Isoprenaline

Identification

Summary

Isoprenaline is a catecholamine non-selective beta-adrenergic agonist typically used to treat bradycardia and heart block.

Brand Names
Isuprel
Generic Name
Isoprenaline
DrugBank Accession Number
DB01064
Background

Isoprenaline is a non-selective beta adrenergic receptor agonist indicated to treat heart block, Adams-Stokes attacks, bronchospasm in anesthesia, cadiac arrest, hypovolemic shocks, septic shock, hypoperfusion, congestive hear failure, and cardiogenic shock.2,14

Isoprenaline research in the 1940s found that this isopropyl analog of epinephrine dilated the bronchi, as well as raising the heart rate and cardiac output, without vasoconstriction.11,12 The US patent from 1943 states that this compound had a wider therapeutic index and a stronger action than adrenaline.16

Isoprenaline was granted FDA approval on 19 February 1948.13

Type
Small Molecule
Groups
Approved, Investigational
Structure
Thumb
Weight
Average: 211.2576
Monoisotopic: 211.120843415
Chemical Formula
C11H17NO3
Synonyms
  • (±)-isoprenaline
  • (±)-isoproterenol
  • 1-(3,4-dihydroxyphenyl)-2-(isopropylamino)ethanol
  • 1-(3,4-dihydroxyphenyl)-2-isopropylaminoethanol
  • 3,4-dihydroxy-α-[(isopropylamino)methyl]benzyl alcohol
  • Isoprenalina
  • Isoprenaline
  • Isoprénaline
  • Isoprenalinum
  • Isopropyl noradrenaline
  • Isoproterenol
  • N-isopropyl-β-dihydroxyphenyl-β-hydroxyethylamine
  • N-Isopropylnoradrenaline
  • N-Isopropylnorepinephrine
  • α-(isopropylaminomethyl)protocatechuyl alcohol

Pharmacology

Indication

Isoprenaline is indicated to treat mild or transient episodes of heart block not requiring electric shock or pacemakers, serious episodes of heart block and Adams-Stokes attacks not caused by ventricular tachycardia or fibrillation, and bronchospasm during anesthesia.14 Isoprenaline is also indicated for cases of cardiac arrest until preferable treatments like electric shock and pacemakers are available.14 Isoprenaline is also indicated as an adjunct therapy to fluid and electrolyte replacement therapy in hypovolemic shock, septic shock, hypoperfusion, congestive heart failure, and cardiogenic shock.14

Pharmacology
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Associated Conditions
Contraindications & Blackbox Warnings
Contraindications
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Pharmacodynamics

Isoprenaline is a non-selective beta adrenergic receptor agonist used in a number of indications for the heart, as well as bronchospasm in anesthesia.2,14 Isoprenaline has a short duration of action as it is rapidly cleared,8,7 and a wide therapeutic index.14 Patients should be counselled regarding the risks of isoprenaline in the treatment of cardiogenic shock following myocardial infarction, paradoxical worsening of heart block, or precipitation of Adams-Stokes attacks.14

Mechanism of action

Isoprenaline is a non-selective beta adrenergic receptor agonist.2 Agonism of beta-1 and beta-2 adrenergic receptors causes the alpha subunit of G-protein coupled receptors to exchange GMP for GTP, activating them, and allowing the alpha subunit to dissociate from the beta and gamma subunits.1,4 Dissociation of the alpha subunit activates adenylate cyclase, converting ATP to cyclic AMP.1 Cyclic AMP activates protein kinase A (PKA), which phosphorylates cardiac L-type calcium channels such as Cav1.2.1,3,4 These channels depolarize cells by inward active transport of calcium ions.3,4

Agonism of beta-1 adrenergic receptors lead to increased strength of contractility, conduction of nerve impulses, speed of relaxation, and rate in the heart.1

Agonism of beta-2 adrenergic receptors leads to glycogenolysis in the liver,5 glucagon release from the pancreas, and activation of the renin-angiotensin-aldosterone system.1

