Oxazepam
Identification
- Summary
Oxazepam is an intermediate-acting benzodiazepine with slow onset commonly used to treat panic disorders, severe anxiety, alcohol withdrawals, and insomnia.
- Brand Names
- Oxpam
- Generic Name
- Oxazepam
- DrugBank Accession Number
- DB00842
- Background
Oxazepam is an intermediate-acting, 3-hydroxybenzodiazepine used in the treatment of alcohol withdrawal and anxiety disorders. Oxazepam, like related 3-hydroxybenzodiazepine lorazepam, is considered less susceptible to pharmacokinetic variability based on patient-specific factors (e.g. age, liver disease) - this feature is advantageous as compared to other benzodiazepines, and is likely owing in part to oxazepam's relatively simple metabolism.11 It is an active metabolite of both diazepam and temazepam12 and undergoes very little biotransformation following absorption, making it unlikely to participate in pharmacokinetic interactions.14
- Type
- Small Molecule
- Groups
- Approved
- Structure
- Weight
- Average: 286.713
Monoisotopic: 286.050905313 - Chemical Formula
- C15H11ClN2O2
- Synonyms
- (+-)-Oxazepam
- (RS)-Oxazepam
- Oxazepam
- External IDs
- J3.308A
- NSC-169448
- WY-3498
Pharmacology
- Indication
Oxazepam is indicated for the management of anxiety disorders and for the short-term relief of symptoms of anxiety.14 It may also be used in the management of alcohol withdrawal symptoms.14
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 Symptomatic treatment of Alcohol withdrawal •••••••••••• ••••••• Symptomatic treatment of Anxiety •••••••••••• ••••••• Management of Anxiety disorders •••••••••••• ••••••• - 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
Benzodiazepines, including oxazepam, exert their sedative and anxiolytic effects by potentiating the effects of endogenous GABA, the primary inhibitory neurotransmitter in the CNS.10 Compared to other benzodiazepines, it has relatively low potency and a moderate duration of action.10 Oxazepam should be administered with caution to patients for whom a drop in blood pressure may lead to cardiac complications as, in rare cases, it may cause hypotension.14
- Mechanism of action
Like other benzodiazepines, oxazepam exerts its anxiolytic effects by potentiating the effect of gamma-aminobutyric acid (GABA) on GABA(A) receptors, the main inhibitory neurotransmitter receptors in the mammalian brain.8 GABA(A) receptors are a component of GABA-gated ionotropic chloride channels that produce inhibitory postsynaptic potentials - following activation by GABA, the channel undergoes a conformational change that allows the passage of chloride ions through the channel. The inhibitory potentials produced by GABA neurotransmission play an integral role in the suppression and control of epileptiform nerve firing such as that seen in epilepsy, which makes the GABA system a desirable target in the treatment of epilepsy.
Benzodiazepines are positive allosteric modulators of GABA(A) function. They bind to the interface between alpha (α) and gamma (γ) subunits on the receptor, commonly referred to as the benzodiazepine binding site, and modulate the receptor such that its inhibitory response to GABA binding is dramatically increased.8
Target Actions Organism AGABA(A) Receptor positive allosteric modulatorHumans AGABA(A) Receptor Benzodiazepine Binding Site ligandHumans - Absorption
Following oral administration, peak plasma levels (Cmax) averaged 450 mg/mL and occurred approximately 3 hours (Tmax) after dosing.14
- Volume of distribution
Not Available
- Protein binding
Plasma protein binding is approximately 89%,15 likely to albumin.7
- Metabolism
Oxazepam has a single major inactive metabolite, a glucuronide conjugate.14 The glucuronidation of the S-isomer is catalyzed by UGT2B15. The glucuronidation of the R-isomer is catalyzed by UGT2B7 and UGT1A9.13
Hover over products below to view reaction partners
- Route of elimination
Oxazepam is primarily eliminated in the urine as its glucuronide metabolite, with the feces containing approximately 21% of the unchanged drug.15 The majority of an orally ingested dose of oxazepam is excreted within 48 hours.15
- Half-life
The mean elimination half-life of oxazepam is 8.2 hours.14
- 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
The oral LD50 in rats and mice is >8000 mg/kg and 1540 mg/kg, respectively.16
Symptoms of oxazepam overdose are likely to be consistent with its adverse effect profile and range from mild to severe, sometimes fatal, CNS depression.14 Treatment should include gastric decontamination, via lavage or induced vomiting, followed by symptomatic and supportive measures. The benzodiazepine antagonist flumazenil may be used in hospitalized patients as an adjunct to non-pharmacological management, but may increase the risk of seizure in long-term benzodiazepine users and in cyclic antidepressant overdose.14
- 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 Oxazepam is combined with 1,2-Benzodiazepine. Abacavir Oxazepam may decrease the excretion rate of Abacavir which could result in a higher serum level. Aceclofenac Aceclofenac may decrease the excretion rate of Oxazepam which could result in a higher serum level. Acemetacin Acemetacin may decrease the excretion rate of Oxazepam which could result in a higher serum level. Acetaminophen Acetaminophen may decrease the excretion rate of Oxazepam which could result in a higher serum level. - Food Interactions
- Avoid alcohol. Co-administration with alcohol may potentiate the CNS effects of oxazepam.
