Terbutaline

Targets (3)Enzymes (1)

Identification

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Name
Terbutaline
Accession Number
DB00871  (APRD00589)
Type
Small Molecule
Groups
Approved
Description

A selective beta-2 adrenergic agonist used as a bronchodilator and tocolytic. [PubChem]

Structure
Thumb
3D
Similar Structures
Synonyms
  • Terbutalin
  • Terbutalina
  • Terbutaline
  • Terbutaline (sulfate de)
  • Terbutalini sulfas
  • Terbutalinsulfat
  • Terbutalinum
External IDs
KWD 2019
Product Ingredients
IngredientUNIICASInChI Key
Terbutaline Sulfate576PU70Y8E23031-32-5MUPQZWGSBCWCAV-UHFFFAOYSA-N
Product Images
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Unlock Additional Data
Bricanyl Tab 2.5 mgTablet2.5 mgOralAstra Zeneca1978-12-312000-07-20Canada
Bricanyl Tab 5 mgTablet5 mgOralAstra Zeneca1975-12-312001-07-23Canada
Bricanyl TurbuhalerPowder, metered0.5 mgRespiratory (inhalation)Astra Zeneca1990-12-31Not applicableCanada
Additional Data Available
  • Application Number
    Application Number

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  • Product Code
    Product Code

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Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Unlock Additional Data
Terbutaline SulfateInjection, solution1 mg/1mLSubcutaneousFresenius Kabi USA, LLC2011-03-10Not applicableUs
Terbutaline SulfateInjection1 mg/1mLSubcutaneousBedford Pharmaceuticals2004-04-282011-12-31Us
Terbutaline SulfateTablet2.5 mg/1OralRebel Distributors2005-03-25Not applicableUs
Terbutaline SulfateTablet5 mg/1OralAv Kare, Inc.2001-06-262015-12-09Us
Terbutaline SulfateTablet5 mg/1OralPD-Rx Pharmaceuticals, Inc.2001-06-262018-08-20Us
Terbutaline SulfateTablet2.5 mg/1OralMarlex Pharmaceuticals Inc2014-10-01Not applicableUs
Terbutaline SulfateTablet5 mg/1OralAmneal Pharmaceuticals of New York Llc2001-06-26Not applicableUs
Terbutaline SulfateInjection1 mg/1mLSubcutaneousHikma Farmaceutica2009-05-202009-05-20Us
Terbutaline SulfateInjection1 mg/1mLSubcutaneousWest-Ward Pharmaceuticals Corp2009-05-20Not applicableUs
Terbutaline SulfateInjection1 mg/1mLSubcutaneousBedford Pharmaceuticals2004-11-162011-12-31Us
Additional Data Available
  • Application Number
    Application Number

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

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  • Product Code
    Product Code

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

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International/Other Brands
Brethaire (Novartis) / Brethine / Bricanyl (AstraZeneca) / Bricardyl (Johnson) / Bricasma (AstraZeneca) / Bricasol (AstraZeneca) / Dracanyl (AstraZeneca) / Terbasmin (AstraZeneca)
Categories
UNII
N8ONU3L3PG
CAS number
23031-25-6
Weight
Average: 225.2842
Monoisotopic: 225.136493479
Chemical Formula
C12H19NO3
InChI Key
XWTYSIMOBUGWOL-UHFFFAOYSA-N
InChI
InChI=1S/C12H19NO3/c1-12(2,3)13-7-11(16)8-4-9(14)6-10(15)5-8/h4-6,11,13-16H,7H2,1-3H3
IUPAC Name
5-[2-(tert-butylamino)-1-hydroxyethyl]benzene-1,3-diol
SMILES
CC(C)(C)NCC(O)C1=CC(O)=CC(O)=C1

Pharmacology

Indication

For the prevention and reversal of bronchospasm in patients 12 years of age and older with reversible, obstructive airway disease, as well as symptomatic management of reversible bronchospasm associated with bronchitis and emphysema. Also used acute IV and sub-Q therapy in selected women to inhibit uterine contractions in preterm labor (tocolysis) and prolong gestation when beneficial.

