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Identification
NameEphedra
Accession NumberDB01363
TypeSmall Molecule
GroupsApproved, Nutraceutical, Withdrawn
DescriptionEphedra is an alkaloid chemical compound traditionally obtained from the plant Ephedra sinica. The sale of ephedra-containing supplements was banned in the United States in 2004. The drug is still sold in Canada in OTC formulations.
Structure
Thumb
Synonyms
Chinese jointfir
Indian jointfir
Ma huang
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Congest-easeCapsule8 mgOralPuresource Inc.Not applicableNot applicableCanada
H.O. Formula With M/hTablet8 mgOralAbundance Marketing Ltd.Not applicableNot applicableCanada
Approved Generic Prescription ProductsNot Available
Approved Over the Counter Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Chi FormulaCapsule4.2 mgOralNature's Sunshine Products Of Canada Ltd.1995-12-312006-07-10Canada
CitrivateCapsule84 mgOralGreat Canadian Lifestyles Co.2001-07-132002-09-03Canada
Decongestionnant - Cap OrlCapsule250 mgOralLaboratoire Lalco Inc.1997-01-202002-09-05Canada
Dp FormulaTablet107 mgOralPep Products Inc.2000-03-012003-01-13Canada
Dp Formula - 133mg TabTablet133 mgOralPep Products Inc.1994-12-312003-01-13Canada
EphedraCapsule300 mgOralKaizen Inc.1997-04-221999-03-15Canada
EphedraCapsule8 mgOralChampion's Choice Advanced Nutrition Inc.1997-06-111999-08-28Canada
EphedraCapsule8 mgOralNatural Balance2002-01-142009-08-17Canada
Ephedra - Cap 300mgCapsule300 mgOralNutrion Health & Fitness Inc.1996-12-311999-08-28Canada
Ephedra -tab 100mgTablet100 mgOralVita Health Products Inc1997-09-082002-07-31Canada
Ephedra Herbal Formula TabletTablet8 mgOralPharmetics (2011) Inc1999-06-202006-07-27Canada
Florasun Ephedra Cap 250mgCapsule250 mgOralLaboratoire Lalco Inc.1995-12-312002-09-05Canada
Formula RF CapsulesCapsule133.4 mgOralTwin Laboratories Inc.1999-10-282005-08-30Canada
Formula T.L.Capsule8 mgOralChanges International2002-02-052004-10-15Canada
Formula T.O.Tablet8 mgOralAbundance Marketing Ltd.2001-05-012002-10-28Canada
Fyto-HB I- Cap 10mgCapsule10 mgOralFytoresearch Inc.1996-10-182002-11-14Canada
Fyto-HB Tea - 10mg/pckKit; Liquid10 mgOralFytoresearch Inc.1997-09-252002-11-14Canada
L.therm FormulaTablet8 mgOralGolden Pride International1999-11-252000-07-26Canada
Ll Formula 2Capsule4 mgOralNutrition For Life International1998-11-301999-08-11Canada
Metacuts CapsulesCapsule100 mgOralMetaform Ltd.1998-12-082001-07-23Canada
Pharmated CapsulesCapsule680 mgOralEnrich International1994-12-312003-09-25Canada
Pro-enz 99Tablet8 mgOralCountry Road Naturals Inc.2001-05-012003-07-08Canada
Pro-enz 99Tablet8 mgOralAbundance Marketing Ltd.1999-02-012009-07-23Canada
Slm Form - TabTablet8 mgOralNatural Balance1995-12-312003-09-22Canada
Stacker 2 Nasal DecongestantCapsule100 mgOralSportika Export Inc2002-01-102003-10-27Canada
Thermo 5000c CapsulesCapsule125 mgOralMarket America, Inc.1996-12-182002-07-10Canada
Ultra 99 TabletsTablet133 mgOralBody Gold, A Division Of Pep Products, Inc.2000-01-012002-08-22Canada
Xenadrine Rfa-1 Decongestant FormulaCapsule167.5 mgOralTrue North Nutrition Inc.2002-02-152003-10-21Canada
Zand Decongestant Herbal CapCapsule4 mgOralZand Herbal Formulas1995-12-312003-06-20Canada
Zap - Cap 7.5mgCapsule7.5 mgOralNu Life Nutrition Ltd.1997-08-152005-03-15Canada
Zap Extra - Cap 10.8mgCapsule10.8 mgOralNu Life Nutrition Ltd.1997-08-152005-03-15Canada
Unapproved/Other Products Not Available
International Brands
NameCompany
Ephedra vulgarisNot Available
SinueazeNot Available
Brand mixturesNot Available
SaltsNot Available
Categories
UNIID0P20CT40D
CAS numberNot Available
WeightNot Available
Chemical FormulaNot Available
InChI KeyNot Available
InChINot Available
IUPAC NameNot Available
SMILESNot Available
Pharmacology
IndicationEphedra is widely used by athletes, despite a lack of evidence that it enhances athletic performance. Ephedra has also been used for weight loss.
