You are using an unsupported browser. Please upgrade your browser to a newer version to get the best experience on DrugBank.
Identification
NameAmphetamine
Accession NumberDB00182  (APRD00480)
TypeSmall Molecule
GroupsApproved, Illicit
DescriptionAmphetamines are non-catecholamine sympathomimetic amines with CNS stimulant activity. By mimicking the structures of the catecholamine neurotransmitters, noradrenaline and dopamine, amphetamines modulate monoamine release, reuptake, and signalling within the brain. Although "amphetamine" is used as a descriptor of its own structural class, amphetamine properly refers to a racemic free base composed of equal parts of its two optical antipodes: levo-amphetamine and dextro-amphetamine. Used in the past for the treatment of depression, stress, and for concentration improvement, it is currently available as a prescription drug for the treatment of attention hyperactivity disorder (ADHD), narcolepsy, and as an adjunct in the treatment of exogenous obesity. Amphetamine is also available in a mixed salt/mixed enantiomer form (Adderall), where d-amphetamine and l-amphetamine are available in a ratio of 3:1. It is also available in a prodrug form as lisdexamfetamine.
Structure
Thumb
Synonyms
1-phenyl-2-aminopropane
1-Phenylpropan-2-amin
alpha-Methylbenzeneethaneamine
alpha-Methylphenylethylamine
Amfetamine
Amfetaminum
Amphetamin
Amphetamine
beta-Aminopropylbenzene
beta-Phenylisopropylamin
beta-Phenylisopropylamine
Desoxynorephedrine
rac-(2R)-1-phenylpropan-2-amine
rac-amphetamine
α-methylbenzeneethaneamine
α-methylphenethylamine
β-aminopropylbenzene
β-phenylisopropylamine
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Adzenys XR-odttablet, orally disintegrating12.5 mg/1oralNeos Therapeutics, Lp2016-02-16Not applicableUs
Adzenys XR-odttablet, orally disintegrating3.1 mg/1oralNeos Therapeutics, Lp2016-02-16Not applicableUs
Adzenys XR-odttablet, orally disintegrating15.7 mg/1oralNeos Therapeutics, Lp2016-02-16Not applicableUs
Adzenys XR-odttablet, orally disintegrating6.3 mg/1oralNeos Therapeutics, Lp2016-02-16Not applicableUs
Adzenys XR-odttablet, orally disintegrating18.8 mg/1oralNeos Therapeutics, Lp2016-02-16Not applicableUs
Adzenys XR-odttablet, orally disintegrating9.4 mg/1oralNeos Therapeutics, Lp2016-02-16Not applicableUs
Dyanavel XRsuspension, extended release2.5 mg/mLoralTris Pharma Inc2015-10-01Not applicableUs
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Evekeotablet5 mg/1oralArbor Pharmaceuticals, Inc.2015-02-01Not applicableUs
Evekeotablet10 mg/1oralArbor Pharmaceuticals, Inc.2015-02-01Not applicableUs
Evekeotablet5 mg/1oralArbor Pharmaceuticals2015-11-01Not applicableUs
Evekeotablet10 mg/1oralArbor Pharmaceuticals2015-11-01Not applicableUs
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixtures
NameLabellerIngredients
Act Amphetamine XRActavis Pharma Company
AdderallTeva Select Brands
Adderall XRShire US Manufacturing Inc.
Apo-amphetamine XRApotex Inc
Dextroamphetamine Saccharate and Amphetamine Aspartate and Dextroamphetamine Sulfate and Amphetamine SulfateMallinckrodt, Inc.
Dextroamphetamine Saccharate, Amphetamine Aspartate (monohydrate), Dextroamphetamine Sulfate, Amphetamine SulfateMylan Pharmaceuticals Inc.
Dextroamphetamine Saccharate, Amphetamine Aspartate Monohydrate, Dextroamphetamine Sulfate and Amphetamine SulfateEon Labs, Inc.
Dextroamphetamine Saccharate, Amphetamine Aspartate Monohydrate, Dextroamphetamine Sulfate, Amphetamine SulfateActavis Pharma, Inc.
Dextroamphetamine Saccharate, Amphetamine Aspartate, Dextroamphetamine Sulfate and Amphetamine SuflateSTAT Rx USA LLC
Dextroamphetamine Saccharate, Amphetamine Aspartate, Dextroamphetamine Sulfate and Amphetamine SulfateGlobal Pharmaceuticals, Division of Impax Laboratories Inc.
Dextroamphetamine Saccharate, Amphetamine Aspartate, Dextroamphetamine Sulfate, and Amphetamine SulfateBarr Laboratories Inc.
PMS-amphetamines XRPharmascience Inc
Salts
Name/CASStructureProperties
Amphetamine adipate
ThumbNot applicableDBSALT001323
Amphetamine aspartate
ThumbNot applicableDBSALT001345
Amphetamine aspartate monohydrate
ThumbNot applicableDBSALT001501
Amphetamine sulfate
ThumbNot applicableDBSALT001205
Categories
UNIICK833KGX7E
CAS number300-62-9
WeightAverage: 135.2062
Monoisotopic: 135.104799421
Chemical FormulaC9H13N
InChI KeyInChIKey=KWTSXDURSIMDCE-UHFFFAOYSA-N
InChI
InChI=1S/C9H13N/c1-8(10)7-9-5-3-2-4-6-9/h2-6,8H,7,10H2,1H3
IUPAC Name
1-phenylpropan-2-amine
SMILES
CC(N)CC1=CC=CC=C1
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as amphetamines and derivatives. These are organic compounds containing or derived from 1-phenylpropan-2-amine.
KingdomOrganic compounds
Super ClassBenzenoids
ClassBenzene and substituted derivatives
Sub ClassPhenethylamines
Direct ParentAmphetamines and derivatives
Alternative Parents
Substituents
  • Amphetamine or derivatives
  • Phenylpropane
  • Aralkylamine
  • Hydrocarbon derivative
  • Primary amine
  • Organonitrogen compound
  • Primary aliphatic amine
  • Amine
  • Aromatic homomonocyclic compound
Molecular FrameworkAromatic homomonocyclic compounds
External DescriptorsNot Available
Pharmacology
IndicationFor treatment of Attention Deficit Disorder with Hyperactivity (ADDH), narcolepsy, and exogenous obesity as a short term (a few weeks) adjunct in a regimen of weight reduction based on caloric restriction for patients refractory to alternative therapy.
PharmacodynamicsNot Available
Mechanism of actionAmphetamines stimulate the release of norepinephrine from central adrenergic receptors. At higher dosages, they cause release of dopamine from the mesocorticolimbic system and the nigrostriatal dopamine systems. Amphetamine may also act as a direct agonist on central 5-HT receptors and may inhibit monoamine oxidase (MAO). In the periphery, amphetamines are believed to cause the release of noradrenaline by acting on the adrenergic nerve terminals and alpha- and beta-receptors. Modulation of serotonergic pathways may contribute to the calming affect. The drug interacts with VMAT enzymes to enhance release of DA and 5-HT from vesicles. It may also directly cause the reversal of DAT and SERT.
Related Articles
AbsorptionAmphetamine forms easily absorbed molecules that are highly lipid soluble. D-amphetamine mean peak plasma concentrations of 44.9 ng/mL occurred at a median time of 5.0 hours after dosing, and L-amphetamine mean peak plasma concentrations of 14.5 ng/mL occurred at a median time of 5.25 hours after dosing.