In the alveoli, agonism of beta-2 adrenergic receptors, activates similar pathways to the heart, however the end result is regulation of sodium channels, the cystic fibrosis transmembrane conductance regulator (CFTR), and sodium potassium ATPase.10 PKA phosphorylates scaffolding proteins and sodium channels, increasing the number of sodium channels on the apical side of alveolar cells and increasing active transport of sodium ions into cells.10 Agonism of beta-2 adrenergic receptors can also increase chloride ion transport across CFTR.10 Together, these actions lead to passive transport of water out of the alveoli, and the clearance of alveolar fluid.10

TargetActionsOrganism
ABeta-1 adrenergic receptor
agonist
Humans
ABeta-2 adrenergic receptor
agonist
binder
Humans
ABeta-3 adrenergic receptor
agonist
Humans
USuperoxide dismutase [Cu-Zn]
stabilization
Humans
Absorption

Data regarding absorption kinetics of isoprenaline are not readily available.8,7

Volume of distribution

In pediatric patients, the volume of distribution was 216 ± 57 mL/kg.7

Protein binding

Isoprenaline is 68.8 ± 1.2% protein bound in plasma, mainly to serum albumin.9

Metabolism

Isoprenaline is predominantly metabolized to glucuronide conjugates.6 Isoprenaline can also be O-methylated by catechol O-methyltransferase to the metabolite 3-O-methylisoprenaline, which can also be further glucuronidated.6

Hover over products below to view reaction partners

Route of elimination

Isoprenaline is 12.2-27.0% recovered in the feces and 59.1-106.8% recovered in the urine after 48 hours.6 The majority of the recovered dose in the urine is conjugated isoprenaline, with 6.5-16.2% free isoprenaline, and 2.6-11.4% 3-O-methylisoprenaline and conjugates.6

Half-life

The half life of intravenous isoprenaline is 2.5-5 minutes.1 Oral isoprenaline has a half life of 40 minutes.6

Clearance

In pediatric patients, the clearance of isoprenaline was 42.5 ± 5.0 mL/kg/min.7

Adverse Effects
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Toxicity

Patients experiencing an overdose may present with tachycardia, arrhythmias, palpitations, angina, hypotension, or hypertension.14 Overdose should be treated by reducing or stopping administration of isoprenaline and monitoring blood pressure, pulse, respiration, and ECG.14

In rats, the LD50 is 2221 mg/kg orally, 128 mg/kg intraperitoneally, and 600 mg/kg subcutaneously.15 In mice, the LD50 is 1260 orally and 450 mg/kg intraperitoneally.15

Pathways
PathwayCategory
Isoprenaline Action PathwayDrug action
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
DrugInteraction
AbaloparatideThe risk or severity of adverse effects can be increased when Isoprenaline is combined with Abaloparatide.
AcebutololThe therapeutic efficacy of Isoprenaline can be decreased when used in combination with Acebutolol.
AceclofenacThe risk or severity of hypertension can be increased when Isoprenaline is combined with Aceclofenac.
AcemetacinThe risk or severity of hypertension can be increased when Isoprenaline is combined with Acemetacin.
Acetylsalicylic acidThe risk or severity of hypertension can be increased when Acetylsalicylic acid is combined with Isoprenaline.
AclidiniumThe risk or severity of Tachycardia can be increased when Isoprenaline is combined with Aclidinium.
AdenosineThe risk or severity of Tachycardia can be increased when Adenosine is combined with Isoprenaline.
AlclofenacThe risk or severity of hypertension can be increased when Isoprenaline is combined with Alclofenac.
AlfentanilThe risk or severity of hypertension can be increased when Alfentanil is combined with Isoprenaline.
AlfuzosinThe therapeutic efficacy of Isoprenaline can be decreased when used in combination with Alfuzosin.
Interactions
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Food Interactions
No interactions found.

