Identification

Name
Ephedra
Accession Number
DB01363
Type
Small Molecule
Groups
Approved, Nutraceutical, Withdrawn
Description

Ephedra 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.

Synonyms
  • Chinese jointfir
  • Indian jointfir
  • Ma huang
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Congest-easeCapsule8 mgOralPuresource Inc.Not applicableNot applicableCanada
H.O. Formula With M/hTablet8 mgOralAbundance Naturally LtdNot applicableNot applicableCanada
Over the Counter Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Chi FormulaCapsule4.2 mgOralNatures Sunshine Products, Inc.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
EphedraCapsule8 mgOralNatural Balance2002-01-142009-08-17Canada
EphedraCapsule300 mgOralKaizen Inc.1997-04-221999-03-15Canada
EphedraCapsule8 mgOralChampion's Choice Advanced Nutrition Inc.1997-06-111999-08-28Canada
Ephedra - Cap 300mgCapsule300 mgOralNutrion Health & Fitness Inc.1996-12-311999-08-28Canada
Ephedra -tab 100mgTablet100 mgOralVita Health Products Inc1997-09-082002-07-31Canada
International/Other Brands
Ephedra vulgaris / Sinueaze
Categories
UNII
D0P20CT40D
CAS number
Not Available
Weight
Not Available
Chemical Formula
Not Available
InChI Key
Not Available
InChI
Not Available
IUPAC Name
Not Available
SMILES
Not Available

Pharmacology

Indication

Ephedra 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
Pharmacodynamics
Not Available
Mechanism of action

The 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.

TargetActionsOrganism
ASodium-dependent dopamine transporter
negative modulator
Human
ASodium-dependent noradrenaline transporter
negative modulator
Human
AAlpha-2A adrenergic receptor
agonist
Human
AAlpha-2B adrenergic receptor
agonist
Human
AAlpha-2C adrenergic receptor
agonist
Human
AAmine oxidase [flavin-containing] A
inhibitor
Human
AAmine oxidase [flavin-containing] B
inhibitor
Human
ABeta-1 adrenergic receptor
agonist
Human
ABeta-2 adrenergic receptor
agonist
Human
ABeta-3 adrenergic receptor
agonist
Human
ASodium-dependent serotonin transporter
negative modulator
Human
ASynaptic vesicular amine transporter
inhibitor
Human
AChromaffin granule amine transporter
inhibitor
Human
Absorption
Not Available
Volume of distribution
Not Available
Protein binding
Not Available
Metabolism
Not Available
Route of elimination
Not Available
Half life
Not Available
Clearance
Not Available
Toxicity
Not Available
Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not 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
AlprenololEphedra may increase the atrioventricular blocking (AV block) activities of Alprenolol.Approved, Withdrawn
AmineptineAmineptine may decrease the antihypertensive activities of Ephedra.Illicit, Withdrawn
AmitriptylineAmitriptyline may decrease the antihypertensive activities of Ephedra.Approved
AmoxapineAmoxapine may decrease the antihypertensive activities of Ephedra.Approved
AmphetamineThe risk or severity of adverse effects can be increased when Amphetamine is combined with Ephedra.Approved, Illicit
ArotinololEphedra may increase the atrioventricular blocking (AV block) activities of Arotinolol.Approved, Investigational
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, Investigational
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
BopindololEphedra may increase the atrioventricular blocking (AV block) activities of Bopindolol.Approved
BrofaromineThe risk or severity of adverse effects can be increased when Brofaromine is combined with Ephedra.Experimental
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
BupranololEphedra may increase the atrioventricular blocking (AV block) activities of Bupranolol.Approved
CaroxazoneThe risk or severity of adverse effects can be increased when Caroxazone is combined with Ephedra.Withdrawn
CarteololEphedra may increase the atrioventricular blocking (AV block) activities of Carteolol.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
CloranololEphedra may increase the atrioventricular blocking (AV block) activities of Cloranolol.Experimental
CyclobenzaprineCyclobenzaprine may decrease the antihypertensive activities of Ephedra.Approved
CyclopenthiazideEphedra may increase the hypokalemic activities of Cyclopenthiazide.Experimental
DesfluraneDesflurane may increase the arrhythmogenic activities of Ephedra.Approved
DesipramineDesipramine may decrease the antihypertensive activities of Ephedra.Approved
DesvenlafaxineDesvenlafaxine may decrease the antihypertensive activities of Ephedra.Approved
DibenzepinDibenzepin may decrease the antihypertensive activities of Ephedra.Experimental
Diethyl etherDiethyl ether may increase the arrhythmogenic activities of Ephedra.Experimental
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
EnfluraneEnflurane may increase the arrhythmogenic activities of Ephedra.Approved, Investigational, Vet Approved
EpanololEphedra may increase the atrioventricular blocking (AV block) activities of Epanolol.Experimental
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, Investigational, Vet Approved
FurosemideEphedra may increase the hypokalemic activities of Furosemide.Approved, Vet Approved
HalothaneHalothane may increase the arrhythmogenic activities of Ephedra.Approved, Vet Approved
HarmalineThe risk or severity of adverse effects can be increased when Harmaline is combined with Ephedra.Experimental
HydracarbazineThe risk or severity of adverse effects can be increased when Hydracarbazine is combined with Ephedra.Experimental
HydrochlorothiazideEphedra may increase the hypokalemic activities of Hydrochlorothiazide.Approved, Vet Approved
HydroflumethiazideEphedra may increase the hypokalemic activities of Hydroflumethiazide.Approved, Investigational
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, Investigational
IprindoleIprindole may decrease the antihypertensive activities of Ephedra.Experimental
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
IsofluraneIsoflurane may increase the arrhythmogenic activities of Ephedra.Approved, Vet Approved
LabetalolEphedra may increase the atrioventricular blocking (AV block) activities of Labetalol.Approved
LandiololEphedra may increase the atrioventricular blocking (AV block) activities of Landiolol.Investigational
LevomilnacipranLevomilnacipran may decrease the antihypertensive activities of Ephedra.Approved
LofepramineLofepramine may decrease the antihypertensive activities of Ephedra.Experimental
MebanazineThe risk or severity of adverse effects can be increased when Mebanazine is combined with Ephedra.Withdrawn
MepindololEphedra may increase the atrioventricular blocking (AV block) activities of Mepindolol.Experimental
MethoxyfluraneMethoxyflurane may increase the arrhythmogenic activities of Ephedra.Approved, Investigational, 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.Approved, 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, Investigational
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
NadololEphedra may increase the atrioventricular blocking (AV block) activities of Nadolol.Approved
NebivololEphedra may increase the atrioventricular blocking (AV block) activities of Nebivolol.Approved, Investigational
NialamideThe risk or severity of adverse effects can be increased when Nialamide is combined with Ephedra.Withdrawn
Nitrous oxideNitrous oxide may increase the arrhythmogenic activities of Ephedra.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
OxprenololEphedra may increase the atrioventricular blocking (AV block) activities of Oxprenolol.Approved
PargylineThe risk or severity of adverse effects can be increased when Pargyline is combined with Ephedra.Approved
PenbutololEphedra may increase the atrioventricular blocking (AV block) activities of Penbutolol.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
PindololEphedra may increase the atrioventricular blocking (AV block) activities of Pindolol.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
Platelet Activating FactorEphedra may increase the atrioventricular blocking (AV block) activities of Platelet Activating Factor.Experimental
PolythiazideEphedra may increase the hypokalemic activities of Polythiazide.Approved
PractololEphedra may increase the atrioventricular blocking (AV block) activities of Practolol.Approved
ProcarbazineThe risk or severity of adverse effects can be increased when Procarbazine is combined with Ephedra.Approved
PropranololEphedra may increase the atrioventricular blocking (AV block) activities of Propranolol.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
SevofluraneSevoflurane may increase the arrhythmogenic activities of Ephedra.Approved, Vet Approved
SotalolEphedra may increase the atrioventricular blocking (AV block) activities of Sotalol.Approved
TalinololEphedra may increase the atrioventricular blocking (AV block) activities of Talinolol.Investigational
TertatololEphedra may increase the atrioventricular blocking (AV block) activities of Tertatolol.Experimental
TianeptineTianeptine may decrease the antihypertensive activities of Ephedra.Approved, Investigational
TimololEphedra may increase the atrioventricular blocking (AV block) activities of Timolol.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
TrichloroethyleneTrichloroethylene may increase the arrhythmogenic activities of Ephedra.Approved
TrimipramineTrimipramine may decrease the antihypertensive activities of Ephedra.Approved
VenlafaxineVenlafaxine may decrease the antihypertensive activities of Ephedra.Approved
XenonXenon may increase the arrhythmogenic activities of Ephedra.Experimental
Food Interactions
Not Available

