Identification

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Name
Nadolol
Accession Number
DB01203  (APRD00301)
Type
Small Molecule
Groups
Approved
Description

Nadolol is a nonselective beta adrenal receptor blocker that is used to lower blood pressure.8,9 Nonselective beta adrenal receptor blockers may no longer be first line in the treatment of hypertension as newer generations of beta adrenal receptor blockers have higher selectivity and offer better rates of adverse effects.7

Nadolol was granted FDA approval on 10 December 1979.8

Structure
Thumb
Synonyms
  • Nadolol
Product Images
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
CorgardTablet20 mg/1OralBristol-Myers Squibb Company2006-02-162006-02-16Us
CorgardTablet20 mg/1OralPfizer Laboratories Div Pfizer Inc.1979-12-10Not applicableUs
CorgardTablet160 mg/1OralBristol-Myers Squibb Company2006-02-162006-02-16Us
CorgardTablet40 mg/1OralPhysicians Total Care, Inc.1979-12-102012-06-30Us
CorgardTablet80 mg/1OralUs World Meds, Llc2016-04-01Not applicableUs
CorgardTablet120 mg/1OralBristol-Myers Squibb Company2006-02-162006-02-16Us
CorgardTablet20 mg/1OralUs World Meds, Llc2016-04-01Not applicableUs
CorgardTablet40 mg/1OralUs World Meds, Llc2016-04-01Not applicableUs
CorgardTablet80 mg/1OralPfizer Laboratories Div Pfizer Inc.1979-12-10Not applicableUs
CorgardTablet80 mg/1OralBristol-Myers Squibb Company2006-02-162006-02-16Us
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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Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
NadololTablet80 mg/1OralCamber Pharmaceuticals2016-01-27Not applicableUs
NadololTablet80 mg/1OralLupin Pharmaceuticals, Inc.2017-10-05Not applicableUs
NadololTablet40 mg/1OralBayshore Pharmaceuticals LLC2019-07-26Not applicableUs
NadololTablet40 mg/1OralBlue Point Laboratories2014-02-05Not applicableUs
NadololTablet20 mg/1OralTeva Pharmaceuticals USA, Inc.2008-11-03Not applicableUs0093 423520180814 13942 19cnmde
NadololTablet20 mg/1OralAmneal Pharmaceuticals NY LLC2017-06-02Not applicableUs
NadololTablet80 mg/1OralPhysicians Total Care, Inc.2004-08-132010-06-30Us
NadololTablet20 mg/1OralInvaGen Pharmaceuticals Inc.2015-12-18Not applicableUs
NadololTablet80 mg/1OralIngenus Pharmaceuticals, LLC2018-06-08Not applicableUs
NadololTablet80 mg/1OralRebel Distributors2008-10-01Not applicableUs
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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Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
CorzideNadolol (80 mg/1) + Bendroflumethiazide (5 mg/1)TabletOralPfizer Laboratories Div Pfizer Inc1983-05-252019-10-31Us
CorzideNadolol (40 mg/1) + Bendroflumethiazide (5 mg/1)TabletOralPfizer Laboratories Div Pfizer Inc1983-05-252019-10-31Us
CorzideNadolol (40 mg/1) + Bendroflumethiazide (5 mg/1)TabletOralMonarch Pharmaceuticals, Inc.2006-10-102006-10-10Us
CorzideNadolol (80 mg/1) + Bendroflumethiazide (5 mg/1)TabletOralMonarch Pharmaceuticals, Inc.2006-10-102006-10-10Us
CorzideNadolol (80 mg/1) + Bendroflumethiazide (5 mg/1)TabletOralPhysicians Total Care, Inc.1983-05-252010-06-30Us
Corzide Tab W Nadolol 40mgNadolol (40 mg) + Bendroflumethiazide (5 mg)TabletOralSquibb Canada Inc., Division Of Bristol Myers Squibb Canada Inc.1987-12-311997-08-14Canada
Corzide Tab W Nadolol 80mgNadolol (80 mg) + Bendroflumethiazide (5 mg)TabletOralSquibb Canada Inc., Division Of Bristol Myers Squibb Canada Inc.1987-12-311997-08-14Canada
Nadolol and BendroflumethiazideNadolol (80 mg/1) + Bendroflumethiazide (5 mg/1)TabletOralMylan Pharmaceuticals2012-04-022012-08-31Us
Nadolol and BendroflumethiazideNadolol (40 mg/1) + Bendroflumethiazide (5 mg/1)TabletOralMylan Pharmaceuticals2012-04-022012-08-31Us
Nadolol and BendroflumethiazideNadolol (80 mg/1) + Bendroflumethiazide (5 mg/1)TabletOralImpax Generics2007-03-30Not applicableUs
International/Other Brands
Anabet / Solgol
Categories
UNII
FEN504330V
CAS number
42200-33-9
Weight
Average: 309.4006
Monoisotopic: 309.194008357
Chemical Formula
C17H27NO4
InChI Key
VWPOSFSPZNDTMJ-UCWKZMIHSA-N
InChI
InChI=1S/C17H27NO4/c1-17(2,3)18-9-12(19)10-22-16-6-4-5-11-7-14(20)15(21)8-13(11)16/h4-6,12,14-15,18-21H,7-10H2,1-3H3/t12?,14-,15+/m1/s1
IUPAC Name
(2R,3S)-5-[3-(tert-butylamino)-2-hydroxypropoxy]-1,2,3,4-tetrahydronaphthalene-2,3-diol
SMILES
CC(C)(C)NCC(O)COC1=CC=CC2=C1C[C@H](O)[C@H](O)C2

