NAV

Pindolol

Identification

Summary

Pindolol is a beta adrenoceptor antagonist used to treat hypertension, edema, ventricular tachycardias, and atrial fibrillation.

Brand Names
Viskazide, Visken
Generic Name
Pindolol
DrugBank Accession Number
DB00960
Background

Pindolol is a first generation non-selective beta blocker used in the treatment of hypertension.9 Early research into the use of pindolol found it had chronotropic effects, and so further investigation focused on the treatment of arrhythmia.6 Research into pindolol's use in the treatment of hypertension began in the early 1970s.7

Pindolol was granted FDA approval on 3 September 1982.8

Type
Small Molecule
Groups
Approved, Investigational
Structure
3D
Similar Structures
Weight
Average: 248.3208
Monoisotopic: 248.152477894
Chemical Formula
C14H20N2O2
Synonyms
  • 1-(1H-indol-4-yloxy)-3-(isopropylamino)propan-2-ol
  • 1-(1H-indol-4-yloxy)-3-(propan-2-ylamino)-propan-2-ol
  • 1-(1H-indol-4-yloxy)-3-[(1-methylethyl)amino]propan-2-ol
  • 4-(2-hydroxy-3-isopropylaminopropoxy)-indole
  • Pindolol
  • Pindololum
External IDs
  • BRN 1536506
  • CCRIS 9215
  • DL-LB-46
  • HSDB 6539
  • LB 46
  • LB-46
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Pharmacology

Indication

Pindolol is indicated in the management of hypertension.9 In Canada, it is also indicated in the prophylaxis of angina.10

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Associated Conditions
Indication TypeIndicationCombined Product DetailsApproval LevelAge GroupPatient CharacteristicsDose Form
Prophylaxis ofAngina pectoris••••••••••••••••••
Used in combination to treatAtrial fibrillationRegimen in combination with: Digoxin (DB00390)••• •••••
Adjunct therapy in treatment ofDepression••• •••••
Used in combination to manageHypertension••••••••••••••••••
Management ofHypertension••••••••••••••••••
Contraindications & Blackbox Warnings
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Pharmacodynamics

Pindolol is a nonselective beta blocker indicated in the management of hypertension9 and prophylaxis of angina.10 It has a short duration of action as it is given twice daily, and a wide therapeutic window as doses can range from 10-60 mg/day.9 Patients should be counselled regarding the risk of cardiac failure, exacerbating ischemic heart disease with sudden withdrawal, nonallergic bronchospasm, masking hypoglycemia in diabetics, and masking hyperthyroidism.9

Mechanism of action

The beta-1 adrenoceptor is a G-protein-coupled receptor.1 Agonism of the beta-1 adrenoceptor allows the Gs subunit to upregulate adenylyl cyclase, converting ATP to cyclic AMP (cAMP).1 Increased concentrations of cAMP activate cAMP-dependant kinase A, phosphorylating calcium channels, raising intracellular calcium, increasing calcium exchange through the sarcoplasmic reticulum, and increasing cardiac inotropy.1 cAMP-dependant kinase A also phosphorylates myosin light chains, increasing smooth muscle contractility.1 Increased smooth muscle contractility in the kidney releases renin.1

Pindolol is a non-selective beta blocker.3 Blocking beta-1 adrenergic receptors in the heart results in decreased heart rate and blood pressure.3 By blocking beta-1 receptors in the juxtaglomerular apparatus, pindolol inhibits the release of renin, which inhibits angiotensin II and aldosterone release.1,2 Reduced angiotensin II inhibits vasoconstriction and reduced aldosterone inhibits water retention.1,2

Beta-2 adrenoceptors located in the kidneys and peripheral blood vessels use a similar mechanism to activate cAMP-dependant kinase A to increase smooth muscle contractility.4 Blocking of the beta-2 adrenoceptor relaxes smooth muscle, leading to vasodilation.4

TargetActionsOrganism
ABeta-1 adrenergic receptor
partial agonist
Humans
ABeta-2 adrenergic receptor
partial agonist
Humans
UBeta-3 adrenergic receptor
agonist
Humans
U5-hydroxytryptamine receptor 1A
antagonist
inhibitor
ligand
Humans
U5-hydroxytryptamine receptor 1B
other/unknown
ligand
Humans
Absorption