Products

Products
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Product Ingredients
IngredientUNIICASInChI Key
Isoprenaline hydrochlorideDIA2A7485551-30-9IROWCYIEJAOFOW-UHFFFAOYSA-N
Isoproterenol sulfate925FX3X7766078-56-4CUQPTVCVZLUXJB-UHFFFAOYSA-N
International/Other Brands
Proternol L (Kowa Souyaku) / Saventrine (Pharmax)
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Isoproterenol HCl Inj 1:5000LiquidIntravenousInternational Medication Systems, Limited1977-12-311997-08-15Canada flag
Isoproterenol Hydrochloride Injection USPSolutionIntramuscular; Intravenous; SubcutaneousMarcan Pharmaceuticals Inc2021-01-06Not applicableCanada flag
Isoproterenol Hydrochloride Injection USPSolutionIntramuscular; Intravenous; SubcutaneousMarcan Pharmaceuticals Inc2020-12-11Not applicableCanada flag
Isoproterenol Hydrochloride Injection USPSolutionIntramuscular; Intravenous; SubcutaneousSandoz Canada Incorporated1991-12-31Not applicableCanada flag
Isoproterenol Hydrochloride Injection USPSolutionIntramuscular; Intravenous; SubcutaneousOmega Laboratories LtdNot applicableNot applicableCanada flag
IsuprelInjection, solution0.2 mg/1mLIntracardiac; Intramuscular; Intravenous; SubcutaneousCardinal Health2012-06-182015-01-31US flag
IsuprelInjection, solution0.2 mg/1mLIntracardiac; Intramuscular; Intravenous; SubcutaneousHospira, Inc.2005-08-012015-02-01US flag
IsuprelInjection, solution0.2 mg/1mLIntracardiac; Intramuscular; Intravenous; SubcutaneousHospira, Inc.2013-11-302021-02-01US flag
IsuprelInjection, solution0.2 mg/1mLIntracardiac; Intramuscular; Intravenous; SubcutaneousGeneral Injectables & Vaccines2010-03-012017-01-17US flag
IsuprelInjection, solution0.2 mg/1mLIntracardiac; Intramuscular; Intravenous; SubcutaneousMarathon Pharmaceuticals2013-12-012016-06-01US flag
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
IsoproterenolInjection, solution0.2 mg/1mLIntracardiac; Intramuscular; Intravenous; SubcutaneousCipla USA Inc.2018-06-26Not applicableUS flag
IsoproterenolInjection, solution1 mg/5mLIntracardiac; Intramuscular; Intravenous; SubcutaneousCipla USA Inc.2018-06-26Not applicableUS flag
Isoproterenol HydrochlorideInjection, solution1 mg/5mLIntracardiac; Intramuscular; Intravenous; SubcutaneousAuroMedics Pharma LLC2021-02-09Not applicableUS flag
Isoproterenol HydrochlorideInjection, solution0.2 mg/1mLIntracardiac; Intramuscular; Intravenous; SubcutaneousAmphastar Pharmaceuticals, Inc.2018-07-16Not applicableUS flag
Isoproterenol HydrochlorideInjection, solution0.2 mg/1mLIntracardiac; Intramuscular; Intravenous; SubcutaneousAmneal Pharmaceuticals LLC2018-10-22Not applicableUS flag
Isoproterenol HydrochlorideInjection0.2 mg/1mLIntracardiac; Intramuscular; Intravenous; SubcutaneousMicro Labs Limited2021-05-01Not applicableUS flag
Isoproterenol HydrochlorideInjection, solution0.2 mg/1mLIntramuscular; IntravenousNexus Pharmaceuticals Inc2017-08-03Not applicableUS flag
Isoproterenol HydrochlorideInjection, solution0.2 mg/1mLIntracardiac; Intramuscular; Intravenous; SubcutaneousAuroMedics Pharma LLC2021-02-09Not applicableUS flag
Isoproterenol HydrochlorideInjection, solution0.2 mg/1mLIntracardiac; Intramuscular; Intravenous; SubcutaneousAmphastar Pharmaceuticals, Inc.2018-07-16Not applicableUS flag
Isoproterenol HydrochlorideInjection0.2 mg/1mLIntracardiac; Intramuscular; Intravenous; SubcutaneousMicro Labs Limited2021-05-01Not applicableUS flag
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
Duo-MedihalerIsoprenaline hydrochloride (0.16 ug/1) + Phenylephrine bitartrate (0.24 ug/1)Aerosol, meteredRespiratory (inhalation)3M Company1962-08-252006-12-29US flag