Pharmacology

Indication

Nadolol is indicated to treat angina pectoris and hypertension.8 Another product formulated with bendroflumethiazide is indicated to treat hypertension.9

Associated Conditions
Pharmacodynamics

Nadolol is a nonselective beta adrenal receptor blocker that is used to lower blood pressure.8,9 It has a long duration of action as it is usually taken once daily and a wide therapeutic index as patients start at doses of 40mg daily but may be increased to doses as high as 240mg daily.8,9 Patients taking nadolol should not aburptly stop taking it as this may lead to exacerbation of ischemic heart disease.8,9

Mechanism of action

Although nadolol is described as a non selective beta blocker, it does not interact with beta 3 adrenal receptors.1 Antagonism of beta-1 and beta-2 adrenoceptors in the heart inhibits cyclic AMP and its signalling pathway, decreasing the strength and speed of contractions as well as the speed of relaxation and conduction.7 Antagonism of beta-2 adrenoceptors in the smooth muscle cells of the vasculature inhibits their relaxation, leading to an increase in peripheral vascular resistance and reducing the risk of severe hypotension.7 The increase in peripheral vascular resistance may contribute to the decrease in insulin sensitivity associated with nadolol use.6 Antagonism of beta-1 adrenoceptors in the juxtaglomerular apparatus of the kidney inhibits the release of renin, and therefore angiotensin II mediated vasoconstriction, aldosterone mediated water retention, and the release of epinephrine.7 Antagonism of beta-2 adrenoceptors in the liver and skeletal muscle inhibits glycogenolysis, in the lungs prevents bronchodilation, and in the pancrease inhibits insulin release.7

TargetActionsOrganism
ABeta-1 adrenergic receptor
antagonist
Humans
UBeta-2 adrenergic receptor
antagonist
Humans
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

Oral doses of nadolol are approximately 30% absorbed.8,9 In healthy subjects, nadolol has a Tmax of 2.7h with a Cmax or 69±15ng/mL following a 60mg oral dose and 132±27ng/mL after a 120mg oral dose.2 The AUC following a 60mg oral dose was 1021ng*h/mL and following a 120mg oral dose was 1913±382ng*h/mL.2

Volume of distribution

In healthy subjects, the volume of distribution of nadolol is 147-157L.3

Protein binding

Nadolol is approximately 30% bound to plasma protein.8,9 Nadolol binds to alpha-1-acid glycoprotein in plasma.4,5

Metabolism

Nadolol is not metabolized by the liver in humans.3,8,9

Route of elimination

Nadolol is not metabolized in the liver and excreted mainly in the urine.8,9 In healthy subjects, following intravenous dosing, 60% of a dose is eliminated in the urine and 15% in the feces after 72 hours.3 The remainder of the dose is expected to be eliminated in the feces afterwards.3

Half life

The half life of nadolol is 20 to 24 hours.8,9

Clearance

In healthy subjects, the total body clearance of nadolol is 219-250mL/min and the renal clearance is 131-150mL/min.3