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 Images
- International/Other Brands
- Adumbran / Alepam / Alopam / Anxiolit / Durazepam / Limbial / Medopam / Murelax / Noripam / Opamox / Ox-Pam / Oxascand / Praxiten / Purata / Serax (Landsteiner (Mexico)) / Serenal / Serenid / Serepax / Seresta / Serpax / Sobril / Tazepam / Vaben / Zaxpam
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Novoxapam Tab 10mg Tablet 10 mg Oral Novopharm Limited 1982-12-31 2015-10-26 Canada Novoxapam Tab 15mg Tablet 15 mg Oral Novopharm Limited 1982-12-31 2015-10-26 Canada Novoxapam Tab 30mg Tablet 30 mg Oral Novopharm Limited 1982-12-31 2015-10-26 Canada Oxazepam 10mg Tablets Tablet 10 mg / tab Oral Laboratoires Confab Inc Not applicable Not applicable Canada Oxazepam 15mg Tablets Tablet 15 mg / tab Oral Laboratoires Confab Inc Not applicable Not applicable Canada - Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Apo-oxazepam Tablet 10 mg Oral Apotex Corporation 1979-12-31 Not applicable Canada Apo-oxazepam Tablet 15 mg Oral Apotex Corporation 1979-12-31 Not applicable Canada Apo-oxazepam Tablet 30 mg Oral Apotex Corporation 1979-12-31 Not applicable Canada Bio-oxazepam Tablet 30 mg Oral Biomed Pharma 2003-04-23 2022-07-19 Canada Bio-oxazepam Tablet 15 mg Oral Biomed Pharma 2003-04-23 2022-07-19 Canada
Categories
- ATC Codes
- N05BA04 — Oxazepam
- Drug Categories
- Anti-Anxiety Agents
- Benzazepines
- Benzodiazepine hypnotics and sedatives
- Benzodiazepines and benzodiazepine derivatives
- Benzodiazepinones
- Central Nervous System Agents
- Central Nervous System Depressants
- Drugs that are Mainly Renally Excreted
- GABA Agents
- GABA Modulators
- Heterocyclic Compounds, Fused-Ring
- Hypnotics and Sedatives
- Nervous System
- Neurotransmitter Agents
- Psycholeptics
- Psychotropic Drugs
- Tranquilizing Agents
- UGT1A9 Substrates
- UGT2B7 substrates
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as 1,4-benzodiazepines. These are organic compounds containing a benzene ring fused to a 1,4-azepine.