Categories

ATC Codes
C01CA02 — IsoprenalineR03AK02 — Isoprenaline and other drugs for obstructive airway diseasesR03AB02 — IsoprenalineR03CB01 — IsoprenalineR03CB51 — Isoprenaline, combinations
Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
This compound belongs to the class of organic compounds known as catechols. These are compounds containing a 1,2-benzenediol moiety.
Kingdom
Organic compounds
Super Class
Benzenoids
Class
Phenols
Sub Class
Benzenediols
Direct Parent
Catechols
Alternative Parents
Aralkylamines / 1-hydroxy-4-unsubstituted benzenoids / 1-hydroxy-2-unsubstituted benzenoids / Benzene and substituted derivatives / Secondary alcohols / 1,2-aminoalcohols / Dialkylamines / Organopnictogen compounds / Hydrocarbon derivatives / Aromatic alcohols
Substituents
1,2-aminoalcohol / 1-hydroxy-2-unsubstituted benzenoid / 1-hydroxy-4-unsubstituted benzenoid / Alcohol / Amine / Aralkylamine / Aromatic alcohol / Aromatic homomonocyclic compound / Catechol / Hydrocarbon derivative
Molecular Framework
Aromatic homomonocyclic compounds
External Descriptors
secondary alcohol, catechols, secondary amino compound (CHEBI:64317)
Affected organisms
  • Humans and other mammals

Chemical Identifiers

UNII
L628TT009W
CAS number
7683-59-2
InChI Key
JWZZKOKVBUJMES-UHFFFAOYSA-N
InChI
InChI=1S/C11H17NO3/c1-7(2)12-6-11(15)8-3-4-9(13)10(14)5-8/h3-5,7,11-15H,6H2,1-2H3
IUPAC Name
4-{1-hydroxy-2-[(propan-2-yl)amino]ethyl}benzene-1,2-diol
SMILES
CC(C)NCC(O)C1=CC(O)=C(O)C=C1

References

Synthesis Reference

U.S. Patent 2,308,232. U.S. Patent 2,715,141.