The mean oral bioavailability of pindolol is 87-92%.10 A 5 mg oral dose reaches a Cmax of 33.1 ± 5.2 ng/mL, with a Tmax of 1-2 hours.10

Volume of distribution

The volume of distribution of pindolol is approximately 2-3 L/kg.9,10

Protein binding

Pindolol is 40% bound to proteins in plasma.9 Pindolol mainly binds more strongly to alpha-1-acid glycoprotein than it does to serum albumin.5

Metabolism

30-40% of a dose of pindolol is not metabolized.10 The remainder is hydroxylated and subsequently undergoes glucuronidation or sulfate conjugation.10

Hover over products below to view reaction partners

Route of elimination

80% of an oral dose is eliminated in the urine,10 with 25-40% of the dose as the unchanged parent compound.9 6-9% of an intravenous dose is eliminated in the feces.9 Overall, 60-65% of a dose is eliminated as glucuronide and sulfate metabolites.9

Half-life

The half life of pindolol varies from 3-4 hours10 but can be as high as 30 hours in patients with cirrhosis of the liver.9

Clearance

In otherwise healthy patients, the systemic clearance of pindolol is 400-500 mL/min.10 In patients with cirrhosis, the clearance of pindolol varies from 50-300 mL/min.9

Adverse Effects
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Toxicity

Patients experiencing an overdose may experience excessive bradycardia, cardiac failure, hypotension, and bronchospasm.9 Initiate treatment with symptomatic and supportive measures.9

Pathways
PathwayCategory
Pindolol Action PathwayDrug action
Pharmacogenomic Effects/ADRs Browse all" title="About SNP Mediated Effects/ADRs" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">
Not Available

Interactions

Drug Interactions Learn More" title="About Drug Interactions" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
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
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interactions in your software
1,2-BenzodiazepineThe risk or severity of CNS depression can be increased when Pindolol is combined with 1,2-Benzodiazepine.
AbacavirPindolol may decrease the excretion rate of Abacavir which could result in a higher serum level.
AbaloparatideThe risk or severity of adverse effects can be increased when Pindolol is combined with Abaloparatide.
AbataceptThe metabolism of Pindolol can be increased when combined with Abatacept.
AbirateroneThe metabolism of Pindolol can be decreased when combined with Abiraterone.
Food Interactions
  • Avoid alcohol. Alcohol may aggravate signs and symptoms of overdose.
  • Take with or without food. Food does not significantly affect absorption.

Products

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Product Images
International/Other Brands
Betapindol / Blockin L / Blocklin L / Calvisken / Decreten / Durapindol / Glauco-Visken / Pectobloc / Pinbetol / Prinodolol / Pynastin
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Pindolol-10 Tab 10mgTablet10 mgOralPro Doc Limitee1989-12-312020-03-09Canada flag
Pindolol-15 Tab 15mgTablet15 mgOralPro Doc Limitee1989-12-312012-07-23Canada flag
Pindolol-5 Tab 5mgTablet5 mgOralPro Doc Limitee1989-12-312020-03-09Canada flag
ViskenTablet5 mg/1OralNovartis Pharmaceuticals Corporation1982-09-032019-09-10US flag
ViskenTablet10 mgOralXediton Pharmaceuticals Inc1978-12-31Not applicableCanada flag
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Apo-pindol Tab 10mgTablet10 mgOralApotex Corporation1988-12-31Not applicableCanada flag
Apo-pindol Tab 15mgTablet15 mgOralApotex Corporation1988-12-31Not applicableCanada flag
Apo-pindol Tab 5mgTablet5 mgOralApotex Corporation1988-12-31Not applicableCanada flag
Dom-pindololTablet15 mgOralDominion Pharmacal1998-09-17Not applicableCanada flag
Dom-pindololTablet10 mgOralDominion Pharmacal1998-09-172018-10-10Canada flag
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
ViskazidePindolol (10 mg) + Hydrochlorothiazide (50 mg)TabletOralXediton Pharmaceuticals Inc1983-12-31Not applicableCanada flag
ViskazidePindolol (10 mg) + Hydrochlorothiazide (25 mg)TabletOralXediton Pharmaceuticals Inc1983-12-31Not applicableCanada flag