Toxicity

The oral LD50 in mice is 4500mg/kg.10

Patients experiencing an overdose may present with bradycardia, cardiac failure, hypotension, and bronchospasm.8,9 An overdose may be treated with atropine for bradycardia, digitalis and diuretics for cardiac failure, vasopressors for hypotension, and beta-2 stimulants for bronchospasms, as well as gastric lavage and hemodialysis.8,9

Affected organisms
  • Humans and other mammals
Pathways
PathwayCategory
Nadolol 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
1-(2-Phenylethyl)-4-phenyl-4-acetoxypiperidineThe metabolism of Nadolol can be decreased when combined with 1-(2-Phenylethyl)-4-phenyl-4-acetoxypiperidine.
1-(3-Mercapto-2-Methyl-Propionyl)-Pyrrolidine-2-Carboxylic Acid1-(3-Mercapto-2-Methyl-Propionyl)-Pyrrolidine-2-Carboxylic Acid may decrease the antihypertensive activities of Nadolol.
1-benzylimidazole1-benzylimidazole may decrease the antihypertensive activities of Nadolol.
1,10-Phenanthroline1,10-Phenanthroline may increase the bradycardic activities of Nadolol.
2,4-thiazolidinedioneThe therapeutic efficacy of 2,4-thiazolidinedione can be increased when used in combination with Nadolol.
2,5-Dimethoxy-4-ethylamphetamineThe therapeutic efficacy of Nadolol can be decreased when used in combination with 2,5-Dimethoxy-4-ethylamphetamine.
2,5-Dimethoxy-4-ethylthioamphetamineThe therapeutic efficacy of Nadolol can be decreased when used in combination with 2,5-Dimethoxy-4-ethylthioamphetamine.
25-desacetylrifapentineThe metabolism of Nadolol can be increased when combined with 25-desacetylrifapentine.
4-Bromo-2,5-dimethoxyamphetamineThe therapeutic efficacy of Nadolol can be decreased when used in combination with 4-Bromo-2,5-dimethoxyamphetamine.
4-Bromo-2,5-dimethoxyphenethylamineThe therapeutic efficacy of 4-Bromo-2,5-dimethoxyphenethylamine can be decreased when used in combination with Nadolol.
Additional Data Available
  • Extended Description
    Extended Description

    Extended description of the mechanism of action and particular properties of each drug interaction.

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  • Severity
    Severity

    A severity rating for each drug interaction, from minor to major.

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  • Evidence Level
    Evidence Level

    A rating for the strength of the evidence supporting each drug interaction.

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  • Action
    Action

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Food Interactions
  • Avoid alcohol.
  • Avoid natural licorice.
  • Magnesium, potassium and zinc needs increased.
  • Take without regard to meals.

