Identification

Name
Flurazepam
Accession Number
DB00690  (APRD00983)
Type
Small Molecule
Groups
Approved, Illicit, Investigational
Description

A benzodiazepine derivative used mainly as a hypnotic.

Structure
Thumb
Synonyms
  • Flurazepam
  • Flurazépam
  • Flurazepamum
External IDs
ID 480 / Ro 5-6901
Product Ingredients
IngredientUNIICASInChI Key
Flurazepam hydrochloride7C4JH842IJ36105-20-1PUGVROXLRUQCAF-UHFFFAOYSA-N
Product Images
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
DalmaneCapsuleOralValeant Canada Lp Valeant Canada S.E.C.1971-12-312016-07-08Canada
DalmaneCapsuleOralValeant Canada Lp Valeant Canada S.E.C.1971-12-312016-07-08Canada
FlurazepamCapsule15 mgOralAa Pharma Inc1982-12-31Not applicableCanada
FlurazepamCapsule30 mgOralAa Pharma Inc1982-12-31Not applicableCanada
Flurazepam 15CapsuleOralPro Doc Limitee1982-12-312018-04-18Canada
Flurazepam 15mg CapsuleCapsuleOralLaboratoires Confab IncNot applicableNot applicableCanada
Flurazepam 30CapsuleOralPro Doc Limitee1982-12-312017-06-30Canada
Flurazepam 30mg CapsuleCapsuleOralLaboratoires Confab IncNot applicableNot applicableCanada
Som-pamCapsuleOralBiomed Pharma1981-12-31Not applicableCanada
Som-pamCapsuleOralBiomed Pharma1981-12-31Not applicableCanada
Additional Data Available
  • Application Number
    Application Number

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

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  • Product Code
    Product Code

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

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Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Bio-flurazepamCapsuleOralBiomed Pharma2004-04-23Not applicableCanada
Bio-flurazepamCapsuleOralBiomed Pharma2004-04-23Not applicableCanada
FlurazepamCapsule30 mg/1OralGolden State Medical Supply1986-12-082017-01-02Us
FlurazepamCapsule15 mg/1OralGolden State Medical Supply1986-12-082017-01-02Us
FlurazepamCapsule30 mg/1OralA S Medication Solutions1986-12-08Not applicableUs54569 089820180907 15195 n3cw01
FlurazepamCapsule15 mg/1Oralbryant ranch prepack1986-12-082014-01-01Us63629 303420180113 27003 1v30avo
FlurazepamCapsule15 mg/1OralA S Medication Solutions1986-12-08Not applicableUs00143 3367 01 nlmimage10 821c4162
FlurazepamCapsule30 mg/1OralPreferred Pharmaceuticals, Inc2012-01-272019-09-24Us00143 3370 01 nlmimage10 4215a14d
FlurazepamCapsule30 mg/1OralRebel Distributors1986-12-08Not applicableUs
FlurazepamCapsule30 mg/1OralHikma Pharmaceuticals USA Inc.1986-12-082015-01-18Us0143 337020180907 15195 c4lj9v
Additional Data Available
  • Application Number
    Application Number

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

    Learn more
  • Product Code
    Product Code

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

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International/Other Brands
Dalmadorm (Meda) / Dalmadorm medium (Meda) / Felison (SIT) / Flunox (Teofarma) / Insumin / Sompan (I.C.N.) / Valdorm (Valeas)
Categories
UNII
IHP475989U
CAS number
17617-23-1
Weight
Average: 387.878
Monoisotopic: 387.151368285
Chemical Formula
C21H23ClFN3O
InChI Key
SAADBVWGJQAEFS-UHFFFAOYSA-N
InChI
InChI=1S/C21H23ClFN3O/c1-3-25(4-2)11-12-26-19-10-9-15(22)13-17(19)21(24-14-20(26)27)16-7-5-6-8-18(16)23/h5-10,13H,3-4,11-12,14H2,1-2H3
IUPAC Name
7-chloro-1-[2-(diethylamino)ethyl]-5-(2-fluorophenyl)-2,3-dihydro-1H-1,4-benzodiazepin-2-one
SMILES
CCN(CC)CCN1C2=C(C=C(Cl)C=C2)C(=NCC1=O)C1=CC=CC=C1F

