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IdentificationPharmacologyInteractionsReferencesTrialsEconomicsPropertiesSpectraTaxonomyIdentification
- 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- Approved, Nutraceutical, Withdrawn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
Name Dosage Strength Route Labeller Marketing Start Marketing End Congest-ease Capsule 8 mg Oral Puresource Inc. Not applicable Not applicable Canada 
H.O. Formula With M/h Tablet 8 mg Oral Abundance Naturally Ltd Not applicable Not applicable Canada - Over the Counter Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Chi Formula Capsule 4.2 mg Oral Natures Sunshine Products, Inc. 1995-12-31 2006-07-10 Canada Citrivate Capsule 84 mg Oral Great Canadian Lifestyles Co. 2001-07-13 2002-09-03 Canada Decongestionnant - Cap Orl Capsule 250 mg Oral Laboratoire Lalco Inc. 1997-01-20 2002-09-05 Canada Dp Formula Tablet 107 mg Oral Pep Products Inc. 2000-03-01 2003-01-13 Canada Dp Formula - 133mg Tab Tablet 133 mg Oral Pep Products Inc. 1994-12-31 2003-01-13 Canada Ephedra Capsule 8 mg Oral Natural Balance 2002-01-14 2009-08-17 Canada Ephedra Capsule 300 mg Oral Kaizen Inc. 1997-04-22 1999-03-15 Canada Ephedra Capsule 8 mg Oral Champion's Choice Advanced Nutrition Inc. 1997-06-11 1999-08-28 Canada Ephedra - Cap 300mg Capsule 300 mg Oral Nutrion Health & Fitness Inc. 1996-12-31 1999-08-28 Canada Ephedra -tab 100mg Tablet 100 mg Oral Vita Health Products Inc 1997-09-08 2002-07-31 Canada - 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.
Target Actions Organism ASodium-dependent dopamine transporter negative modulatorHuman ASodium-dependent noradrenaline transporter negative modulatorHuman AAlpha-2A adrenergic receptor agonistHuman AAlpha-2B adrenergic receptor agonistHuman AAlpha-2C adrenergic receptor agonistHuman AAmine oxidase [flavin-containing] A inhibitorHuman AAmine oxidase [flavin-containing] B inhibitorHuman ABeta-1 adrenergic receptor agonistHuman ABeta-2 adrenergic receptor agonistHuman ABeta-3 adrenergic receptor agonistHuman ASodium-dependent serotonin transporter negative modulatorHuman ASynaptic vesicular amine transporter inhibitorHuman AChromaffin granule amine transporter inhibitorHuman - 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
Drug Interaction Drug group 7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline The risk or severity of adverse effects can be increased when 7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline is combined with Ephedra. Experimental Acebutolol Ephedra may increase the atrioventricular blocking (AV block) activities of Acebutolol. Approved, Investigational Alprenolol Alprenolol may decrease the bronchodilatory activities of Ephedra. Approved, Withdrawn Amineptine Amineptine may decrease the antihypertensive activities of Ephedra. Illicit, Withdrawn Amitriptyline Amitriptyline may decrease the antihypertensive activities of Ephedra. Approved Amoxapine Amoxapine may decrease the antihypertensive activities of Ephedra. Approved Amphetamine The risk or severity of adverse effects can be increased when Amphetamine is combined with Ephedra. Approved, Illicit, Investigational Arotinolol Ephedra may increase the atrioventricular blocking (AV block) activities of Arotinolol. Investigational Atenolol Ephedra may increase the atrioventricular blocking (AV block) activities of Atenolol. Approved Atomoxetine Atomoxetine may increase the tachycardic activities of Ephedra. Approved Atosiban The risk or severity of adverse effects can be increased when Ephedra is combined with Atosiban. Approved, Investigational Azosemide Ephedra may increase the hypokalemic activities of Azosemide. Investigational Befunolol Ephedra may increase the atrioventricular blocking (AV block) activities of Befunolol. Experimental Bendroflumethiazide Ephedra may increase the hypokalemic activities of Bendroflumethiazide. Approved Benmoxin The risk or severity of adverse effects can be increased when Benmoxin is combined with Ephedra. Withdrawn Betahistine The therapeutic efficacy of Ephedra can be decreased when used in combination with Betahistine. Approved, Investigational Betaxolol Ephedra may increase the atrioventricular blocking (AV block) activities of Betaxolol. Approved, Investigational Bevantolol Ephedra may increase the atrioventricular blocking (AV block) activities of Bevantolol. Approved Bisoprolol Ephedra may increase the atrioventricular blocking (AV block) activities of Bisoprolol. Approved Bopindolol Bopindolol may decrease the bronchodilatory activities of Ephedra. Approved Brofaromine The risk or severity