAN (propofol) injectable emulsion for intravenous use [Link]
- External Links
- Human Metabolome Database
- HMDB0014956
- KEGG Drug
- D00549
- KEGG Compound
- C07523
- PubChem Compound
- 4943
- PubChem Substance
- 46504991
- ChemSpider
- 4774
- BindingDB
- 50058046
- 8782
- ChEBI
- 44915
- ChEMBL
- CHEMBL526
- ZINC
- ZINC000000968303
- Therapeutic Targets Database
- DAP000662
- PharmGKB
- PA451141
- PDBe Ligand
- PFL
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Propofol
- PDB Entries
- 1e7a / 3p50 / 5muo / 5mur / 5mvm / 5mvn / 5mzr / 6x3t
- FDA label
- Download (168 KB)
- MSDS
- Download (71.9 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 4 Active Not Recruiting Treatment Acute Pain / Coronary Artery Disease (CAD) / Postoperative pain / Valvular Heart Disease 1 4 Active Not Recruiting Treatment Anesthesia therapy 1 4 Active Not Recruiting Treatment Driving Performance After Minor Ambulatory Surgery / Minor Surgical Procedures With Monitored Anesthesia Care 1 4 Active Not Recruiting Treatment General Anesthesia / Surgical Oncology 1 4 Completed Not Available Digestive System Diseases / Disorientation 1
Pharmacoeconomics
- Manufacturers
- App pharmaceuticals llc
- Bedford laboratories div ben venue laboratories inc
- Hospira inc
- Teva parenteral medicines inc
- Packagers
- APP Pharmaceuticals
- AstraZeneca Inc.
- Baxter International Inc.
- Cardinal Health
- Hospira Inc.
- Pfizer Inc.
- Sicor Pharmaceuticals
- Teva Pharmaceutical Industries Ltd.
- Dosage Forms
Form Route Strength Injection, emulsion; kit Intravenous; Topical Emulsion 20.000 mg Emulsion Intravenous; Parenteral 10 MG/ML Emulsion Parenteral 1.000 g Emulsion Intravenous 500 mg Solution Parenteral 20 mg Suspension Intravenous 10 mg Emulsion Intravenous 20 mg/1mL Emulsion Intravenous 0.2 g Emulsion Parenteral 0.200 g Injection Intravenous Injection Intravenous 1 % Injection, emulsion Intravenous 1 % Emulsion 20 mg/1ml Emulsion Intravenous 2 % Emulsion Parenteral 10 mg Emulsion Intravenous 500.00 mg Emulsion Intravenous 0.5 g Injection Injection Parenteral 200 mg Emulsion Intravenous 200 mg/20ml Injection Intravenous 10 MG/ML Injection, emulsion Intravenous 10 mg/1mL Injection, emulsion Intravenous Injection, solution Intravenous Emulsion Intravenous 1 % Emulsion Parenteral Emulsion Intravenous 10 mg Emulsion Intravenous 1 g Emulsion Parenteral 5 MG/ML Injection, emulsion Parenteral Emulsion 10 MG/ML Emulsion 20 MG/ML Injection Intravenous 1000 mg/100ml Injection Intravenous 200 mg/20ml Injection Intravenous 500 mg/50ml Injection, emulsion Intravenous 10 MG/ML Injection, emulsion Intravenous 20 MG/ML Emulsion Intravenous 10 mg / mL Emulsion Emulsion Intravenous 100 mg Emulsion Intravenous 200 mg Injection, emulsion Intravenous 2 % Emulsion Intravenous 20.0 mg/ml Emulsion Intravenous 10 mg/ml Emulsion Parenteral 1 % Injection Intravenous 10 mg/1mL Emulsion Intravenous 220.000 mg Emulsion Intravenous 10.000 mg Injection Intravenous 20 mg/ml Emulsion Intravenous 200.00 mg Emulsion Parenteral 10 MG/ML Emulsion Parenteral 20 MG/ML Injection Intravenous 10 mg Emulsion Intravenous 200.000 mg Injection, emulsion 10 mg/1ml Emulsion 10 mg/1ml Solution Parenteral 10 mg/1ml - Prices