- Kingdom
- Organic compounds
- Super Class
- Organoheterocyclic compounds
- Class
- Benzodiazepines
- Sub Class
- 1,4-benzodiazepines
- Direct Parent
- 1,4-benzodiazepines
- Alternative Parents
- Benzene and substituted derivatives / Aryl chlorides / Cyclic carboximidic acids / Ketimines / Propargyl-type 1,3-dipolar organic compounds / Azacyclic compounds / Alkanolamines / Organopnictogen compounds / Organooxygen compounds / Organochlorides show 1 more
- Substituents
- 1,4-benzodiazepine / Alkanolamine / Aromatic heteropolycyclic compound / Aryl chloride / Aryl halide / Azacycle / Benzenoid / Cyclic carboximidic acid / Hydrocarbon derivative / Imine show 11 more
- Molecular Framework
- Aromatic heteropolycyclic compounds
- External Descriptors
- organochlorine compound, 1,4-benzodiazepinone (CHEBI:7823)
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- 6GOW6DWN2A
- CAS number
- 604-75-1
- InChI Key
- ADIMAYPTOBDMTL-UHFFFAOYSA-N
- InChI
- InChI=1S/C15H11ClN2O2/c16-10-6-7-12-11(8-10)13(9-4-2-1-3-5-9)18-15(20)14(19)17-12/h1-8,15,20H,(H,17,19)
- IUPAC Name
- 7-chloro-3-hydroxy-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepin-2-one
- SMILES
- OC1N=C(C2=CC=CC=C2)C2=C(NC1=O)C=CC(Cl)=C2
References
- General References
- Peppers MP: Benzodiazepines for alcohol withdrawal in the elderly and in patients with liver disease. Pharmacotherapy. 1996 Jan-Feb;16(1):49-57. [Article]
- Skerritt JH, Johnston GA: Enhancement of GABA binding by benzodiazepines and related anxiolytics. Eur J Pharmacol. 1983 May 6;89(3-4):193-8. [Article]
- Oelschlager H: [Chemical and pharmacologic aspects of benzodiazepines]. Schweiz Rundsch Med Prax. 1989 Jul 4;78(27-28):766-72. [Article]
- Christensen P, Lolk A, Gram LF, Kragh-Sorensen P: Benzodiazepine-induced sedation and cortisol suppression. A placebo-controlled comparison of oxazepam and nitrazepam in healthy male volunteers. Psychopharmacology (Berl). 1992;106(4):511-6. [Article]
- Olive G, Dreux C: [Pharmacologic bases of use of benzodiazepines in pereinatal medicine]. Arch Fr Pediatr. 1977 Jan;34(1):74-89. [Article]
- Altamura AC, Moliterno D, Paletta S, Maffini M, Mauri MC, Bareggi S: Understanding the pharmacokinetics of anxiolytic drugs. Expert Opin Drug Metab Toxicol. 2013 Apr;9(4):423-40. doi: 10.1517/17425255.2013.759209. Epub 2013 Jan 21. [Article]
- Chin PK, Jensen BP, Larsen HS, Begg EJ: Adult age and ex vivo protein binding of lorazepam, oxazepam and temazepam in healthy subjects. Br J Clin Pharmacol. 2011 Dec;72(6):985-9. doi: 10.1111/j.1365-2125.2011.04036.x. [Article]
- Sigel E, Steinmann ME: Structure, function, and modulation of GABA(A) receptors. J Biol Chem. 2012 Nov 23;287(48):40224-31. doi: 10.1074/jbc.R112.386664. Epub 2012 Oct 4. [Article]
- Zhu S, Noviello CM, Teng J, Walsh RM Jr, Kim JJ, Hibbs RE: Structure of a human synaptic GABAA receptor. Nature. 2018 Jul;559(7712):67-72. doi: 10.1038/s41586-018-0255-3. Epub 2018 Jun 27. [Article]
- Griffin CE 3rd, Kaye AM, Bueno FR, Kaye AD: Benzodiazepine pharmacology and central nervous system-mediated effects. Ochsner J. 2013 Summer;13(2):214-23. [Article]
- Shader RI, Greenblatt DJ: The use of benzodiazepines in clinical practice. Br J Clin Pharmacol. 1981;11 Suppl 1:5S-9S. doi: 10.1111/j.1365-2125.1981.tb01832.x. [Article]
