You are using an unsupported browser. Please upgrade your browser to a newer version to get the best experience on DrugBank.
Identification
NameModafinil
Accession NumberDB00745  (APRD00534)
TypeSmall Molecule
GroupsApproved, Investigational
Description

Modafinil is a stimulant drug marketed as a ‘wakefulness promoting agent’ and is one of the stimulants used in the treatment of narcolepsy. Narcolepsy is caused by dysfunction of a family of wakefulness-promoting and sleep-suppressing peptides, the orexins, whose neurons are activated by modafinil. The prexin neuron activation is associated with psychoactivation and euphoria. The exact mechanism of action is unclear, although in vitro studies have shown it to inhibit the reuptake of dopamine by binding to the dopamine reuptake pump, and lead to an increase in extracellular dopamine. Modafinil activates glutamatergic circuits while inhibiting GABA.

Structure
Thumb
Synonyms
Modafinil
Modafinilo
Modafinilum
Moderateafinil
Provigil
External Identifiers
  • CEP 1538
  • CRL 40476
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Alertectablet100 mgoralTeva Canada Limited1999-03-24Not applicableCanada
Auro-modafiniltablet100 mgoralAuro Pharma Inc2014-10-24Not applicableCanada
Bio-modafiniltablet100 mgoralBiomed Pharma2015-10-06Not applicableCanada
Ipg-modafiniltablet100 mgoralMarcan Pharmaceuticals IncNot applicableNot applicableCanada
Mar-modafiniltablet100 mgoralMarcan Pharmaceuticals Inc2015-01-09Not applicableCanada
Modafiniltablet200 mg/1oralPar Pharmaceutical2012-04-06Not applicableUs
Modafiniltablet200 mg/1oralCima Labs Inc.2012-03-29Not applicableUs
Modafiniltablet100 mg/1oralPar Pharmaceutical2012-04-06Not applicableUs
Modafiniltablet100 mg/1oralCima Labs Inc.2012-03-29Not applicableUs
Modafiniltablet200 mg/1oralAphena Pharma Solutions Tennessee, Llc2012-03-29Not applicableUs
Modafiniltablet200 mg/1oralSTAT Rx USA LLC2012-04-06Not applicableUs
Modafiniltablet200 mg/1oralDispensing Solutions, Inc.2012-03-29Not applicableUs
Provigiltablet100 mg/1oralCephalon, Incorporated1999-02-15Not applicableUs
Provigiltablet200 mg/1oralbryant ranch prepack1998-12-24Not applicableUs
Provigiltablet100 mg/1oralRebel Distributors Corp2005-06-03Not applicableUs
Provigiltablet100 mg/1oralCardinal Health1998-12-24Not applicableUs
Provigiltablet200 mg/1oralPhysicians Total Care, Inc.2004-01-19Not applicableUs
Provigiltablet200 mg/1oralLake Erie Medical Surgical & Supply DBA Quality Care Products LLC2011-07-20Not applicableUs
Provigiltablet100 mg/1oralPhysicians Total Care, Inc.2005-06-03Not applicableUs
Provigiltablet200 mg/1oralCephalon, Incorporated1999-02-15Not applicableUs
Provigiltablet100 mg/1oralbryant ranch prepack1998-12-24Not applicableUs
Provigiltablet200 mg/1oralRebel Distributors Corp2004-01-19Not applicableUs
Provigiltablet200 mg/1oralUnit Dose Services1998-12-24Not applicableUs
Teva-modafiniltablet100 mgoralTeva Canada Limited2014-07-02Not applicableCanada
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo-modafiniltablet100 mgoralApotex Inc2008-05-01Not applicableCanada
Modafiniltablet100 mg/1oralIngenus Pharmaceuticals, LLC2014-04-01Not applicableUs
Modafiniltablet100 mg/1oralAmerican Health Packaging2014-04-01Not applicableUs
Modafiniltablet100 mg/1oralMylan Pharmaceuticals Inc.2012-08-10Not applicableUs
Modafiniltablet100 mg/1oralMylan Institutional Inc.2012-09-06Not applicableUs
Modafiniltablet100 mg/1oralMajor Pharmaceuticals2013-04-03Not applicableUs