Volume of distributionNot Available
Protein binding15-40%
Metabolism

Amphetamine is reported to be oxidized at the 4 position of the benzene ring to form 4-hydroxyamphetamine, or on the side chain α or β carbons to form alpha-hydroxy-amphetamine or norephedrine, respectively. Norephedrine and 4-hydroxy-amphetamine are both active and each is subsequently oxidized to form 4-hydroxy-norephedrine. Alpha-hydroxy-amphetamine undergoes deamination to form phenylacetone, which ultimately forms benzoic acid and its glucuronide and the glycine conjugate hippuric acid. Although the enzymes involved in amphetamine metabolism have not been clearly defined, CYP2D6 is known to be involved with formation of 4-hydroxy-amphetamine. Since CYP2D6 is genetically polymorphic, population variations in amphetamine metabolism are a possibility.

Route of eliminationWith normal urine pHs, approximately half of an administered dose of amphetamine is recoverable in urine as derivatives of alpha-hydroxy-amphetamine and approximately another 30-40% of the dose is recoverable in urine as amphetamine itself. Since amphetamine has a pKa of 9 .9, urinary recovery of amphetamine is highly dependent on pH and urine flow rates. Alkaline urine pHs result in less ionization and reduced renal elimination, and acidic pHs and high flow rates result in increased renal elimination with clearances greater than glomerular filtration rates, indicating the involvement of active secretion.
Half lifeThe half life for adults in the fasted state was found to be 11.25 hr.
ClearanceNot Available
ToxicityLD50=180 mg/kg(subcutaneous injection in rat). The most common presenting symptoms seen are agitation, hallucinations, suicidal behaviour, and chest pain.
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+0.9972
Blood Brain Barrier+0.9565
Caco-2 permeable+0.8395
P-glycoprotein substrateNon-substrate0.7379
P-glycoprotein inhibitor INon-inhibitor0.9519
P-glycoprotein inhibitor IINon-inhibitor0.9859
Renal organic cation transporterNon-inhibitor0.8002
CYP450 2C9 substrateNon-substrate0.8114
CYP450 2D6 substrateSubstrate0.8919
CYP450 3A4 substrateNon-substrate0.795
CYP450 1A2 substrateNon-inhibitor0.5697
CYP450 2C9 inhibitorNon-inhibitor0.9313
CYP450 2D6 inhibitorInhibitor0.657
CYP450 2C19 inhibitorNon-inhibitor0.8445
CYP450 3A4 inhibitorNon-inhibitor0.8709
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.8732
Ames testNon AMES toxic0.93
CarcinogenicityNon-carcinogens0.6869
BiodegradationNot ready biodegradable0.6575
Rat acute toxicity3.2491 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9452
hERG inhibition (predictor II)Non-inhibitor0.9231
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Lannett co inc
  • Akorn inc
  • Teva pharmaceuticals usa inc
Packagers
Dosage forms
FormRouteStrength
Capsule (extended release)oral
Tablet, orally disintegratingoral12.5 mg/1
Tablet, orally disintegratingoral15.7 mg/1
Tablet, orally disintegratingoral18.8 mg/1
Tablet, orally disintegratingoral3.1 mg/1
Tablet, orally disintegratingoral6.3 mg/1
Tablet, orally disintegratingoral9.4 mg/1
Capsuleoral
Tabletoral
Capsule, extended releaseoral
Suspension, extended releaseoral2.5 mg/mL
Tabletoral10 mg/1
Tabletoral5 mg/1
Prices
Unit descriptionCostUnit
Desoxyn 5 mg tablet5.1USD tablet
Dexedrine 15 mg 24 Hour Capsule4.22USD capsule
Dexedrine 10 mg 24 Hour Capsule3.23USD capsule
Dexedrine 5 mg 24 Hour Capsule3.0USD capsule
Dexedrine spansule 15 mg2.45USD each
Dexedrine spansule 10 mg1.91USD each
Dexedrine spansule 5 mg1.91USD each
Amphetamine salts 12.5 mg tablet1.43USD tablet
Amphetamine salts 15 mg tablet1.43USD tablet
Amphetamine salts 7.5 mg tablet1.43USD tablet
Amphetamine salts 10 mg tablet1.37USD tablet
Amphetamine salts 20 mg tablet1.37USD tablet
Amphetamine salts 30 mg tablet1.37USD tablet
Amphetamine salts 5 mg tablet1.37USD tablet
Amphetamine Salt Combo 7.5 mg tablet1.3USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US6322819 Yes1999-04-212019-04-21Us
US6384020 Yes2001-01-062021-01-06Us
US6605300 Yes1999-04-212019-04-21Us
US8062667 No2009-03-292029-03-29Us
US8597684 No2007-03-152027-03-15Us
US8709491 No2012-06-282032-06-28Us
US8747902 No2007-03-152027-03-15Us
US8840924 No2006-06-052026-06-05Us
US8883217 No2007-03-152027-03-15Us
US9017731 No2012-06-282032-06-28Us
US9265737 No2012-06-282032-06-28Us
USRE41148 Yes1999-04-212019-04-21Us
USRE42096 Yes1999-04-212019-04-21Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting pointVolatizes slowly at room temperatureNot Available
water solubilitySlightlyNot Available
logP1.76HANSCH,C ET AL. (1995)
pKa10.1 (at 20 °C)PERRIN,DD (1965)
Predicted Properties
PropertyValueSource
Water Solubility1.74 mg/mLALOGPS
logP1.85ALOGPS
logP1.8ChemAxon
logS-1.9ALOGPS
pKa (Strongest Basic)10.01ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count1ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area26.02 Å2ChemAxon
Rotatable Bond Count2ChemAxon
Refractivity43.71 m3·mol-1ChemAxon
Polarizability16.17 Å3ChemAxon
Number of Rings1ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Download (7.59 KB)
Spectra
Spectrum TypeDescriptionSplash Key
MSMass Spectrum (Electron Ionization)splash10-0006-9000000000-98cd0a725199f943d6cfView in MoNA
References
Synthesis Reference

Guohong Wang, “Composition and methods for synthesis of novel tracers for detecting amphetamine and methamphetamine in samples.” U.S. Patent US20020090661, issued July 11, 2002.

US20020090661
General References
  1. Leith NJ, Kuczenski R: Chronic amphetamine: tolerance and reverse tolerance reflect different behavioral actions of the drug. Pharmacol Biochem Behav. 1981 Sep;15(3):399-404. [PubMed:7291243 ]
  2. Chaudhry IA, Turkanis SA, Karler R: Characteristics of "reverse tolerance" to amphetamine-induced locomotor stimulation in mice. Neuropharmacology. 1988 Aug;27(8):777-81. [PubMed:3216957 ]
  3. Sax KW, Strakowski SM: Behavioral sensitization in humans. J Addict Dis. 2001;20(3):55-65. [PubMed:11681593 ]
  4. Sulzer D, Sonders MS, Poulsen NW, Galli A: Mechanisms of neurotransmitter release by amphetamines: a review. Prog Neurobiol. 2005 Apr;75(6):406-33. [PubMed:15955613 ]
  5. Heal DJ, Smith SL, Gosden J, Nutt DJ: Amphetamine, past and present--a pharmacological and clinical perspective. J Psychopharmacol. 2013 Jun;27(6):479-96. doi: 10.1177/0269881113482532. Epub 2013 Mar 28. [PubMed:23539642 ]
External Links
ATC CodesN06BA01
AHFS Codes
  • 28:20.04
PDB EntriesNot Available
FDA labelDownload (10.4 MB)
MSDSNot Available
Interactions
Drug Interactions
Drug
7,8-DICHLORO-1,2,3,4-TETRAHYDROISOQUINOLINE7,8-DICHLORO-1,2,3,4-TETRAHYDROISOQUINOLINE may increase the hypertensive activities of Amphetamine.
AbirateroneThe metabolism of Amphetamine can be decreased when combined with Abiraterone.
AcebutololThe risk or severity of adverse effects can be increased when Amphetamine is combined with Acebutolol.
AcepromazineAcepromazine may decrease the stimulatory activities of Amphetamine.
AceprometazineAceprometazine may decrease the stimulatory activities of Amphetamine.