General References
  1. Szymanski MW, Singh DP: Isoproterenol . [Article]
  2. Baker JG: The selectivity of beta-adrenoceptor agonists at human beta1-, beta2- and beta3-adrenoceptors. Br J Pharmacol. 2010 Jul;160(5):1048-61. doi: 10.1111/j.1476-5381.2010.00754.x. [Article]
  3. Striessnig J, Pinggera A, Kaur G, Bock G, Tuluc P: L-type Ca(2+) channels in heart and brain. Wiley Interdiscip Rev Membr Transp Signal. 2014 Mar 1;3(2):15-38. doi: 10.1002/wmts.102. [Article]
  4. Harvey RD, Hell JW: CaV1.2 signaling complexes in the heart. J Mol Cell Cardiol. 2013 May;58:143-52. doi: 10.1016/j.yjmcc.2012.12.006. Epub 2012 Dec 22. [Article]
  5. Authors unspecified: Beta-2 Adrenergic Agonists . [Article]
  6. Conolly ME, Davies DS, Dollery CT, Morgan CD, Paterson JW, Sandler M: Metabolism of isoprenaline in dog and man. Br J Pharmacol. 1972 Nov;46(3):458-72. doi: 10.1111/j.1476-5381.1972.tb08143.x. [Article]
  7. Reyes G, Schwartz PH, Newth CJ, Eldadah MK: The pharmacokinetics of isoproterenol in critically ill pediatric patients. J Clin Pharmacol. 1993 Jan;33(1):29-34. doi: 10.1002/j.1552-4604.1993.tb03899.x. [Article]
  8. Goldstein DS, Horwitz D, Keiser HR, Polinsky RJ, Kopin IJ: Plasma l-[3H]norepinephrine, d-[14C]norepinephrine, and d,l-[3H]isoproterenol kinetics in essential hypertension. J Clin Invest. 1983 Nov;72(5):1748-58. doi: 10.1172/JCI111134. [Article]
  9. Kelly JG, McDevitt DG: Plasma protein binding of propranolol and isoprenaline in hyperthyroidism and hypothyroidism. Br J Clin Pharmacol. 1978 Aug;6(2):123-7. doi: 10.1111/j.1365-2125.1978.tb00836.x. [Article]
  10. Mutlu GM, Factor P: Alveolar epithelial beta2-adrenergic receptors. Am J Respir Cell Mol Biol. 2008 Feb;38(2):127-34. doi: 10.1165/rcmb.2007-0198TR. Epub 2007 Aug 20. [Article]
  11. SEGAL MS, BEAKEY JF: The use of isuprel for the management of bronchial asthma. Bull New Engl Med Cent. 1947 Apr;9(2):62-7. [Article]
  12. BARCROFT H, KONZETT H: On the actions of noradrenaline, adrenaline and isopropyl noradrenaline on the arterial blood pressure, heart rate and muscle blood flow in man. J Physiol. 1949 Dec 15;110(1-2):194-204. doi: 10.1113/jphysiol.1949.sp004431. [Article]
  13. FDA Approved Drugs Products: Isuprel (Isoprenaline) Sublingual and Rectal Tablets (Discontinued) [Link]
  14. FDA Approved Drug Products: Isuprel (Isoprenaline) Intravenous, Intramuscular, Subcutaneous, and Intracardiac Injection [Link]
  15. Cayman Chemical: Isoproterenol MSDS [Link]
  16. US Patent: US2308232A [Link]
Human Metabolome Database
HMDB0015197
KEGG Compound
C07056
PubChem Compound
3779
PubChem Substance
46507323
ChemSpider
3647
BindingDB
25392
RxNav
6054
ChEBI
64317
ChEMBL
CHEMBL434
Therapeutic Targets Database
DNC000819
PharmGKB
PA450121
Guide to Pharmacology
GtP Drug Page
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Isoprenaline
AHFS Codes
  • 12:12.08.04 — Non-selective Beta-adrenergic Agonists
FDA label
Download (314 KB)
MSDS
Download (73.3 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
2CompletedTreatmentAtrial Fibrillation1
2Unknown StatusTreatmentKidney Stones / Ureteroscopy1
2, 3CompletedTreatmentBenignant Tumour Mass in the Upper Urinary Tract / Kidney Stones / Unexplained Haematuria1
1Active Not RecruitingScreeningAutonomic Nervous System Diseases / Dopamine Beta-Hydroxylase Deficiency / Orthostatic Hypotension / Orthostatic Intolerance1
1, 2CompletedTreatmentLipomas1
Not AvailableActive Not RecruitingTreatmentAnorexia Nervosa (AN)1
Not AvailableCompletedNot AvailableCoronary Heart Disease (CHD)1
Not AvailableCompletedBasic ScienceHeart Failure1
Not AvailableCompletedPreventionHypotension1
Not AvailableCompletedTreatmentIntraoperative Awareness1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
  • Amend
  • Baxter International Inc.
  • ESI Lederle
  • Hospira Inc.
Dosage Forms
FormRouteStrength
TabletSublingual
Aerosol, meteredRespiratory (inhalation)
Injection, solution, concentrateIntravenous
Injection, solution
Injection, solutionIntracardiac; Intramuscular; Intravenous; Subcutaneous1 mg/5mL
LiquidIntravenous
InjectionIntracardiac; Intramuscular; Intravenous; Subcutaneous0.2 mg/1mL
Injection, solutionIntramuscular; Intravenous0.2 mg/1mL
SolutionIntramuscular; Intravenous; Subcutaneous
SolutionIntravenous
Injection, solutionIntracardiac; Intramuscular; Intravenous; Subcutaneous0.2 mg/1mL
LiquidIntramuscular; Intravenous; Subcutaneous
LiquidIntracardiac; Intramuscular; Intravenous; Subcutaneous
LiquidRespiratory (inhalation)
Aerosol, meteredRespiratory (inhalation)
AerosolRespiratory (inhalation)0.08 ug/1
Prices
Unit descriptionCostUnit
Isuprel 0.2 mg/ml ampul17.63USD ml
Isoproterenol sulfate cryst2.86USD g
Isoproterenol 0.2 mg/ml amp0.73USD ml
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Not Available