Pharmacology

Indication

For short-term and intermittent use in patients with recurring insomnia and poor sleeping habits

Associated Conditions
Pharmacodynamics

Flurazepam, a benzodiazepine derivative, is a hypnotic agent which does not appear to decrease dream time as measured by rapid eye movements (REM). Furthermore, it decreases sleep latency and number of awakenings for a consequent increase in total sleep time.

Mechanism of action

Flurazepam binds to an allosteric site on GABA-A receptors. Binding potentiates the action of GABA on GABA-A receptors by opening the chloride channel within the receptor, causing chloride influx and hyperpolarization.

TargetActionsOrganism
AGABA(A) Receptor
positive allosteric modulator
Humans
AGABA(A) Receptor Benzodiazepine Binding Site
ligand
Humans
Additional Data Available
Adverse Effects

Comprehensive structured data on known drug adverse effects with statistical prevalence. MedDRA and ICD10 ids are provided for adverse effect conditions and symptoms.

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Additional Data Available
Contraindications

Structured data covering drug contraindications. Each contraindication describes a scenario in which the drug is not to be used. Includes restrictions on co-administration, contraindicated populations, and more.

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Additional Data Available
Blackbox Warnings

Structured data representing warnings from the black box section of drug labels. These warnings cover important and dangerous risks, contraindications, or adverse effects.

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Absorption

Flurazepam hydrochloride is rapidly (30 minutes) absorbed from the gastrointestinal tract

Volume of distribution
Not Available
Protein binding

83%

Metabolism

Flurazepam is rapidly metabolized and is excreted primarily in the urine. Both hydroxyethyl flurazepam (the major metabolite) and N-desalkyl flurazepam are active. The N-desalkyl metabolite is slowly excreted in the urine as the conjugated form

Route of elimination

Flurazepam is rapidly metabolized and is excreted primarily in the urine. Less than 1% of the dose is excreted in the urine as N1-desalkyl-flurazepam.

Half life

The mean apparent half-life of flurazepam is 2.3 hours. The half life of elimination of N1-des-alkyl- flurazepam ranged from 47 to 100 hours

Clearance
Not Available
Toxicity

Coma, confusion, low blood pressure, sleepiness

Affected organisms
  • Humans and other mammals
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.
DrugInteraction
2,5-Dimethoxy-4-ethylthioamphetamineThe risk or severity of adverse effects can be increased when Flurazepam is combined with 2,5-Dimethoxy-4-ethylthioamphetamine.
3-isobutyl-1-methyl-7H-xanthineThe therapeutic efficacy of Flurazepam can be decreased when used in combination with 3-isobutyl-1-methyl-7H-xanthine.
4-Bromo-2,5-dimethoxyamphetamineThe risk or severity of adverse effects can be increased when Flurazepam is combined with 4-Bromo-2,5-dimethoxyamphetamine.
4-MethoxyamphetamineThe risk or severity of adverse effects can be increased when Flurazepam is combined with 4-Methoxyamphetamine.
5-methoxy-N,N-dimethyltryptamineThe risk or severity of adverse effects can be increased when Flurazepam is combined with 5-methoxy-N,N-dimethyltryptamine.
6-O-benzylguanineThe therapeutic efficacy of Flurazepam can be decreased when used in combination with 6-O-benzylguanine.
7-DeazaguanineThe therapeutic efficacy of Flurazepam can be decreased when used in combination with 7-Deazaguanine.
7-NitroindazoleThe risk or severity of adverse effects can be increased when Flurazepam is combined with 7-Nitroindazole.
7,8-Dichloro-1,2,3,4-tetrahydroisoquinolineThe risk or severity of adverse effects can be increased when Flurazepam is combined with 7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline.
7,9-DimethylguanineThe therapeutic efficacy of Flurazepam can be decreased when used in combination with 7,9-Dimethylguanine.
Additional Data Available
  • Extended Description
    Extended Description

    Extended description of the mechanism of action and particular properties of each drug interaction.

