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Identification
NameBenzphetamine
Accession NumberDB00865  (APRD00759)
TypeSmall Molecule
GroupsApproved, Illicit
Description

A sympathomimetic agent with properties similar to dextroamphetamine. It is used in the treatment of obesity. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1222)

Structure
Thumb
Synonyms
SynonymLanguageCode
(+)-benzphetamineNot AvailableNot Available
(+)-N-Benzyl-N,alpha-dimethylphenethylamineNot AvailableNot Available
(+)-N-benzyl-N,α-dimethylphenethylamineNot AvailableNot Available
(+)-N,alpha-Dimethyl-N-(phenylmethyl)-benzeneethanamineNot AvailableNot Available
(+)-N,α-dimethyl-N-(phenylmethyl)-benzeneethanamineNot AvailableNot Available
(AlphaS)-N,alpha-dimethylphenethylamineNot AvailableNot Available
(S)-(+)-benzphetamineNot AvailableNot Available
(S)-(+)-N-Benzyl-N,alpha-dimethylphenethylamineNot AvailableNot Available
(S)-(+)-N-benzyl-N,α-dimethylphenethylamineNot AvailableNot Available
(S)-benzphetamineNot AvailableNot Available
BenzaphetamineNot AvailableNot Available
BenzfetaminaNot AvailableNot Available
BenzfetamineNot AvailableINN
BenzfetaminumNot AvailableNot Available
BenzphetamineNot AvailableNot Available
BenzylamphetamineNot AvailableNot Available
D-N-Methyl-N-benzyl-beta-phenylisopropylamineNot AvailableNot Available
d-N-methyl-N-benzyl-β-phenylisopropylamineNot AvailableNot Available
N-methyl-1-phenyl-N-(phenylmethyl)propan-2-amineNot AvailableNot Available
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Didrextablet50 mgoralPharmacia and Upjohn Company1960-10-26Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Didrextablet50 mgoralA S Medication Solutions Llc1960-10-26Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Didrextablet50 mgoralA S Medication Solutions Llc1960-10-26Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Didrextablet50 mgoralPd Rx Pharmaceuticals, Inc.1960-10-26Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Benzphetamine Hydrochloridetablet50 mgoralGlobal Pharmaceuticals, Division of Impax Laboratories Inc.2008-12-01Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Benzphetamine Hydrochloridetablet50 mgoralC.O. Truxton, Inc.2011-11-01Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Benzphetamine Hydrochloridetablet, coated50 mgoralPaddock Laboratories, Inc.2007-05-01Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Benzphetamine Hydrochloridetablet50 mgoralKvk Tech, Inc2010-07-21Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Benzphetamine Hydrochloridetablet50 mgoralApotheca Inc.2009-12-09Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Benzphetamine Hydrochloridetablet, film coated50 mgoralHeritage Pharmaceuticals Inc.2012-10-19Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Benzphetamine Hydrochloridetablet50 mgoralAidarex Pharmaceuticals LLC2010-07-21Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Benzphetamine Hydrochloridetablet50 mgoralPd Rx Pharmaceuticals, Inc.2011-11-01Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Benzphetamine Hydrochloridetablet50 mgoralPd Rx Pharmaceuticals, Inc.2010-07-21Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Benzphetamine Hydrochloridetablet50 mgoralSolco Healthcare US LLC2011-08-01Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Benzphetamine Hydrochloridetablet50 mgoralMikart, Inc.2011-11-01Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Benzphetamine