Categories

ATC Codes
C07CA03 — Pindolol and other diureticsC07AA03 — Pindolol
Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
This compound belongs to the class of organic compounds known as indoles. These are compounds containing an indole moiety, which consists of pyrrole ring fused to benzene to form 2,3-benzopyrrole.
Kingdom
Organic compounds
Super Class
Organoheterocyclic compounds
Class
Indoles and derivatives
Sub Class
Indoles
Direct Parent
Indoles
Alternative Parents
Alkyl aryl ethers / Benzenoids / Pyrroles / Heteroaromatic compounds / Secondary alcohols / 1,2-aminoalcohols / Dialkylamines / Azacyclic compounds / Organopnictogen compounds / Hydrocarbon derivatives
Substituents
1,2-aminoalcohol / Alcohol / Alkyl aryl ether / Amine / Aromatic heteropolycyclic compound / Azacycle / Benzenoid / Ether / Heteroaromatic compound / Hydrocarbon derivative
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
indoles, secondary amine (CHEBI:8214)
Affected organisms
  • Humans and other mammals

Chemical Identifiers

UNII
BJ4HF6IU1D
CAS number
13523-86-9
InChI Key
JZQKKSLKJUAGIC-UHFFFAOYSA-N
InChI
InChI=1S/C14H20N2O2/c1-10(2)16-8-11(17)9-18-14-5-3-4-13-12(14)6-7-15-13/h3-7,10-11,15-17H,8-9H2,1-2H3
IUPAC Name
1-(1H-indol-4-yloxy)-3-[(propan-2-yl)amino]propan-2-ol
SMILES
CC(C)NCC(O)COC1=CC=CC2=C1C=CN2

References

Synthesis Reference
US3471515
General References
  1. Alhayek S, Preuss CV: Beta 1 Receptors . [Article]
  2. Blumenfeld JD, Sealey JE, Mann SJ, Bragat A, Marion R, Pecker MS, Sotelo J, August P, Pickering TG, Laragh JH: Beta-adrenergic receptor blockade as a therapeutic approach for suppressing the renin-angiotensin-aldosterone system in normotensive and hypertensive subjects. Am J Hypertens. 1999 May;12(5):451-9. doi: 10.1016/s0895-7061(99)00005-9. [Article]
  3. Clark BJ, Menninger K, Bertholet A: Pindolol--the pharmacology of a partial agonist. Br J Clin Pharmacol. 1982;13(Suppl 2):149S-158S. doi: 10.1111/j.1365-2125.1982.tb01904.x. [Article]
  4. Ferguson SS, Feldman RD: beta-adrenoceptors as molecular targets in the treatment of hypertension. Can J Cardiol. 2014 May;30(5 Suppl):S3-8. doi: 10.1016/j.cjca.2014.01.017. Epub 2014 Feb 12. [Article]
  5. Belpaire FM, Bogaert MG, Rosseneu M: Binding of beta-adrenoceptor blocking drugs to human serum albumin, to alpha 1-acid glycoprotein and to human serum. Eur J Clin Pharmacol. 1982;22(3):253-6. doi: 10.1007/BF00545224. [Article]
  6. Robak J, Gryglewski R: Influence of INPEA, pindolol and propranolol on the chronotropic and metabolic responses to -adrenergic stimulation in intact rats. Biochem Pharmacol. 1971 Oct;20(10):2749-58. doi: 10.1016/0006-2952(71)90184-5. [Article]
  7. Walter I, Kusus T, Lydtin H: [Clinical test of a new beta-receptor blockader in labile hypertension]. Verh Dtsch Ges Inn Med. 1971;77:940-3. [Article]
  8. FDA Approved Drug Products: Visken (Pindolol) Oral Tablets [Link]
  9. Dailymed: Pindolol Oral Tablet [Link]
  10. Health Canada Approved Drug Products: Apo-Pindolol (Pindolol) Oral Tablet [Link]
Human Metabolome Database
HMDB0015095
KEGG Drug
D00513
KEGG Compound
C07445
PubChem Compound
4828
PubChem Substance
46508362
ChemSpider
4662
BindingDB
50019443
RxNav
8332
ChEBI
8214
ChEMBL
CHEMBL500
Therapeutic Targets Database
DAP000025
PharmGKB
PA450966
Guide to Pharmacology
GtP Drug Page
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
PDRhealth
PDRhealth Drug Page
Wikipedia
Pindolol
MSDS
Download (74.7 KB)