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  • Severity
    Severity

    A severity rating for each drug interaction, from minor to major.

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  • Evidence Level
    Evidence Level

    A rating for the strength of the evidence supporting each drug interaction.

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  • Action
    Action

    An effect category for each drug interaction. Know how this interaction affects the subject drug.

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Food Interactions
  • Avoid alcohol.
  • Take with or without food. The absorption is unaffected by food.

References

Synthesis Reference

Fryer, R. and Sternbach, L.H.; U.S. Patent 3,567,710; March 2, 1971; assigned to Hoffman-La Roche, Inc.

General References
  1. Rickels K: The clinical use of hypnotics: indications for use and the need for a variety of hypnotics. Acta Psychiatr Scand Suppl. 1986;332:132-41. [PubMed:2883820]
  2. Vermeeren A: Residual effects of hypnotics: epidemiology and clinical implications. CNS Drugs. 2004;18(5):297-328. [PubMed:15089115]
  3. Oelschlager H: [Chemical and pharmacologic aspects of benzodiazepines]. Schweiz Rundsch Med Prax. 1989 Jul 4;78(27-28):766-72. [PubMed:2570451]
  4. Rooke KC: The use of flurazepam (dalmane) as a substitute for barbiturates and methaqualone/diphenhydramine (mandrax) in general practice. J Int Med Res. 1976;4(5):355-9. [PubMed:18375]
  5. Olive G, Dreux C: [Pharmacologic bases of use of benzodiazepines in pereinatal medicine]. Arch Fr Pediatr. 1977 Jan;34(1):74-89. [PubMed:851373]
  6. Link [Link]
External Links
Human Metabolome Database
HMDB0014828
KEGG Drug
D00329
PubChem Compound
3393
PubChem Substance
46508451
ChemSpider
3276
RxNav
4501
ChEBI
5128
ChEMBL
CHEMBL968
ZINC
ZINC000000537752
Therapeutic Targets Database
DAP000242
PharmGKB
PA449681
PDBe Ligand
FL7
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
PDRhealth
PDRhealth Drug Page
Wikipedia
Flurazepam
ATC Codes
N05CD01 — Flurazepam
AHFS Codes
  • 28:24.08 — Benzodiazepines
PDB Entries
2yoe
MSDS
Download (50.5 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1CompletedTreatmentInsomnia Disorder1
3TerminatedTreatmentAnxiety Disorders / Dementias / Depression / Psychosomatic Disorders / Schizophrenia1