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)180U.S. Patent 2,308,232. U.S. Patent 2,715,141.
Predicted Properties
PropertyValueSource
Water Solubility5.86 mg/mLALOGPS
logP-0.27ALOGPS
logP0.24ChemAxon
logS-1.6ALOGPS
pKa (Strongest Acidic)9.81ChemAxon
pKa (Strongest Basic)8.96ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count4ChemAxon
Hydrogen Donor Count4ChemAxon
Polar Surface Area72.72 Å2ChemAxon
Rotatable Bond Count4ChemAxon
Refractivity58.4 m3·mol-1ChemAxon
Polarizability23.04 Å3ChemAxon
Number of Rings1ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET Features
PropertyValueProbability
Human Intestinal Absorption+0.9936
Blood Brain Barrier-0.9705
Caco-2 permeable-0.6775
P-glycoprotein substrateSubstrate0.5776
P-glycoprotein inhibitor INon-inhibitor0.9039
P-glycoprotein inhibitor IINon-inhibitor0.9709
Renal organic cation transporterNon-inhibitor0.8983
CYP450 2C9 substrateNon-substrate0.7778
CYP450 2D6 substrateNon-substrate0.6679
CYP450 3A4 substrateNon-substrate0.6939
CYP450 1A2 substrateInhibitor0.6221
CYP450 2C9 inhibitorNon-inhibitor0.9558
CYP450 2D6 inhibitorNon-inhibitor0.9231
CYP450 2C19 inhibitorNon-inhibitor0.9484
CYP450 3A4 inhibitorNon-inhibitor0.9556
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.9318
Ames testNon AMES toxic0.9133
CarcinogenicityNon-carcinogens0.9182
BiodegradationNot ready biodegradable0.8925
Rat acute toxicity2.7434 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9576
hERG inhibition (predictor II)Non-inhibitor0.8045
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available

Targets

Drugtargets
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Kind
Protein
Organism
Humans
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. Sato M, Gong H, Terracciano CM, Ranu H, Harding SE: Loss of beta-adrenoceptor response in myocytes overexpressing the Na+/Ca(2+)-exchanger. J Mol Cell Cardiol. 2004 Jan;36(1):43-8. [Article]
  2. Jurgens CW, Rau KE, Knudson CA, King JD, Carr PA, Porter JE, Doze VA: Beta1 adrenergic receptor-mediated enhancement of hippocampal CA3 network activity. J Pharmacol Exp Ther. 2005 Aug;314(2):552-60. Epub 2005 May 20. [Article]
  3. Kobayashi H, Narita Y, Nishida M, Kurose H: Beta-arrestin2 enhances beta2-adrenergic receptor-mediated nuclear translocation of ERK. Cell Signal. 2005 Oct;17(10):1248-53. Epub 2005 Feb 12. [Article]
  4. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
  5. Ahlquist RP: Present state of alpha- and beta-adrenergic drugs I. The adrenergic receptor. Am Heart J. 1976 Nov;92(5):661-4. [Article]
  6. Szymanski MW, Singh DP: Isoproterenol . [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Agonist
Binder
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. Abraham G, Kottke C, Dhein S, Ungemach FR: Pharmacological and biochemical characterization of the beta-adrenergic signal transduction pathway in different segments of the respiratory tract. Biochem Pharmacol. 2003 Sep 15;66(6):1067-81. [Article]
  2. Jones SM, Hiller FC, Jacobi SE, Foreman SK, Pittman LM, Cornett LE: Enhanced beta2-adrenergic receptor (beta2AR) signaling by adeno-associated viral (AAV)-mediated gene transfer. BMC Pharmacol. 2003 Dec 4;3:15. [Article]
  3. Teixeira CE, Baracat JS, Zanesco A, Antunes E, De Nucci G: Atypical beta-adrenoceptor subtypes mediate relaxations of rabbit corpus cavernosum. J Pharmacol Exp Ther. 2004 May;309(2):587-93. Epub 2004 Jan 29. [Article]
  4. Odley A, Hahn HS, Lynch RA, Marreez Y, Osinska H, Robbins J, Dorn GW 2nd: Regulation of cardiac contractility by Rab4-modulated beta2-adrenergic receptor recycling. Proc Natl Acad Sci U S A. 2004 May 4;101(18):7082-7. Epub 2004 Apr 22. [Article]
  5. Uezono Y, Kaibara M, Murasaki O, Taniyama K: Involvement of G protein betagamma-subunits in diverse signaling induced by G(i/o)-coupled receptors: study using the Xenopus oocyte expression system. Am J Physiol Cell Physiol. 2004 Oct;287(4):C885-94. Epub 2004 May 19. [Article]
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
  7. Ahlquist RP: Present state of alpha- and beta-adrenergic drugs I. The adrenergic receptor. Am Heart J. 1976 Nov;92(5):661-4. [Article]
  8. Szymanski MW, Singh DP: Isoproterenol . [Article]
  9. Hardin AO, Lima JJ: Beta 2-adrenoceptor agonist-induced down-regulation after short-term exposure. J Recept Signal Transduct Res. 1999 Sep;19(5):835-52. doi: 10.3109/10799899909042876. [Article]
Kind
Protein
Organism
Humans
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. Ahlquist RP: Present state of alpha- and beta-adrenergic drugs I. The adrenergic receptor. Am Heart J. 1976 Nov;92(5):661-4. [Article]
  2. Schiffelers SL, Blaak EE, Saris WH, van Baak MA: In vivo beta3-adrenergic stimulation of human thermogenesis and lipid use. Clin Pharmacol Ther. 2000 May;67(5):558-66. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Stabilization
General Function
Zinc ion binding
Specific Function
Destroys radicals which are normally produced within the cells and which are toxic to biological systems.
Gene Name
SOD1
Uniprot ID
P00441
Uniprot Name
Superoxide dismutase [Cu-Zn]
Molecular Weight
15935.685 Da
References
  1. Wright GS, Antonyuk SV, Kershaw NM, Strange RW, Samar Hasnain S: Ligand binding and aggregation of pathogenic SOD1. Nat Commun. 2013;4:1758. doi: 10.1038/ncomms2750. [Article]