Structured Indications Not Available
PharmacodynamicsNot Available
Mechanism of actionThe alkaloids ephedrine and pseudoephedrine are the active constituents of Ephedra. Pseudoephedrine is used in over-the-counter decongestants. Derivatives of ephedrine are used to treat low blood pressure, but alternatives with reduced cardiovascular risk have replaced it for treating asthma. Ephedrine is also considered a performance-enhancing drug and is prohibited in most competitive sports. Ephedrine is a sympathomimetic amine - that is, its principal mechanism of action relies on its direct and indirect actions on the adrenergic receptor system, which is part of the sympathetic nervous system. Ephedrine increases post-synaptic noradrenergic receptor activity by (weakly) directly activating post-synaptic α-receptors and β-receptors, but the bulk of its effect comes from the pre-synaptic neuron being unable to distinguish between real adrenaline or noradrenaline from ephedrine. The ephedrine, mixed with noradrenaline, is transported through the noradrenaline reuptake complex and packaged (along with real noradrenaline) into vesicles that reside at the terminal button of a nerve cell. Ephedrine's action as an agonist at most major noradrenaline receptors and its ability to increase the release of both dopamine and to a lesser extent, serotonin by the same mechanism is presumed to have a major role in its mechanism of action.
TargetKindPharmacological actionActionsOrganismUniProt ID
Sodium-dependent dopamine transporterProteinyes
negative modulator
HumanQ01959 details
Sodium-dependent noradrenaline transporterProteinyes
negative modulator
HumanP23975 details
Alpha-2A adrenergic receptorProteinyes
agonist
HumanP08913 details
Alpha-2B adrenergic receptorProteinyes
agonist
HumanP18089 details
Alpha-2C adrenergic receptorProteinyes
agonist
HumanP18825 details
Amine oxidase [flavin-containing] AProteinyes
inhibitor
HumanP21397 details
Amine oxidase [flavin-containing] BProteinyes
inhibitor
HumanP27338 details
Beta-1 adrenergic receptorProteinyes
agonist
HumanP08588 details
Beta-2 adrenergic receptorProteinyes
agonist
HumanP07550 details
Beta-3 adrenergic receptorProteinyes
agonist
HumanP13945 details
Sodium-dependent serotonin transporterProteinyes
negative modulator
HumanP31645 details
Synaptic vesicular amine transporterProteinyes
inhibitor
HumanQ05940 details
Chromaffin granule amine transporterProteinyes
inhibitor
HumanP54219 details
Related Articles
AbsorptionNot Available
Volume of distributionNot Available
Protein bindingNot Available
MetabolismNot Available
Route of eliminationNot Available
Half lifeNot Available
ClearanceNot Available
ToxicityNot Available
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
Interactions
Drug Interactions
DrugInteractionDrug group
7,8-DICHLORO-1,2,3,4-TETRAHYDROISOQUINOLINEThe risk or severity of adverse effects can be increased when 7,8-DICHLORO-1,2,3,4-TETRAHYDROISOQUINOLINE is combined with Ephedra.Experimental
AcebutololEphedra may increase the atrioventricular blocking (AV block) activities of Acebutolol.Approved
AlprenololAlprenolol may decrease the bronchodilatory activities of Ephedra.Approved, Withdrawn
AmineptineAmineptine may decrease the antihypertensive activities of Ephedra.Illicit, Withdrawn
AmitriptylineAmitriptyline may decrease the antihypertensive activities of Ephedra.Approved
Aop200704Ephedra may increase the atrioventricular blocking (AV block) activities of Aop200704.Investigational
ArotinololEphedra may increase the atrioventricular blocking (AV block) activities of Arotinolol.Approved
AtenololEphedra may increase the atrioventricular blocking (AV block) activities of Atenolol.Approved