Hydrochloridetablet50 mgoralA S Medication Solutions Llc2010-07-21Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Recedetablet25 mgoralPoly Pharmaceuticals, Inc.2012-02-01Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Benzphetamine Hydrochloridetablet50 mgoralA S Medication Solutions Llc2010-07-21Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Benzphetamine Hydrochloridetablet50 mgoralPd Rx Pharmaceuticals, Inc.2009-12-09Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Benzphetamine Hydrochloridetablet50 mgoralbryant ranch prepack2010-02-01Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Benzphetamine Hydrochloridetablet50 mgoralBoca Pharmacal, LLC2010-09-07Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Regimextablet25 mgoralWraser Pharmaceuticals2013-02-01Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Over the Counter ProductsNot Available
International BrandsNot Available
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Benzphetamine Hydrochloride
Thumb
  • InChI Key: ANFSNXAXVLRZCG-UHFFFAOYNA-N
  • Monoisotopic Mass: 275.144077416
  • Average Mass: 275.816
DBSALT000832
Categories
CAS number156-08-1
WeightAverage: 239.3553
Monoisotopic: 239.167399677
Chemical FormulaC17H21N
InChI KeyYXKTVDFXDRQTKV-HNNXBMFYSA-N
InChI
InChI=1S/C17H21N/c1-15(13-16-9-5-3-6-10-16)18(2)14-17-11-7-4-8-12-17/h3-12,15H,13-14H2,1-2H3/t15-/m0/s1
IUPAC Name
benzyl(methyl)[(2S)-1-phenylpropan-2-yl]amine
SMILES
C[C@@H](CC1=CC=CC=C1)N(C)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
  • Phenylmethylamine
  • Benzylamine
  • Aralkylamine
  • Tertiary aliphatic amine
  • Tertiary amine
  • Hydrocarbon derivative
  • Organonitrogen compound
  • Amine
  • Aromatic homomonocyclic compound
Molecular FrameworkAromatic homomonocyclic compounds
External Descriptors
Pharmacology
IndicationFor the management of exogenous obesity as a short term adjunct (a few weeks) in a regimen of weight reduction based on caloric restriction
PharmacodynamicsBenzphetamine, a phenylalkylamin, is related to amphetamine both chemically and pharmacologically. It is an anorectic agent indicated in the management of exogenous obesity as a short term adjunct (a few weeks) in a regimen of weight reduction based on caloric restriction. Benzphetamine is a sympathomimetic amine with pharmacologic activity similar to the prototype drugs of this class used in obesity, the amphetamines. Actions include central nervous system stimulation and elevation of blood pressure. Tachyphylaxis and tolerance have been demonstrated with all drugs of this class in which these phenomena have been looked for.
Mechanism of actionAlthough the mechanism of action of the sympathomimetic appetite suppressants in the treatment of obesity is not fully known, these medications have pharmacological effects similar to those of amphetamines. Amphetamine and related sympathomimetic medications (such as benzphetamine) are thought to stimulate the release of norepinephrine and/or dopamine from storage sites in nerve terminals in the lateral hypothalamic feeding center, thereby producing a decrease in appetite. This release is mediated by the binding of benzphetamine to centrally located adrenergic receptors.
AbsorptionReadily absorbed from the gastro-intestinal tract and buccal mucosa. It Is resistant to metabolism by monoamine oxidase.
Volume of distributionNot Available
Protein binding75-99%
Metabolism