Pharmacoeconomics

Manufacturers
  • Valeant pharmaceuticals international
  • Halsey drug co inc
  • Mutual pharmaceutical co inc
  • Mylan pharmaceuticals inc
  • Par pharmaceutical inc
  • Purepac pharmaceutical co
  • Sandoz inc
  • Superpharm corp
  • Usl pharma inc
  • Warner chilcott inc
  • Warner chilcott div warner lambert co
  • Watson laboratories inc
  • West ward pharmaceutical corp
Packagers
  • Amerisource Health Services Corp.
  • A-S Medication Solutions LLC
  • Bryant Ranch Prepack
  • Corepharma LLC
  • Direct Dispensing Inc.
  • Dispensing Solutions
  • Diversified Healthcare Services Inc.
  • H.J. Harkins Co. Inc.
  • Hl Moore Drug Exchange
  • Kaiser Foundation Hospital
  • Lake Erie Medical and Surgical Supply
  • Legacy Pharmaceuticals Packaging LLC
  • Major Pharmaceuticals
  • Mylan
  • Nucare Pharmaceuticals Inc.
  • Par Pharmaceuticals
  • PCA LLC
  • PD-Rx Pharmaceuticals Inc.
  • Physicians Total Care Inc.
  • Prepackage Specialists
  • Prepak Systems Inc.
  • Rebel Distributors Corp.
  • Remedy Repack
  • Southwood Pharmaceuticals
  • UDL Laboratories
  • Valeant Ltd.
  • West-Ward Pharmaceuticals
Dosage forms
FormRouteStrength
CapsuleOral15 mg
CapsuleOral15 mg/1
CapsuleOral30 mg/1
CapsuleOral30 mg
CapsuleOral
TabletOral
Prices
Unit descriptionCostUnit
Dalmane 30 mg capsule2.01USD capsule
Dalmane 15 mg capsule1.79USD capsule
Flurazepam HCl 15 mg capsule0.43USD capsule
Flurazepam HCl 30 mg capsule0.4USD capsule
Flurazepam 30 mg capsule0.34USD capsule
Flurazepam 15 mg capsule0.28USD capsule
Apo-Flurazepam 30 mg Capsule0.1USD capsule
Apo-Flurazepam 15 mg Capsule0.08USD capsule
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Not Available

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)190-220British Patent 1,040,548.
water solubility500 mg/mL (HCl salt)Not Available
logP3.8Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.01 mg/mLALOGPS
logP3.81ALOGPS
logP3.95ChemAxon
logS-4.6ALOGPS
pKa (Strongest Basic)8.71ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count3ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area35.91 Å2ChemAxon
Rotatable Bond Count6ChemAxon
Refractivity107.54 m3·mol-1ChemAxon
Polarizability41.22 Å3ChemAxon
Number of Rings3ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+1.0
Blood Brain Barrier+0.9898
Caco-2 permeable+0.6115
P-glycoprotein substrateSubstrate0.8553
P-glycoprotein inhibitor IInhibitor0.9455
P-glycoprotein inhibitor IIInhibitor0.6624
Renal organic cation transporterInhibitor0.6523
CYP450 2C9 substrateNon-substrate0.7716
CYP450 2D6 substrateNon-substrate0.9116
CYP450 3A4 substrateSubstrate0.7794
CYP450 1A2 substrateInhibitor0.5194
CYP450 2C9 inhibitorNon-inhibitor0.7112
CYP450 2D6 inhibitorNon-inhibitor0.5469
CYP450 2C19 inhibitorInhibitor0.5082
CYP450 3A4 inhibitorInhibitor0.6347
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.6231
Ames testNon AMES toxic0.9132
CarcinogenicityNon-carcinogens0.7597
BiodegradationNot ready biodegradable1.0
Rat acute toxicity2.5654 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9528
hERG inhibition (predictor II)Inhibitor0.7183
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-000i-0009000000-c0e65a54e856d501ed8c
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-014r-0009000000-5a2839fdce5817956437
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-014i-0009000000-ef2f40465f355c7e04c0
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-014i-0049000000-aeef40f08b145e9212fb
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-014i-0392000000-706f2398b20890152e43

Taxonomy

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
Alpha amino acids and derivatives / Fluorobenzenes / Aryl chlorides / Aryl fluorides / Tertiary carboxylic acid amides / Trialkylamines / Lactams / Ketimines / Propargyl-type 1,3-dipolar organic compounds / Azacyclic compounds
show 6 more
Substituents
1,4-benzodiazepine / Alpha-amino acid or derivatives / Halobenzene / Fluorobenzene / Aryl chloride / Monocyclic benzene moiety / Benzenoid / Aryl fluoride / Aryl halide / Tertiary carboxylic acid amide
show 24 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
Not Available

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
  1. 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. [PubMed:23038269]
  2. 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. [PubMed:29950725]
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
  1. 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. [PubMed:23038269]
  2. 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. [PubMed:29950725]