AtomoxetineAtomoxetine may increase the tachycardic activities of Ephedra.Approved
AtosibanThe risk or severity of adverse effects can be increased when Ephedra is combined with Atosiban.Approved
BefunololEphedra may increase the atrioventricular blocking (AV block) activities of Befunolol.Experimental
BendroflumethiazideEphedra may increase the hypokalemic activities of Bendroflumethiazide.Approved
BenmoxinThe risk or severity of adverse effects can be increased when Benmoxin is combined with Ephedra.Withdrawn
BetahistineThe therapeutic efficacy of Ephedra can be decreased when used in combination with Betahistine.Approved
BetaxololEphedra may increase the atrioventricular blocking (AV block) activities of Betaxolol.Approved
BevantololEphedra may increase the atrioventricular blocking (AV block) activities of Bevantolol.Approved
BisoprololEphedra may increase the atrioventricular blocking (AV block) activities of Bisoprolol.Approved
BopindololBopindolol may decrease the bronchodilatory activities of Ephedra.Approved
BucindololEphedra may increase the atrioventricular blocking (AV block) activities of Bucindolol.Investigational
BufuralolEphedra may increase the atrioventricular blocking (AV block) activities of Bufuralol.Experimental, Investigational
BumetanideEphedra may increase the hypokalemic activities of Bumetanide.Approved
BupranololBupranolol may decrease the bronchodilatory activities of Ephedra.Approved
CaroxazoneThe risk or severity of adverse effects can be increased when Caroxazone is combined with Ephedra.Withdrawn
CarteololCarteolol may decrease the bronchodilatory activities of Ephedra.Approved
CarvedilolEphedra may increase the atrioventricular blocking (AV block) activities of Carvedilol.Approved, Investigational
CeliprololEphedra may increase the atrioventricular blocking (AV block) activities of Celiprolol.Approved, Investigational
ChlorothiazideEphedra may increase the hypokalemic activities of Chlorothiazide.Approved, Vet Approved
ChlorthalidoneEphedra may increase the hypokalemic activities of Chlorthalidone.Approved
ClomipramineClomipramine may decrease the antihypertensive activities of Ephedra.Approved, Vet Approved
CyclobenzaprineCyclobenzaprine may decrease the antihypertensive activities of Ephedra.Approved
DesfluraneEphedra may increase the arrhythmogenic activities of Desflurane.Approved
DesipramineDesipramine may decrease the antihypertensive activities of Ephedra.Approved
DesvenlafaxineDesvenlafaxine may decrease the antihypertensive activities of Ephedra.Approved
DosulepinDosulepin may decrease the antihypertensive activities of Ephedra.Approved
DoxepinDoxepin may decrease the antihypertensive activities of Ephedra.Approved
DroxidopaEphedra may increase the hypertensive activities of Droxidopa.Approved, Investigational
DuloxetineDuloxetine may decrease the antihypertensive activities of Ephedra.Approved
EnfluraneEphedra may increase the arrhythmogenic activities of Enflurane.Approved, Vet Approved
EsmirtazapineEsmirtazapine may decrease the antihypertensive activities of Ephedra.Investigational
EsmololEphedra may increase the atrioventricular blocking (AV block) activities of Esmolol.Approved
Etacrynic acidEphedra may increase the hypokalemic activities of Etacrynic acid.Approved
FurazolidoneThe risk or severity of adverse effects can be increased when Furazolidone is combined with Ephedra.Approved, Vet Approved
FurosemideEphedra may increase the hypokalemic activities of Furosemide.Approved, Vet Approved
HalothaneEphedra may increase the arrhythmogenic activities of Halothane.Approved, Vet Approved
HydracarbazineThe risk or severity of adverse effects can be increased when Hydracarbazine is combined with Ephedra.Approved