Hepatic. Benzphetamine's metabolites include amphetamine and methamphetamine.

SubstrateEnzymesProduct
Benzphetamine
Not Available
AmphetamineDetails
Benzphetamine
Not Available
MethamphetamineDetails
Route of eliminationNot Available
Half life16 to 31 hours
ClearanceNot Available
ToxicityLD50=160 mg/kg (orally in rats). Acute overdosage may result in restlessness, tremor, tachypnea, confusion, assaultiveness, and panic states.
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+0.9933
Blood Brain Barrier+0.9864
Caco-2 permeable+0.8815
P-glycoprotein substrateSubstrate0.541
P-glycoprotein inhibitor INon-inhibitor0.8803
P-glycoprotein inhibitor IINon-inhibitor0.9437
Renal organic cation transporterInhibitor0.7013
CYP450 2C9 substrateNon-substrate0.769
CYP450 2D6 substrateNon-substrate0.588
CYP450 3A4 substrateNon-substrate0.5135
CYP450 1A2 substrateInhibitor0.8684
CYP450 2C9 substrateNon-inhibitor0.9146
CYP450 2D6 substrateInhibitor0.539
CYP450 2C19 substrateNon-inhibitor0.5997
CYP450 3A4 substrateNon-inhibitor0.8789
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.8047
Ames testNon AMES toxic0.888
CarcinogenicityNon-carcinogens0.6584
BiodegradationNot ready biodegradable0.9825
Rat acute toxicity3.1442 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.8779
hERG inhibition (predictor II)Non-inhibitor0.5331
Pharmacoeconomics
Manufacturers
  • Corepharma llc
  • Impax laboratories inc
  • Kvk tech inc
  • Paddock laboratories inc
  • Tedor pharma inc
  • Tyco healthcare mallinckrodt
  • Pharmacia and upjohn co
Packagers
Dosage forms
FormRouteStrength
Tabletoral25 mg
Tabletoral50 mg
Tablet, coatedoral50 mg
Tablet, film coatedoral50 mg
Prices
Unit descriptionCostUnit
Didrex 50 mg tablet1.71USD tablet
Benzphetamine hcl 50 mg tablet1.43USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point129-130Heinzelman, R.V. and Aspergren, B.D.; US. Patent 2,789,138; April 16,1957; assigned to The Upjohn Company.
water solubilityReadily solubleNot Available
logP4.1Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.0233 mg/mLALOGPS
logP3.72ALOGPS
logP4.34ChemAxon
logS-4ALOGPS
pKa (Strongest Basic)9.8ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count1ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area3.24 Å2ChemAxon
Rotatable Bond Count5ChemAxon
Refractivity78.39 m3·mol-1ChemAxon
Polarizability29.03 Å3ChemAxon
Number of Rings2ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Download (8.86 KB)
SpectraNot Available
References
Synthesis Reference

Dennis J. Kalota, Keith G. Tomazi, “Crystallization Method for Benzphetamine.” U.S. Patent US20080262268, issued October 23, 2008.

