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Identification
NameZaleplon
Accession NumberDB00962  (APRD00411)
TypeSmall Molecule
GroupsApproved, Illicit, Investigational
Description

Zaleplon is a sedative/hypnotic, mainly used for insomnia. It is known as a nonbenzodiazepine hypnotic. Zaleplon interacts with the GABA receptor complex and shares some of the pharmacological properties of the benzodiazepines. Zaleplon is a schedule IV drug in the United States.

Structure
Thumb
Synonyms
3'-(3-Cyanopyrazolo(1,5-a)pyrimidin-7-yl)-N-ethylacetanilide
External Identifiers
  • DEA No. 2781
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Sonatacapsule10 mg/1oralPfizer Laboratories Div Pfizer Inc1999-08-13Not applicableUs
Sonatacapsule5 mg/1oralPfizer Laboratories Div Pfizer Inc1999-08-13Not applicableUs
Sonatacapsule5 mg/1oralPhysicians Total Care, Inc.2007-09-05Not applicableUs
Sonatacapsule10 mg/1oralPhysicians Total Care, Inc.2004-04-01Not applicableUs
Starnoccapsule5 mgoralServier Canada Inc2000-06-272007-09-27Canada
Starnoccapsule10 mgoralPfizer Canada IncNot applicableNot applicableCanada
Starnoccapsule5 mgoralPfizer Canada IncNot applicableNot applicableCanada
Starnoccapsule10 mgoralServier Canada Inc2000-06-272007-09-27Canada
Zaleploncapsule10 mg/1oralRebel Distributors Corp.2008-05-01Not applicableUs
Zaleploncapsule5 mg/1oralbryant ranch prepack2008-05-01Not applicableUs
Zaleploncapsule10 mg/1oralLake Erie Medical & Surgical Supply DBA Quality Care Products LLC2011-12-05Not applicableUs
Zaleploncapsule5 mg/1oralRebel Distributors Corp.2008-05-01Not applicableUs
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Zaleploncapsule10 mg/1oralRebel Distributors Corp2009-05-05Not applicableUs
Zaleploncapsule5 mg/1oralNorthstar Rx LLC2010-06-23Not applicableUs
Zaleploncapsule5 mg/1oralRoxane Laboratories, Inc2008-06-06Not applicableUs
Zaleploncapsule10 mg/1oralAscend Laboratories, LLC2010-12-15Not applicableUs
Zaleploncapsule5 mg/1oralPhysicians Total Care, Inc.2008-06-19Not applicableUs
Zaleploncapsule5 mg/1oralRebel Distributors Corp2009-05-05Not applicableUs
Zaleploncapsule5 mg/1oralRebel Distributors Corp2009-05-05Not applicableUs
Zaleploncapsule, gelatin coated10 mg/1oralUpsher Smith Laboratories, Inc.2008-06-06Not applicableUs
Zaleploncapsule5 mg/1oralAscend Laboratories, LLC2010-12-15Not applicableUs
Zaleploncapsule10 mg/1oralPhysicians Total Care, Inc.2008-06-19Not applicableUs
Zaleploncapsule10 mg/1oralLake Erie Medical & Surgical Supply DBA Quality Care Products LLC2009-05-05Not applicableUs
Zaleploncapsule, gelatin coated5 mg/1oralUpsher Smith Laboratories, Inc.2008-06-06Not applicableUs
Zaleploncapsule5 mg/1oralDispensing Solutions, Inc.2008-06-06Not applicableUs
Zaleploncapsule10 mg/1oralA S Medication Solutions Llc2008-06-06Not applicableUs
Zaleploncapsule5 mg/1oralAidarex Pharmaceuticals LLC2009-05-05Not applicableUs
Zaleploncapsule10 mg/1oralMylan Pharmaceuticals Inc.2008-06-06Not applicableUs
Zaleploncapsule10 mg/1oralAurobindo Pharma Limited2008-06-06Not applicableUs
Zaleploncapsule10 mg/1oralH.J. Harkins Company, Inc.2010-12-15Not applicableUs
Zaleploncapsule10 mg/1oralAidarex Pharmaceuticals LLC2009-05-05Not applicableUs
Zaleploncapsule5 mg/1oralMylan Pharmaceuticals Inc.2008-06-06Not applicableUs
Zaleploncapsule5 mg/1oralAurobindo Pharma Limited2008-06-06Not applicableUs
Zaleploncapsule10 mg/1oralUnit Dose Services2008-06-06Not applicableUs
Zaleploncapsule10 mg/1oralbryant ranch prepack2009-05-05Not applicableUs
Zaleploncapsule10 mg/1oralA S Medication Solutions Llc2008-06-06Not applicableUs
Zaleploncapsule10 mg/1oralUnichem Pharmaceuticals (USA), Inc.2009-05-05Not applicableUs