HydrochlorothiazideEphedra may increase the hypokalemic activities of Hydrochlorothiazide.Approved, Vet Approved
HydroflumethiazideEphedra may increase the hypokalemic activities of Hydroflumethiazide.Approved
ImipramineImipramine may decrease the antihypertensive activities of Ephedra.Approved
IndapamideEphedra may increase the hypokalemic activities of Indapamide.Approved
IndenololEphedra may increase the atrioventricular blocking (AV block) activities of Indenolol.Withdrawn
IobenguaneThe therapeutic efficacy of Iobenguane can be decreased when used in combination with Ephedra.Approved
IproclozideThe risk or severity of adverse effects can be increased when Iproclozide is combined with Ephedra.Withdrawn
IproniazidThe risk or severity of adverse effects can be increased when Iproniazid is combined with Ephedra.Withdrawn
IsocarboxazidThe risk or severity of adverse effects can be increased when Isocarboxazid is combined with Ephedra.Approved
IsofluraneEphedra may increase the arrhythmogenic activities of Isoflurane.Approved, Vet Approved
LabetalolEphedra may increase the atrioventricular blocking (AV block) activities of Labetalol.Approved
LevomilnacipranLevomilnacipran may decrease the antihypertensive activities of Ephedra.Approved
MebanazineThe risk or severity of adverse effects can be increased when Mebanazine is combined with Ephedra.Withdrawn
MethoxyfluraneEphedra may increase the arrhythmogenic activities of Methoxyflurane.Approved, Vet Approved
MethyclothiazideEphedra may increase the hypokalemic activities of Methyclothiazide.Approved
Methylene blueThe risk or severity of adverse effects can be increased when Methylene blue is combined with Ephedra.Investigational
MetolazoneEphedra may increase the hypokalemic activities of Metolazone.Approved
MetoprololEphedra may increase the atrioventricular blocking (AV block) activities of Metoprolol.Approved, Investigational
MianserinThe therapeutic efficacy of Ephedra can be decreased when used in combination with Mianserin.Approved
MilnacipranMilnacipran may decrease the antihypertensive activities of Ephedra.Approved
MinaprineThe risk or severity of adverse effects can be increased when Minaprine is combined with Ephedra.Approved
MirtazapineMirtazapine may decrease the antihypertensive activities of Ephedra.Approved
MoclobemideThe risk or severity of adverse effects can be increased when Moclobemide is combined with Ephedra.Approved
NadololNadolol may decrease the bronchodilatory activities of Ephedra.Approved
NebivololNebivolol may decrease the bronchodilatory activities of Ephedra.Approved, Investigational
NialamideThe risk or severity of adverse effects can be increased when Nialamide is combined with Ephedra.Withdrawn
Nitrous oxideEphedra may increase the arrhythmogenic activities of Nitrous oxide.Approved, Vet Approved
NortriptylineNortriptyline may decrease the antihypertensive activities of Ephedra.Approved
OctamoxinThe risk or severity of adverse effects can be increased when Octamoxin is combined with Ephedra.Withdrawn
OpipramolOpipramol may decrease the antihypertensive activities of Ephedra.Investigational
OxprenololOxprenolol may decrease the bronchodilatory activities of Ephedra.Approved
PargylineThe risk or severity of adverse effects can be increased when Pargyline is combined with Ephedra.Approved
PenbutololPenbutolol may decrease the bronchodilatory activities of Ephedra.Approved, Investigational
PhenelzineThe risk or severity of adverse effects can be increased when Phenelzine is combined with Ephedra.Approved
PheniprazineThe risk or severity of adverse effects can be increased when Pheniprazine is combined with Ephedra.Withdrawn
PhenoxypropazineThe risk or severity of adverse effects can be increased when Phenoxypropazine is combined with Ephedra.Withdrawn