of adverse effects can be increased when Brofaromine is combined with Ephedra. Experimental Bucindolol Ephedra may increase the atrioventricular blocking (AV block) activities of Bucindolol. Investigational Bufuralol Ephedra may increase the atrioventricular blocking (AV block) activities of Bufuralol. Experimental, Investigational Bumetanide Ephedra may increase the hypokalemic activities of Bumetanide. Approved Bupranolol Bupranolol may decrease the bronchodilatory activities of Ephedra. Approved Caroxazone The risk or severity of adverse effects can be increased when Caroxazone is combined with Ephedra. Withdrawn Carteolol Carteolol may decrease the bronchodilatory activities of Ephedra. Approved Carvedilol Ephedra may increase the atrioventricular blocking (AV block) activities of Carvedilol. Approved, Investigational Celiprolol Ephedra may increase the atrioventricular blocking (AV block) activities of Celiprolol. Approved, Investigational Chlorothiazide Ephedra may increase the hypokalemic activities of Chlorothiazide. Approved, Vet Approved Chlorthalidone Ephedra may increase the hypokalemic activities of Chlorthalidone. Approved Clomipramine Clomipramine may decrease the antihypertensive activities of Ephedra. Approved, Investigational, Vet Approved Cloranolol Cloranolol may decrease the bronchodilatory activities of Ephedra. Experimental Cyclobenzaprine Cyclobenzaprine may decrease the antihypertensive activities of Ephedra. Approved Cyclopenthiazide Ephedra may increase the hypokalemic activities of Cyclopenthiazide. Experimental Desflurane Desflurane may increase the arrhythmogenic activities of Ephedra. Approved Desipramine Desipramine may decrease the antihypertensive activities of Ephedra. Approved, Investigational Desvenlafaxine Desvenlafaxine may decrease the antihypertensive activities of Ephedra. Approved, Investigational Dibenzepin Dibenzepin may decrease the antihypertensive activities of Ephedra. Experimental Diethyl ether Diethyl ether may increase the arrhythmogenic activities of Ephedra. Experimental Dosulepin Dosulepin may decrease the antihypertensive activities of Ephedra. Approved Doxepin Doxepin may decrease the antihypertensive activities of Ephedra. Approved, Investigational Droxidopa Ephedra may increase the hypertensive activities of Droxidopa. Approved, Investigational Duloxetine Duloxetine may decrease the antihypertensive activities of Ephedra. Approved Enflurane Enflurane may increase the arrhythmogenic activities of Ephedra. Approved, Investigational, Vet Approved Epanolol Ephedra may increase the atrioventricular blocking (AV block) activities of Epanolol. Experimental Epitizide Ephedra may increase the hypokalemic activities of Epitizide. Experimental Esmirtazapine Esmirtazapine may decrease the antihypertensive activities of Ephedra. Investigational Esmolol Ephedra may increase the atrioventricular blocking (AV block) activities of Esmolol. Approved Etacrynic acid Ephedra may increase the hypokalemic activities of Etacrynic acid. Approved, Investigational Furazolidone The risk or severity of adverse effects can be increased when Furazolidone is combined with Ephedra. Approved, Investigational, Vet Approved Furosemide Ephedra may increase the hypokalemic activities of Furosemide. Approved, Vet Approved Halothane Halothane may increase the arrhythmogenic activities of Ephedra. Approved, Vet Approved Harmaline The risk or severity of adverse effects can be increased when Harmaline is combined with Ephedra. Experimental Hydracarbazine The risk or severity of adverse effects can be increased when Hydracarbazine is combined with Ephedra. Experimental Hydrochlorothiazide Ephedra may increase the hypokalemic activities of Hydrochlorothiazide. Approved, Vet Approved Hydroflumethiazide Ephedra may increase the hypokalemic activities of Hydroflumethiazide. Approved, Investigational Imipramine Imipramine may decrease the antihypertensive activities of Ephedra. Approved Indapamide Ephedra may increase the hypokalemic activities of Indapamide. Approved Indenolol Ephedra may increase the atrioventricular blocking (AV block) activities of Indenolol. Withdrawn Iobenguane The therapeutic efficacy of Iobenguane can be decreased when used in combination with Ephedra. Approved, Investigational Iprindole Iprindole may decrease the antihypertensive activities of Ephedra. Experimental Iproclozide The risk or severity of adverse effects can be increased when Iproclozide is combined with Ephedra. Withdrawn Iproniazid The risk or severity of adverse effects can be increased when Iproniazid is combined with Ephedra. Withdrawn