Clinical Trials

Clinical Trials Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
PhaseStatusPurposeConditionsCount
4CompletedOtherCardiac Failure / Cardiovascular Disease (CVD) / Heart Failure / Heart Failure With Preserved Ejection Fraction (HFpEF) / Heart Failure, Diastolic2
2CompletedTreatmentAntidepressant Treatment Response / Major Depressive Disorder (MDD)1
2RecruitingBasic ScienceHealthy Subjects (HS)1
2, 3TerminatedTreatmentUnipolar Depression1
1CompletedBasic ScienceAmphetamine-Related Disorders / Moods Disorders / Substance Related Disorders1

Pharmacoeconomics

Manufacturers
  • Genpharm pharmaceuticals inc
  • Ivax pharmaceuticals inc sub teva pharmaceuticals usa
  • Mutual pharmaceutical co inc
  • Mylan pharmaceuticals inc
  • Nostrum laboratories inc
  • Purepac pharmaceutical co
  • Sandoz inc
  • Teva pharmaceuticals usa inc
  • Watson laboratories inc
  • Novartis pharmaceuticals corp
Packagers
  • Advanced Pharmaceutical Services Inc.
  • Ivax Pharmaceuticals
  • Major Pharmaceuticals
  • Merckle GmbH
  • Murfreesboro Pharmaceutical Nursing Supply
  • Mylan
  • Novartis AG
  • Novopharm Ltd.
  • Pharmaceutical Utilization Management Program VA Inc.
  • Physicians Total Care Inc.
  • Qualitest
  • Sandhills Packaging Inc.
Dosage Forms
FormRouteStrength
TabletOral
TabletOral10 mg/1
TabletOral5 mg/1
TabletOral10 mg / tab
TabletOral15 mg / tab
TabletOral5 mg / tab
TabletOral10 mg
TabletOral15 mg
TabletOral5 mg
TabletOral
Solution / dropsOral5 mg/ml
TabletOral5.000 mg
Prices
Unit descriptionCostUnit
Visken 15 mg Tablet1.52USD tablet
Visken 10 mg Tablet1.05USD tablet
Pindolol 10 mg tablet1.0USD tablet
Pindolol 5 mg tablet0.73USD tablet
Apo-Pindol 15 mg Tablet0.61USD tablet
Gen-Pindolol 15 mg Tablet0.61USD tablet
Novo-Pindol 15 mg Tablet0.61USD tablet
Nu-Pindol 15 mg Tablet0.61USD tablet
Pms-Pindolol 15 mg Tablet0.61USD tablet
Sandoz Pindolol 15 mg Tablet0.61USD tablet
Visken 5 mg Tablet0.61USD tablet
Apo-Pindol 10 mg Tablet0.42USD tablet
Gen-Pindolol 10 mg Tablet0.42USD tablet
Novo-Pindol 10 mg Tablet0.42USD tablet
Nu-Pindol 10 mg Tablet0.42USD tablet
Pms-Pindolol 10 mg Tablet0.42USD tablet
Sandoz Pindolol 10 mg Tablet0.42USD tablet
Apo-Pindol 5 mg Tablet0.24USD tablet
Gen-Pindolol 5 mg Tablet0.24USD tablet
Novo-Pindol 5 mg Tablet0.24USD tablet
Nu-Pindol 5 mg Tablet0.24USD tablet
Pms-Pindolol 5 mg Tablet0.24USD tablet
Sandoz Pindolol 5 mg Tablet0.24USD 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)171 °CPhysProp
water solubilityPractically InsolubleFDA Label
logP1.75SANGSTER (1994)
Caco2 permeability-4.78ADME Research, USCD
pKa9.25SANGSTER (1994)
Predicted Properties
PropertyValueSource
Water Solubility0.861 mg/mLALOGPS
logP2.17ALOGPS
logP1.69Chemaxon
logS-2.5ALOGPS
pKa (Strongest Acidic)14.09Chemaxon
pKa (Strongest Basic)9.67Chemaxon
Physiological Charge1Chemaxon
Hydrogen Acceptor Count3Chemaxon
Hydrogen Donor Count3Chemaxon