Unit description Cost Unit Diprivan 10 mg/ml vial 0.93USD ml Propoven 1000 mg/100 ml vial 0.19USD ml Propoven 200 mg/20 ml ampul 0.19USD ml Propoven 500 mg/50 ml vial 0.19USD ml Propofol 10 mg/ml vial 0.13USD ml Propofol 1% emulsion vial 0.1USD ml DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region CA2212794 No 2000-09-12 2015-03-17 Canada US8476010 Yes 2013-07-02 2025-06-01 US US5908869 Yes 1999-06-01 2015-09-22 US US5731356 Yes 1998-03-24 2015-09-22 US US5731355 Yes 1998-03-24 2015-09-22 US US5714520 Yes 1998-02-03 2015-09-22 US
Properties
- State
- Liquid
- Experimental Properties
Property Value Source melting point (°C) 18 °C PhysProp boiling point (°C) 256 °C PhysProp water solubility 124 mg/L Not Available logP 3.79 HANSCH,C ET AL. (1995) pKa 11.1 (at 20 °C) SERJEANT,EP & DEMPSEY,B (1979) - Predicted Properties
Property Value Source Water Solubility 0.158 mg/mL ALOGPS logP 3.81 ALOGPS logP 4.16 Chemaxon logS -3 ALOGPS pKa (Strongest Acidic) 10.98 Chemaxon pKa (Strongest Basic) -5 Chemaxon Physiological Charge 0 Chemaxon Hydrogen Acceptor Count 1 Chemaxon Hydrogen Donor Count 1 Chemaxon Polar Surface Area 20.23 Å2 Chemaxon Rotatable Bond Count 2 Chemaxon Refractivity 56.42 m3·mol-1 Chemaxon Polarizability 21.61 Å3 Chemaxon Number of Rings 1 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 + 0.9955 Blood Brain Barrier + 0.9381 Caco-2 permeable + 0.9153 P-glycoprotein substrate Non-substrate 0.722 P-glycoprotein inhibitor I Non-inhibitor 0.9343 P-glycoprotein inhibitor II Non-inhibitor 0.9883 Renal organic cation transporter Non-inhibitor 0.9036 CYP450 2C9 substrate Non-substrate 0.7352 CYP450 2D6 substrate Substrate 0.7838 CYP450 3A4 substrate Non-substrate 0.5667 CYP450 1A2 substrate Inhibitor 0.9107 CYP450 2C9 inhibitor Non-inhibitor 0.907 CYP450 2D6 inhibitor Non-inhibitor 0.9368 CYP450 2C19 inhibitor Non-inhibitor 0.9026 CYP450 3A4 inhibitor Non-inhibitor 0.9196 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.7429 Ames test Non AMES toxic 0.9282 Carcinogenicity Non-carcinogens 0.7195 Biodegradation Not ready biodegradable 0.7808 Rat acute toxicity 2.2996 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.8987 hERG inhibition (predictor II) Non-inhibitor 0.9087
Spectra
- Mass Spec (NIST)
- Download (7.9 KB)
- Spectra
- Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 149.0734608 predictedDarkChem Lite v0.1.0 [M-H]- 138.5598058 predictedDarkChem Lite v0.1.0 [M-H]- 148.7001608 predictedDarkChem Lite v0.1.0 [M-H]- 144.76744 predictedDeepCCS 1.0 (2019) [M-H]- 149.0734608 predictedDarkChem Lite v0.1.0 [M-H]- 138.5598058 predictedDarkChem Lite v0.1.0 [M-H]- 148.7001608 predictedDarkChem Lite v0.1.0 [M-H]- 144.76744 predictedDeepCCS 1.0 (2019) [M+H]+ 148.8474608 predictedDarkChem Lite v0.1.0 [M+H]+ 144.6142271 predictedDarkChem Lite v0.1.0 [M+H]+ 149.0566608 predictedDarkChem Lite v0.1.0 [M+H]+ 147.26515 predictedDeepCCS 1.0 (2019) [M+H]+ 148.8474608 predictedDarkChem Lite v0.1.0 [M+H]+ 144.6142271 predictedDarkChem Lite v0.1.0 [M+H]+ 149.0566608 predictedDarkChem Lite v0.1.0 [M+H]+ 147.26515 predictedDeepCCS 1.0 (2019) [M+Na]+ 149.1342608 predictedDarkChem Lite v0.1.0 [M+Na]+ 150.9871662 predictedDarkChem Lite v0.1.0 [M+Na]+ 148.6840608 predictedDarkChem Lite v0.1.0 [M+Na]+ 155.7483 predictedDeepCCS 1.0 (2019) [M+Na]+ 149.1342608 predictedDarkChem Lite v0.1.0 [M+Na]+ 150.9871662 predictedDarkChem Lite v0.1.0 [M+Na]+ 148.6840608 predictedDarkChem Lite v0.1.0 [M+Na]+ 155.7483 predictedDeepCCS 1.0 (2019)
Targets
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Use our structured and evidence-based datasets to unlock newinsights and accelerate drug research.