Zaleploncapsule10 mg/1oralTeva Pharmaceuticals USA Inc2008-06-06Not applicableUs
Zaleploncapsule10 mg/1oralDIRECT RX2015-01-01Not applicableUs
Zaleploncapsule5 mg/1oralPd Rx Pharmaceuticals, Inc.2008-06-06Not applicableUs
Zaleploncapsule5 mg/1oralUnichem Pharmaceuticals (USA), Inc.2009-05-05Not applicableUs
Zaleploncapsule5 mg/1oralTeva Pharmaceuticals USA Inc2008-06-06Not applicableUs
Zaleploncapsule5 mg/1oralPd Rx Pharmaceuticals, Inc.2011-12-02Not applicableUs
Zaleploncapsule10 mg/1oralNorthstar Rx LLC2010-06-23Not applicableUs
Zaleploncapsule10 mg/1oralRoxane Laboratories, Inc2008-06-06Not applicableUs
Zaleploncapsule10 mg/1oralSt Marys Medical Park Pharmacy2010-12-15Not applicableUs
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
ZalaplonNot Available
Brand mixturesNot Available
SaltsNot Available
Categories
UNIIS62U433RMH
CAS number151319-34-5
WeightAverage: 305.3339
Monoisotopic: 305.127660127
Chemical FormulaC17H15N5O
InChI KeyInChIKey=HUNXMJYCHXQEGX-UHFFFAOYSA-N
InChI
InChI=1S/C17H15N5O/c1-3-21(12(2)23)15-6-4-5-13(9-15)16-7-8-19-17-14(10-18)11-20-22(16)17/h4-9,11H,3H2,1-2H3
IUPAC Name
N-(3-{3-cyanopyrazolo[1,5-a]pyrimidin-7-yl}phenyl)-N-ethylacetamide
SMILES
CCN(C(C)=O)C1=CC=CC(=C1)C1=CC=NC2=C(C=NN12)C#N
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as phenylpyrimidines. These are polycyclic aromatic compounds containing a benzene ring linked to a pyrimidine ring through a CC or CN bond. Pyrimidine is a 6-membered ring consisting of four carbon atoms and two nitrogen centers at the 1- and 3- ring positions.
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassDiazines
Sub ClassPyrimidines and pyrimidine derivatives
Direct ParentPhenylpyrimidines
Alternative Parents
Substituents
  • 4-phenylpyrimidine
  • Acetanilide
  • Pyrazolopyrimidine
  • Benzenoid
  • Monocyclic benzene moiety
  • Heteroaromatic compound
  • Acetamide
  • Tertiary carboxylic acid amide
  • Pyrazole
  • Azole
  • Tertiary amine
  • Carboxamide group
  • Azacycle
  • Nitrile
  • Carbonitrile
  • Carboxylic acid derivative
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Carbonyl group
  • Amine
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External Descriptors
Pharmacology
IndicationFor the treatment of short-term treatment of insomnia in adults.
PharmacodynamicsZaleplon is a nonbenzodiazepine hypnotic from the pyrazolopyrimidine class and is indicated for the short-term treatment of insomnia. While Zaleplon is a hypnotic agent with a chemical structure unrelated to benzodiazepines, barbiturates, or other drugs with known hypnotic properties, it interacts with the gamma-aminobutyric acid-benzodiazepine (GABABZ) receptor complex. Subunit modulation of the GABABZ receptor chloride channel macromolecular complex is hypothesized to be responsible for some of the pharmacological properties of benzodiazepines, which include sedative, anxiolytic, muscle relaxant, and anticonvulsive effects in animal models. Zaleplon also binds selectively to the CNS GABAA-receptor chloride ionophore complex at benzodiazepine(BZ) omega-1 (BZ1, ο1) receptors.
Mechanism of actionZaleplon exerts its action through subunit modulation of the GABABZ receptor chloride channel macromolecular complex. Zaleplon also binds selectively to the brain omega-1 receptor located on the alpha subunit of the GABA-A/chloride ion channel receptor complex and potentiates t-butyl-bicyclophosphorothionate (TBPS) binding.
Related Articles
AbsorptionAbsorption Zaleplon is rapidly and almost completely absorbed following oral administration.
Volume of distribution
  • 1.4 L/kg
Protein bindingApproximately 60% (in vitro plasma protein binding).
Metabolism

Zaleplon is primarily metabolized by aldehyde oxidase.