US20080262268
General ReferenceNot Available
External Links
ATC CodesNot Available
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelNot Available
MSDSDownload (16.6 KB)
Interactions
Drug Interactions
Drug
AcebutololMay enhance the adverse/toxic effect of other Sympathomimetics.
AcepromazineMay diminish the stimulatory effect of Amphetamines.
AcetazolamideMay decrease the excretion of Amphetamines. Exceptions: Brinzolamide; Dorzolamide.
AcetophenazineMay diminish the stimulatory effect of Amphetamines.
Aluminum hydroxideMay decrease the excretion of Amphetamines.
AminophyllineMay enhance the adverse/toxic effect of other Sympathomimetics.
AmisulprideMay diminish the stimulatory effect of Amphetamines.
Ammonium chlorideMay decrease the serum concentration of Amphetamines. This effect is likely due to an enhanced excretion of amphetamines in the urine.
AmphetamineMay enhance the adverse/toxic effect of other Sympathomimetics.
AprepitantMay increase the serum concentration of CYP3A4 Substrates.
ArformoterolMay enhance the adverse/toxic effect of other Sympathomimetics.
AripiprazoleMay diminish the stimulatory effect of Amphetamines.
armodafinilMay enhance the adverse/toxic effect of other Sympathomimetics.
ArticaineMay enhance the adverse/toxic effect of other Sympathomimetics.
AtomoxetineAtoMOXetine may enhance the hypertensive effect of Sympathomimetics. AtoMOXetine may enhance the tachycardic effect of Sympathomimetics.
BenzquinamideMay diminish the stimulatory effect of Amphetamines.
BosentanMay decrease the serum concentration of CYP3A4 Substrates.
CaffeineMay enhance the adverse/toxic effect of other Sympathomimetics.
Calcium carbonateMay decrease the excretion of Amphetamines.
CarphenazineMay diminish the stimulatory effect of Amphetamines.
ChlormezanoneMay diminish the stimulatory effect of Amphetamines.
ChlorphentermineMay enhance the adverse/toxic effect of other Sympathomimetics.
ChlorpromazineMay diminish the stimulatory effect of Amphetamines.
ChlorprothixeneMay diminish the stimulatory effect of Amphetamines.
ClenbuterolMay enhance the adverse/toxic effect of other Sympathomimetics.
ClozapineMay diminish the stimulatory effect of Amphetamines.
CocaineMay enhance the adverse/toxic effect of other Sympathomimetics.
ConivaptanMay increase the serum concentration of CYP3A4 Substrates.
DabrafenibMay decrease the serum concentration of CYP3A4 Substrates.
DasatinibMay increase the serum concentration of CYP3A4 Substrates.
DeferasiroxMay decrease the serum concentration of CYP3A4 Substrates.
DexmethylphenidateMay enhance the adverse/toxic effect of other Sympathomimetics.
DextroamphetamineMay enhance the adverse/toxic effect of other Sympathomimetics.
DiclofenamideMay decrease the excretion of Amphetamines. Exceptions: Brinzolamide; Dorzolamide.
DiethylpropionMay enhance the adverse/toxic effect of other Sympathomimetics.
DihydrocodeineMay enhance the adverse/toxic effect of other Sympathomimetics.
DipivefrinMay enhance the adverse/toxic effect of other Sympathomimetics.
DobutamineMay enhance the adverse/toxic effect of other Sympathomimetics.
DopamineMay enhance the adverse/toxic effect of other Sympathomimetics.
DoxapramMay enhance the adverse/toxic effect of other Sympathomimetics.
DronabinolCannabinoid-Containing Products may enhance the tachycardic effect of Sympathomimetics.
DroperidolMay diminish the stimulatory effect of Amphetamines.
EpinephrineMay enhance the adverse/toxic effect of other Sympathomimetics.
EthosuximideAmphetamines may diminish the therapeutic effect of Ethosuximide. Amphetamines may decrease the serum concentration of Ethosuximide.
EthoxzolamideMay decrease the excretion of Amphetamines. Exceptions: Brinzolamide; Dorzolamide.
FencamfamineMay diminish the stimulatory effect of Amphetamines.
FenoterolMay enhance the adverse/toxic effect of other Sympathomimetics.
FlupentixolMay diminish the stimulatory effect of Amphetamines.
FluphenazineMay diminish the stimulatory effect of Amphetamines.
FluspirileneMay diminish the stimulatory effect of Amphetamines.
Fluticasone furoateMay enhance the adverse/toxic effect of other Sympathomimetics.
FormoterolMay enhance the adverse/toxic effect of other Sympathomimetics.
FosaprepitantMay increase the serum concentration of CYP3A4 Substrates.
HaloperidolMay diminish the stimulatory effect of Amphetamines.
IndacaterolMay enhance the adverse/toxic effect of other Sympathomimetics.
IobenguaneMay diminish the therapeutic effect of Iobenguane I 123.
Ioflupane I 123Amphetamines may diminish the diagnostic effect of Ioflupane I 123.
Ipratropium bromideMay enhance the adverse/toxic effect of other Sympathomimetics.
IsomethepteneMay enhance the adverse/toxic effect of other Sympathomimetics.
IsoprenalineMay enhance the adverse/toxic effect of other Sympathomimetics.