AcetazolamideAcetazolamide may decrease the excretion rate of Amphetamine which could result in a lower serum level and potentially a reduction in efficacy.
AcetophenazineAcetophenazine may decrease the stimulatory activities of Amphetamine.
AcrivastineAmphetamine may decrease the sedative activities of Acrivastine.
AlcaftadineAmphetamine may decrease the sedative activities of Alcaftadine.
AlfentanilAmphetamine may increase the analgesic activities of Alfentanil.
AlimemazineAmphetamine may decrease the sedative activities of Alimemazine.
AlphacetylmethadolAmphetamine may increase the analgesic activities of Alphacetylmethadol.
Aluminum hydroxideAluminum hydroxide may decrease the excretion rate of Amphetamine which could result in a lower serum level and potentially a reduction in efficacy.
Aluminum phosphateAluminum phosphate may decrease the excretion rate of Amphetamine which could result in a lower serum level and potentially a reduction in efficacy.
AmineptineAmineptine may increase the stimulatory activities of Amphetamine.
AmiodaroneThe metabolism of Amphetamine can be decreased when combined with Amiodarone.
AmisulprideAmisulpride may decrease the stimulatory activities of Amphetamine.
AmitriptylineAmitriptyline may increase the stimulatory activities of Amphetamine.
Ammonium chlorideThe serum concentration of Amphetamine can be decreased when it is combined with Ammonium chloride.
AmperozideAmperozide may decrease the stimulatory activities of Amphetamine.
AntazolineAmphetamine may decrease the sedative activities of Antazoline.
AripiprazoleAripiprazole may decrease the stimulatory activities of Amphetamine.
ArtemetherThe metabolism of Amphetamine can be decreased when combined with Artemether.
ArtesunateThe serum concentration of the active metabolites of Artesunate can be reduced when Artesunate is used in combination with Amphetamine resulting in a loss in efficacy.
AsenapineAsenapine may decrease the stimulatory activities of Amphetamine.
AstemizoleAmphetamine may decrease the sedative activities of Astemizole.
AtomoxetineAtomoxetine may increase the hypertensive activities of Amphetamine.
AzaperoneAzaperone may decrease the stimulatory activities of Amphetamine.
AzatadineAmphetamine may decrease the sedative activities of Azatadine.
AzelastineAmphetamine may decrease the sedative activities of Azelastine.
BenmoxinBenmoxin may increase the hypertensive activities of Amphetamine.
BenzphetamineThe risk or severity of adverse effects can be increased when Amphetamine is combined with Benzphetamine.
BetaxololThe metabolism of Amphetamine can be decreased when combined with Betaxolol.
BezitramideAmphetamine may increase the analgesic activities of Bezitramide.
BifeprunoxBifeprunox may decrease the stimulatory activities of Amphetamine.
Bismuth SubcitrateBismuth Subcitrate may decrease the excretion rate of Amphetamine which could result in a lower serum level and potentially a reduction in efficacy.
BrexpiprazoleBrexpiprazole may decrease the stimulatory activities of Amphetamine.
BrompheniramineAmphetamine may decrease the sedative activities of Brompheniramine.
BuclizineAmphetamine may decrease the sedative activities of Buclizine.
BuprenorphineAmphetamine may increase the analgesic activities of Buprenorphine.
BupropionThe metabolism of Amphetamine can be decreased when combined with Bupropion.
Butanoic AcidAmphetamine may decrease the sedative activities of Butanoic Acid.
ButorphanolAmphetamine may increase the analgesic activities of Butorphanol.
Calcium carbonateCalcium carbonate may decrease the excretion rate of Amphetamine which could result in a lower serum level and potentially a reduction in efficacy.
CarbinoxamineAmphetamine may decrease the sedative activities of Carbinoxamine.
CarfentanilAmphetamine may increase the analgesic activities of Carfentanil.
CariprazineCariprazine may decrease the stimulatory activities of Amphetamine.
CaroxazoneCaroxazone may increase the hypertensive activities of Amphetamine.
CelecoxibThe metabolism of Amphetamine can be decreased when combined with Celecoxib.
CeliprololThe risk or severity of adverse effects can be increased when Amphetamine is combined with Celiprolol.
CetirizineAmphetamine may decrease the sedative activities of Cetirizine.
ChloropyramineAmphetamine may decrease the sedative activities of Chloropyramine.
ChloroquineThe metabolism of Amphetamine can be decreased when combined with Chloroquine.
ChlorphenamineAmphetamine may decrease the sedative activities of Chlorphenamine.
ChlorphenoxamineAmphetamine may decrease the sedative activities of Chlorphenoxamine.
ChlorphentermineThe risk or severity of adverse effects can be increased when Amphetamine is combined with Chlorphentermine.
ChlorpromazineChlorpromazine may decrease the stimulatory activities of Amphetamine.
ChlorprothixeneChlorprothixene may decrease the stimulatory activities of Amphetamine.
CholecalciferolThe metabolism of Amphetamine can be decreased when combined with Cholecalciferol.
CimetidineAmphetamine may decrease the sedative activities of Cimetidine.
CimetidineThe metabolism of Amphetamine can be decreased when combined with Cimetidine.
CinacalcetThe metabolism of Amphetamine can be decreased when combined with Cinacalcet.
CinnarizineAmphetamine may decrease the sedative activities of Cinnarizine.
CitalopramThe metabolism of Amphetamine can be decreased when combined with Citalopram.
ClemastineAmphetamine may decrease the sedative activities of Clemastine.
ClemastineThe metabolism of Amphetamine can be decreased when combined with Clemastine.
ClenbuterolThe risk or severity of adverse effects can be increased when Amphetamine is combined with Clenbuterol.
ClobazamThe metabolism of Amphetamine can be decreased when combined with Clobazam.
ClomipramineClomipramine may increase the stimulatory activities of Amphetamine.
ClotrimazoleThe metabolism of Amphetamine can be decreased when combined with Clotrimazole.
ClozapineClozapine may decrease the stimulatory activities of Amphetamine.
CobicistatThe serum concentration of Amphetamine can be increased when it is combined with Cobicistat.
CocaineThe metabolism of Amphetamine can be decreased when combined with Cocaine.
CodeineAmphetamine may increase the analgesic activities of Codeine.
CyamemazineCyamemazine may decrease the stimulatory activities of Amphetamine.
CyclizineAmphetamine may decrease the sedative activities of Cyclizine.
CyclobenzaprineCyclobenzaprine may increase the stimulatory activities of Amphetamine.
CyproheptadineAmphetamine may decrease the sedative activities of Cyproheptadine.
DapiprazoleDapiprazole may decrease the stimulatory activities of Amphetamine.
DarifenacinThe metabolism of Amphetamine can be decreased when combined with Darifenacin.
DarunavirThe serum concentration of Amphetamine can be increased when it is combined with Darunavir.
DelavirdineThe metabolism of Amphetamine can be decreased when combined with Delavirdine.
DesipramineDesipramine may increase the stimulatory activities of Amphetamine.
DesloratadineAmphetamine may decrease the sedative activities of Desloratadine.
DexbrompheniramineAmphetamine may decrease the sedative activities of Dexbrompheniramine.
Dexchlorpheniramine maleateAmphetamine may decrease the sedative activities of Dexchlorpheniramine maleate.
DextromoramideAmphetamine may increase the analgesic activities of Dextromoramide.
DextropropoxypheneAmphetamine may increase the analgesic activities of Dextropropoxyphene.
DezocineAmphetamine may increase the analgesic activities of Dezocine.
DiclofenamideDiclofenamide may decrease the excretion rate of Amphetamine which could result in a lower serum level and potentially a reduction in efficacy.
DihydrocodeineAmphetamine may increase the analgesic activities of Dihydrocodeine.
DihydroetorphineAmphetamine may increase the analgesic activities of Dihydroetorphine.