PindololPindolol may decrease the bronchodilatory activities of Ephedra.Approved
PiretanideEphedra may increase the hypokalemic activities of Piretanide.Experimental
PirlindoleThe risk or severity of adverse effects can be increased when Pirlindole is combined with Ephedra.Approved
PivhydrazineThe risk or severity of adverse effects can be increased when Pivhydrazine is combined with Ephedra.Withdrawn
PolythiazideEphedra may increase the hypokalemic activities of Polythiazide.Approved
PractololEphedra may increase the atrioventricular blocking (AV block) activities of Practolol.Approved
PropranololPropranolol may decrease the bronchodilatory activities of Ephedra.Approved, Investigational
ProtriptylineProtriptyline may decrease the antihypertensive activities of Ephedra.Approved
QuinethazoneEphedra may increase the hypokalemic activities of Quinethazone.Approved
RasagilineThe risk or severity of adverse effects can be increased when Rasagiline is combined with Ephedra.Approved
SafrazineThe risk or severity of adverse effects can be increased when Safrazine is combined with Ephedra.Withdrawn
SelegilineThe risk or severity of adverse effects can be increased when Selegiline is combined with Ephedra.Approved, Investigational, Vet Approved
SevofluraneEphedra may increase the arrhythmogenic activities of Sevoflurane.Approved, Vet Approved
SotalolSotalol may decrease the bronchodilatory activities of Ephedra.Approved
TianeptineTianeptine may decrease the antihypertensive activities of Ephedra.Approved
TimololTimolol may decrease the bronchodilatory activities of Ephedra.Approved
ToloxatoneThe risk or severity of adverse effects can be increased when Toloxatone is combined with Ephedra.Approved
TorasemideEphedra may increase the hypokalemic activities of Torasemide.Approved
Trans-2-PhenylcyclopropylamineThe risk or severity of adverse effects can be increased when Trans-2-Phenylcyclopropylamine is combined with Ephedra.Experimental
TranylcypromineThe risk or severity of adverse effects can be increased when Tranylcypromine is combined with Ephedra.Approved
TrichlormethiazideEphedra may increase the hypokalemic activities of Trichlormethiazide.Approved, Vet Approved
TrimipramineTrimipramine may decrease the antihypertensive activities of Ephedra.Approved
VenlafaxineVenlafaxine may decrease the antihypertensive activities of Ephedra.Approved
Food InteractionsNot Available
References
Synthesis ReferenceNot Available
General References
  1. Gurley BJ, Wang P, Gardner SF: Ephedrine-type alkaloid content of nutritional supplements containing Ephedra sinica (Ma-huang) as determined by high performance liquid chromatography. J Pharm Sci. 1998 Dec;87(12):1547-53. [PubMed:10189265 ]
  2. Abourashed EA, El-Alfy AT, Khan IA, Walker L: Ephedra in perspective--a current review. Phytother Res. 2003 Aug;17(7):703-12. [PubMed:12916063 ]
  3. Haller CA, Benowitz NL: Adverse cardiovascular and central nervous system events associated with dietary supplements containing ephedra alkaloids. N Engl J Med. 2000 Dec 21;343(25):1833-8. [PubMed:11117974 ]
  4. Bent S, Tiedt TN, Odden MC, Shlipak MG: The relative safety of ephedra compared with other herbal products. Ann Intern Med. 2003 Mar 18;138(6):468-71. [PubMed:12639079 ]
External Links
ATC CodesNot Available
AHFS Codes
  • 92:01.00*
  • 92:02.00*
PDB EntriesNot Available
FDA labelNot Available
MSDSNot Available
ADMET
Predicted ADMET featuresNot Available
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage forms
FormRouteStrength
CapsuleOral4.2 mg
CapsuleOral84 mg
TabletOral107 mg
TabletOral133 mg
CapsuleOral300 mg
TabletOral100 mg
CapsuleOral250 mg
CapsuleOral133.4 mg
CapsuleOral8 mg
TabletOral8 mg