Modafiniltablet100 mg/1oralGolden State Medical Supply, Inc.2014-02-03Not applicableUs
Modafiniltablet200 mg/1oralAphena Pharma Solutions Tennessee, Llc2012-08-10Not applicableUs
Modafiniltablet200 mg/1oralAurobindo Pharma Limited2012-09-27Not applicableUs
Modafiniltablet200 mg/1oralQualitest Pharmaceuticals2013-01-29Not applicableUs
Modafiniltablet100 mg/1oralHikma Pharmaceutical2008-04-04Not applicableUs
Modafiniltablet200 mg/1oralAv Kare, Inc.2014-02-24Not applicableUs
Modafiniltablet100 mg/1oralAurobindo Pharma Limited2012-09-27Not applicableUs
Modafiniltablet100 mg/1oralQualitest Pharmaceuticals2013-01-29Not applicableUs
Modafiniltablet200 mg/1oralHikma Pharmaceutical2008-04-04Not applicableUs
Modafiniltablet100 mg/1oralAv Kare, Inc.2014-02-24Not applicableUs
Modafiniltablet200 mg/1oralbryant ranch prepack2013-04-03Not applicableUs
Modafiniltablet200 mg/1oralActavis Pharma, Inc.2013-04-03Not applicableUs
Modafiniltablet200 mg/1oralCitron Pharma LLC2012-09-27Not applicableUs
Modafiniltablet200 mg/1oralOrchid Pharma Inc2013-08-01Not applicableUs
Modafiniltablet200 mg/1oralApotex Corp.2014-02-03Not applicableUs
Modafiniltablet100 mg/1oralActavis Pharma, Inc.2013-04-03Not applicableUs
Modafiniltablet100 mg/1oralCitron Pharma LLC2012-09-27Not applicableUs
Modafiniltablet100 mg/1oralOrchid Pharma Inc2013-08-01Not applicableUs
Modafiniltablet100 mg/1oralApotex Corp.2014-02-03Not applicableUs
Modafiniltablet200 mg/1oralAmerican Health Packaging2014-04-01Not applicableUs
Modafiniltablet200 mg/1oralIngenus Pharmaceuticals, LLC2014-04-01Not applicableUs
Modafiniltablet200 mg/1oralMylan Pharmaceuticals Inc.2012-08-10Not applicableUs
Modafiniltablet200 mg/1oralMylan Institutional Inc.2012-09-06Not applicableUs
Modafiniltablet200 mg/1oralMajor Pharmaceuticals2013-04-03Not applicableUs
Modafiniltablet200 mg/1oralGolden State Medical Supply, Inc.2014-02-03Not applicableUs
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
AlertexSaval
AspendosMedochemie
ForcilinLKM
MentixRoyal Pharma
ModasomilCephalon
ModavigilCSL
ModiodalCephalon
ProvakeRanbaxy
ResotylDrugtech
SparlonCephalon
StavigileLibbs
VigicerBeta
VigilCephalon
ZaluxNot Available
Brand mixturesNot Available
SaltsNot Available
Categories
UNIIR3UK8X3U3D
CAS number68693-11-8
WeightAverage: 273.35
Monoisotopic: 273.082349419
Chemical FormulaC15H15NO2S
InChI KeyInChIKey=YFGHCGITMMYXAQ-UHFFFAOYSA-N
InChI
InChI=1S/C15H15NO2S/c16-14(17)11-19(18)15(12-7-3-1-4-8-12)13-9-5-2-6-10-13/h1-10,15H,11H2,(H2,16,17)
IUPAC Name
2-diphenylmethanesulfinylacetamide
SMILES
NC(=O)CS(=O)C(C1=CC=CC=C1)C1=CC=CC=C1
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as diphenylmethanes. These are compounds containing a diphenylmethane moiety, which consists of a methane wherein two hydrogen atoms are replaced by two phenyl groups.
KingdomOrganic compounds
Super ClassBenzenoids
ClassBenzene and substituted derivatives
Sub ClassDiphenylmethanes
Direct ParentDiphenylmethanes
Alternative Parents
Substituents
  • Diphenylmethane
  • Sulfoxide
  • Primary carboxylic acid amide
  • Carboxamide group
  • Sulfinyl compound
  • Carboxylic acid derivative
  • Carboxylic acid amide
  • Hydrocarbon derivative
  • Organosulfur compound
  • Organooxygen compound
  • Organonitrogen compound
  • Carbonyl group
  • Aromatic homomonocyclic compound
Molecular FrameworkAromatic homomonocyclic compounds
External DescriptorsNot Available
Pharmacology
IndicationTo improve wakefulness in patients with excessive daytime sleepiness (EDS) associated with narcolepsy.