Associated Conditions
Pharmacodynamics

Terbutaline is a relatively selective beta2-adrenergic bronchodilator that has little or no effect on alpha-adrenergic receptors. The drug has exerts a preferential effect on beta2-adrenergic receptors but stimulates beta-adrenergic receptors less selectively than relatively selective beta2-agonists. Terbutaline appears to have a greater stimulating effect on beta-receptors of the bronchial, vascular, and uterine smooth muscles (beta2 receptors) than on the beta-receptors of the heart (beta1 receptors). This drug relaxes smooth muscle and inhibits uterine contractions, but may also cause some cardiostimulatory effects and CNS stimulation.

Mechanism of action

The pharmacologic effects of terbutaline are at least in part attributable to stimulation through beta-adrenergic receptors of intracellular adenyl cyclase, the enzyme that catalyzes the conversion of adenosine triphosphate (ATP) to cyclic- 3',5'- adenosine monophosphate (c-AMP). Increased c-AMP levels are associated with relaxation of bronchial smooth muscle and inhibition of release of mediators of immediate hypersensitivity from cells, especially from mast cells.

TargetActionsOrganism
ABeta-2 adrenergic receptor
agonist
Humans
UBeta-3 adrenergic receptor
agonist
Humans
UBeta-1 adrenergic receptor
antagonist
Humans
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Additional Data Available
Adverse Effects

Comprehensive structured data on known drug adverse effects with statistical prevalence. MedDRA and ICD10 ids are provided for adverse effect conditions and symptoms.

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Additional Data Available
Contraindications

Structured data covering drug contraindications. Each contraindication describes a scenario in which the drug is not to be used. Includes restrictions on co-administration, contraindicated populations, and more.

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Additional Data Available
Blackbox Warnings

Structured data representing warnings from the black box section of drug labels. These warnings cover important and dangerous risks, contraindications, or adverse effects.

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Absorption

Approximately 30-50% if administered orally and well absorbed subcutaneously.

Volume of distribution
Not Available
Protein binding
Not Available
Metabolism
Not Available
Route of elimination

About 90% of the drug was excreted in the urine at 96 hours after subcutaneous administration, with about 60% of this being unchanged drug. It appears that the sulfate conjugate is a major metabolite of terbutaline and urinary excretion is the primary route of elimination

Half life

5.5-5.9 hours

Clearance
  • 311 +/- 112 mL/min
Toxicity

Terbutaline Sulfate: Oral LD50(rat) = 8.7 g/kg; Oral LD50(mouse) = 205 mg/kg; Oral LD50(dog) = 1.5 g/kg; IP LD50(rat)= 220 mg/kg ; IP LD50(mouse) = 130 mg/kg; Oral LD50(rabbit) = >8 g/kg; IV LD50(mouse) = 36 mg/kg; IV LD50(dog) = 116 mg/kg; IV LD50(rabbit) = 110 mg/kg

Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteraction
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1-(3-Mercapto-2-Methyl-Propionyl)-Pyrrolidine-2-Carboxylic AcidThe risk or severity of hypertension can be increased when Terbutaline is combined with 1-(3-Mercapto-2-Methyl-Propionyl)-Pyrrolidine-2-Carboxylic Acid.
1-benzylimidazoleThe risk or severity of hypertension can be increased when Terbutaline is combined with 1-benzylimidazole.
2,5-Dimethoxy-4-ethylamphetamineThe risk or severity of adverse effects can be increased when Terbutaline is combined with 2,5-Dimethoxy-4-ethylamphetamine.
2,5-Dimethoxy-4-ethylthioamphetamineThe risk or severity of adverse effects can be increased when Terbutaline is combined with 2,5-Dimethoxy-4-ethylthioamphetamine.
3-isobutyl-1-methyl-7H-xanthineThe risk or severity of adverse effects can be increased when Terbutaline is combined with 3-isobutyl-1-methyl-7H-xanthine.
3,5-diiodothyropropionic acidThe risk or severity of adverse effects can be increased when Terbutaline is combined with 3,5-diiodothyropropionic acid.
4-Bromo-2,5-dimethoxyamphetamineThe risk or severity of adverse effects can be increased when Terbutaline is combined with 4-Bromo-2,5-dimethoxyamphetamine.
4-MethoxyamphetamineThe risk or severity of hypertension can be increased when Terbutaline is combined with 4-Methoxyamphetamine.
5-methoxy-N,N-dimethyltryptamineThe risk or severity of hypertension can be increased when Terbutaline is combined with 5-methoxy-N,N-dimethyltryptamine.
6-O-benzylguanineThe risk or severity of adverse effects can be increased when Terbutaline is combined with 6-O-benzylguanine.
Additional Data Available
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    Extended Description