SubstrateEnzymesProduct
Zaleplon
desethylzaleplonDetails
Route of eliminationZaleplon is metabolized primarily by the liver and undergoes significant presystemic metabolism. After oral administration, zaleplon is extensively metabolized, with less than 1% of the dose excreted unchanged in urine. Renal excretion of unchanged zaleplon accounts for less than 1% of the administered dose.
Half lifeApproximately 1 hour
Clearance
  • 1 L/h/kg
ToxicitySide effects include abdominal pain, amnesia, dizziness, drowsiness, eye pain, headache, memory loss, menstrual pain, nausea, sleepiness, tingling, weakness
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+1.0
Blood Brain Barrier+0.9751
Caco-2 permeable+0.5973
P-glycoprotein substrateNon-substrate0.6094
P-glycoprotein inhibitor INon-inhibitor0.5232
P-glycoprotein inhibitor IIInhibitor0.8239
Renal organic cation transporterNon-inhibitor0.745
CYP450 2C9 substrateNon-substrate0.8607
CYP450 2D6 substrateNon-substrate0.8551
CYP450 3A4 substrateSubstrate0.6341
CYP450 1A2 substrateNon-inhibitor0.5
CYP450 2C9 inhibitorInhibitor0.5986
CYP450 2D6 inhibitorNon-inhibitor0.9507
CYP450 2C19 inhibitorNon-inhibitor0.5238
CYP450 3A4 inhibitorNon-inhibitor0.8396
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.7673
Ames testNon AMES toxic0.5372
CarcinogenicityNon-carcinogens0.6481
BiodegradationNot ready biodegradable1.0
Rat acute toxicity2.6277 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9806
hERG inhibition (predictor II)Non-inhibitor0.8931
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • King pharmaceuticals research and development inc sub king pharmaceuticals inc
  • Aurobindo pharma ltd
  • Cipla ltd
  • Mylan pharmaceuticals inc
  • Orchid healthcare div orchid chemicals and pharmaceuticals ltd
  • Roxane laboratories inc
  • Sandoz inc
  • Teva pharmaceuticals usa
  • Unichem laboratories ltd
  • Upsher smith laboratories inc
  • West ward pharmaceutical corp
Packagers
Dosage forms
FormRouteStrength
Capsuleoral10 mg
Capsuleoral5 mg
Capsuleoral10 mg/1
Capsuleoral5 mg/1
Capsule, gelatin coatedoral10 mg/1
Capsule, gelatin coatedoral5 mg/1
Prices
Unit descriptionCostUnit
Sonata 10 mg capsule6.83USD capsule
Sonata 5 mg capsule5.26USD capsule
Zaleplon 5 mg capsule2.13USD capsule
Zaleplon 10 mg capsule2.09USD capsule
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point157-159 °CNot Available
logP0.9Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.0403 mg/mLALOGPS
logP2ALOGPS
logP1.53ChemAxon
logS-3.9ALOGPS
pKa (Strongest Basic)0.3ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count4ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area74.29 Å2ChemAxon
Rotatable Bond Count3ChemAxon
Refractivity97.24 m3·mol-1ChemAxon
Polarizability32.09 Å3ChemAxon
Number of Rings3ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
Spectra
Spectrum TypeDescriptionSplash Key
MSMass Spectrum (Electron Ionization)splash10-01ot-3391000000-78a75199aa0ab8c426beView in MoNA
References
Synthesis Reference

Farhan Aslam, “Polymorphs of zaleplon and methods for the preparation thereof.” U.S. Patent US20020072527, issued June 13, 2002.