References

Synthesis Reference
US3935267
General References
  1. Cernecka H, Sand C, Michel MC: The odd sibling: features of beta3-adrenoceptor pharmacology. Mol Pharmacol. 2014 Nov;86(5):479-84. doi: 10.1124/mol.114.092817. Epub 2014 Jun 2. [PubMed:24890609]
  2. Schafer-Korting M, Bach N, Knauf H, Mutschler E: Pharmacokinetics of nadolol in healthy subjects. Eur J Clin Pharmacol. 1984;26(1):125-7. [PubMed:6714285]
  3. Morrison RA, Singhvi SM, Creasey WA, Willard DA: Dose proportionality of nadolol pharmacokinetics after intravenous administration to healthy subjects. Eur J Clin Pharmacol. 1988;33(6):625-8. [PubMed:3366166]
  4. Patel L, Johnson A, Turner P: Nadolol binding to human serum proteins. J Pharm Pharmacol. 1984 Jun;36(6):414-5. doi: 10.1111/j.2042-7158.1984.tb04413.x. [PubMed:6146679]
  5. Israili ZH, Dayton PG: Human alpha-1-glycoprotein and its interactions with drugs. Drug Metab Rev. 2001 May;33(2):161-235. doi: 10.1081/DMR-100104402 . [PubMed:11495502]
  6. Lee WG, Murphy R, McCall JL, Gane EJ, Soop M, Tura A, Plank LD: Nadolol reduces insulin sensitivity in liver cirrhosis: a randomized double-blind crossover trial. Diabetes Metab Res Rev. 2017 Mar;33(3). doi: 10.1002/dmrr.2859. Epub 2016 Nov 10. [PubMed:27667324]
  7. Gorre F, Vandekerckhove H: Beta-blockers: focus on mechanism of action. Which beta-blocker, when and why? Acta Cardiol. 2010 Oct;65(5):565-70. doi: 10.2143/AC.65.5.2056244. [PubMed:21125979]
  8. FDA Approved Drug Products: Nadolol Oral Tablets [Link]
  9. FDA Approved Drug Products: Nadolol and Bendroflumethiazide Oral Tablets [Link]
  10. The Human Metabolome Database: Nadolol MSDS [Link]
External Links
Human Metabolome Database
HMDB0015334
KEGG Drug
D00432
PubChem Compound
39147
PubChem Substance
46505509
ChemSpider
35815
BindingDB
25766
ChEBI
7444
ChEMBL
CHEMBL649
Therapeutic Targets Database
DAP000122
PharmGKB
PA450573
Guide to Pharmacology
GtP Drug Page
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
PDRhealth
PDRhealth Drug Page
Wikipedia
Nadolol
ATC Codes
C07BA12 — Nadolol and thiazidesC07AA12 — Nadolol
AHFS Codes
  • 24:24.00 — Beta-adrenergic Blocking Agents
MSDS
Download (74.1 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1CompletedNot AvailableHealthy Volunteers2
1CompletedTreatmentHigh Blood Pressure (Hypertension) / Migraine / Thoracic Pain1
1, 2CompletedTreatmentAsthma Bronchial1
2Active Not RecruitingTreatmentMild Persistent Asthma, Uncomplicated1
2CompletedTreatmentCessation, Smoking1
2CompletedTreatmentInfantile Hemangiomas1
3RecruitingTreatmentInfantile Hemangiomas1
3WithdrawnPreventionHemorrhage, Gastrointestinal / Portal Hypertension1
4CompletedPreventionHemorrhage, Gastrointestinal / Liver Cirrhosis / Portal Hypertension1
4CompletedPreventionLiver Cirrhosis / Variceal Bleeding1
4CompletedPreventionVariceal Rebleeding1
4CompletedTreatmentMigraine1
4Unknown StatusPreventionGastric Variceal Bleeding / Liver Cirrhosis and Hepatoma1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
  • Apothecon
  • Cardinal Health
  • Dispensing Solutions
  • Diversified Healthcare Services Inc.
  • E.R. Squibb and Sons LLC
  • Emcure Pharmaceuticals Ltd.
  • Global Pharmaceuticals
  • Impax Laboratories Inc.
  • Ivax Pharmaceuticals
  • King Pharmaceuticals Inc.
  • Major Pharmaceuticals
  • Mead Johnson and Co.
  • Murfreesboro Pharmaceutical Nursing Supply
  • Mylan
  • Pharmaceutical Utilization Management Program VA Inc.
  • Pharmedix
  • Physicians Total Care Inc.
  • Professional Co.