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- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Potentiator
- General Function
- Inhibitory extracellular ligand-gated ion channel activity
- Specific Function
- Component of the heteropentameric receptor for GABA, the major inhibitory neurotransmitter in the vertebrate brain. Functions also as histamine receptor and mediates cellular responses to histamine...
- Gene Name
- GABRB2
- Uniprot ID
- P47870
- Uniprot Name
- Gamma-aminobutyric acid receptor subunit beta-2
- Molecular Weight
- 59149.895 Da
References
- Franks NP: Molecular targets underlying general anaesthesia. Br J Pharmacol. 2006 Jan;147 Suppl 1:S72-81. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Potentiator
- General Function
- Gaba-gated chloride ion channel activity
- Specific Function
- Component of the heteropentameric receptor for GABA, the major inhibitory neurotransmitter in the vertebrate brain. Functions also as histamine receptor and mediates cellular responses to histamine...
- Gene Name
- GABRB3
- Uniprot ID
- P28472
- Uniprot Name
- Gamma-aminobutyric acid receptor subunit beta-3
- Molecular Weight
- 54115.04 Da
References
- Franks NP: Molecular targets underlying general anaesthesia. Br J Pharmacol. 2006 Jan;147 Suppl 1:S72-81. [Article]
- Kind
- Protein group
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Positive allosteric modulator
- General Function
- Inhibitory extracellular ligand-gated ion channel activity
- Specific Function
- Component of the heteropentameric receptor for GABA, the major inhibitory neurotransmitter in the vertebrate brain. Functions also as histamine receptor and mediates cellular responses to histamine...
Components:
References
- ChEMBL Compound Report Card [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Voltage-gated sodium channel activity
- Specific Function
- This protein mediates the voltage-dependent sodium ion permeability of excitable membranes. Assuming opened or closed conformations in response to the voltage difference across the membrane, the pr...
- Gene Name
- SCN4A
- Uniprot ID
- P35499
- Uniprot Name
- Sodium channel protein type 4 subunit alpha
- Molecular Weight
- 208059.175 Da
References
- Haeseler G, Karst M, Foadi N, Gudehus S, Roeder A, Hecker H, Dengler R, Leuwer M: High-affinity blockade of voltage-operated skeletal muscle and neuronal sodium channels by halogenated propofol analogues. Br J Pharmacol. 2008 Sep;155(2):265-75. doi: 10.1038/bjp.2008.255. Epub 2008 Jun 23. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Voltage-gated sodium channel activity
- Specific Function
- Mediates the voltage-dependent sodium ion permeability of excitable membranes. Assuming opened or closed conformations in response to the voltage difference across the membrane, the protein forms a...