DihydromorphineAmphetamine may increase the analgesic activities of Dihydromorphine.
DimenhydrinateAmphetamine may decrease the sedative activities of Dimenhydrinate.
DimetindeneAmphetamine may decrease the sedative activities of Dimetindene.
DimetotiazineAmphetamine may decrease the sedative activities of Dimetotiazine.
DiphenhydramineAmphetamine may decrease the sedative activities of Diphenhydramine.
DiphenhydramineThe metabolism of Amphetamine can be decreased when combined with Diphenhydramine.
DiphenoxylateAmphetamine may increase the analgesic activities of Diphenoxylate.
DobutamineThe risk or severity of adverse effects can be increased when Amphetamine is combined with Dobutamine.
DopamineThe risk or severity of adverse effects can be increased when Amphetamine is combined with Dopamine.
DosulepinDosulepin may increase the stimulatory activities of Amphetamine.
DoxepinAmphetamine may decrease the sedative activities of Doxepin.
DoxepinDoxepin may increase the stimulatory activities of Amphetamine.
DoxofyllineThe risk or severity of adverse effects can be increased when Amphetamine is combined with Doxofylline.
DoxylamineAmphetamine may decrease the sedative activities of Doxylamine.
DPDPEAmphetamine may increase the analgesic activities of DPDPE.
DronabinolDronabinol may increase the tachycardic activities of Amphetamine.
DronedaroneThe metabolism of Amphetamine can be decreased when combined with Dronedarone.
DroperidolDroperidol may decrease the stimulatory activities of Amphetamine.
DuloxetineThe metabolism of Amphetamine can be decreased when combined with Duloxetine.
EliglustatThe metabolism of Amphetamine can be decreased when combined with Eliglustat.
EmedastineAmphetamine may decrease the sedative activities of Emedastine.
EphedrineThe risk or severity of adverse effects can be increased when Amphetamine is combined with Ephedrine.
EpinastineAmphetamine may decrease the sedative activities of Epinastine.
EpinephrineThe risk or severity of adverse effects can be increased when Epinephrine is combined with Amphetamine.
EsmirtazapineAmphetamine may decrease the sedative activities of Esmirtazapine.
EsmirtazapineEsmirtazapine may increase the stimulatory activities of Amphetamine.
EsomeprazoleEsomeprazole can cause an increase in the absorption of Amphetamine resulting in an increased serum concentration and potentially a worsening of adverse effects.
EthopropazineAmphetamine may decrease the sedative activities of Ethopropazine.
EthosuximideThe therapeutic efficacy of Ethosuximide can be decreased when used in combination with Amphetamine.
EthoxzolamideEthoxzolamide may decrease the excretion rate of Amphetamine which could result in a lower serum level and potentially a reduction in efficacy.
EthylmorphineAmphetamine may increase the analgesic activities of Ethylmorphine.
EtilefrineThe risk or severity of adverse effects can be increased when Amphetamine is combined with Etilefrine.
EtorphineAmphetamine may increase the analgesic activities of Etorphine.
FamotidineAmphetamine may decrease the sedative activities of Famotidine.
FencamfamineFencamfamine may decrease the stimulatory activities of Amphetamine.
FenoterolThe risk or severity of adverse effects can be increased when Amphetamine is combined with Fenoterol.
FentanylAmphetamine may increase the analgesic activities of Fentanyl.
FesoterodineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Amphetamine.
FexofenadineAmphetamine may decrease the sedative activities of Fexofenadine.
FlunarizineAmphetamine may decrease the sedative activities of Flunarizine.
FluoxetineThe metabolism of Amphetamine can be decreased when combined with Fluoxetine.
FlupentixolFlupentixol may decrease the stimulatory activities of Amphetamine.
FluphenazineFluphenazine may decrease the stimulatory activities of Amphetamine.
FluspirileneFluspirilene may decrease the stimulatory activities of Amphetamine.
FluvoxamineThe metabolism of Amphetamine can be decreased when combined with Fluvoxamine.
FurazolidoneFurazolidone may increase the hypertensive activities of Amphetamine.
GuanethidineThe serum concentration of Amphetamine can be decreased when it is combined with Guanethidine.
HaloperidolHaloperidol may decrease the stimulatory activities of Amphetamine.
HeroinAmphetamine may increase the analgesic activities of Heroin.
HexamethylenetetramineThe serum concentration of Amphetamine can be decreased when it is combined with Hexamethylenetetramine.
HydracarbazineHydracarbazine may increase the hypertensive activities of Amphetamine.
HydrocodoneAmphetamine may increase the analgesic activities of Hydrocodone.
HydromorphoneAmphetamine may increase the analgesic activities of Hydromorphone.
Hydroxyamphetamine hydrobromideThe risk or severity of adverse effects can be increased when Amphetamine is combined with Hydroxyamphetamine hydrobromide.
HydroxyzineAmphetamine may decrease the sedative activities of Hydroxyzine.
IloperidoneIloperidone may decrease the stimulatory activities of Amphetamine.
ImipramineImipramine may increase the stimulatory activities of Amphetamine.
IndinavirThe metabolism of Amphetamine can be decreased when combined with Indinavir.
Ioflupane I-123Amphetamine may decrease effectiveness of Ioflupane I 123 as a diagnostic agent.
IproclozideIproclozide may increase the hypertensive activities of Amphetamine.
IproniazidIproniazid may increase the hypertensive activities of Amphetamine.
IsocarboxazidIsocarboxazid may increase the hypertensive activities of Amphetamine.
IsoniazidThe metabolism of Amphetamine can be decreased when combined with Isoniazid.
IsoprenalineThe risk or severity of adverse effects can be increased when Amphetamine is combined with Isoprenaline.
IsothipendylAmphetamine may decrease the sedative activities of Isothipendyl.
IsoxsuprineThe risk or severity of adverse effects can be increased when Amphetamine is combined with Isoxsuprine.
KetobemidoneAmphetamine may increase the analgesic activities of Ketobemidone.
KetoconazoleThe metabolism of Amphetamine can be decreased when combined with Ketoconazole.
KetotifenAmphetamine may decrease the sedative activities of Ketotifen.
L-Glutamic AcidThe serum concentration of Amphetamine can be decreased when it is combined with L-Glutamic Acid.
LabetalolThe risk or severity of adverse effects can be increased when Amphetamine is combined with Labetalol.
LansoprazoleLansoprazole can cause an increase in the absorption of Amphetamine resulting in an increased serum concentration and potentially a worsening of adverse effects.
LevocabastineAmphetamine may decrease the sedative activities of Levocabastine.
LevocetirizineAmphetamine may decrease the sedative activities of Levocetirizine.
Levomethadyl AcetateAmphetamine may increase the analgesic activities of Levomethadyl Acetate.
LevorphanolAmphetamine may increase the analgesic activities of Levorphanol.
LinezolidLinezolid may increase the hypertensive activities of Amphetamine.
LithiumLithium may decrease the stimulatory activities of Amphetamine.
LodoxamideAmphetamine may decrease the sedative activities of Lodoxamide.
LofentanilAmphetamine may increase the analgesic activities of Lofentanil.
LopinavirThe metabolism of Amphetamine can be decreased when combined with Lopinavir.
LoratadineAmphetamine may decrease the sedative activities of Loratadine.
LorcaserinThe metabolism of Amphetamine can be decreased when combined with Lorcaserin.
LoxapineLoxapine may decrease the stimulatory activities of Amphetamine.
LumefantrineThe metabolism of Amphetamine can be decreased when combined with Lumefantrine.
LurasidoneLurasidone may decrease the stimulatory activities of Amphetamine.
MagaldrateMagaldrate may decrease the excretion rate of Amphetamine which could result in a lower serum level and potentially a reduction in efficacy.