  • Qualitest
  • Quality Care
  • Resource Optimization and Innovation LLC
  • Sandhills Packaging Inc.
  • Sandoz
  • Teva Pharmaceutical Industries Ltd.
  • UDL Laboratories
Dosage forms
FormRouteStrength
TabletOral120 mg/1
TabletOral
TabletOral160 mg
TabletOral160 mg/1
TabletOral20 mg/1
TabletOral40 mg/1
TabletOral40 mg
TabletOral80 mg/1
TabletOral80 mg
TabletOral
Prices
Unit descriptionCostUnit
Nadolol powder94.8USD g
Corgard 160 mg tablet4.4USD tablet
Corgard 80 mg tablet4.33USD tablet
Corgard 120 mg tablet3.96USD tablet
Corgard 40 mg tablet3.11USD tablet
Corgard 20 mg tablet3.04USD tablet
Nadolol 160 mg tablet2.25USD tablet
Nadolol 80 mg tablet1.45USD tablet
Apo-Nadol 160 mg Tablet1.26USD tablet
Nadolol 40 mg tablet1.07USD tablet
Naldol 80 mg tablet1.03USD tablet
Nadolol 20 mg tablet0.92USD tablet
Apo-Nadol 80 mg Tablet0.37USD tablet
Novo-Nadolol 80 mg Tablet0.37USD tablet
Apo-Nadol 40 mg Tablet0.26USD tablet
Novo-Nadolol 40 mg Tablet0.26USD tablet
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)124-130http://www.chemspider.com/Chemical-Structure.35815.html?rid=dffe98eb-8fd9-4c28-9a11-8dfe26bcaad3
boiling point (°C)526.437http://www.chemspider.com/Chemical-Structure.35815.html?rid=dffe98eb-8fd9-4c28-9a11-8dfe26bcaad3
water solubility8330 mg/L (at 25 °C)MCFARLAND,JW ET AL. (2001)
logP0.81SANGSTER (1994)
Caco2 permeability-5.41ADME Research, USCD
pKa9.67MERCK INDEX (2001)
Predicted Properties
PropertyValueSource
Water Solubility2.25 mg/mLALOGPS
logP1.23ALOGPS
logP0.87ChemAxon
logS-2.1ALOGPS
pKa (Strongest Acidic)13.59ChemAxon
pKa (Strongest Basic)9.76ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count5ChemAxon
Hydrogen Donor Count4ChemAxon
Polar Surface Area81.95 Å2ChemAxon
Rotatable Bond Count6ChemAxon
Refractivity85.53 m3·mol-1ChemAxon
Polarizability34.63 Å3ChemAxon
Number of Rings2ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9788
Blood Brain Barrier-0.966
Caco-2 permeable-0.8957
P-glycoprotein substrateSubstrate0.8317
P-glycoprotein inhibitor IInhibitor0.6192
P-glycoprotein inhibitor IINon-inhibitor0.7842
Renal organic cation transporterNon-inhibitor0.8736
CYP450 2C9 substrateNon-substrate0.7934
CYP450 2D6 substrateSubstrate0.7284
CYP450 3A4 substrateNon-substrate0.5456
CYP450 1A2 substrateNon-inhibitor0.9046
CYP450 2C9 inhibitorNon-inhibitor0.9106
CYP450 2D6 inhibitorNon-inhibitor0.9231
CYP450 2C19 inhibitorNon-inhibitor0.9026
CYP450 3A4 inhibitorNon-inhibitor0.8308
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.8072
Ames testNon AMES toxic0.9133
CarcinogenicityNon-carcinogens0.8934
BiodegradationNot ready biodegradable1.0
Rat acute toxicity1.7972 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9455
hERG inhibition (predictor II)Inhibitor0.5781
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/MSNot Available
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-03di-0019000000-fdb4087c676d8d8d4a8e
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0udi-0092000000-e09452da687c6073a284
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0uk9-4690000000-81baaf08e07647128956
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0kmi-4930000000-adbaba8c066f6c5c5558
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0aba-3900000000-3784678375e682bb5b2f
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-05te-3900000000-52bc796915dc7eb2ff30
MS/MS Spectrum - , positiveLC-MS/MSsplash10-0ik9-0379000000-d94563052914b6b9e468
MS/MS Spectrum - , positiveLC-MS/MSsplash10-0k92-2920000000-2a6eb574de4bc8d52292