Polar Surface Area57.28 Å2Chemaxon
Rotatable Bond Count6Chemaxon
Refractivity71.46 m3·mol-1Chemaxon
Polarizability28.27 Å3Chemaxon
Number of Rings2Chemaxon
Bioavailability1Chemaxon
Rule of FiveYesChemaxon
Ghose FilterYesChemaxon
Veber's RuleNoChemaxon
MDDR-like RuleNoChemaxon
Predicted ADMET Features
PropertyValueProbability
Human Intestinal Absorption+0.9951
Blood Brain Barrier+0.6929
Caco-2 permeable+0.8867
P-glycoprotein substrateSubstrate0.6667
P-glycoprotein inhibitor INon-inhibitor0.9272
P-glycoprotein inhibitor IINon-inhibitor0.9423
Renal organic cation transporterNon-inhibitor0.8179
CYP450 2C9 substrateNon-substrate0.8315
CYP450 2D6 substrateSubstrate0.8919
CYP450 3A4 substrateNon-substrate0.708
CYP450 1A2 substrateNon-inhibitor0.7809
CYP450 2C9 inhibitorNon-inhibitor0.9071
CYP450 2D6 inhibitorInhibitor0.5
CYP450 2C19 inhibitorNon-inhibitor0.9025
CYP450 3A4 inhibitorNon-inhibitor0.831
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.8331
Ames testNon AMES toxic0.9218
CarcinogenicityNon-carcinogens0.9367
BiodegradationNot ready biodegradable0.9843
Rat acute toxicity2.9438 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9404
hERG inhibition (predictor II)Non-inhibitor0.5774
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Download (8.77 KB)
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSsplash10-001i-9810000000-7bc0638a69aba25ecb87
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-01b9-2900000000-e773b852c7d4839b531d
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-01c3-1900000000-97bebf43acd96bd5cf5b
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-01ba-0920000000-9c68ad2e49235b630737
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-01b9-0900000000-e0edd57b20d4dcecb440
MS/MS Spectrum - , positiveLC-MS/MSsplash10-0002-1690000000-c5bffa0f5938ebc6de4b
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSsplash10-0002-0090000000-107fbefe20f40c572468
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSsplash10-006t-9220000000-8dade9ca008784c85c8f
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSsplash10-000t-6910000000-1acea807542650dd8d04
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSsplash10-052f-9500000000-ab9eef433256c056a9d3
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSsplash10-001i-1900000000-d420cee27b7c01f4573d
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSsplash10-001i-2900000000-492198b1124efa2dc8f2
Predicted 1H NMR Spectrum1D NMRNot Applicable
Predicted 13C NMR Spectrum1D NMRNot Applicable
Chromatographic Properties
Collision Cross Sections (CCS)
AdductCCS Value (Å2)Source typeSource
[M-H]-168.5728657
predicted
DarkChem Lite v0.1.0
[M-H]-153.39436
predicted
DeepCCS 1.0 (2019)
[M+H]+168.4701657
predicted
DarkChem Lite v0.1.0
[M+H]+155.75237
predicted
DeepCCS 1.0 (2019)
[M+Na]+168.6079657
predicted
DarkChem Lite v0.1.0
[M+Na]+162.33968
predicted
DeepCCS 1.0 (2019)