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    Severity

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    Evidence Level

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Food Interactions
Not Available

References

Synthesis Reference

Alison B. Lukacsko, Joseph J. Piala, "Effect of a combination of a terbutaline, diphenhydramine and ranitidine composition on gastrointestinal injury produced by nonsteroidal anti-inflammatory compositions." U.S. Patent US5260333, issued December, 1983.

US5260333
General References
  1. Rhodes MC, Seidler FJ, Abdel-Rahman A, Tate CA, Nyska A, Rincavage HL, Slotkin TA: Terbutaline is a developmental neurotoxicant: effects on neuroproteins and morphology in cerebellum, hippocampus, and somatosensory cortex. J Pharmacol Exp Ther. 2004 Feb;308(2):529-37. Epub 2003 Nov 10. [PubMed:14610225]
  2. Hochhaus G, Mollmann H: Pharmacokinetic/pharmacodynamic characteristics of the beta-2-agonists terbutaline, salbutamol and fenoterol. Int J Clin Pharmacol Ther Toxicol. 1992 Sep;30(9):342-62. [PubMed:1358833]
  3. Haahtela T, Jarvinen M, Kava T, Kiviranta K, Koskinen S, Lehtonen K, Nikander K, Persson T, Reinikainen K, Selroos O, et al.: Comparison of a beta 2-agonist, terbutaline, with an inhaled corticosteroid, budesonide, in newly detected asthma. N Engl J Med. 1991 Aug 8;325(6):388-92. [PubMed:2062329]
External Links
Human Metabolome Database
HMDB0015009
KEGG Compound
C07129
PubChem Compound
5403
PubChem Substance
46506887
ChemSpider
5210
BindingDB
25770
ChEBI
9449
ChEMBL
CHEMBL1760
Therapeutic Targets Database
DAP000246
PharmGKB
PA451616
Guide to Pharmacology
GtP Drug Page
Wikipedia
Terbutaline
ATC Codes
R03CC53 — Terbutaline, combinationsR03CC03 — TerbutalineR03AC03 — Terbutaline
AHFS Codes
  • 12:12.08.12 — Selective Beta 2-adrenergic Agonists
MSDS
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Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1CompletedPreventionType 1 Insulin-Dependent Diabetes Mellitus1
2CompletedTreatmentExercised Induced Asthma1
2, 3TerminatedTreatmentExternal Cephalic Version1
3CompletedTreatmentAcute Exacerbation of Chronic Obstructive Airways Disease / Chronic Obstructive Pulmonary Disease Exacerbation1
3CompletedTreatmentAsthma Bronchial3
3CompletedTreatmentChronic Obstructive Pulmonary Disease (COPD)1
4CompletedTreatmentAsthma Bronchial1
4CompletedTreatmentHeart Failure1
4CompletedTreatmentStatus Asthmaticus1
4TerminatedTreatmentExternal Cephalic Version1
4Unknown StatusNot AvailableAsthma Bronchial1
4Unknown StatusTreatmentLabour Pain1
Not AvailableCompletedBasic ScienceSkeletal Muscle Fatigue in Humans1
Not AvailableCompletedTreatmentFoetal distress syndrome1
Not AvailableCompletedTreatmentReproductive Techniques, Assisted1
Not AvailableCompletedTreatmentType 1 Insulin-Dependent Diabetes Mellitus1
Not AvailableNot Yet RecruitingBasic ScienceHypertrophy / Physical Activity / Physiologic Hypertrophy1
Not AvailableRecruitingBasic ScienceMuscle Hypertrophy in Healthy Young Men1