- Gene Name
- SCN2A
- Uniprot ID
- Q99250
- Uniprot Name
- Sodium channel protein type 2 subunit alpha
- Molecular Weight
- 227972.64 Da
References
- Haeseler G, Karst M, Foadi N, Gudehus S, Roeder A, Hecker H, Dengler R, Leuwer M: High-affinity blockade of voltage-operated skeletal muscle and neuronal sodium channels by halogenated propofol analogues. Br J Pharmacol. 2008 Sep;155(2):265-75. doi: 10.1038/bjp.2008.255. Epub 2008 Jun 23. [Article]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Steroid hydroxylase activity
- 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
- CYP2C9
- Uniprot ID
- P11712
- Uniprot Name
- Cytochrome P450 2C9
- Molecular Weight
- 55627.365 Da
References
- Mikstacki A, Zakerska-Banaszak O, Skrzypczak-Zielinska M, Tamowicz B, Prendecki M, Dorszewska J, Molinska-Glura M, Waszak M, Slomski R: The effect of UGT1A9, CYP2B6 and CYP2C9 genes polymorphism on individual differences in propofol pharmacokinetics among Polish patients undergoing general anaesthesia. J Appl Genet. 2017 May;58(2):213-220. doi: 10.1007/s13353-016-0373-2. Epub 2016 Nov 8. [Article]
- Ouchi K, Sugiyama K: Required propofol dose for anesthesia and time to emerge are affected by the use of antiepileptics: prospective cohort study. BMC Anesthesiol. 2015 Mar 15;15:34. doi: 10.1186/s12871-015-0006-z. eCollection 2015. [Article]
- 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]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Steroid hydroxylase activity
- 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
- CYP2B6
- Uniprot ID
- P20813
- Uniprot Name
- Cytochrome P450 2B6
- Molecular Weight
- 56277.81 Da
References
- Mourao AL, de Abreu FG, Fiegenbaum M: Impact of the Cytochrome P450 2B6 (CYP2B6) Gene Polymorphism c.516G>T (rs3745274) on Propofol Dose Variability. Eur J Drug Metab Pharmacokinet. 2016 Oct;41(5):511-5. doi: 10.1007/s13318-015-0289-y. [Article]
- Eugene AR: CYP2B6 Genotype Guided Dosing of Propofol Anesthesia in the Elderly based on Nonparametric Population Pharmacokinetic Modeling and Simulations. Int J Clin Pharmacol Toxicol. 2017;6(1):242-249. Epub 2017 Jan 3. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Steroid binding
- Specific Function
- UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds. Isoform 2 lacks transferase activity but acts as a negative reg...
- Gene Name
- UGT1A8
- Uniprot ID
- Q9HAW9
- Uniprot Name
- UDP-glucuronosyltransferase 1-8
- Molecular Weight
- 59741.035 Da
References
- Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Retinoic acid binding
- Specific Function
- UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds. This isoform has specificity for phenols. Isoform 2 lacks trans...
- Gene Name
- UGT1A9
- Uniprot ID
- O60656
- Uniprot Name
- UDP-glucuronosyltransferase 1-9
- Molecular Weight
- 59940.495 Da
References
- Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [Article]
- Takahashi H, Maruo Y, Mori A, Iwai M, Sato H, Takeuchi Y: Effect of D256N and Y483D on propofol glucuronidation by human uridine 5'-diphosphate glucuronosyltransferase (UGT1A9). Basic Clin Pharmacol Toxicol. 2008 Aug;103(2):131-6. doi: 10.1111/j.1742-7843.2008.00247.x. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- SubstrateInhibitor
- General Function
- Steroid binding
- 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
- UGT1A1
- Uniprot ID
- P22309
- Uniprot Name
- UDP-glucuronosyltransferase 1-1
- Molecular Weight
- 59590.91 Da
References
- Mano Y, Usui T, Kamimura H: Substrate-dependent modulation of UDP-glucuronosyltransferase 1A1 (UGT1A1) by propofol in recombinant human UGT1A1 and human liver microsomes. Basic Clin Pharmacol Toxicol. 2007 Sep;101(3):211-4. [Article]
- Williams JA, Hyland R, Jones BC, Smith DA, Hurst S, Goosen TC, Peterkin V, Koup JR, Ball SE: Drug-drug interactions for UDP-glucuronosyltransferase substrates: a pharmacokinetic explanation for typically observed low exposure (AUCi/AUC) ratios. Drug Metab Dispos. 2004 Nov;32(11):1201-8. doi: 10.1124/dmd.104.000794. Epub 2004 Aug 10. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Fatty acid amide hydrolase activity
- Specific Function
- Degrades bioactive fatty acid amides like oleamide, the endogenous cannabinoid, anandamide and myristic amide to their corresponding acids, thereby serving to terminate the signaling functions of t...