Enzymes

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Vitamin d3 25-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 performs a variety of oxidation react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
Molecular Weight
57342.67 Da
References
  1. Capello S, Henderson L, DeGrazia F, Liberato D, Garland W, Town C: The effect of the cytochrome P-450 suicide inactivator, 1-aminobenzotriazole, on the in vivo metabolism and pharmacologic activity of flurazepam. Drug Metab Dispos. 1990 Mar-Apr;18(2):190-6. [PubMed:1971572]
  2. Linder CD, Renaud NA, Hutzler JM: Is 1-aminobenzotriazole an appropriate in vitro tool as a nonspecific cytochrome P450 inactivator? Drug Metab Dispos. 2009 Jan;37(1):10-3. doi: 10.1124/dmd.108.024075. Epub 2008 Oct 20. [PubMed:18936109]
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
  1. Rendic S: Summary of information on human CYP enzymes: human P450 metabolism data. Drug Metab Rev. 2002 Feb-May;34(1-2):83-448. [PubMed:11996015]
  2. Tassaneeyakul W, Birkett DJ, Miners JO: Inhibition of human hepatic cytochrome P4502E1 by azole antifungals, CNS-active drugs and non-steroidal anti-inflammatory agents. Xenobiotica. 1998 Mar;28(3):293-301. doi: 10.1080/004982598239579 . [PubMed:9574817]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Steroid hydroxylase activity
Specific Function
Exhibits a high coumarin 7-hydroxylase activity. Can act in the hydroxylation of the anti-cancer drugs cyclophosphamide and ifosphamide. Competent in the metabolic activation of aflatoxin B1. Const...
Gene Name
CYP2A6
Uniprot ID
P11509
Uniprot Name
Cytochrome P450 2A6
Molecular Weight
56501.005 Da
References
  1. Capello S, Henderson L, DeGrazia F, Liberato D, Garland W, Town C: The effect of the cytochrome P-450 suicide inactivator, 1-aminobenzotriazole, on the in vivo metabolism and pharmacologic activity of flurazepam. Drug Metab Dispos. 1990 Mar-Apr;18(2):190-6. [PubMed:1971572]
  2. Linder CD, Renaud NA, Hutzler JM: Is 1-aminobenzotriazole an appropriate in vitro tool as a nonspecific cytochrome P450 inactivator? Drug Metab Dispos. 2009 Jan;37(1):10-3. doi: 10.1124/dmd.108.024075. Epub 2008 Oct 20. [PubMed:18936109]

Transporters

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Xenobiotic-transporting atpase activity
Specific Function
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name
ABCB1
Uniprot ID
P08183
Uniprot Name
Multidrug resistance protein 1
Molecular Weight
141477.255 Da
References
  1. Mahar Doan KM, Humphreys JE, Webster LO, Wring SA, Shampine LJ, Serabjit-Singh CJ, Adkison KK, Polli JW: Passive permeability and P-glycoprotein-mediated efflux differentiate central nervous system (CNS) and non-CNS marketed drugs. J Pharmacol Exp Ther. 2002 Dec;303(3):1029-37. [PubMed:12438524]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Quaternary ammonium group transmembrane transporter activity
Specific Function
Mediates tubular uptake of organic compounds from circulation. Mediates the influx of agmatine, dopamine, noradrenaline (norepinephrine), serotonin, choline, famotidine, ranitidine, histamin, creat...
Gene Name
SLC22A2
Uniprot ID
O15244
Uniprot Name
Solute carrier family 22 member 2
Molecular Weight
62579.99 Da
References
  1. Zolk O, Solbach TF, Konig J, Fromm MF: Functional characterization of the human organic cation transporter 2 variant p.270Ala>Ser. Drug Metab Dispos. 2009 Jun;37(6):1312-8. doi: 10.1124/dmd.108.023762. Epub 2009 Feb 27. [PubMed:19251820]

Drug created on June 13, 2005 07:24 / Updated on July 09, 2020 11:59

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