IvacaftorMay increase the serum concentration of CYP3A4 Substrates.
LabetalolMay enhance the adverse/toxic effect of other Sympathomimetics.
LevonordefrinMay enhance the adverse/toxic effect of other Sympathomimetics.
LinezolidLinezolid may enhance the hypertensive effect of Sympathomimetics.
LisdexamfetamineMay enhance the adverse/toxic effect of other Sympathomimetics.
LithiumMay diminish the stimulatory effect of Amphetamines.
LoxapineMay diminish the stimulatory effect of Amphetamines.
LULICONAZOLEMay increase the serum concentration of CYP3A4 Substrates.
Magnesium oxideMay decrease the excretion of Amphetamines.
MephentermineMay enhance the adverse/toxic effect of other Sympathomimetics.
MesoridazineMay diminish the stimulatory effect of Amphetamines.
MetaraminolMay enhance the adverse/toxic effect of other Sympathomimetics.
MethamphetamineMay enhance the adverse/toxic effect of other Sympathomimetics.
MethotrimeprazineMay diminish the stimulatory effect of Amphetamines.
MethoxamineMay enhance the adverse/toxic effect of other Sympathomimetics.
MethylphenidateMay enhance the adverse/toxic effect of other Sympathomimetics.
MidodrineMay enhance the adverse/toxic effect of other Sympathomimetics.
MifepristoneMay increase the serum concentration of CYP3A4 Substrates.
MitotaneMay decrease the serum concentration of CYP3A4 Substrates.
ModafinilMay enhance the adverse/toxic effect of other Sympathomimetics.
MolindoneMay diminish the stimulatory effect of Amphetamines.
NabiloneCannabinoid-Containing Products may enhance the tachycardic effect of Sympathomimetics.
NaphazolineMay enhance the adverse/toxic effect of other Sympathomimetics.
NorepinephrineMay enhance the adverse/toxic effect of other Sympathomimetics.
OlanzapineMay diminish the stimulatory effect of Amphetamines.
OndansetronMay diminish the stimulatory effect of Amphetamines.
OrciprenalineMay enhance the adverse/toxic effect of other Sympathomimetics.
OxymetazolineMay enhance the adverse/toxic effect of other Sympathomimetics.
PaliperidoneMay diminish the stimulatory effect of Amphetamines.
PerphenazineMay diminish the stimulatory effect of Amphetamines.
PhendimetrazineMay enhance the adverse/toxic effect of other Sympathomimetics.
PheniramineMay enhance the adverse/toxic effect of other Sympathomimetics.
PhenmetrazineMay enhance the adverse/toxic effect of other Sympathomimetics.
PhentermineMay enhance the adverse/toxic effect of other Sympathomimetics.
PhenylephrineMay enhance the adverse/toxic effect of other Sympathomimetics.
PhenylpropanolamineMay enhance the adverse/toxic effect of other Sympathomimetics.
PimozideMay diminish the stimulatory effect of Amphetamines.
PiperacetazineMay diminish the stimulatory effect of Amphetamines.
PirbuterolMay enhance the adverse/toxic effect of other Sympathomimetics.
ProchlorperazineMay diminish the stimulatory effect of Amphetamines.
PromazineMay diminish the stimulatory effect of Amphetamines.
PropylhexedrineMay enhance the adverse/toxic effect of other Sympathomimetics.
PseudoephedrineMay enhance the adverse/toxic effect of other Sympathomimetics.
QuetiapineMay diminish the stimulatory effect of Amphetamines.
RemoxiprideMay diminish the stimulatory effect of Amphetamines.
ReserpineMay diminish the stimulatory effect of Amphetamines.
RisperidoneMay diminish the stimulatory effect of Amphetamines.
RitodrineMay enhance the adverse/toxic effect of other Sympathomimetics.
SalbutamolMay enhance the adverse/toxic effect of other Sympathomimetics.
SalmeterolMay enhance the adverse/toxic effect of other Sympathomimetics.
SertindoleMay diminish the stimulatory effect of Amphetamines.
SiltuximabMay decrease the serum concentration of CYP3A4 Substrates.
SimeprevirMay increase the serum concentration of CYP3A4 Substrates.
SulpirideMay diminish the stimulatory effect of Amphetamines.
Tedizolid PhosphateTedizolid may enhance the hypertensive effect of Sympathomimetics. Tedizolid may enhance the tachycardic effect of Sympathomimetics.
TerbutalineMay enhance the adverse/toxic effect of other Sympathomimetics.
TheophyllineMay enhance the adverse/toxic effect of other Sympathomimetics.
ThioridazineMay diminish the stimulatory effect of Amphetamines.
ThiothixeneMay diminish the stimulatory effect of Amphetamines.
TocilizumabMay decrease the serum concentration of CYP3A4 Substrates.
TrifluoperazineMay diminish the stimulatory effect of Amphetamines.
TriflupromazineMay diminish the stimulatory effect of Amphetamines.
TriprolidineMay enhance the adverse/toxic effect of other Sympathomimetics.
Vitamin CMay decrease the serum concentration of Amphetamines.
ZiprasidoneMay diminish the stimulatory effect of Amphetamines.
ZuclopenthixolMay diminish the stimulatory effect of Amphetamines.
Food InteractionsNot Available