- Gene Name
- FAAH
- Uniprot ID
- O00519
- Uniprot Name
- Fatty-acid amide hydrolase 1
- Molecular Weight
- 63065.28 Da
References
- Zhu F, Han B, Kumar P, Liu X, Ma X, Wei X, Huang L, Guo Y, Han L, Zheng C, Chen Y: Update of TTD: Therapeutic Target Database. Nucleic Acids Res. 2010 Jan;38(Database issue):D787-91. doi: 10.1093/nar/gkp1014. Epub 2009 Nov 20. [Article]
- 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]
- 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
- Chen TL, Ueng TH, Chen SH, Lee PH, Fan SZ, Liu CC: Human cytochrome P450 mono-oxygenase system is suppressed by propofol. Br J Anaesth. 1995 May;74(5):558-62. [Article]
- Lejus C, Fautrel A, Malledant Y, Guillouzo A: Inhibition of cytochrome P450 2E1 by propofol in human and porcine liver microsomes. Biochem Pharmacol. 2002 Oct 1;64(7):1151-6. doi: 10.1016/s0006-2952(02)01226-1. [Article]
- Yang LQ, Yu WF, Cao YF, Gong B, Chang Q, Yang GS: Potential inhibition of cytochrome P450 3A4 by propofol in human primary hepatocytes. World J Gastroenterol. 2003 Sep;9(9):1959-62. doi: 10.3748/wjg.v9.i9.1959. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Oxygen binding
- 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
- CYP1B1
- Uniprot ID
- Q16678
- Uniprot Name
- Cytochrome P450 1B1
- Molecular Weight
- 60845.33 Da
References
- Chen TL, Ueng TH, Chen SH, Lee PH, Fan SZ, Liu CC: Human cytochrome P450 mono-oxygenase system is suppressed by propofol. Br J Anaesth. 1995 May;74(5):558-62. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Vitamin d 24-hydroxylase activity
- 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
- CYP1A1
- Uniprot ID
- P04798
- Uniprot Name
- Cytochrome P450 1A1
- Molecular Weight
- 58164.815 Da
References
- Chen TL, Ueng TH, Chen SH, Lee PH, Fan SZ, Liu CC: Human cytochrome P450 mono-oxygenase system is suppressed by propofol. Br J Anaesth. 1995 May;74(5):558-62. [Article]
- Campos SP, de Lurdes Pinto M, Gomes G, de Pinho PG, Monteiro JA, Felix LM, Branco PS, Ferreira LM, Antunes LM: Expression of CYP1A1 and CYP1A2 in the liver and kidney of rabbits after prolonged infusion of propofol. Exp Toxicol Pathol. 2016 Oct;68(9):521-531. doi: 10.1016/j.etp.2016.07.006. Epub 2016 Aug 13. [Article]
- Yang LQ, Yu WF, Cao YF, Gong B, Chang Q, Yang GS: Potential inhibition of cytochrome P450 3A4 by propofol in human primary hepatocytes. World J Gastroenterol. 2003 Sep;9(9):1959-62. doi: 10.3748/wjg.v9.i9.1959. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- Curator comments
- Current data available supporting this enzyme action are in vitro studies.