- Calcaterra NE, Barrow JC: Classics in chemical neuroscience: diazepam (valium). ACS Chem Neurosci. 2014 Apr 16;5(4):253-60. doi: 10.1021/cn5000056. Epub 2014 Feb 27. [Article]
- Court MH, Duan SX, Guillemette C, Journault K, Krishnaswamy S, Von Moltke LL, Greenblatt DJ: Stereoselective conjugation of oxazepam by human UDP-glucuronosyltransferases (UGTs): S-oxazepam is glucuronidated by UGT2B15, while R-oxazepam is glucuronidated by UGT2B7 and UGT1A9. Drug Metab Dispos. 2002 Nov;30(11):1257-65. [Article]
- FDA Approved Drug Products: Oxazepam oral capsules [Link]
- Health Canada Product Monograph: Oxazepam oral tablets [Link]
- CaymanChem: Oxazepam MSDS [Link]
- External Links
- Human Metabolome Database
- HMDB0014980
- KEGG Drug
- D00464
- KEGG Compound
- C07359
- PubChem Compound
- 4616
- PubChem Substance
- 46506031
- ChemSpider
- 4455
- BindingDB
- 85031
- 7781
- ChEBI
- 7823
- ChEMBL
- CHEMBL568
- Therapeutic Targets Database
- DAP000243
- PharmGKB
- PA450731
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- PDRhealth
- PDRhealth Drug Page
- Wikipedia
- Oxazepam
- MSDS
- Download (44.2 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 Completed Treatment Alcohol Dependency / Alcohol Withdrawal Syndrome 1 3 Terminated Treatment Anxiety Disorders / Dementia / Depression / Psychosomatic Disorders / Schizophrenia 1 2, 3 Recruiting Treatment Smoking, Cessation / Tobacco Use Disorders 1 1 Completed Treatment Cocaine Use Disorders 1 1 Completed Treatment Cocaine Use Disorders / Tobacco Use Disorders 1
Pharmacoeconomics
- Manufacturers
- Actavis elizabeth llc
- American therapeutics inc
- Ivax pharmaceuticals inc sub teva pharmaceuticals usa
- Mutual pharmaceutical co inc
- Mylan pharmaceuticals inc
- Sandoz inc
- Watson laboratories inc
- Alpharma us pharmaceuticals division
- Quantum pharmics ltd
- Parke davis div warner lambert co
- Packagers
- Actavis Group
- Amerisource Health Services Corp.
- Centaur Pharmaceuticals Pvt Ltd.
- Direct Dispensing Inc.
- Dispensing Solutions
- Heartland Repack Services LLC
- Ivax Pharmaceuticals
- Kaiser Foundation Hospital
- Liberty Pharmaceuticals
- Major Pharmaceuticals
- Murfreesboro Pharmaceutical Nursing Supply
- Nucare Pharmaceuticals Inc.
- Physicians Total Care Inc.
- Prepak Systems Inc.
- Qualitest
- Remedy Repack
- Sandoz
- Stat Rx Usa
- Dosage Forms
Form Route Strength Tablet Oral Capsule Oral Tablet Oral 10 mg Tablet Oral 15 mg Tablet Oral 30 mg Tablet Oral 50 MG Pill Solution / drops Oral Capsule Oral 10 mg/1 Capsule Oral 15 mg/1 Capsule Oral 30 mg/1 Capsule, gelatin coated Oral 10 mg/1 Capsule, gelatin coated Oral 15 mg/1 Capsule, gelatin coated Oral 30 mg/1 Tablet Oral 15 mg / tab Tablet Oral 30 mg / tab Tablet Oral 10 mg / tab - Prices
Unit description Cost Unit Oxazepam 30 mg capsule 1.2USD capsule Serax 10 mg capsule 1.17USD capsule Oxazepam 15 mg capsule 0.73USD capsule Oxazepam 10 mg capsule 0.6USD capsule Apo-Oxazepam 30 mg Tablet 0.09USD tablet Apo-Oxazepam 15 mg Tablet 0.07USD tablet Apo-Oxazepam 10 mg Tablet 0.04USD 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 melting point (°C) 205-206 °C PhysProp logP 2.24 HANSCH,C ET AL. (1995) - Predicted Properties