Isocarboxazid The risk or severity of adverse effects can be increased when Isocarboxazid is combined with Ephedra. Approved Isoflurane Isoflurane may increase the arrhythmogenic activities of Ephedra. Approved, Vet Approved Labetalol Ephedra may increase the atrioventricular blocking (AV block) activities of Labetalol. Approved Landiolol Ephedra may increase the atrioventricular blocking (AV block) activities of Landiolol. Investigational Levomilnacipran Levomilnacipran may decrease the antihypertensive activities of Ephedra. Approved, Investigational Lofepramine Lofepramine may decrease the antihypertensive activities of Ephedra. Experimental Mebanazine The risk or severity of adverse effects can be increased when Mebanazine is combined with Ephedra. Withdrawn Mepindolol Mepindolol may decrease the bronchodilatory activities of Ephedra. Experimental Methoxyflurane Methoxyflurane may increase the arrhythmogenic activities of Ephedra. Approved, Investigational, Vet Approved Methyclothiazide Ephedra may increase the hypokalemic activities of Methyclothiazide. Approved Methylene blue The risk or severity of adverse effects can be increased when Methylene blue is combined with Ephedra. Approved, Investigational Metolazone Ephedra may increase the hypokalemic activities of Metolazone. Approved Metoprolol Ephedra may increase the atrioventricular blocking (AV block) activities of Metoprolol. Approved, Investigational Mianserin The therapeutic efficacy of Ephedra can be decreased when used in combination with Mianserin. Approved, Investigational Milnacipran Milnacipran may decrease the antihypertensive activities of Ephedra. Approved, Investigational Minaprine The risk or severity of adverse effects can be increased when Minaprine is combined with Ephedra. Approved Mirtazapine Mirtazapine may decrease the antihypertensive activities of Ephedra. Approved Moclobemide The risk or severity of adverse effects can be increased when Moclobemide is combined with Ephedra. Approved, Investigational Nadolol Ephedra may increase the atrioventricular blocking (AV block) activities of Nadolol. Approved Nebivolol Ephedra may increase the atrioventricular blocking (AV block) activities of Nebivolol. Approved, Investigational Nialamide The risk or severity of adverse effects can be increased when Nialamide is combined with Ephedra. Withdrawn Nitrous oxide Nitrous oxide may increase the arrhythmogenic activities of Ephedra. Approved, Vet Approved Nortriptyline Nortriptyline may decrease the antihypertensive activities of Ephedra. Approved Octamoxin The risk or severity of adverse effects can be increased when Octamoxin is combined with Ephedra. Withdrawn Opipramol Opipramol may decrease the antihypertensive activities of Ephedra. Investigational Oxprenolol Oxprenolol may decrease the bronchodilatory activities of Ephedra. Approved Pargyline The risk or severity of adverse effects can be increased when Pargyline is combined with Ephedra. Approved Penbutolol Penbutolol may decrease the bronchodilatory activities of Ephedra. Approved, Investigational Phenelzine The risk or severity of adverse effects can be increased when Phenelzine is combined with Ephedra. Approved Pheniprazine The risk or severity of adverse effects can be increased when Pheniprazine is combined with Ephedra. Withdrawn Phenoxypropazine The risk or severity of adverse effects can be increased when Phenoxypropazine is combined with Ephedra. Withdrawn Pindolol Ephedra may increase the atrioventricular blocking (AV block) activities of Pindolol. Approved, Investigational Piretanide Ephedra may increase the hypokalemic activities of Piretanide. Approved Pirlindole The risk or severity of adverse effects can be increased when Pirlindole is combined with Ephedra. Approved Pivhydrazine The risk or severity of adverse effects can be increased when Pivhydrazine is combined with Ephedra. Withdrawn Platelet Activating Factor Ephedra may increase the atrioventricular blocking (AV block) activities of Platelet Activating Factor. Experimental Polythiazide Ephedra may increase the hypokalemic activities of Polythiazide. Approved Practolol Ephedra may increase the atrioventricular blocking (AV block) activities of Practolol. Approved Procarbazine The risk or severity of adverse effects can be increased when Procarbazine is combined with Ephedra. Approved, Investigational Propranolol Ephedra may increase the atrioventricular blocking (AV block) activities of Propranolol. Approved, Investigational Protriptyline Protriptyline may decrease the antihypertensive activities of Ephedra. Approved Quinethazone Ephedra may increase