PharmacodynamicsModafinil is a stimulant drug marketed as a 'wakefulness promoting agent' and is one of the stimulants used in the treatment of narcolepsy. Narcolepsy is caused by dysfunction of a family of wakefulness-promoting and sleep-suppressing peptides, the orexins, whose neurons are activated by modafinil. The prexin neuron activation is associated with psychoactivation and euphoria. Modafinil is not indicated for complaints of lack of energy or fatigue; but it appears to be very helpful for some patients. Also, it has been used in the treatment of hypersomnia, a disorder in which patients lack the capacity for meaningful sleep and may require ten or more hours per day. Recent studies have have found that modafinil may help recovering cocaine addicts fight their addiction.
Mechanism of actionThe exact mechanism of action is unclear, although in vitro studies have shown it to inhibit the reuptake of dopamine by binding to the dopamine reuptake pump, and lead to an increase in extracellular dopamine. Modafinil activates glutamatergic circuits while inhibiting GABA. Modafinil is thought to have less potential for abuse than other stimulants due to the absence of any significant euphoric or pleasurable effects. It is possible that modafinil acts by a synergistic combination of mechanisms including direct inhibition of dopamine reuptake, indirect inhibition of noradrenalin reuptake in the VLPO and orexin activation. Modafinil has partial alpha 1B-adrenergic agonist effects by directly stimulating the receptors.
Related Articles
AbsorptionRapid following oral administration.
Volume of distribution
  • 0.9 L/kg
Protein binding60%
Metabolism

Hepatic

SubstrateEnzymesProduct
Modafinil
modafinil acidDetails
Route of eliminationThe major route of elimination is metabolism (~90%), primarily by the liver, with subsequent renal elimination of the metabolites.
Half life23-215 hours
ClearanceNot Available
ToxicityNot Available
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated Effects
Interacting Gene/EnzymeSNP RS IDAllele nameDefining changeEffectReference(s)
Catechol O-methyltransferase
Gene symbol: COMT
UniProt: P21964
rs4680 Not AvailableAA allelePoor response to modafinil19037200
Catechol O-methyltransferase
Gene symbol: COMT
UniProt: P21964
rs4680 Not AvailableGG alleleThose with the GG genotype respond better to drug therapy (improved vigor and well being). Those with the AA genotype do not respond well to drug therapy19037200
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+1.0
Blood Brain Barrier+0.9947
Caco-2 permeable+0.5066
P-glycoprotein substrateNon-substrate0.8912
P-glycoprotein inhibitor INon-inhibitor0.8842
P-glycoprotein inhibitor IINon-inhibitor0.9962
Renal organic cation transporterNon-inhibitor0.8153
CYP450 2C9 substrateNon-substrate0.793
CYP450 2D6 substrateNon-substrate0.8659
CYP450 3A4 substrateNon-substrate0.5971
CYP450 1A2 substrateNon-inhibitor0.6653
CYP450 2C9 inhibitorNon-inhibitor0.6045
CYP450 2D6 inhibitorNon-inhibitor0.9117
CYP450 2C19 inhibitorNon-inhibitor0.6952
CYP450 3A4 inhibitorNon-inhibitor0.8309
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.6395
Ames testNon AMES toxic0.6562
CarcinogenicityNon-carcinogens0.6665
BiodegradationReady biodegradable0.6304
Rat acute toxicity2.0926 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9799
hERG inhibition (predictor II)Non-inhibitor0.9279
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Cephalon inc
  • Cephalon, Inc.
Packagers
Dosage forms
FormRouteStrength
Tabletoral100 mg
Tabletoral100 mg/1
Tabletoral200 mg/1
Prices
Unit descriptionCostUnit
Provigil 200 mg tablet15.33USD tablet
Provigil 100 mg tablet13.58USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA2165824 No2005-08-022014-06-14Canada
CA2201967 No2002-12-102015-10-04Canada
US7297346 Yes2004-05-292024-05-29Us
USRE37516 No1994-10-062014-10-06Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point164-166 °CNot Available
water solubilitySlightly solubleNot Available
logP0.6Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.622 mg/mLALOGPS
logP1.75ALOGPS
logP1.53ChemAxon
logS-2.6ALOGPS
pKa (Strongest Acidic)8.84ChemAxon
pKa (Strongest Basic)-4.4ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count2ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area60.16 Å2ChemAxon
Rotatable Bond Count5ChemAxon
Refractivity77.39 m3·mol-1ChemAxon
Polarizability28.71 Å3ChemAxon
Number of Rings2ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
References
Synthesis Reference

DrugSyn.org

US4177290
General References
  1. Lindsay SE, Gudelsky GA, Heaton PC: Use of modafinil for the treatment of attention deficit/hyperactivity disorder. Ann Pharmacother. 2006 Oct;40(10):1829-33. Epub 2006 Sep 5. [PubMed:16954326 ]
  2. Ishizuka T, Sakamoto Y, Sakurai T, Yamatodani A: Modafinil increases histamine release in the anterior hypothalamus of rats. Neurosci Lett. 2003 Mar 20;339(2):143-6. [PubMed:12614915 ]
External Links
ATC CodesN06BA07
AHFS Codes
  • 28:20.92
PDB EntriesNot Available
FDA labelDownload (98.9 KB)
MSDSDownload (57 KB)
Interactions
Drug Interactions
Drug
AcebutololThe risk or severity of adverse effects can be increased when Acebutolol is combined with Modafinil.