Property Value Source Water Solubility 0.0881 mg/mL ALOGPS logP 2.01 ALOGPS logP 2.92 Chemaxon logS -3.5 ALOGPS pKa (Strongest Acidic) 10.61 Chemaxon pKa (Strongest Basic) -1.5 Chemaxon Physiological Charge 0 Chemaxon Hydrogen Acceptor Count 3 Chemaxon Hydrogen Donor Count 2 Chemaxon Polar Surface Area 61.69 Å2 Chemaxon Rotatable Bond Count 1 Chemaxon Refractivity 77.89 m3·mol-1 Chemaxon Polarizability 28.38 Å3 Chemaxon Number of Rings 3 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter Yes Chemaxon Veber's Rule No Chemaxon MDDR-like Rule No Chemaxon - Predicted ADMET Features
Property Value Probability Human Intestinal Absorption + 0.9826 Blood Brain Barrier + 0.9641 Caco-2 permeable + 0.8867 P-glycoprotein substrate Substrate 0.517 P-glycoprotein inhibitor I Non-inhibitor 0.8866 P-glycoprotein inhibitor II Non-inhibitor 0.9167 Renal organic cation transporter Non-inhibitor 0.8812 CYP450 2C9 substrate Non-substrate 0.7692 CYP450 2D6 substrate Non-substrate 0.8685 CYP450 3A4 substrate Substrate 0.5631 CYP450 1A2 substrate Inhibitor 0.8262 CYP450 2C9 inhibitor Non-inhibitor 0.5063 CYP450 2D6 inhibitor Non-inhibitor 0.8445 CYP450 2C19 inhibitor Inhibitor 0.5065 CYP450 3A4 inhibitor Non-inhibitor 0.6563 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.6407 Ames test Non AMES toxic 0.9133 Carcinogenicity Non-carcinogens 0.7711 Biodegradation Not ready biodegradable 1.0 Rat acute toxicity 1.8229 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.999 hERG inhibition (predictor II) Non-inhibitor 0.8734
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 166.9946419 predictedDarkChem Lite v0.1.0 [M-H]- 166.9908419 predictedDarkChem Lite v0.1.0 [M-H]- 167.0011419 predictedDarkChem Lite v0.1.0 [M-H]- 160.16872 predictedDeepCCS 1.0 (2019) [M-H]- 166.9946419 predictedDarkChem Lite v0.1.0 [M-H]- 166.9908419 predictedDarkChem Lite v0.1.0 [M-H]- 167.0011419 predictedDarkChem Lite v0.1.0 [M-H]- 160.16872 predictedDeepCCS 1.0 (2019) [M+H]+ 167.5434419 predictedDarkChem Lite v0.1.0 [M+H]+ 167.5123419 predictedDarkChem Lite v0.1.0 [M+H]+ 167.6384419 predictedDarkChem Lite v0.1.0 [M+H]+ 162.52672 predictedDeepCCS 1.0 (2019) [M+H]+ 167.5434419 predictedDarkChem Lite v0.1.0 [M+H]+ 167.5123419 predictedDarkChem Lite v0.1.0 [M+H]+ 167.6384419 predictedDarkChem Lite v0.1.0 [M+H]+ 162.52672 predictedDeepCCS 1.0 (2019) [M+Na]+ 167.4315419 predictedDarkChem Lite v0.1.0 [M+Na]+ 167.3345419 predictedDarkChem Lite v0.1.0 [M+Na]+ 167.0114419 predictedDarkChem Lite v0.1.0 [M+Na]+ 168.61986 predictedDeepCCS 1.0 (2019) [M+Na]+ 167.4315419 predictedDarkChem Lite v0.1.0 [M+Na]+ 167.3345419 predictedDarkChem Lite v0.1.0 [M+Na]+ 167.0114419 predictedDarkChem Lite v0.1.0 [M+Na]+ 168.61986 predictedDeepCCS 1.0 (2019)
Targets
- Kind
- Protein group
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Positive allosteric modulator
- Curator comments
- The GABA(A) receptor is pentameric (i.e. comprising 5 subunit proteins) and therefore has a multitude of potential isoforms. The above target is a collection of all possible GABA(A) subunits that may participate in the formation of the pentameric receptor and is not meant to imply direct a drug-protein interaction for each individual subunit.