Magnesium carbonateMagnesium carbonate may decrease the excretion rate of Amphetamine which could result in a lower serum level and potentially a reduction in efficacy.
Magnesium hydroxideMagnesium hydroxide may decrease the excretion rate of Amphetamine which could result in a lower serum level and potentially a reduction in efficacy.
Magnesium oxideMagnesium oxide may decrease the excretion rate of Amphetamine which could result in a lower serum level and potentially a reduction in efficacy.
Magnesium TrisilicateMagnesium Trisilicate may decrease the excretion rate of Amphetamine which could result in a lower serum level and potentially a reduction in efficacy.
MebanazineMebanazine may increase the hypertensive activities of Amphetamine.
MeclizineAmphetamine may decrease the sedative activities of Meclizine.
MelperoneMelperone may decrease the stimulatory activities of Amphetamine.
MephentermineThe risk or severity of adverse effects can be increased when Amphetamine is combined with Mephentermine.
MepyramineAmphetamine may decrease the sedative activities of Mepyramine.
MequitazineAmphetamine may decrease the sedative activities of Mequitazine.
MesoridazineMesoridazine may decrease the stimulatory activities of Amphetamine.
MetaraminolThe risk or severity of adverse effects can be increased when Amphetamine is combined with Metaraminol.
MethadoneAmphetamine may increase the analgesic activities of Methadone.
MethadoneThe metabolism of Amphetamine can be decreased when combined with Methadone.
Methadyl AcetateAmphetamine may increase the analgesic activities of Methadyl Acetate.
MethamphetamineThe risk or severity of adverse effects can be increased when Amphetamine is combined with Methamphetamine.
MethapyrileneAmphetamine may decrease the sedative activities of Methapyrilene.
MethazolamideMethazolamide may decrease the excretion rate of Amphetamine which could result in a lower serum level and potentially a reduction in efficacy.
MethotrimeprazineMethotrimeprazine may decrease the stimulatory activities of Amphetamine.
MethoxamineThe risk or severity of adverse effects can be increased when Amphetamine is combined with Methoxamine.
Methylene blueMethylene blue may increase the hypertensive activities of Amphetamine.
MetiamideAmphetamine may decrease the sedative activities of Metiamide.
MetoprololThe serum concentration of Metoprolol can be increased when it is combined with Amphetamine.
MetoprololThe metabolism of Amphetamine can be decreased when combined with Metoprolol.
MianserinAmphetamine may decrease the sedative activities of Mianserin.
MidodrineThe risk or severity of adverse effects can be increased when Amphetamine is combined with Midodrine.
MinaprineMinaprine may increase the hypertensive activities of Amphetamine.
MirabegronThe metabolism of Amphetamine can be decreased when combined with Mirabegron.
MirtazapineAmphetamine may decrease the sedative activities of Mirtazapine.
MirtazapineMirtazapine may increase the stimulatory activities of Amphetamine.
MoclobemideMoclobemide may increase the hypertensive activities of Amphetamine.
MolindoneMolindone may decrease the stimulatory activities of Amphetamine.
MorphineAmphetamine may increase the analgesic activities of Morphine.
NabiloneNabilone may increase the tachycardic activities of Amphetamine.
NalbuphineAmphetamine may increase the analgesic activities of Nalbuphine.
NevirapineThe metabolism of Amphetamine can be decreased when combined with Nevirapine.
NialamideNialamide may increase the hypertensive activities of Amphetamine.
NicardipineThe metabolism of Amphetamine can be decreased when combined with Nicardipine.
NilotinibThe metabolism of Amphetamine can be decreased when combined with Nilotinib.
NizatidineAmphetamine may decrease the sedative activities of Nizatidine.
NorepinephrineThe risk or severity of adverse effects can be increased when Amphetamine is combined with Norepinephrine.
NormethadoneAmphetamine may increase the analgesic activities of Normethadone.
NortriptylineNortriptyline may increase the stimulatory activities of Amphetamine.
NylidrinThe risk or severity of adverse effects can be increased when Amphetamine is combined with Nylidrin.
OctamoxinOctamoxin may increase the hypertensive activities of Amphetamine.
OlanzapineOlanzapine may decrease the stimulatory activities of Amphetamine.
OlopatadineAmphetamine may decrease the sedative activities of Olopatadine.
OmeprazoleOmeprazole can cause an increase in the absorption of Amphetamine resulting in an increased serum concentration and potentially a worsening of adverse effects.
OndansetronOndansetron may decrease the stimulatory activities of Amphetamine.
OpiumAmphetamine may increase the analgesic activities of Opium.
OrciprenalineThe risk or severity of adverse effects can be increased when Amphetamine is combined with Orciprenaline.
OsanetantOsanetant may decrease the stimulatory activities of Amphetamine.
OxycodoneAmphetamine may increase the analgesic activities of Oxycodone.
OxymetazolineThe risk or severity of adverse effects can be increased when Amphetamine is combined with Oxymetazoline.
OxymorphoneAmphetamine may increase the analgesic activities of Oxymorphone.
PaliperidonePaliperidone may decrease the stimulatory activities of Amphetamine.
PanobinostatThe metabolism of Amphetamine can be decreased when combined with Panobinostat.
PantoprazolePantoprazole can cause an increase in the absorption of Amphetamine resulting in an increased serum concentration and potentially a worsening of adverse effects.
PargylinePargyline may increase the hypertensive activities of Amphetamine.
ParoxetineThe metabolism of Amphetamine can be decreased when combined with Paroxetine.
Peginterferon alfa-2bThe serum concentration of Amphetamine can be decreased when it is combined with Peginterferon alfa-2b.
PemirolastAmphetamine may decrease the sedative activities of Pemirolast.
PentazocineAmphetamine may increase the analgesic activities of Pentazocine.
PerospironePerospirone may decrease the stimulatory activities of Amphetamine.
PerphenazinePerphenazine may decrease the stimulatory activities of Amphetamine.
PethidineAmphetamine may increase the analgesic activities of Pethidine.
PhenelzinePhenelzine may increase the hypertensive activities of Amphetamine.
PhenindamineAmphetamine may decrease the sedative activities of Phenindamine.
PheniprazinePheniprazine may increase the hypertensive activities of Amphetamine.
PheniramineAmphetamine may decrease the sedative activities of Pheniramine.
PhenmetrazineThe risk or severity of adverse effects can be increased when Amphetamine is combined with Phenmetrazine.
PhenobarbitalThe serum concentration of Phenobarbital can be decreased when it is combined with Amphetamine.
PhenoxypropazinePhenoxypropazine may increase the hypertensive activities of Amphetamine.
PhentermineThe risk or severity of adverse effects can be increased when Amphetamine is combined with Phentermine.
PhenylephrineThe risk or severity of adverse effects can be increased when Amphetamine is combined with Phenylephrine.
PhenylpropanolamineThe risk or severity of adverse effects can be increased when Amphetamine is combined with Phenylpropanolamine.
PhenytoinThe serum concentration of Phenytoin can be decreased when it is combined with Amphetamine.
PimozidePimozide may decrease the stimulatory activities of Amphetamine.
PipamperonePipamperone may decrease the stimulatory activities of Amphetamine.
PipotiazinePipotiazine may decrease the stimulatory activities of Amphetamine.
PirlindolePirlindole may increase the hypertensive activities of Amphetamine.
PivhydrazinePivhydrazine may increase the hypertensive activities of Amphetamine.
ProcaterolThe risk or severity of adverse effects can be increased when Amphetamine is combined with Procaterol.
ProchlorperazineProchlorperazine may decrease the stimulatory activities of Amphetamine.
PromazinePromazine may decrease the stimulatory activities of Amphetamine.
PromethazineAmphetamine may decrease the sedative activities of Promethazine.
PropericiazinePropericiazine may decrease the stimulatory activities of Amphetamine.