Pharmacoeconomics

Manufacturers
  • Novartis pharmaceuticals corp
  • Sanofi aventis us llc
  • Aaipharma llc
  • Akorn inc
  • App pharmaceuticals llc
  • Bedford laboratories div ben venue laboratories inc
  • Hikma farmaceutica (portugal) sa
  • Teva parenteral medicines inc
  • Impax laboratories inc
  • Lannett holdings inc
Packagers
  • Akorn Inc.
  • Amerisource Health Services Corp.
  • APP Pharmaceuticals
  • AstraZeneca Inc.
  • Bedford Labs
  • Ben Venue Laboratories Inc.
  • Cardinal Health
  • Dept Health Central Pharmacy
  • Dispensing Solutions
  • Gallipot
  • Global Pharmaceuticals
  • Hikma Pharmaceuticals
  • Lannett Co. Inc.
  • Mckesson Corp.
  • Murfreesboro Pharmaceutical Nursing Supply
  • Novartis AG
  • Nucare Pharmaceuticals Inc.
  • Pharmaceutical Utilization Management Program VA Inc.
  • Physicians Total Care Inc.
  • Rebel Distributors Corp.
  • Redpharm Drug
  • Remedy Repack
  • Resource Optimization and Innovation LLC
  • Rite Aid Corp.
  • Teva Pharmaceutical Industries Ltd.
  • Tya Pharmaceuticals
  • West-Ward Pharmaceuticals
Dosage forms
FormRouteStrength
TabletOral2.5 mg
TabletOral5 mg
Powder, meteredRespiratory (inhalation)0.5 mg
InjectionSubcutaneous1 mg/1mL
Injection, solutionSubcutaneous1 mg/1mL
TabletOral2.5 mg/1
TabletOral5 mg/1
Prices
Unit descriptionCostUnit
Terbutaline sulfate powder38.4USD g
Terbutaline Sulfate 1 mg/ml vial12.99USD vial
Terbutaline sulf 1 mg/ml vial4.8USD ml
Brethine 5 mg tablet0.83USD tablet
Terbutaline sulfate 5 mg tablet0.63USD tablet
Brethine 2.5 mg tablet0.57USD tablet
Terbutaline sulfate 2.5 mg tablet0.47USD tablet
Bricanyl Turbuhaler 0.5 mg/dose Metered Inhalation Powder0.08USD dose
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)119-122 °CNot Available
water solubility213 mg/mLNot Available
logP0.90TACAKS-NOVAK,K ET AL. (1995)
Caco2 permeability-6.38ADME Research, USCD
Predicted Properties
PropertyValueSource
Water Solubility5.84 mg/mLALOGPS
logP0.55ALOGPS
logP0.44ChemAxon
logS-1.6ALOGPS
pKa (Strongest Acidic)8.86ChemAxon
pKa (Strongest Basic)9.76ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count4ChemAxon
Hydrogen Donor Count4ChemAxon
Polar Surface Area72.72 Å2ChemAxon
Rotatable Bond Count4ChemAxon
Refractivity63.04 m3·mol-1ChemAxon
Polarizability24.78 Å3ChemAxon
Number of Rings1ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.987
Blood Brain Barrier-0.9355
Caco-2 permeable-0.8404
P-glycoprotein substrateSubstrate0.6335
P-glycoprotein inhibitor INon-inhibitor0.8954
P-glycoprotein inhibitor IINon-inhibitor0.9672
Renal organic cation transporterNon-inhibitor0.9067
CYP450 2C9 substrateNon-substrate0.7678
CYP450 2D6 substrateNon-substrate0.7922
CYP450 3A4 substrateNon-substrate0.6291
CYP450 1A2 substrateNon-inhibitor0.9516
CYP450 2C9 inhibitorNon-inhibitor0.9303
CYP450 2D6 inhibitorNon-inhibitor0.923
CYP450 2C19 inhibitorNon-inhibitor0.9115
CYP450 3A4 inhibitorNon-inhibitor0.8766
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.9117
Ames testNon AMES toxic0.9119
CarcinogenicityNon-carcinogens0.8484
BiodegradationNot ready biodegradable0.9808
Rat acute toxicity2.1080 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9548
hERG inhibition (predictor II)Non-inhibitor0.9467
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
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-004i-0290000000-8c26dbc913131cf49bc4
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-0udi-0900000000-3148282c5452a80b16c3
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-0udi-0900000000-9122151a6e70e6f2b536
LC-MS/MS Spectrum - LC-ESI-QQ , positiveLC-MS/MSsplash10-004i-0090000000-aab7f309385309d8884b
LC-MS/MS Spectrum - LC-ESI-QQ , positiveLC-MS/MSsplash10-0udi-0920000000-1e85cd2bf4a0358c22d7
LC-MS/MS Spectrum - LC-ESI-QQ , positiveLC-MS/MSsplash10-0udi-0900000000-82b70479a4e38921e06b
LC-MS/MS Spectrum - LC-ESI-QQ , positiveLC-MS/MSsplash10-0a4i-2900000000-aff994ffd107ef3b6e71
LC-MS/MS Spectrum - LC-ESI-QQ , positiveLC-MS/MSsplash10-0a6r-7900000000-cfe77aa0133facea1c75
LC-MS/MS Spectrum - LC-ESI-IT , positiveLC-MS/MSsplash10-0udi-0900000000-1a0ccd393797b19105a0
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-004i-0190000000-f9271bb736a512dbdbab
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-0udi-0900000000-a70c8697ca7633839444
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-0a6r-1900000000-4a9c0ddb9af4ce93b4ae
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-0a6r-6900000000-0cc68c4a50196d6ffab6
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-004i-9400000000-e1cec349ffb2fcd3ebe2