- 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
- Sigel E, Steinmann ME: Structure, function, and modulation of GABA(A) receptors. J Biol Chem. 2012 Nov 23;287(48):40224-31. doi: 10.1074/jbc.R112.386664. Epub 2012 Oct 4. [Article]
- Zhu S, Noviello CM, Teng J, Walsh RM Jr, Kim JJ, Hibbs RE: Structure of a human synaptic GABAA receptor. Nature. 2018 Jul;559(7712):67-72. doi: 10.1038/s41586-018-0255-3. Epub 2018 Jun 27. [Article]
- Kind
- Protein group
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Ligand
- Curator comments
- Benzodiazepines modulate GABA(A) function by binding at the interface between alpha (α) and gamma (γ) subunits. Of the 6 α-subunits, only 4 (α-1, -2, -3, and -5) participate in the formation of this binding site. The above target is a collection of all α- and γ-subunits that are known to participate in the formation of the benzodiazepine binding site.
- 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
- Sigel E, Steinmann ME: Structure, function, and modulation of GABA(A) receptors. J Biol Chem. 2012 Nov 23;287(48):40224-31. doi: 10.1074/jbc.R112.386664. Epub 2012 Oct 4. [Article]
- Zhu S, Noviello CM, Teng J, Walsh RM Jr, Kim JJ, Hibbs RE: Structure of a human synaptic GABAA receptor. Nature. 2018 Jul;559(7712):67-72. doi: 10.1038/s41586-018-0255-3. Epub 2018 Jun 27. [Article]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Glucuronosyltransferase activity
- Specific Function
- UDPGTs are of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds. This isozyme displays activity toward several classes of xeno...
- Gene Name
- UGT2B15
- Uniprot ID
- P54855
- Uniprot Name
- UDP-glucuronosyltransferase 2B15
- Molecular Weight
- 61035.815 Da
References
- Court MH, Duan SX, Guillemette C, Journault K, Krishnaswamy S, Von Moltke LL, Greenblatt DJ: Stereoselective conjugation of oxazepam by human UDP-glucuronosyltransferases (UGTs): S-oxazepam is glucuronidated by UGT2B15, while R-oxazepam is glucuronidated by UGT2B7 and UGT1A9. Drug Metab Dispos. 2002 Nov;30(11):1257-65. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Glucuronosyltransferase activity
- Specific Function
- UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds.Its unique specificity for 3,4-catechol estrogens and estriol su...
- Gene Name
- UGT2B7
- Uniprot ID
- P16662
- Uniprot Name
- UDP-glucuronosyltransferase 2B7
- Molecular Weight
- 60694.12 Da
References
- Court MH, Duan SX, Guillemette C, Journault K, Krishnaswamy S, Von Moltke LL, Greenblatt DJ: Stereoselective conjugation of oxazepam by human UDP-glucuronosyltransferases (UGTs): S-oxazepam is glucuronidated by UGT2B15, while R-oxazepam is glucuronidated by UGT2B7 and UGT1A9. Drug Metab Dispos. 2002 Nov;30(11):1257-65. [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
- Court MH, Duan SX, Guillemette C, Journault K, Krishnaswamy S, Von Moltke LL, Greenblatt DJ: Stereoselective conjugation of oxazepam by human UDP-glucuronosyltransferases (UGTs): S-oxazepam is glucuronidated by UGT2B15, while R-oxazepam is glucuronidated by UGT2B7 and UGT1A9. Drug Metab Dispos. 2002 Nov;30(11):1257-65. [Article]
Carriers
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Binder
- 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
- Chin PK, Jensen BP, Larsen HS, Begg EJ: Adult age and ex vivo protein binding of lorazepam, oxazepam and temazepam in healthy subjects. Br J Clin Pharmacol. 2011 Dec;72(6):985-9. doi: 10.1111/j.1365-2125.2011.04036.x. [Article]
Drug created at June 13, 2005 13:24 / Updated at February 20, 2024 23:55