Taxonomy

Description
This compound belongs to the class of organic compounds known as tetralins. These are polycyclic aromatic compounds containing a tetralin moiety, which consists of a benzene fused to a cyclohexane.
Kingdom
Organic compounds
Super Class
Benzenoids
Class
Tetralins
Sub Class
Not Available
Direct Parent
Tetralins
Alternative Parents
Alkyl aryl ethers / Secondary alcohols / 1,2-aminoalcohols / Dialkylamines / Organopnictogen compounds / Hydrocarbon derivatives
Substituents
Tetralin / Alkyl aryl ether / 1,2-aminoalcohol / Secondary alcohol / Secondary aliphatic amine / Ether / Secondary amine / Organic nitrogen compound / Organooxygen compound / Organonitrogen compound
Molecular Framework
Aromatic homopolycyclic compounds
External Descriptors
Not Available

Targets

Kind
Protein
Organism
Humans
Pharmacological action
Yes
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. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
  2. Wheeldon NM, McDevitt DG, Lipworth BJ: The effects of lower than conventional doses of oral nadolol on relative beta 1/beta 2-adrenoceptor blockade. Br J Clin Pharmacol. 1994 Aug;38(2):103-8. [PubMed:7981009]
  3. Koshiji M, Ito H, Minatoguchi S, Watanabe H, Imai Y, Kakami M, Hirakawa S: A comparison of guanfacine, bunazosin, atenolol and nadolol on blood pressure and plasma noradrenaline responses to cold pressor testing. Clin Exp Pharmacol Physiol. 1992 Jul;19(7):481-8. [PubMed:1354084]
  4. Varma DR, Shen H, Deng XF, Peri KG, Chemtob S, Mulay S: Inverse agonist activities of beta-adrenoceptor antagonists in rat myocardium. Br J Pharmacol. 1999 Jun;127(4):895-902. [PubMed:10433496]
  5. Varma DR: Ligand-independent negative chronotropic responses of rat and mouse right atria to beta-adrenoceptor antagonists. Can J Physiol Pharmacol. 1999 Dec;77(12):943-9. [PubMed:10606440]
  6. Wheeldon NM, McDevitt DG, Lipworth BJ: Cardiac effects of the beta 3-adrenoceptor agonist BRL35135 in man. Br J Clin Pharmacol. 1994 Apr;37(4):363-9. [PubMed:7912539]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Antagonist
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. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
  2. Wheeldon NM, McDevitt DG, Lipworth BJ: The effects of lower than conventional doses of oral nadolol on relative beta 1/beta 2-adrenoceptor blockade. Br J Clin Pharmacol. 1994 Aug;38(2):103-8. [PubMed:7981009]
  3. Ozakca I, Arioglu E, Guner S, Altan VM, Ozcelikay AT: Role of beta-3-adrenoceptor in catecholamine-induced relaxations in gastric fundus from control and diabetic rats. Pharmacology. 2007;80(4):227-38. Epub 2007 Jul 6. [PubMed:17622774]
  4. Liu YL, Toubro S, Astrup A, Stock MJ: Contribution of beta 3-adrenoceptor activation to ephedrine-induced thermogenesis in humans. Int J Obes Relat Metab Disord. 1995 Sep;19(9):678-85. [PubMed:8574280]
  5. Wheeldon NM, McDevitt DG, Lipworth BJ: Evaluation of in vivo partial beta 1/beta 2-agonist activity: a dose-ranging study with carteolol. Br J Clin Pharmacol. 1992 Apr;33(4):411-6. [PubMed:1349493]
  6. Varma DR, Shen H, Deng XF, Peri KG, Chemtob S, Mulay S: Inverse agonist activities of beta-adrenoceptor antagonists in rat myocardium. Br J Pharmacol. 1999 Jun;127(4):895-902. [PubMed:10433496]

Carriers

Kind
Protein group
Organism
Humans
Pharmacological action
Unknown
Actions
Binder
General Function
Not Available
Specific Function
Functions as transport protein in the blood stream. Binds various ligands in the interior of its beta-barrel domain. Also binds synthetic drugs and influences their distribution and availability in...

Components:
References
  1. Patel L, Johnson A, Turner P: Nadolol binding to human serum proteins. J Pharm Pharmacol. 1984 Jun;36(6):414-5. doi: 10.1111/j.2042-7158.1984.tb04413.x. [PubMed:6146679]
  2. Israili ZH, Dayton PG: Human alpha-1-glycoprotein and its interactions with drugs. Drug Metab Rev. 2001 May;33(2):161-235. doi: 10.1081/DMR-100104402 . [PubMed:11495502]