Taxonomy

Description
This compound belongs to the class of organic compounds known as resorcinols. These are compounds containing a resorcinol moiety, which is a benzene ring bearing two hydroxyl groups at positions 1 and 3.
Kingdom
Organic compounds
Super Class
Benzenoids
Class
Phenols
Sub Class
Benzenediols
Direct Parent
Resorcinols
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
Resorcinol / 1-hydroxy-4-unsubstituted benzenoid / 1-hydroxy-2-unsubstituted benzenoid / Aralkylamine / Monocyclic benzene moiety / 1,2-aminoalcohol / Secondary alcohol / Secondary amine / Secondary aliphatic amine / Aromatic alcohol
Molecular Framework
Aromatic homomonocyclic compounds
External Descriptors
phenylethanolamines, resorcinols (CHEBI:9449)

Targets

Details1. Beta-2 adrenergic receptor
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. 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. Schafers RF, Piest U, von Birgelen C, Jakubetz J, Daul AE, Philipp T, Brodde OE: Disodium cromoglycate does not prevent terbutaline-induced desensitization of beta 2-adrenoceptor-mediated cardiovascular in vivo functions in human volunteers. J Cardiovasc Pharmacol. 1999 May;33(5):822-7. [PubMed:10226872]
  2. Ramer-Quinn DS, Swanson MA, Lee WT, Sanders VM: Cytokine production by naive and primary effector CD4+ T cells exposed to norepinephrine. Brain Behav Immun. 2000 Dec;14(4):239-55. [PubMed:11120594]
  3. Zetterlund A, Hjemdahl P, Larsson K: beta2-Adrenoceptor desensitization in human alveolar macrophages induced by inhaled terbutaline in vivo is not counteracted by budesonide. Clin Sci (Lond). 2001 Apr;100(4):451-7. [PubMed:11256987]
  4. Nakamura A, Johns EJ, Imaizumi A, Yanagawa Y, Kohsaka T: Activation of beta(2)-adrenoceptor prevents shiga toxin 2-induced TNF-alpha gene transcription. J Am Soc Nephrol. 2001 Nov;12(11):2288-99. [PubMed:11675405]
  5. Chong LK, Suvarna K, Chess-Williams R, Peachell PT: Desensitization of beta2-adrenoceptor-mediated responses by short-acting beta2-adrenoceptor agonists in human lung mast cells. Br J Pharmacol. 2003 Feb;138(3):512-20. [PubMed:12569076]
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
  7. Riether C, Kavelaars A, Wirth T, Pacheco-Lopez G, Doenlen R, Willemen H, Heijnen CJ, Schedlowski M, Engler H: Stimulation of beta(2)-adrenergic receptors inhibits calcineurin activity in CD4(+) T cells via PKA-AKAP interaction. Brain Behav Immun. 2011 Jan;25(1):59-66. doi: 10.1016/j.bbi.2010.07.248. Epub 2010 Jul 30. [PubMed:20674738]