- 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
- McKillop D, Wild MJ, Butters CJ, Simcock C: Effects of propofol on human hepatic microsomal cytochrome P450 activities. Xenobiotica. 1998 Sep;28(9):845-53. doi: 10.1080/004982598239092 . [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Steroid hydroxylase activity
- 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
- CYP2C18
- Uniprot ID
- P33260
- Uniprot Name
- Cytochrome P450 2C18
- Molecular Weight
- 55710.075 Da
References
- Dinis-Oliveira RJ: Metabolic Profiles of Propofol and Fospropofol: Clinical and Forensic Interpretative Aspects. Biomed Res Int. 2018 May 24;2018:6852857. doi: 10.1155/2018/6852857. eCollection 2018. [Article]
- Guitton J, Buronfosse T, Desage M, Flinois JP, Perdrix JP, Brazier JL, Beaune P: Possible involvement of multiple human cytochrome P450 isoforms in the liver metabolism of propofol. Br J Anaesth. 1998 Jun;80(6):788-95. doi: 10.1093/bja/80.6.788. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Steroid hydroxylase activity
- Specific Function
- Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and im...
- Gene Name
- CYP2C19
- Uniprot ID
- P33261
- Uniprot Name
- Cytochrome P450 2C19
- Molecular Weight
- 55930.545 Da
References
- Guitton J, Buronfosse T, Desage M, Flinois JP, Perdrix JP, Brazier JL, Beaune P: Possible involvement of multiple human cytochrome P450 isoforms in the liver metabolism of propofol. Br J Anaesth. 1998 Jun;80(6):788-95. doi: 10.1093/bja/80.6.788. [Article]
- Ouchi K, Sugiyama K: Required propofol dose for anesthesia and time to emerge are affected by the use of antiepileptics: prospective cohort study. BMC Anesthesiol. 2015 Mar 15;15:34. doi: 10.1186/s12871-015-0006-z. eCollection 2015. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Steroid hydroxylase activity
- 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
- CYP2C8
- Uniprot ID
- P10632
- Uniprot Name
- Cytochrome P450 2C8
- Molecular Weight
- 55824.275 Da
References
- 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 has specificity for phenols. Isoform 3 lacks trans...
- Gene Name
- UGT1A6
- Uniprot ID
- P19224
- Uniprot Name
- UDP-glucuronosyltransferase 1-6
- Molecular Weight
- 60750.215 Da
References
- Gu J, Lu K, Xia P, Tang M, Dai Q, Ma D, Tao G: Pharmacokinetics of propofol and extrahepatic UGT1A6 gene expression in anhepatic rats. Pharmacology. 2009;84(4):219-26. doi: 10.1159/000236523. Epub 2009 Sep 10. [Article]
Carriers
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- General Function
- Toxic substance binding
- Specific Function
- Serum albumin, the main protein of plasma, has a good binding capacity for water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs. Its main function is the regulation of the colloid...
- Gene Name
- ALB
- Uniprot ID
- P02768
- Uniprot Name
- Serum albumin
- Molecular Weight
- 69365.94 Da
References
- Bright DP, Adham SD, Lemaire LC, Benavides R, Gruss M, Taylor GW, Smith EH, Franks NP: Identification of anesthetic binding sites on human serum albumin using a novel etomidate photolabel. J Biol Chem. 2007 Apr 20;282(16):12038-47. Epub 2007 Feb 20. [Article]
- Liu R, Eckenhoff RG: Weak polar interactions confer albumin binding site selectivity for haloether anesthetics. Anesthesiology. 2005 Apr;102(4):799-805. [Article]
- Sawas AH, Pentyala SN, Rebecchi MJ: Binding of volatile anesthetics to serum albumin: measurements of enthalpy and solvent contributions. Biochemistry. 2004 Oct 5;43(39):12675-85. [Article]
- Schywalsky M, Ihmsen H, Knoll R, Schwilden H: Binding of propofol to human serum albumin. Arzneimittelforschung. 2005;55(6):303-6. [Article]
Transporters
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inducer
- 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
- Regev R, Katzir H, Yeheskely-Hayon D, Eytan GD: Modulation of P-glycoprotein-mediated multidrug resistance by acceleration of passive drug permeation across the plasma membrane. FEBS J. 2007 Dec;274(23):6204-14. doi: 10.1111/j.1742-4658.2007.06140.x. Epub 2007 Nov 6. [Article]
Drug created at June 13, 2005 13:24 / Updated at February 20, 2024 23:55