CapsuleOral10 mg
Kit; liquidOral10 mg
CapsuleOral100 mg
CapsuleOral680 mg
CapsuleOral125 mg
CapsuleOral167.5 mg
CapsuleOral4 mg
CapsuleOral7.5 mg
CapsuleOral10.8 mg
PricesNot Available
PatentsNot Available
Properties
StateSolid
Experimental PropertiesNot Available
Predicted PropertiesNot Available
Spectra
Mass Spec (NIST)Not Available
Spectra
Spectrum TypeDescriptionSplash Key
Taxonomy
ClassificationNot classified

Targets

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. 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. Wee S, Ordway GA, Woolverton WL: Reinforcing effect of pseudoephedrine isomers and the mechanism of action. Eur J Pharmacol. 2004 Jun 16;493(1-3):117-25. [PubMed:15189772 ]
  3. 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 ]
  4. 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 ]
  5. Haughey HM, Brown JM, Wilkins DG, Hanson GR, Fleckenstein AE: Differential effects of methamphetamine on Na(+)/Cl(-)-dependent transporters. Brain Res. 2000 Apr 28;863(1-2):59-65. [PubMed:10773193 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
negative modulator
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. Wee S, Ordway GA, Woolverton WL: Reinforcing effect of pseudoephedrine isomers and the mechanism of action. Eur J Pharmacol. 2004 Jun 16;493(1-3):117-25. [PubMed:15189772 ]
  2. 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 ]
  3. 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 ]
  4. 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 ]
  5. Haughey HM, Brown JM, Wilkins DG, Hanson GR, Fleckenstein AE: Differential effects of methamphetamine on Na(+)/Cl(-)-dependent transporters. Brain Res. 2000 Apr 28;863(1-2):59-65. [PubMed:10773193 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
agonist
General Function:
Thioesterase binding
Specific Function:
Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins. The rank order of potency for agonists of this receptor is oxymetazoline > clonidine > epinephrine > norepinephrine > phenylephrine > dopamine > p-synephrine > p-tyramine > serotonin = p-octopamine. For antagonists, the rank order is yohimbine > phentolamine = mianser...
Gene Name:
ADRA2A
Uniprot ID:
P08913
Molecular Weight:
48956.275 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. Kobayashi S, Endou M, Sakuraya F, Matsuda N, Zhang XH, Azuma M, Echigo N, Kemmotsu O, Hattori Y, Gando S: The sympathomimetic actions of l-ephedrine and d-pseudoephedrine: direct receptor activation or norepinephrine release? Anesth Analg. 2003 Nov;97(5):1239-45. [PubMed:14570629 ]
  3. 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 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
agonist
General Function:
Epinephrine binding
Specific Function:
Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins. The rank order of potency for agonists of this receptor is clonidine > norepinephrine > epinephrine = oxymetazoline > dopamine > p-tyramine = phenylephrine > serotonin > p-synephrine / p-octopamine. For antagonists, the rank order is yohimbine > chlorpromazine > phent...
Gene Name:
ADRA2B
Uniprot ID:
P18089
Molecular Weight:
49565.8 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. Kobayashi S, Endou M, Sakuraya F, Matsuda N, Zhang XH, Azuma M, Echigo N, Kemmotsu O, Hattori Y, Gando S: The sympathomimetic actions of l-ephedrine and d-pseudoephedrine: direct receptor activation or norepinephrine release? Anesth Analg. 2003 Nov;97(5):1239-45. [PubMed:14570629 ]
  3. 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 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
agonist
General Function:
Protein homodimerization activity
Specific Function:
Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins.