  8. Cooperberg BA, Breckenridge SM, Arbelaez AM, Cryer PE: Terbutaline and the prevention of nocturnal hypoglycemia in type 1 diabetes. Diabetes Care. 2008 Dec;31(12):2271-2. doi: 10.2337/dc08-0520. Epub 2008 Sep 9. [PubMed:18782903]
  9. Hochhaus G, Mollmann H: Pharmacokinetic/pharmacodynamic characteristics of the beta-2-agonists terbutaline, salbutamol and fenoterol. Int J Clin Pharmacol Ther Toxicol. 1992 Sep;30(9):342-62. [PubMed:1358833]
  10. Haahtela T, Jarvinen M, Kava T, Kiviranta K, Koskinen S, Lehtonen K, Nikander K, Persson T, Reinikainen K, Selroos O, et al.: Comparison of a beta 2-agonist, terbutaline, with an inhaled corticosteroid, budesonide, in newly detected asthma. N Engl J Med. 1991 Aug 8;325(6):388-92. [PubMed:2062329]
Details2. Beta-3 adrenergic receptor
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
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. Hoffmann C, Leitz MR, Oberdorf-Maass S, Lohse MJ, Klotz KN: Comparative pharmacology of human beta-adrenergic receptor subtypes--characterization of stably transfected receptors in CHO cells. Naunyn Schmiedebergs Arch Pharmacol. 2004 Feb;369(2):151-9. Epub 2004 Jan 17. [PubMed:14730417]
  2. Behr B, Hoffmann C, Ottolina G, Klotz KN: Novel mutants of the human beta1-adrenergic receptor reveal amino acids relevant for receptor activation. J Biol Chem. 2006 Jun 30;281(26):18120-5. Epub 2006 Apr 28. [PubMed:16648137]
Details3. Beta-1 adrenergic receptor
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Antagonist
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. Hoffmann C, Leitz MR, Oberdorf-Maass S, Lohse MJ, Klotz KN: Comparative pharmacology of human beta-adrenergic receptor subtypes--characterization of stably transfected receptors in CHO cells. Naunyn Schmiedebergs Arch Pharmacol. 2004 Feb;369(2):151-9. Epub 2004 Jan 17. [PubMed:14730417]

Enzymes

Details1. Cholinesterase
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Identical protein binding
Specific Function
Esterase with broad substrate specificity. Contributes to the inactivation of the neurotransmitter acetylcholine. Can degrade neurotoxic organophosphate esters.
Gene Name
BCHE
Uniprot ID
P06276
Uniprot Name
Cholinesterase
Molecular Weight
68417.575 Da
References
  1. Kovarik Z, Simeon-Rudolf V: Interaction of human butyrylcholinesterase variants with bambuterol and terbutaline. J Enzyme Inhib Med Chem. 2004 Apr;19(2):113-7. [PubMed:15449725]

Drug created on June 13, 2005 07:24 / Updated on July 13, 2019 00:35