US20020072527
General References
  1. Dundar Y, Dodd S, Strobl J, Boland A, Dickson R, Walley T: Comparative efficacy of newer hypnotic drugs for the short-term management of insomnia: a systematic review and meta-analysis. Hum Psychopharmacol. 2004 Jul;19(5):305-22. [PubMed:15252823 ]
  2. Noguchi H, Kitazumi K, Mori M, Shiba T: Electroencephalographic properties of zaleplon, a non-benzodiazepine sedative/hypnotic, in rats. J Pharmacol Sci. 2004 Mar;94(3):246-51. [PubMed:15037809 ]
  3. Ramakrishnan K, Scheid DC: Treatment options for insomnia. Am Fam Physician. 2007 Aug 15;76(4):517-26. [PubMed:17853625 ]
  4. Barbera J, Shapiro C: Benefit-risk assessment of zaleplon in the treatment of insomnia. Drug Saf. 2005;28(4):301-18. [PubMed:15783240 ]
  5. Dooley M, Plosker GL: Zaleplon: a review of its use in the treatment of insomnia. Drugs. 2000 Aug;60(2):413-45. [PubMed:10983740 ]
  6. Holm KJ, Goa KL: Zolpidem: an update of its pharmacology, therapeutic efficacy and tolerability in the treatment of insomnia. Drugs. 2000 Apr;59(4):865-89. [PubMed:10804040 ]
  7. Patat A, Paty I, Hindmarch I: Pharmacodynamic profile of Zaleplon, a new non-benzodiazepine hypnotic agent. Hum Psychopharmacol. 2001 Jul;16(5):369-392. [PubMed:12404558 ]
External Links
ATC CodesN05CF03
AHFS Codes
  • 28:24.92
PDB EntriesNot Available
FDA labelDownload (66.1 KB)
MSDSDownload (57.6 KB)
Interactions
Drug Interactions
Drug
AzelastineZaleplon may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
BaclofenThe risk or severity of adverse effects can be increased when Baclofen is combined with Zaleplon.
BrimonidineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Zaleplon.
BuprenorphineZaleplon may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
CarbamazepineThe serum concentration of Zaleplon can be decreased when it is combined with Carbamazepine.
CimetidineThe metabolism of Zaleplon can be decreased when combined with Cimetidine.
DoxylamineDoxylamine may increase the central nervous system depressant (CNS depressant) activities of Zaleplon.
DronabinolDronabinol may increase the central nervous system depressant (CNS depressant) activities of Zaleplon.
DroperidolDroperidol may increase the central nervous system depressant (CNS depressant) activities of Zaleplon.
EnzalutamideThe serum concentration of Zaleplon can be decreased when it is combined with Enzalutamide.
EthanolZaleplon may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
FlumazenilFlumazenil may decrease the sedative activities of Zaleplon.
FosphenytoinThe serum concentration of Zaleplon can be decreased when it is combined with Fosphenytoin.
HydrocodoneZaleplon may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
HydroxyzineHydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Zaleplon.
LorazepamThe risk or severity of adverse effects can be increased when Lorazepam is combined with Zaleplon.
Magnesium SulfateMagnesium Sulfate may increase the central nervous system depressant (CNS depressant) activities of Zaleplon.
MethotrimeprazineZaleplon may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
MetyrosineZaleplon may increase the sedative activities of Metyrosine.
MinocyclineMinocycline may increase the central nervous system depressant (CNS depressant) activities of Zaleplon.
MirtazapineZaleplon may increase the central nervous system depressant (CNS depressant) activities of Mirtazapine.
MitotaneThe serum concentration of Zaleplon can be decreased when it is combined with Mitotane.
NabiloneNabilone may increase the central nervous system depressant (CNS depressant) activities of Zaleplon.
OrphenadrineZaleplon may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
ParaldehydeZaleplon may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.
ParoxetineThe risk or severity of adverse effects can be increased when Zaleplon is combined with Paroxetine.
PerampanelPerampanel may increase the central nervous system depressant (CNS depressant) activities of Zaleplon.
PhenobarbitalThe serum concentration of Zaleplon can be decreased when it is combined with Phenobarbital.
PhenytoinThe serum concentration of Zaleplon can be decreased when it is combined with Phenytoin.
PramipexoleZaleplon may increase the sedative activities of Pramipexole.
PrimidoneThe serum concentration of Zaleplon can be decreased when it is combined with Primidone.
RifabutinThe serum concentration of Zaleplon can be decreased when it is combined with Rifabutin.
RifampicinThe serum concentration of Zaleplon can be decreased when it is combined with Rifampicin.
RifapentineThe serum concentration of Zaleplon can be decreased when it is combined with Rifapentine.
RopiniroleZaleplon may increase the sedative activities of Ropinirole.
RotigotineZaleplon may increase the sedative activities of Rotigotine.
RufinamideThe risk or severity of adverse effects can be increased when Rufinamide is combined with Zaleplon.
Sodium oxybateZaleplon may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
SuvorexantZaleplon may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
TapentadolTapentadol may increase the central nervous system depressant (CNS depressant) activities of Zaleplon.
ThalidomideZaleplon may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
ZolpidemZaleplon may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Food InteractionsNot Available