AmphetamineThe risk or severity of adverse effects can be increased when Amphetamine is combined with Modafinil.
AprepitantThe serum concentration of Modafinil can be increased when it is combined with Aprepitant.
AripiprazoleThe serum concentration of Aripiprazole can be decreased when it is combined with Modafinil.
AtomoxetineAtomoxetine may increase the hypertensive activities of Modafinil.
AxitinibThe serum concentration of Axitinib can be decreased when it is combined with Modafinil.
BedaquilineThe serum concentration of Bedaquiline can be decreased when it is combined with Modafinil.
BenzphetamineThe risk or severity of adverse effects can be increased when Benzphetamine is combined with Modafinil.
BexaroteneThe serum concentration of Modafinil can be decreased when it is combined with Bexarotene.
BortezomibThe metabolism of Bortezomib can be decreased when combined with Modafinil.
BosentanThe serum concentration of Modafinil can be decreased when it is combined with Bosentan.
BosutinibThe serum concentration of Bosutinib can be decreased when it is combined with Modafinil.
ChlorotrianiseneThe serum concentration of Chlorotrianisene can be decreased when it is combined with Modafinil.
ChlorphentermineThe risk or severity of adverse effects can be increased when Chlorphentermine is combined with Modafinil.
CilostazolThe serum concentration of Cilostazol can be increased when it is combined with Modafinil.
CitalopramThe serum concentration of Citalopram can be increased when it is combined with Modafinil.
ClarithromycinThe serum concentration of the active metabolites of Clarithromycin can be increased when Clarithromycin is used in combination with Modafinil.
ClenbuterolThe risk or severity of adverse effects can be increased when Clenbuterol is combined with Modafinil.
ClopidogrelThe serum concentration of the active metabolites of Clopidogrel can be reduced when Clopidogrel is used in combination with Modafinil resulting in a loss in efficacy.
ConivaptanThe serum concentration of Modafinil can be increased when it is combined with Conivaptan.
CyclosporineThe serum concentration of Cyclosporine can be decreased when it is combined with Modafinil.
DabrafenibThe serum concentration of Modafinil can be decreased when it is combined with Dabrafenib.
DaclatasvirThe serum concentration of Daclatasvir can be decreased when it is combined with Modafinil.
DasatinibThe serum concentration of Modafinil can be increased when it is combined with Dasatinib.
DeferasiroxThe serum concentration of Modafinil can be decreased when it is combined with Deferasirox.
DobutamineThe risk or severity of adverse effects can be increased when Dobutamine is combined with Modafinil.
DopamineThe risk or severity of adverse effects can be increased when Dopamine is combined with Modafinil.
DoxofyllineThe risk or severity of adverse effects can be increased when Modafinil is combined with Doxofylline.
DronabinolDronabinol may increase the tachycardic activities of Modafinil.
EnzalutamideThe serum concentration of Enzalutamide can be decreased when it is combined with Modafinil.
EpinephrineThe risk or severity of adverse effects can be increased when Epinephrine is combined with Modafinil.
FenoterolThe risk or severity of adverse effects can be increased when Fenoterol is combined with Modafinil.
FentanylThe serum concentration of Fentanyl can be decreased when it is combined with Modafinil.
FlibanserinThe serum concentration of Flibanserin can be decreased when it is combined with Modafinil.
FluconazoleThe metabolism of Modafinil can be decreased when combined with Fluconazole.
FlunisolideThe serum concentration of Flunisolide can be decreased when it is combined with Modafinil.
FormoterolThe risk or severity of adverse effects can be increased when Formoterol is combined with Modafinil.
FosaprepitantThe serum concentration of Modafinil can be increased when it is combined with Fosaprepitant.