References

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
PubChem Substance
46504840
PharmGKB
PA164777031
Drugs.com
Drugs.com Drug Page
PDRhealth
PDRhealth Drug Page
Wikipedia
Ephedra
AHFS Codes
  • 12:12.12 — Alpha-and Beta-adrenergic Agonists
  • 92:01.00* — Herbs and Natural Products
  • 12:12.00 — Sympathomimetic (Adrenergic) Agents

Clinical Trials

Clinical Trials
Not Available

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not 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
Prices
Not Available
Patents
Not Available

Properties

State
Solid
Experimental Properties
Not Available
Predicted Properties
Not Available
Predicted ADMET features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
Not Available

Taxonomy

Classification
Not 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
Uniprot Name
Sodium-dependent dopamine transporter
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
Uniprot Name
Sodium-dependent noradrenaline transporter
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 oxymetazo...
Gene Name
ADRA2A
Uniprot ID
P08913
Uniprot Name
Alpha-2A adrenergic receptor
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...
Gene Name
ADRA2B
Uniprot ID
P18089
Uniprot Name
Alpha-2B adrenergic receptor
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
Uniprot Name
Alpha-2C adrenergic receptor
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...
Gene Name
MAOA
Uniprot ID
P21397
Uniprot Name
Amine oxidase [flavin-containing] A
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...
Gene Name
MAOB
Uniprot ID
P27338
Uniprot Name
Amine oxidase [flavin-containing] B
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 e...
Gene Name
ADRB1
Uniprot ID
P08588
Uniprot Name
Beta-1 adrenergic receptor
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 ...
Gene Name
ADRB2
Uniprot ID
P07550
Uniprot Name
Beta-2 adrenergic receptor
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
Uniprot Name
Beta-3 adrenergic receptor
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 t...
Gene Name
SLC6A4
Uniprot ID
P31645
Uniprot Name
Sodium-dependent serotonin transporter
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...
Gene Name
SLC18A2
Uniprot ID
Q05940
Uniprot Name
Synaptic vesicular amine transporter
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
Uniprot Name
Chromaffin granule amine transporter
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]

Drug created on July 06, 2007 13:55 / Updated on January 14, 2018 10:04