Gene Name:
ADRA2C
Uniprot ID:
P18825
Molecular Weight:
49521.585 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. Kobayashi S, Endou M, Sakuraya F, Matsuda N, Zhang XH, Azuma M, Echigo N, Kemmotsu O, Hattori Y, Gando S: The sympathomimetic actions of l-ephedrine and d-pseudoephedrine: direct receptor activation or norepinephrine release? Anesth Analg. 2003 Nov;97(5):1239-45. [PubMed:14570629 ]
  3. 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 ]
Kind
Protein
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.
Gene Name:
MAOA
Uniprot ID:
P21397
Molecular Weight:
59681.27 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. Ulus IH, Maher TJ, Wurtman RJ: Characterization of phentermine and related compounds as monoamine oxidase (MAO) inhibitors. Biochem Pharmacol. 2000 Jun 15;59(12):1611-21. [PubMed:10799660 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
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. 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. Ulus IH, Maher TJ, Wurtman RJ: Characterization of phentermine and related compounds as monoamine oxidase (MAO) inhibitors. Biochem Pharmacol. 2000 Jun 15;59(12):1611-21. [PubMed:10799660 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
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.
Gene Name:
ADRB1
Uniprot ID:
P08588
Molecular Weight:
51322.1 Da
References
  1. Vansal SS, Feller DR: Direct effects of ephedrine isomers on human beta-adrenergic receptor subtypes. Biochem Pharmacol. 1999 Sep 1;58(5):807-10. [PubMed:10449190 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
agonist
General Function:
Protein homodimerization activity
Specific Function:
Beta-adrenergic receptors mediate the catecholamine-induced activation of adenylate cyclase through the action of G proteins. The beta-2-adrenergic receptor binds epinephrine with an approximately 30-fold greater affinity than it does norepinephrine.
Gene Name:
ADRB2
Uniprot ID:
P07550
Molecular Weight:
46458.32 Da
References
  1. Vansal SS, Feller DR: Direct effects of ephedrine isomers on human beta-adrenergic receptor subtypes. Biochem Pharmacol. 1999 Sep 1;58(5):807-10. [PubMed:10449190 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
agonist
General Function:
Protein homodimerization activity
Specific Function:
Beta-adrenergic receptors mediate the catecholamine-induced activation of adenylate cyclase through the action of G proteins. Beta-3 is involved in the regulation of lipolysis and thermogenesis.
Gene Name:
ADRB3
Uniprot ID:
P13945
Molecular Weight:
43518.615 Da
References
  1. Vansal SS, Feller DR: Direct effects of ephedrine isomers on human beta-adrenergic receptor subtypes. Biochem Pharmacol. 1999 Sep 1;58(5):807-10. [PubMed:10449190 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
negative modulator
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. Wee S, Ordway GA, Woolverton WL: Reinforcing effect of pseudoephedrine isomers and the mechanism of action. Eur J Pharmacol. 2004 Jun 16;493(1-3):117-25. [PubMed:15189772 ]
  2. 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
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. Henry JP, Sagne C, Bedet C, Gasnier B: The vesicular monoamine transporter: from chromaffin granule to brain. Neurochem Int. 1998 Mar;32(3):227-46. [PubMed:9587917 ]
  3. 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
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Serotonin transmembrane transporter activity
Specific Function:
Involved in the transport of biogenic monoamines, such as serotonin, from the cytoplasm into the secretory vesicles of neuroendocrine and endocrine cells.
Gene Name:
SLC18A1
Uniprot ID:
P54219
Molecular Weight:
56256.71 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. Henry JP, Sagne C, Bedet C, Gasnier B: The vesicular monoamine transporter: from chromaffin granule to brain. Neurochem Int. 1998 Mar;32(3):227-46. [PubMed:9587917 ]
  3. 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 ]
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Drug created on July 06, 2007 13:55 / Updated on August 17, 2016 12:23