Fusidic AcidThe serum concentration of Modafinil can be increased when it is combined with Fusidic Acid.
HydrocodoneThe serum concentration of Hydrocodone can be decreased when it is combined with Modafinil.
IbrutinibThe serum concentration of Ibrutinib can be decreased when it is combined with Modafinil.
IdelalisibThe serum concentration of Modafinil can be increased when it is combined with Idelalisib.
IfosfamideThe serum concentration of the active metabolites of Ifosfamide can be reduced when Ifosfamide is used in combination with Modafinil resulting in a loss in efficacy.
IobenguaneThe therapeutic efficacy of Iobenguane can be decreased when used in combination with Modafinil.
IsoprenalineThe risk or severity of adverse effects can be increased when Isoprenaline is combined with Modafinil.
IvacaftorThe serum concentration of Modafinil can be increased when it is combined with Ivacaftor.
LabetalolThe risk or severity of adverse effects can be increased when Labetalol is combined with Modafinil.
LinezolidLinezolid may increase the hypertensive activities of Modafinil.
LuliconazoleThe serum concentration of Modafinil can be increased when it is combined with Luliconazole.
MephentermineThe risk or severity of adverse effects can be increased when Mephentermine is combined with Modafinil.
MetaraminolThe risk or severity of adverse effects can be increased when Metaraminol is combined with Modafinil.
MethamphetamineThe risk or severity of adverse effects can be increased when Methamphetamine is combined with Modafinil.
MethoxamineThe risk or severity of adverse effects can be increased when Methoxamine is combined with Modafinil.
MidodrineThe risk or severity of adverse effects can be increased when Midodrine is combined with Modafinil.
MifepristoneThe serum concentration of Modafinil can be increased when it is combined with Mifepristone.
MitotaneThe serum concentration of Modafinil can be decreased when it is combined with Mitotane.
NaphazolineThe risk or severity of adverse effects can be increased when Naphazoline is combined with Modafinil.
NelfinavirThe metabolism of Modafinil can be decreased when combined with Nelfinavir.
NetupitantThe serum concentration of Modafinil can be increased when it is combined with Netupitant.
NimodipineThe serum concentration of Nimodipine can be decreased when it is combined with Modafinil.
NisoldipineThe serum concentration of Nisoldipine can be decreased when it is combined with Modafinil.
NorepinephrineThe risk or severity of adverse effects can be increased when Norepinephrine is combined with Modafinil.
OlaparibThe serum concentration of Olaparib can be decreased when it is combined with Modafinil.
OrciprenalineThe risk or severity of adverse effects can be increased when Orciprenaline is combined with Modafinil.
OxymetazolineThe risk or severity of adverse effects can be increased when Oxymetazoline is combined with Modafinil.
PalbociclibThe serum concentration of Palbociclib can be decreased when it is combined with Modafinil.
PantoprazoleThe metabolism of Pantoprazole can be decreased when combined with Modafinil.
PhenmetrazineThe risk or severity of adverse effects can be increased when Phenmetrazine is combined with Modafinil.
PhentermineThe risk or severity of adverse effects can be increased when Phentermine is combined with Modafinil.
PhenylephrineThe risk or severity of adverse effects can be increased when Phenylephrine is combined with Modafinil.
PhenylpropanolamineThe risk or severity of adverse effects can be increased when Phenylpropanolamine is combined with Modafinil.
PhenytoinThe metabolism of Modafinil can be increased when combined with Phenytoin.
RanolazineThe serum concentration of Ranolazine can be decreased when it is combined with Modafinil.
RitodrineThe risk or severity of adverse effects can be increased when Ritodrine is combined with Modafinil.
RolapitantThe serum concentration of Rolapitant can be decreased when it is combined with Modafinil.
SalmeterolThe risk or severity of adverse effects can be increased when Salmeterol is combined with Modafinil.
SaxagliptinThe serum concentration of Saxagliptin can be decreased when it is combined with Modafinil.
SiltuximabThe serum concentration of Modafinil can be decreased when it is combined with Siltuximab.
SimeprevirThe serum concentration of Simeprevir can be decreased when it is combined with Modafinil.
SofosbuvirThe serum concentration of Sofosbuvir can be decreased when it is combined with Modafinil.
SonidegibThe serum concentration of Sonidegib can be decreased when it is combined with Modafinil.
St. John's WortThe serum concentration of Modafinil can be decreased when it is combined with St. John's Wort.