Targets

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Details1. Beta-1 adrenergic receptor
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Partial 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. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
  2. Joseph SS, Lynham JA, Molenaar P, Grace AA, Colledge WH, Kaumann AJ: Intrinsic sympathomimetic activity of (-)-pindolol mediated through a (-)-propranolol-resistant site of the beta1-adrenoceptor in human atrium and recombinant receptors. Naunyn Schmiedebergs Arch Pharmacol. 2003 Dec;368(6):496-503. Epub 2003 Nov 8. [Article]
  3. Doggrell SA: Effects of (+/-)- (+)- and (-)-metoprolol, (+/-)- (+)- and (-)-pindolol, (+/-)-mepindolol and (+/-)-bopindolol on the rat left atria and portal vein. Gen Pharmacol. 1991;22(6):1169-77. [Article]
  4. Berendsen HH, Broekkamp CL, Van Delft AM: Antagonism of 8-OH-DPAT-induced behaviour in rats. Eur J Pharmacol. 1990 Oct 2;187(1):97-103. [Article]
  5. Watkins DJ, Lawrence AJ, Lewis SJ, Jarrott B: Loss of [125I]-pindolol binding to beta-adrenoceptors on rat nodose ganglion after chronic isoprenaline treatment. J Auton Nerv Syst. 1996 Aug 27;60(1-2):12-6. [Article]
  6. Brodde OE, Michel MC, Wang XL, Zerkowski HR: Chronic beta-adrenoceptor antagonist treatment modulates human cardiac and vascular beta-adrenoceptor density in a subtype-selective fashion. J Hypertens Suppl. 1988 Dec;6(4):S497-500. [Article]
  7. Feve B, Emorine LJ, Lasnier F, Blin N, Baude B, Nahmias C, Strosberg AD, Pairault J: Atypical beta-adrenergic receptor in 3T3-F442A adipocytes. Pharmacological and molecular relationship with the human beta 3-adrenergic receptor. J Biol Chem. 1991 Oct 25;266(30):20329-36. [Article]
Details2. Beta-2 adrenergic receptor
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Partial 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. Rubenstein LA, Zauhar RJ, Lanzara RG: Molecular dynamics of a biophysical model for beta2-adrenergic and G protein-coupled receptor activation. J Mol Graph Model. 2006 Dec;25(4):396-409. Epub 2006 Mar 30. [Article]
  2. Dejgaard A, Liggett SB, Christensen NJ, Cryer PE, Hilsted J: Adrenergic receptors are a fallible index of adrenergic denervation hypersensitivity. Scand J Clin Lab Invest. 1991 Dec;51(8):659-66. [Article]
  3. Wheeldon NM, Newnham DM, Fraser GC, McDevitt DG, Lipworth BJ: The effect of pindolol on creatine kinase is not due to beta 2-adrenoceptor partial agonist activity. Br J Clin Pharmacol. 1991 Jun;31(6):723-4. [Article]
  4. Doggrell SA: Effects of (+/-)- (+)- and (-)-metoprolol, (+/-)- (+)- and (-)-pindolol, (+/-)-mepindolol and (+/-)-bopindolol on the rat left atria and portal vein. Gen Pharmacol. 1991;22(6):1169-77. [Article]
  5. Doggrell SA: Relaxant and beta 2-adrenoceptor blocking activities of (+/- )-, (+)- and (-)-pindolol on the rat isolated aorta. J Pharm Pharmacol. 1990 Jun;42(6):444-6. [Article]
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
  7. Feve B, Emorine LJ, Lasnier F, Blin N, Baude B, Nahmias C, Strosberg AD, Pairault J: Atypical beta-adrenergic receptor in 3T3-F442A adipocytes. Pharmacological and molecular relationship with the human beta 3-adrenergic receptor. J Biol Chem. 1991 Oct 25;266(30):20329-36. [Article]
Details3. 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. [Article]
  2. Feve B, Emorine LJ, Lasnier F, Blin N, Baude B, Nahmias C, Strosberg AD, Pairault J: Atypical beta-adrenergic receptor in 3T3-F442A adipocytes. Pharmacological and molecular relationship with the human beta 3-adrenergic receptor. J Biol Chem. 1991 Oct 25;266(30):20329-36. [Article]
Details4. 5-hydroxytryptamine receptor 1A
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Antagonist
Inhibitor
Ligand
General Function
Serotonin receptor activity
Specific Function
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances. Ligand binding causes a conformation change that triggers...
Gene Name
HTR1A
Uniprot ID
P08908
Uniprot Name
5-hydroxytryptamine receptor 1A
Molecular Weight
46106.335 Da
References