Targets

1. Synaptic vesicular amine transporter

Kind: protein

Organism: Human

Pharmacological action: yes

Actions: inducer

Components

Name UniProt ID Details
Synaptic vesicular amine transporter Q05940 Details

References:

  1. 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

2. Alpha-2A adrenergic receptor

Kind: protein

Organism: Human

Pharmacological action: yes

Actions: agonist

Components

Name UniProt ID Details
Alpha-2A adrenergic receptor P08913 Details

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
  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

3. Alpha-1A adrenergic receptor

Kind: protein

Organism: Human

Pharmacological action: yes

Actions: agonist

Components

Name UniProt ID Details
Alpha-1A adrenergic receptor P35348 Details

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
  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

4. Sodium-dependent dopamine transporter

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Sodium-dependent dopamine transporter Q01959 Details

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
  2. 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

Enzymes

1. Cytochrome P450 3A4

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
Cytochrome P450 3A4 P08684 Details

References:

  1. Seree EJ, Pisano PJ, Placidi M, Rahmani R, Barra YA: Identification of the human and animal hepatic cytochromes P450 involved in clonazepam metabolism. Fundam Clin Pharmacol. 1993;7(2):69-75. Pubmed

2. Cytochrome P450 2B6

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
Cytochrome P450 2B6 P20813 Details

References:

  1. Bumpus NN, Sridar C, Kent UM, Hollenberg PF: The naturally occurring cytochrome P450 (P450) 2B6 K262R mutant of P450 2B6 exhibits alterations in substrate metabolism and inactivation. Drug Metab Dispos. 2005 Jun;33(6):795-802. Epub 2005 Mar 15. Pubmed
  2. Shebley M, Kent UM, Ballou DP, Hollenberg PF: Mechanistic analysis of the inactivation of cytochrome P450 2B6 by phencyclidine: effects on substrate binding, electron transfer, and uncoupling. Drug Metab Dispos. 2009 Apr;37(4):745-52. Epub 2009 Jan 14. Pubmed

3. NADPH--cytochrome P450 reductase

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
NADPH--cytochrome P450 reductase P16435 Details

References:

  1. Kanaeva IP, Nikityuk OV, Davydov DR, Dedinskii IR, Koen YM, Kuznetsova GP, Skotselyas ED, Bachmanova GI, Archakov AI: Comparative study of monomeric reconstituted and membrane microsomal monooxygenase systems of the rabbit liver. II. Kinetic parameters of reductase and monooxygenase reactions. Arch Biochem Biophys. 1992 Nov 1;298(2):403-12. Pubmed
  2. Matsumoto T, Emi Y, Kawabata S, Omura T: Purification and characterization of three male-specific and one female-specific forms of cytochrome P-450 from rat liver microsomes. J Biochem (Tokyo). 1986 Nov;100(5):1359-71. Pubmed
  3. Kojima H, Takahashi K, Sakane F, Koyama J: Purification and characterization of NADPH-cytochrome c reductase from porcine polymorphonuclear leukocytes. J Biochem (Tokyo). 1987 Nov;102(5):1083-8. Pubmed
  4. Dutton DR, McMillen SK, Parkinson A: Purification of rat liver microsomal cytochrome P-450b without the use of nonionic detergent. J Biochem Toxicol. 1988 Summer;3:131-45. Pubmed
  5. Halpert JR, Miller NE, Gorsky LD: On the mechanism of the inactivation of the major phenobarbital-inducible isozyme of rat liver cytochrome P-450 by chloramphenicol. J Biol Chem. 1985 Jul 15;260(14):8397-403. Pubmed

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Drug created on June 13, 2005 07:24 / Updated on September 16, 2013 17:12