ProtriptylineProtriptyline may increase the stimulatory activities of Amphetamine.
PseudoephedrineThe risk or severity of adverse effects can be increased when Amphetamine is combined with Pseudoephedrine.
QuetiapineQuetiapine may decrease the stimulatory activities of Amphetamine.
QuinidineThe metabolism of Amphetamine can be decreased when combined with Quinidine.
QuinineThe metabolism of Amphetamine can be decreased when combined with Quinine.
RabeprazoleRabeprazole can cause an increase in the absorption of Amphetamine resulting in an increased serum concentration and potentially a worsening of adverse effects.
RacepinephrineThe risk or severity of adverse effects can be increased when Amphetamine is combined with Racepinephrine.
RanitidineAmphetamine may decrease the sedative activities of Ranitidine.
RanolazineThe metabolism of Amphetamine can be decreased when combined with Ranolazine.
RasagilineRasagiline may increase the hypertensive activities of Amphetamine.
RemifentanilAmphetamine may increase the analgesic activities of Remifentanil.
RemoxiprideRemoxipride may decrease the stimulatory activities of Amphetamine.
ReserpineReserpine may decrease the stimulatory activities of Amphetamine.
RisperidoneRisperidone may decrease the stimulatory activities of Amphetamine.
RitodrineThe risk or severity of adverse effects can be increased when Amphetamine is combined with Ritodrine.
RitonavirThe metabolism of Amphetamine can be decreased when combined with Ritonavir.
RolapitantThe metabolism of Amphetamine can be decreased when combined with Rolapitant.
RopiniroleThe metabolism of Amphetamine can be decreased when combined with Ropinirole.
Roxatidine acetateAmphetamine may decrease the sedative activities of Roxatidine acetate.
SafrazineSafrazine may increase the hypertensive activities of Amphetamine.
SelegilineSelegiline may increase the hypertensive activities of Amphetamine.
SertindoleSertindole may decrease the stimulatory activities of Amphetamine.
SertralineThe metabolism of Amphetamine can be decreased when combined with Sertraline.
Spaglumic AcidAmphetamine may decrease the sedative activities of Spaglumic Acid.
StiripentolThe metabolism of Amphetamine can be decreased when combined with Stiripentol.
SufentanilAmphetamine may increase the analgesic activities of Sufentanil.
SulpirideSulpiride may decrease the stimulatory activities of Amphetamine.
SynephrineThe risk or severity of adverse effects can be increased when Amphetamine is combined with Synephrine.
TAK-390MRTAK-390MR can cause an increase in the absorption of Amphetamine resulting in an increased serum concentration and potentially a worsening of adverse effects.
TapentadolAmphetamine may increase the analgesic activities of Tapentadol.
Tedizolid PhosphateTedizolid Phosphate may increase the hypertensive activities of Amphetamine.
TerbinafineThe metabolism of Amphetamine can be decreased when combined with Terbinafine.
TerbutalineThe risk or severity of adverse effects can be increased when Amphetamine is combined with Terbutaline.
TerfenadineAmphetamine may decrease the sedative activities of Terfenadine.
TesmilifeneAmphetamine may decrease the sedative activities of Tesmilifene.
TetryzolineThe risk or severity of adverse effects can be increased when Amphetamine is combined with Tetryzoline.
ThioproperazineThioproperazine may decrease the stimulatory activities of Amphetamine.
ThioridazineThe serum concentration of Thioridazine can be increased when it is combined with Amphetamine.
ThioridazineThioridazine may decrease the stimulatory activities of Amphetamine.
ThiothixeneThiothixene may decrease the stimulatory activities of Amphetamine.
ThonzylamineAmphetamine may decrease the sedative activities of Thonzylamine.
TianeptineTianeptine may increase the stimulatory activities of Amphetamine.
TiclopidineThe metabolism of Amphetamine can be decreased when combined with Ticlopidine.
TipranavirThe metabolism of Amphetamine can be decreased when combined with Tipranavir.
ToloxatoneToloxatone may increase the hypertensive activities of Amphetamine.
TramadolAmphetamine may increase the analgesic activities of Tramadol.
TranilastAmphetamine may decrease the sedative activities of Tranilast.
Trans-2-PhenylcyclopropylamineTrans-2-Phenylcyclopropylamine may increase the hypertensive activities of Amphetamine.
TranylcypromineTranylcypromine may increase the hypertensive activities of Amphetamine.
TrifluoperazineTrifluoperazine may decrease the stimulatory activities of Amphetamine.
TriflupromazineTriflupromazine may decrease the stimulatory activities of Amphetamine.
TrimipramineTrimipramine may increase the stimulatory activities of Amphetamine.
TripelennamineAmphetamine may decrease the sedative activities of Tripelennamine.
TriprolidineAmphetamine may decrease the sedative activities of Triprolidine.
TyramineThe risk or severity of adverse effects can be increased when Amphetamine is combined with Tyramine.
VenlafaxineThe metabolism of Amphetamine can be decreased when combined with Venlafaxine.
Vitamin CThe serum concentration of Amphetamine can be decreased when it is combined with Vitamin C.
ZiprasidoneZiprasidone may decrease the stimulatory activities of Amphetamine.
ZotepineZotepine may decrease the stimulatory activities of Amphetamine.
ZuclopenthixolZuclopenthixol may decrease the stimulatory activities of Amphetamine.
Food InteractionsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Monoamine transmembrane transporter activity
Specific Function:
Involved in the ATP-dependent vesicular transport of biogenic amine neurotransmitters. Pumps cytosolic monoamines including dopamine, norepinephrine, serotonin, and histamine into synaptic vesicles. Requisite for vesicular amine storage prior to secretion via exocytosis.
Gene Name:
SLC18A2
Uniprot ID:
Q05940
Molecular Weight:
55712.075 Da
References
  1. Sulzer D, Sonders MS, Poulsen NW, Galli A: Mechanisms of neurotransmitter release by amphetamines: a review. Prog Neurobiol. 2005 Apr;75(6):406-33. [PubMed:15955613 ]
  2. Sulzer D, Chen TK, Lau YY, Kristensen H, Rayport S, Ewing A: Amphetamine redistributes dopamine from synaptic vesicles to the cytosol and promotes reverse transport. J Neurosci. 1995 May;15(5 Pt 2):4102-8. [PubMed:7751968 ]
  3. Teng L, Crooks PA, Dwoskin LP: Lobeline displaces [3H]dihydrotetrabenazine binding and releases [3H]dopamine from rat striatal synaptic vesicles: comparison with d-amphetamine. J Neurochem. 1998 Jul;71(1):258-65. [PubMed:9648873 ]
  4. Eiden LE, Weihe E: VMAT2: a dynamic regulator of brain monoaminergic neuronal function interacting with drugs of abuse. Ann N Y Acad Sci. 2011 Jan;1216:86-98. doi: 10.1111/j.1749-6632.2010.05906.x. [PubMed:21272013 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
negative modulator
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. Lott DC, Kim SJ, Cook EH Jr, de Wit H: Dopamine transporter gene associated with diminished subjective response to amphetamine. Neuropsychopharmacology. 2005 Mar;30(3):602-9. [PubMed:15602501 ]
  2. Fone KC, Nutt DJ: Stimulants: use and abuse in the treatment of attention deficit hyperactivity disorder. Curr Opin Pharmacol. 2005 Feb;5(1):87-93. [PubMed:15661631 ]
  3. Miller GM, Verrico CD, Jassen A, Konar M, Yang H, Panas H, Bahn M, Johnson R, Madras BK: Primate trace amine receptor 1 modulation by the dopamine transporter. J Pharmacol Exp Ther. 2005 Jun;313(3):983-94. Epub 2005 Mar 11. [PubMed:15764732 ]
  4. Garcia BG, Wei Y, Moron JA, Lin RZ, Javitch JA, Galli A: Akt is essential for insulin modulation of amphetamine-induced human dopamine transporter cell-surface redistribution. Mol Pharmacol. 2005 Jul;68(1):102-9. Epub 2005 Mar 28. [PubMed:15795321 ]
  5. Madras BK, Miller GM, Fischman AJ: The dopamine transporter and attention-deficit/hyperactivity disorder. Biol Psychiatry. 2005 Jun 1;57(11):1397-409. Epub 2005 Jan 5. [PubMed:15950014 ]
  6. Kahlig KM, Binda F, Khoshbouei H, Blakely RD, McMahon DG, Javitch JA, Galli A: Amphetamine induces dopamine efflux through a dopamine transporter channel. Proc Natl Acad Sci U S A. 2005 Mar 1;102(9):3495-500. Epub 2005 Feb 22. [PubMed:15728379 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
agonist
General Function:
Not Available
Specific Function:
Satiety factor closely associated with the actions of leptin and neuropeptide y; this anorectic peptide inhibits both normal and starvation-induced feeding and completely blocks the feeding response induced by neuropeptide Y and regulated by leptin in the hypothalamus. It promotes neuronal development and survival in vitro.