  1. Smeraldi E, Benedetti F, Barbini B, Campori E, Colombo C: Sustained antidepressant effect of sleep deprivation combined with pindolol in bipolar depression. A placebo-controlled trial. Neuropsychopharmacology. 1999 Apr;20(4):380-5. [Article]
  2. Haddjeri N, de Montigny C, Blier P: Modulation of the firing activity of rat serotonin and noradrenaline neurons by (+/-)pindolol. Biol Psychiatry. 1999 May 1;45(9):1163-9. [Article]
  3. Gobert A, Millan MJ: Modulation of dialysate levels of dopamine, noradrenaline, and serotonin (5-HT) in the frontal cortex of freely-moving rats by (-)-pindolol alone and in association with 5-HT reuptake inhibitors: comparative roles of beta-adrenergic, 5-HT1A, and 5-HT1B receptors. Neuropsychopharmacology. 1999 Aug;21(2):268-84. [Article]
  4. Andree B, Thorberg SO, Halldin C, Farde L: Pindolol binding to 5-HT1A receptors in the human brain confirmed with positron emission tomography. Psychopharmacology (Berl). 1999 Jun;144(3):303-5. [Article]
  5. Fornal CA, Martin FJ, Metzler CW, Jacobs BL: Pindolol suppresses serotonergic neuronal activity and does not block the inhibition of serotonergic neurons produced by 8-hydroxy-2-(di-n-propylamino)tetralin in awake cats. J Pharmacol Exp Ther. 1999 Oct;291(1):229-38. [Article]
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
  7. Wada Y, Hirao N, Shiraishi J, Nakamura M, Koshino Y: Pindolol potentiates the effect of fluoxetine on hippocampal seizures in rats. Neurosci Lett. 1999 May 21;267(1):61-4. doi: 10.1016/s0304-3940(99)00321-3. [Article]
  8. Sandell J, Halldin C, Hall H, Thorberg SO, Werner T, Sohn D, Sedvall G, Farde L: Radiosynthesis and autoradiographic evaluation of [11C]NAD-299, a radioligand for visualization of the 5-HT1A receptor. Nucl Med Biol. 1999 Feb;26(2):159-64. doi: 10.1016/s0969-8051(98)00091-2. [Article]
  9. Hayes ES, Adaikan PG, Ratnam SS, Ng SC: 5-HT4 receptors in isolated human corpus cavernosum? Int J Impot Res. 1999 Aug;11(4):219-25. doi: 10.1038/sj.ijir.3900425. [Article]
  10. Clemett DA, Kendall DA, Cockett MI, Marsden CA, Fone KC: Pindolol-insensitive [3H]-5-hydroxytryptamine binding in the rat hypothalamus; identity with 5-hydroxytryptamine7 receptors. Br J Pharmacol. 1999 May;127(1):236-42. doi: 10.1038/sj.bjp.0702503. [Article]
Details5. 5-hydroxytryptamine receptor 1B
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Other/unknown
Ligand
General Function
Serotonin receptor activity
Specific Function
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for ergot alkaloid derivatives, various anxiolytic and antidepressant drugs and other psychoactive subst...
Gene Name
HTR1B
Uniprot ID
P28222
Uniprot Name
5-hydroxytryptamine receptor 1B
Molecular Weight
43567.535 Da
References
  1. Dawson LA, Nguyen HQ: The role of 5-HT(1A) and 5-HT(1B/1D) receptors on the modulation of acute fluoxetine-induced changes in extracellular 5-HT: the mechanism of action of (+/-)pindolol. Neuropharmacology. 2000 Apr 3;39(6):1044-52. [Article]
  2. Ariani K, Hamblin MW, Tan GL, Stratford CA, Ciaranello RD: G protein dependent alterations in [125I]iodocyanopindolol and +/- cyanopindolol binding at 5-HT1B binding sites in rat brain membranes. Neurochem Res. 1989 Sep;14(9):835-43. [Article]
  3. Leonhardt S, Herrick-Davis K, Titeler M: Detection of a novel serotonin receptor subtype (5-HT1E) in human brain: interaction with a GTP-binding protein. J Neurochem. 1989 Aug;53(2):465-71. [Article]
  4. Herrick-Davis K, Titeler M, Leonhardt S, Struble R, Price D: Serotonin 5-HT1D receptors in human prefrontal cortex and caudate: interaction with a GTP binding protein. J Neurochem. 1988 Dec;51(6):1906-12. [Article]
  5. Terron JA, Lopez-Munoz FJ, Hong E, Villalon CM: 2-(2-Aminoethyl)-quinoline (D-1997): a novel agonist at 5-hydroxytryptamine1-like receptors in the canine basilar artery. Arch Int Pharmacodyn Ther. 1994 Jan-Feb;327(1):56-68. [Article]
  6. Clemett DA, Kendall DA, Cockett MI, Marsden CA, Fone KC: Pindolol-insensitive [3H]-5-hydroxytryptamine binding in the rat hypothalamus; identity with 5-hydroxytryptamine7 receptors. Br J Pharmacol. 1999 May;127(1):236-42. doi: 10.1038/sj.bjp.0702503. [Article]