Targets

Kind
Protein
Organism
Human
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. Functions as receptor for diazepines and various anesthetics, such as pentobarbital; these are bound at a separate allosteric effector binding site. Functions as ligand-gated chloride channel (By si...
Gene Name:
GABRA1
Uniprot ID:
P14867
Molecular Weight:
51801.395 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284 ]
  2. 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. [PubMed:17016423 ]
  3. Patat A, Paty I, Hindmarch I: Pharmacodynamic profile of Zaleplon, a new non-benzodiazepine hypnotic agent. Hum Psychopharmacol. 2001 Jul;16(5):369-392. [PubMed:12404558 ]
  4. Barbera J, Shapiro C: Benefit-risk assessment of zaleplon in the treatment of insomnia. Drug Saf. 2005;28(4):301-18. [PubMed:15783240 ]
  5. Sanger DJ, Griebel G, Perrault G, Claustre Y, Schoemaker H: Discriminative stimulus effects of drugs acting at GABA(A) receptors: differential profiles and receptor selectivity. Pharmacol Biochem Behav. 1999 Oct;64(2):269-73. [PubMed:10515302 ]
  6. Terzano MG, Rossi M, Palomba V, Smerieri A, Parrino L: New drugs for insomnia: comparative tolerability of zopiclone, zolpidem and zaleplon. Drug Saf. 2003;26(4):261-82. [PubMed:12608888 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
other
General Function:
Cholesterol binding
Specific Function:
Can bind protoporphyrin IX and may play a role in the transport of porphyrins and heme (By similarity). Promotes the transport of cholesterol across mitochondrial membranes and may play a role in lipid metabolism (PubMed:24814875), but its precise physiological role is controversial. It is apparently not required for steroid hormone biosynthesis. Was initially identified as peripheral-type benz...
Gene Name:
TSPO
Uniprot ID:
P30536
Molecular Weight:
18827.81 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284 ]
  2. 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. [PubMed:17016423 ]

Enzymes

Kind
Protein
Organism
Human
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 reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
Molecular Weight:
57342.67 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
  2. Foye, William O.;Williams, David A.;Lemke, Thomas L. (2002). Foye's Principles of Medicinal Chemistry (5th ed.). Lippincott Williams & Wilkins. [ISBN:0683307371 ]
  3. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
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 unrelated compounds, including steroids, fatty acids, and xenobiotics.
Gene Name:
CYP3A5
Uniprot ID:
P20815
Molecular Weight:
57108.065 Da
References
  1. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
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 unrelated compounds, including steroids, fatty acids, and xenobiotics.
Gene Name:
CYP3A7
Uniprot ID:
P24462
Molecular Weight:
57525.03 Da
References
  1. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Xanthine dehydrogenase activity
Specific Function:
Oxidase with broad substrate specificity, oxidizing aromatic azaheterocycles, such as N1-methylnicotinamide and N-methylphthalazinium, as well as aldehydes, such as benzaldehyde, retinal, pyridoxal, and vanillin. Plays a key role in the metabolism of xenobiotics and drugs containing aromatic azaheterocyclic substituents. Participates in the bioactivation of prodrugs such as famciclovir, catalyz...
Gene Name:
AOX1
Uniprot ID:
Q06278
Molecular Weight:
147916.735 Da
References
  1. Lake BG, Ball SE, Kao J, Renwick AB, Price RJ, Scatina JA: Metabolism of zaleplon by human liver: evidence for involvement of aldehyde oxidase. Xenobiotica. 2002 Oct;32(10):835-47. [PubMed:12419014 ]
  2. Obach RS: Potent inhibition of human liver aldehyde oxidase by raloxifene. Drug Metab Dispos. 2004 Jan;32(1):89-97. [PubMed:14709625 ]
Comments
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Drug created on June 13, 2005 07:24 / Updated on April 15, 2016 12:10