Enzymes

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
Inducer
General Function
Vitamin d 24-hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP1A1
Uniprot ID
P04798
Uniprot Name
Cytochrome P450 1A1
Molecular Weight
58164.815 Da
References
  1. Konstandi M, Kostakis D, Harkitis P, Marselos M, Johnson EO, Adamidis K, Lang MA: Role of adrenoceptor-linked signaling pathways in the regulation of CYP1A1 gene expression. Biochem Pharmacol. 2005 Jan 15;69(2):277-87. [Article]
  2. Althurwi HN, Tse MM, Abdelhamid G, Zordoky BN, Hammock BD, El-Kadi AO: Soluble epoxide hydrolase inhibitor, TUPS, protects against isoprenaline-induced cardiac hypertrophy. Br J Pharmacol. 2013 Apr;168(8):1794-807. doi: 10.1111/bph.12066. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inducer
General Function
Oxygen binding
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP1B1
Uniprot ID
Q16678
Uniprot Name
Cytochrome P450 1B1
Molecular Weight
60845.33 Da
References
  1. Althurwi HN, Tse MM, Abdelhamid G, Zordoky BN, Hammock BD, El-Kadi AO: Soluble epoxide hydrolase inhibitor, TUPS, protects against isoprenaline-induced cardiac hypertrophy. Br J Pharmacol. 2013 Apr;168(8):1794-807. doi: 10.1111/bph.12066. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
O-methyltransferase activity
Specific Function
Catalyzes the O-methylation, and thereby the inactivation, of catecholamine neurotransmitters and catechol hormones. Also shortens the biological half-lives of certain neuroactive drugs, like L-DOP...
Gene Name
COMT
Uniprot ID
P21964
Uniprot Name
Catechol O-methyltransferase
Molecular Weight
30036.77 Da
References
  1. Conolly ME, Davies DS, Dollery CT, Morgan CD, Paterson JW, Sandler M: Metabolism of isoprenaline in dog and man. Br J Pharmacol. 1972 Nov;46(3):458-72. doi: 10.1111/j.1476-5381.1972.tb08143.x. [Article]
  2. FDA Approved Drug Products: Isuprel (Isoprenaline) Intravenous, Intramuscular, Subcutaneous, and Intracardiac Injection [Link]

Carriers

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Binder
General Function
Toxic substance binding
Specific Function
Serum albumin, the main protein of plasma, has a good binding capacity for water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs. Its main function is the regulation of the colloid...
Gene Name
ALB
Uniprot ID
P02768
Uniprot Name
Serum albumin
Molecular Weight
69365.94 Da
References
  1. Kelly JG, McDevitt DG: Plasma protein binding of propranolol and isoprenaline in hyperthyroidism and hypothyroidism. Br J Clin Pharmacol. 1978 Aug;6(2):123-7. doi: 10.1111/j.1365-2125.1978.tb00836.x. [Article]

Drug created on June 13, 2005 13:24 / Updated on May 11, 2021 01:04