the hypokalemic activities of Quinethazone. Approved Rasagiline The risk or severity of adverse effects can be increased when Rasagiline is combined with Ephedra. Approved Safrazine The risk or severity of adverse effects can be increased when Safrazine is combined with Ephedra. Withdrawn Selegiline The risk or severity of adverse effects can be increased when Selegiline is combined with Ephedra. Approved, Investigational, Vet Approved Sevoflurane Sevoflurane may increase the arrhythmogenic activities of Ephedra. Approved, Vet Approved Sotalol Ephedra may increase the atrioventricular blocking (AV block) activities of Sotalol. Approved Talinolol Ephedra may increase the atrioventricular blocking (AV block) activities of Talinolol. Investigational Tertatolol Tertatolol may decrease the bronchodilatory activities of Ephedra. Experimental Tianeptine Tianeptine may decrease the antihypertensive activities of Ephedra. Approved, Investigational Timolol Ephedra may increase the atrioventricular blocking (AV block) activities of Timolol. Approved Toloxatone The risk or severity of adverse effects can be increased when Toloxatone is combined with Ephedra. Approved Torasemide Ephedra may increase the hypokalemic activities of Torasemide. Approved Tranylcypromine The risk or severity of adverse effects can be increased when Tranylcypromine is combined with Ephedra. Approved, Investigational Trichlormethiazide Ephedra may increase the hypokalemic activities of Trichlormethiazide. Approved, Vet Approved Trichloroethylene Trichloroethylene may increase the arrhythmogenic activities of Ephedra. Approved Trimipramine Trimipramine may decrease the antihypertensive activities of Ephedra. Approved Venlafaxine Venlafaxine may decrease the antihypertensive activities of Ephedra. Approved Xenon Xenon may increase the arrhythmogenic activities of Ephedra. Experimental - Food Interactions
- Not Available
References
- General References
- 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]
- 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]
- 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]
- 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
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage forms
Form Route Strength Capsule Oral 4.2 mg Capsule Oral 84 mg Tablet Oral 107 mg Tablet Oral 133 mg Capsule Oral 300 mg Tablet Oral 100 mg Capsule Oral 250 mg Capsule Oral 133.4 mg Capsule Oral 8 mg Tablet Oral 8 mg Capsule Oral 10 mg Kit; liquid Oral 10 mg Capsule Oral 100 mg Capsule Oral 680 mg Capsule Oral 125 mg Capsule Oral 167.5 mg Capsule Oral 4 mg Capsule Oral 7.5 mg Capsule Oral 10.8 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
- 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]
- 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]
- 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]
- 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]
- 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
- 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]
- 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]
- 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]
- 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]
- 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
- 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]
- 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]
- 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
- 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]
- 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]
- 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
- 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]
- 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]
- 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
- 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]
- 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
- 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]
- 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
- 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
- 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
- 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
- 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]
- 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
- 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]
- 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]
- 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
- 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]
- 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]
- 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 April 23, 2018 23:08