Gene Name:
CARTPT
Uniprot ID:
Q16568
Molecular Weight:
12828.975 Da
References
  1. Loos RJ, Rankinen T, Tremblay A, Perusse L, Chagnon Y, Bouchard C: Melanocortin-4 receptor gene and physical activity in the Quebec Family Study. Int J Obes (Lond). 2005 Apr;29(4):420-8. [PubMed:15597110 ]
  2. McAlister ED, Van Vugt DA: Effect of leptin administration versus re-feeding on hypothalamic neuropeptide gene expression in fasted male rats. Can J Physiol Pharmacol. 2004 Dec;82(12):1128-34. [PubMed:15644956 ]
  3. Muhlhausler BS, Adam CL, Marrocco EM, Findlay PA, Roberts CT, McFarlane JR, Kauter KG, McMillen IC: Impact of glucose infusion on the structural and functional characteristics of adipose tissue and on hypothalamic gene expression for appetite regulatory neuropeptides in the sheep fetus during late gestation. J Physiol. 2005 May 15;565(Pt 1):185-95. Epub 2005 Jan 20. [PubMed:15661821 ]
  4. Scruggs P, Lai CC, Scruggs JE, Dun NJ: Cocaine- and amphetamine-regulated transcript peptide potentiates spinal glutamatergic sympathoexcitation in anesthetized rats. Regul Pept. 2005 Apr 15;127(1-3):79-85. [PubMed:15680473 ]
  5. Oliveira VX Jr, Fazio MA, Miranda MT, da Silva JM, Bittencourt JC, Elias CF, Miranda A: Leptin fragments induce Fos immunoreactivity in rat hypothalamus. Regul Pept. 2005 Apr 15;127(1-3):123-32. [PubMed:15680478 ]
  6. Vicentic A, Lakatos A, Jones D: The CART receptors: background and recent advances. Peptides. 2006 Aug;27(8):1934-7. Epub 2006 May 19. [PubMed:16713658 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
agonist
General Function:
Trace-amine receptor activity
Specific Function:
Receptor for trace amines, including beta-phenylethylamine (b-PEA), p-tyramine (p-TYR), octopamine and tryptamine, with highest affinity for b-PEA and p-TYR. Unresponsive to classical biogenic amines, such as epinephrine and histamine and only partially activated by dopamine and serotonine. Trace amines are biogenic amines present in very low levels in mammalian tissues. Although some trace ami...
Gene Name:
TAAR1
Uniprot ID:
Q96RJ0
Molecular Weight:
39091.34 Da
References
  1. Reese EA, Bunzow JR, Arttamangkul S, Sonders MS, Grandy DK: Trace amine-associated receptor 1 displays species-dependent stereoselectivity for isomers of methamphetamine, amphetamine, and para-hydroxyamphetamine. J Pharmacol Exp Ther. 2007 Apr;321(1):178-86. Epub 2007 Jan 11. [PubMed:17218486 ]
  2. Xie Z, Westmoreland SV, Bahn ME, Chen GL, Yang H, Vallender EJ, Yao WD, Madras BK, Miller GM: Rhesus monkey trace amine-associated receptor 1 signaling: enhancement by monoamine transporters and attenuation by the D2 autoreceptor in vitro. J Pharmacol Exp Ther. 2007 Apr;321(1):116-27. Epub 2007 Jan 18. [PubMed:17234900 ]
  3. Wolinsky TD, Swanson CJ, Smith KE, Zhong H, Borowsky B, Seeman P, Branchek T, Gerald CP: The Trace Amine 1 receptor knockout mouse: an animal model with relevance to schizophrenia. Genes Brain Behav. 2007 Oct;6(7):628-39. Epub 2006 Dec 21. [PubMed:17212650 ]
  4. Xie Z, Miller GM: Trace amine-associated receptor 1 is a modulator of the dopamine transporter. J Pharmacol Exp Ther. 2007 Apr;321(1):128-36. Epub 2007 Jan 18. [PubMed:17234899 ]
  5. Miller GM, Verrico CD, Jassen A, Konar M, Yang H, Panas H, Bahn M, Johnson R, Madras BK: Primate trace amine receptor 1 modulation by the dopamine transporter. J Pharmacol Exp Ther. 2005 Jun;313(3):983-94. Epub 2005 Mar 11. [PubMed:15764732 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
stimulator
General Function:
Norepinephrine:sodium symporter activity
Specific Function:
Amine transporter. Terminates the action of noradrenaline by its high affinity sodium-dependent reuptake into presynaptic terminals.
Gene Name:
SLC6A2
Uniprot ID:
P23975
Molecular Weight:
69331.42 Da
References
  1. Rothman RB, Vu N, Partilla JS, Roth BL, Hufeisen SJ, Compton-Toth BA, Birkes J, Young R, Glennon RA: In vitro characterization of ephedrine-related stereoisomers at biogenic amine transporters and the receptorome reveals selective actions as norepinephrine transporter substrates. J Pharmacol Exp Ther. 2003 Oct;307(1):138-45. Epub 2003 Sep 3. [PubMed:12954796 ]
  2. Wall SC, Gu H, Rudnick G: Biogenic amine flux mediated by cloned transporters stably expressed in cultured cell lines: amphetamine specificity for inhibition and efflux. Mol Pharmacol. 1995 Mar;47(3):544-50. [PubMed:7700252 ]
Kind
Protein group
Organism
Human
Pharmacological action
unknown
Actions
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.
Components:
NameUniProt IDDetails
Alpha-1A adrenergic receptorP35348 Details
Alpha-1B adrenergic receptorP35368 Details
Alpha-1D adrenergic receptorP25100 Details
Alpha-2A adrenergic receptorP08913 Details
Alpha-2B adrenergic receptorP18089 Details
Alpha-2C adrenergic receptorP18825 Details
References
  1. Leibowitz SF: Reciprocal hunger-regulating circuits involving alpha- and beta-adrenergic receptors located, respectively, in the ventromedial and lateral hypothalamus. Proc Natl Acad Sci U S A. 1970 Oct;67(2):1063-70. [PubMed:4399738 ]
  2. Reisine TD, U'Prichard DC, Wiech NL, Ursillo RC, Yamamura HI: Effects of combined administration of amphetamine and iprindole on brain adrenergic receptors. Brain Res. 1980 Apr 28;188(2):587-92. [PubMed:6245760 ]
Kind
Protein group
Organism
Human
Pharmacological action
unknown
Actions
agonist
General Function:
Receptor signaling protein activity
Specific Function:
Beta-adrenergic receptors mediate the catecholamine-induced activation of adenylate cyclase through the action of G proteins. This receptor binds epinephrine and norepinephrine with approximately equal affinity. Mediates Ras activation through G(s)-alpha- and cAMP-mediated signaling.