Enzymes

Details1. UDP-glucuronosyltransferases (UGTs) (Protein Group)
Kind
Protein group
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Steroid binding
Specific Function
UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds. This isoform glucuronidates bilirubin IX-alpha to form both the...
Components:
NameUniProt ID
UDP-glucuronosyltransferase 1-1P22309
UDP-glucuronosyltransferase 1-10Q9HAW8
UDP-glucuronosyltransferase 1-3P35503
UDP-glucuronosyltransferase 1-4P22310
UDP-glucuronosyltransferase 1-6P19224
UDP-glucuronosyltransferase 1-7Q9HAW7
UDP-glucuronosyltransferase 1-8Q9HAW9
UDP-glucuronosyltransferase 1-9O60656
UDP-glucuronosyltransferase 2B15P54855
UDP-glucuronosyltransferase 2B4P06133
UDP-glucuronosyltransferase 2B7P16662
References
  1. Health Canada Approved Drug Products: Apo-Pindolol (Pindolol) Oral Tablet [Link]
  2. Dailymed: Pindolol Oral Tablet [Link]
Details2. Sulfotransferase (Protein Group)
Kind
Protein group
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Sulfotransferase activity
Specific Function
Sulfotransferase that utilizes 3'-phospho-5'-adenylyl sulfate (PAPS) as sulfonate donor to catalyze the sulfonation of steroids and bile acids in the liver and adrenal glands.
Components:
NameUniProt ID
Bile salt sulfotransferaseQ06520
Sulfotransferase 1A1P50225
Sulfotransferase 1A2P50226
Sulfotransferase 1A3P0DMM9
Sulfotransferase 1A4P0DMN0
Sulfotransferase 1C2O00338
Sulfotransferase 1C3Q6IMI6
Sulfotransferase 1C4O75897
Sulfotransferase 4A1Q9BR01
Sulfotransferase 6B1Q6IMI4
Sulfotransferase family cytosolic 1B member 1O43704
References
  1. Dailymed: Pindolol Oral Tablet [Link]
  2. Health Canada Approved Drug Products: Apo-Pindolol (Pindolol) Oral Tablet [Link]
Details3. Cytochrome P450 2D6
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
General Function
Steroid hydroxylase activity
Specific Function
Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic...
Gene Name
CYP2D6
Uniprot ID
P10635
Uniprot Name
Cytochrome P450 2D6
Molecular Weight
55768.94 Da
References
  1. Smith DA, Jones BC: Speculations on the substrate structure-activity relationship (SSAR) of cytochrome P450 enzymes. Biochem Pharmacol. 1992 Dec 1;44(11):2089-98. [Article]
  2. Ferrari S, Leemann T, Dayer P: The role of lipophilicity in the inhibition of polymorphic cytochrome P450IID6 oxidation by beta-blocking agents in vitro. Life Sci. 1991;48(23):2259-65. [Article]

Carriers

Details1. alpha1-acid glycoprotein (Protein Group)
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:
NameUniProt ID
Alpha-1-acid glycoprotein 1P02763
Alpha-1-acid glycoprotein 2P19652
References
  1. Belpaire FM, Bogaert MG, Rosseneu M: Binding of beta-adrenoceptor blocking drugs to human serum albumin, to alpha 1-acid glycoprotein and to human serum. Eur J Clin Pharmacol. 1982;22(3):253-6. doi: 10.1007/BF00545224. [Article]

Transporters

Details1. Solute carrier family 22 member 2
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Quaternary ammonium group transmembrane transporter activity
Specific Function
Mediates tubular uptake of organic compounds from circulation. Mediates the influx of agmatine, dopamine, noradrenaline (norepinephrine), serotonin, choline, famotidine, ranitidine, histamin, creat...
Gene Name
SLC22A2
Uniprot ID
O15244
Uniprot Name
Solute carrier family 22 member 2
Molecular Weight
62579.99 Da
References
  1. Ciarimboli G, Schroter R, Neugebauer U, Vollenbroker B, Gabriels G, Brzica H, Sabolic I, Pietig G, Pavenstadt H, Schlatter E, Edemir B: Kidney transplantation down-regulates expression of organic cation transporters, which translocate beta-blockers and fluoroquinolones. Mol Pharm. 2013 Jun 3;10(6):2370-80. doi: 10.1021/mp4000234. Epub 2013 May 3. [Article]

Drug created at June 13, 2005 13:24 / Updated at February 20, 2024 23:55