StiripentolThe serum concentration of Modafinil can be increased when it is combined with Stiripentol.
Tedizolid PhosphateTedizolid Phosphate may increase the hypertensive activities of Modafinil.
TerbutalineThe risk or severity of adverse effects can be increased when Terbutaline is combined with Modafinil.
TocilizumabThe serum concentration of Modafinil can be decreased when it is combined with Tocilizumab.
Food Interactions
  • Take without regard to meals.

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Monoamine transmembrane transporter activity
Specific Function:
Amine transporter. Terminates the action of dopamine by its high affinity sodium-dependent reuptake into presynaptic terminals.
Gene Name:
SLC6A3
Uniprot ID:
Q01959
Molecular Weight:
68494.255 Da
References
  1. Zhou J, He R, Johnson KM, Ye Y, Kozikowski AP: Piperidine-based nocaine/modafinil hybrid ligands as highly potent monoamine transporter inhibitors: efficient drug discovery by rational lead hybridization. J Med Chem. 2004 Nov 18;47(24):5821-4. [PubMed:15537337 ]
  2. Madras BK, Xie Z, Lin Z, Jassen A, Panas H, Lynch L, Johnson R, Livni E, Spencer TJ, Bonab AA, Miller GM, Fischman AJ: Modafinil occupies dopamine and norepinephrine transporters in vivo and modulates the transporters and trace amine activity in vitro. J Pharmacol Exp Ther. 2006 Nov;319(2):561-9. Epub 2006 Aug 2. [PubMed:16885432 ]
  3. Swanson JM: Role of executive function in ADHD. J Clin Psychiatry. 2003;64 Suppl 14:35-9. [PubMed:14658934 ]
  4. Dopheide MM, Morgan RE, Rodvelt KR, Schachtman TR, Miller DK: Modafinil evokes striatal [(3)H]dopamine release and alters the subjective properties of stimulants. Eur J Pharmacol. 2007 Jul 30;568(1-3):112-23. Epub 2007 Apr 5. [PubMed:17477916 ]
  5. Wisor JP, Nishino S, Sora I, Uhl GH, Mignot E, Edgar DM: Dopaminergic role in stimulant-induced wakefulness. J Neurosci. 2001 Mar 1;21(5):1787-94. [PubMed:11222668 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
partial agonist
General Function:
Protein heterodimerization activity
Specific Function:
This alpha-adrenergic receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. Its effect is mediated by G(q) and G(11) proteins. Nuclear ADRA1A-ADRA1B heterooligomers regulate phenylephrine (PE)-stimulated ERK signaling in cardiac myocytes.
Gene Name:
ADRA1B
Uniprot ID:
P35368
Molecular Weight:
56835.375 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. Chen CR, Qu WM, Qiu MH, Xu XH, Yao MH, Urade Y, Huang ZL: Modafinil exerts a dose-dependent antiepileptic effect mediated by adrenergic alpha1 and histaminergic H1 receptors in mice. Neuropharmacology. 2007 Sep;53(4):534-41. Epub 2007 Jun 30. [PubMed:17681557 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitorinducer
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. Robertson P Jr, Hellriegel ET: Clinical pharmacokinetic profile of modafinil. Clin Pharmacokinet. 2003;42(2):123-37. [PubMed:12537513 ]
  2. 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 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitorinducer
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 imipramine.
Gene Name:
CYP2C19
Uniprot ID:
P33261
Molecular Weight:
55930.545 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. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitorinducer
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 unrelated compounds, including steroids, fatty acids, and xenobiotics. Most active in catalyzing 2-hydroxylation. Caffeine is metabolized primarily by cytochrome CYP1A2 in the liver through an initial N...
Gene Name:
CYP1A2
Uniprot ID:
P05177
Molecular Weight:
58293.76 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. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitorinducer
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 unrelated compounds, including steroids, fatty acids, and xenobiotics. Acts as a 1,4-cineole 2-exo-monooxygenase.
Gene Name:
CYP2B6
Uniprot ID:
P20813
Molecular Weight:
56277.81 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 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitorinducer
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 unrelated compounds, including steroids, fatty acids, and xenobiotics. This enzyme contributes to the wide pharmacokinetics variability of the metabolism of drugs such as S-warfarin, diclofenac, phenyto...
Gene Name:
CYP2C9
Uniprot ID:
P11712
Molecular Weight:
55627.365 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 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitorinducer
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. 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 ]
Comments
comments powered by Disqus
Drug created on June 13, 2005 07:24 / Updated on July 30, 2016 03:07