Components:
NameUniProt IDDetails
Beta-1 adrenergic receptorP08588 Details
Beta-2 adrenergic receptorP07550 Details
Beta-3 adrenergic receptorP13945 Details
References
  1. Leibowitz SF: Reciprocal hunger-regulating circuits involving alpha- and beta-adrenergic receptors located, respectively, in the ventromedial and lateral hypothalamus. Proc Natl Acad Sci U S A. 1970 Oct;67(2):1063-70. [PubMed:4399738 ]
  2. Reisine TD, U'Prichard DC, Wiech NL, Ursillo RC, Yamamura HI: Effects of combined administration of amphetamine and iprindole on brain adrenergic receptors. Brain Res. 1980 Apr 28;188(2):587-92. [PubMed:6245760 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
binder
General Function:
Potassium channel regulator activity
Specific Function:
Dopamine receptor whose activity is mediated by G proteins which inhibit adenylyl cyclase.
Gene Name:
DRD2
Uniprot ID:
P14416
Molecular Weight:
50618.91 Da
References
  1. Innis RB, Malison RT, al-Tikriti M, Hoffer PB, Sybirska EH, Seibyl JP, Zoghbi SS, Baldwin RM, Laruelle M, Smith EO, et al.: Amphetamine-stimulated dopamine release competes in vivo for [123I]IBZM binding to the D2 receptor in nonhuman primates. Synapse. 1992 Mar;10(3):177-84. [PubMed:1532675 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Primary amine oxidase activity
Specific Function:
Catalyzes the oxidative deamination of biogenic and xenobiotic amines and has important functions in the metabolism of neuroactive and vasoactive amines in the central nervous system and peripheral tissues. MAOB preferentially degrades benzylamine and phenylethylamine.
Gene Name:
MAOB
Uniprot ID:
P27338
Molecular Weight:
58762.475 Da
References
  1. Clarke DE, Lyles GA, Callingham BA: A comparison of cardiac and vascular clorgyline-resistant amine oxidase and monoamine oxidase. Inhibition by amphetamine, mexiletine and other drugs. Biochem Pharmacol. 1982 Jan 1;31(1):27-35. [PubMed:7059347 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
binder
General Function:
Serotonin:sodium symporter activity
Specific Function:
Serotonin transporter whose primary function in the central nervous system involves the regulation of serotonergic signaling via transport of serotonin molecules from the synaptic cleft back into the pre-synaptic terminal for re-utilization. Plays a key role in mediating regulation of the availability of serotonin to other receptors of serotonergic systems. Terminates the action of serotonin an...
Gene Name:
SLC6A4
Uniprot ID:
P31645
Molecular Weight:
70324.165 Da
References
  1. Fleckenstein AE, Volz TJ, Riddle EL, Gibb JW, Hanson GR: New insights into the mechanism of action of amphetamines. Annu Rev Pharmacol Toxicol. 2007;47:681-98. [PubMed:17209801 ]
Kind
Protein group
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Serotonin binding
Specific Function:
Catalyzes the oxidative deamination of biogenic and xenobiotic amines and has important functions in the metabolism of neuroactive and vasoactive amines in the central nervous system and peripheral tissues. MAOA preferentially oxidizes biogenic amines such as 5-hydroxytryptamine (5-HT), norepinephrine and epinephrine.
Components:
NameUniProt IDDetails
Amine oxidase [flavin-containing] AP21397 Details
Amine oxidase [flavin-containing] BP27338 Details
References
  1. Heal DJ, Smith SL, Gosden J, Nutt DJ: Amphetamine, past and present--a pharmacological and clinical perspective. J Psychopharmacol. 2013 Jun;27(6):479-96. doi: 10.1177/0269881113482532. Epub 2013 Mar 28. [PubMed:23539642 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
General Function:
Not Available
Specific Function:
Not Available
Gene Name:
Not Available
Uniprot ID:
Q99870
Molecular Weight:
Not Available
References
  1. Heal DJ, Smith SL, Gosden J, Nutt DJ: Amphetamine, past and present--a pharmacological and clinical perspective. J Psychopharmacol. 2013 Jun;27(6):479-96. doi: 10.1177/0269881113482532. Epub 2013 Mar 28. [PubMed:23539642 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
General Function:
Steroid hydroxylase activity
Specific Function:
Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic antidepressants.
Gene Name:
CYP2D6
Uniprot ID:
P10635
Molecular Weight:
55768.94 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. Wu D, Otton SV, Inaba T, Kalow W, Sellers EM: Interactions of amphetamine analogs with human liver CYP2D6. Biochem Pharmacol. 1997 Jun 1;53(11):1605-12. [PubMed:9264312 ]
  3. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
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. Constitutes the major nicotine C-oxidase. Acts as a 1,4-cineole 2-exo-monooxygenase. Possesses low phenacetin O-deethylation activity.
Gene Name:
CYP2A6
Uniprot ID:
P11509
Molecular Weight:
56501.005 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. Siu EC, Tyndale RF: Selegiline is a mechanism-based inactivator of CYP2A6 inhibiting nicotine metabolism in humans and mice. J Pharmacol Exp Ther. 2008 Mar;324(3):992-9. Epub 2007 Dec 7. [PubMed:18065502 ]

Transporters

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Toxin transporter activity
Specific Function:
Mediates potential-dependent transport of a variety of organic cations. May play a significant role in the disposition of cationic neurotoxins and neurotransmitters in the brain.
Gene Name:
SLC22A3
Uniprot ID:
O75751
Molecular Weight:
61279.485 Da
References
  1. Wu X, Kekuda R, Huang W, Fei YJ, Leibach FH, Chen J, Conway SJ, Ganapathy V: Identity of the organic cation transporter OCT3 as the extraneuronal monoamine transporter (uptake2) and evidence for the expression of the transporter in the brain. J Biol Chem. 1998 Dec 4;273(49):32776-86. [PubMed:9830022 ]
  2. Zhu HJ, Appel DI, Grundemann D, Markowitz JS: Interaction of organic cation transporter 3 (SLC22A3) and amphetamine. J Neurochem. 2010 Jul;114(1):142-9. doi: 10.1111/j.1471-4159.2010.06738.x. Epub 2010 Apr 6. [PubMed:20402963 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Symporter activity
Specific Function:
Sodium-ion dependent, high affinity carnitine transporter. Involved in the active cellular uptake of carnitine. Transports one sodium ion with one molecule of carnitine. Also transports organic cations such as tetraethylammonium (TEA) without the involvement of sodium. Also relative uptake activity ratio of carnitine to TEA is 11.3.
Gene Name:
SLC22A5
Uniprot ID:
O76082
Molecular Weight:
62751.08 Da
References
  1. Wu X, Prasad PD, Leibach FH, Ganapathy V: cDNA sequence, transport function, and genomic organization of human OCTN2, a new member of the organic cation transporter family. Biochem Biophys Res Commun. 1998 May 29;246(3):589-95. [PubMed:9618255 ]
  2. Wu X, Huang W, Prasad PD, Seth P, Rajan DP, Leibach FH, Chen J, Conway SJ, Ganapathy V: Functional characteristics and tissue distribution pattern of organic cation transporter 2 (OCTN2), an organic cation/carnitine transporter. J Pharmacol Exp Ther. 1999 Sep;290(3):1482-92. [PubMed:10454528 ]
  3. Rytting E, Audus KL: Novel organic cation transporter 2-mediated carnitine uptake in placental choriocarcinoma (BeWo) cells. J Pharmacol Exp Ther. 2005 Jan;312(1):192-8. Epub 2004 Aug 17. [PubMed:15316089 ]
Comments
comments powered by Disqus
Drug created on June 13, 2005 07:24 / Updated on September 24, 2016 03:31