Transporters

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Xenobiotic-transporting atpase activity
Specific Function
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name
ABCB1
Uniprot ID
P08183
Uniprot Name
Multidrug resistance protein 1
Molecular Weight
141477.255 Da
References
  1. Terao T, Hisanaga E, Sai Y, Tamai I, Tsuji A: Active secretion of drugs from the small intestinal epithelium in rats by P-glycoprotein functioning as an absorption barrier. J Pharm Pharmacol. 1996 Oct;48(10):1083-9. [PubMed:8953513]
  2. Misaka S, Knop J, Singer K, Hoier E, Keiser M, Muller F, Glaeser H, Konig J, Fromm MF: The Nonmetabolized beta-Blocker Nadolol Is a Substrate of OCT1, OCT2, MATE1, MATE2-K, and P-Glycoprotein, but Not of OATP1B1 and OATP1B3. Mol Pharm. 2016 Feb 1;13(2):512-9. doi: 10.1021/acs.molpharmaceut.5b00733. Epub 2016 Jan 19. [PubMed:26702643]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Transcription factor that binds to the octamer motif (5'-ATTTGCAT-3') and activates the promoters of the genes for some small nuclear RNAs (snRNA) and of genes such as those for histone H2B and immunoglobulins. Modulates transcription transactivation by NR3C1, AR and PGR (By similarity). In case of human herpes simplex virus (HSV) infection, POU2F1 forms a multiprotein-DNA complex with the viral transactivator protein VP16 and HCFC1 thereby enabling the transcription of the viral immediate early genes.
Specific Function
Dna binding
Gene Name
POU2F1
Uniprot ID
P14859
Uniprot Name
POU domain, class 2, transcription factor 1
Molecular Weight
76470.82 Da
References
  1. Misaka S, Knop J, Singer K, Hoier E, Keiser M, Muller F, Glaeser H, Konig J, Fromm MF: The Nonmetabolized beta-Blocker Nadolol Is a Substrate of OCT1, OCT2, MATE1, MATE2-K, and P-Glycoprotein, but Not of OATP1B1 and OATP1B3. Mol Pharm. 2016 Feb 1;13(2):512-9. doi: 10.1021/acs.molpharmaceut.5b00733. Epub 2016 Jan 19. [PubMed:26702643]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Transcriptional activator activity, rna polymerase ii core promoter proximal region sequence-specific binding
Specific Function
Transcription factor that specifically binds to the octamer motif (5'-ATTTGCAT-3'). Regulates transcription in a number of tissues in addition to activating immunoglobulin gene expression. Modulate...
Gene Name
POU2F2
Uniprot ID
P09086
Uniprot Name
POU domain, class 2, transcription factor 2
Molecular Weight
51208.51 Da
References
  1. Misaka S, Knop J, Singer K, Hoier E, Keiser M, Muller F, Glaeser H, Konig J, Fromm MF: The Nonmetabolized beta-Blocker Nadolol Is a Substrate of OCT1, OCT2, MATE1, MATE2-K, and P-Glycoprotein, but Not of OATP1B1 and OATP1B3. Mol Pharm. 2016 Feb 1;13(2):512-9. doi: 10.1021/acs.molpharmaceut.5b00733. Epub 2016 Jan 19. [PubMed:26702643]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Monovalent cation:proton antiporter activity
Specific Function
Solute transporter for tetraethylammonium (TEA), 1-methyl-4-phenylpyridinium (MPP), cimetidine, N-methylnicotinamide (NMN), metformin, creatinine, guanidine, procainamide, topotecan, estrone sulfat...
Gene Name
SLC47A1
Uniprot ID
Q96FL8
Uniprot Name
Multidrug and toxin extrusion protein 1
Molecular Weight
61921.585 Da
References
  1. Misaka S, Knop J, Singer K, Hoier E, Keiser M, Muller F, Glaeser H, Konig J, Fromm MF: The Nonmetabolized beta-Blocker Nadolol Is a Substrate of OCT1, OCT2, MATE1, MATE2-K, and P-Glycoprotein, but Not of OATP1B1 and OATP1B3. Mol Pharm. 2016 Feb 1;13(2):512-9. doi: 10.1021/acs.molpharmaceut.5b00733. Epub 2016 Jan 19. [PubMed:26702643]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Drug transmembrane transporter activity
Specific Function
Solute transporter for tetraethylammonium (TEA), 1-methyl-4-phenylpyridinium (MPP), cimetidine, N-methylnicotinamide, metformin, creatinine, guanidine, procainamide, topotecan, estrone sulfate, acy...
Gene Name
SLC47A2
Uniprot ID
Q86VL8
Uniprot Name
Multidrug and toxin extrusion protein 2
Molecular Weight
65083.915 Da
References
  1. Misaka S, Knop J, Singer K, Hoier E, Keiser M, Muller F, Glaeser H, Konig J, Fromm MF: The Nonmetabolized beta-Blocker Nadolol Is a Substrate of OCT1, OCT2, MATE1, MATE2-K, and P-Glycoprotein, but Not of OATP1B1 and OATP1B3. Mol Pharm. 2016 Feb 1;13(2):512-9. doi: 10.1021/acs.molpharmaceut.5b00733. Epub 2016 Jan 19. [PubMed:26702643]

Drug created on June 13, 2005 07:24 / Updated on October 14, 2019 08:02