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Identification
NamePindolol
Accession NumberDB00960  (APRD00678)
TypeSmall Molecule
GroupsApproved
Description

A moderately lipophilic beta blocker (adrenergic beta-antagonists). It is non-cardioselective and has intrinsic sympathomimetic actions, but little membrane-stabilizing activity. (From Martindale, The Extra Pharmocopoeia, 30th ed, p638)

Structure
Thumb
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
Betapindol
Blockin L
Blocklin L
Blocklin-L
Calvisken
Cardilate
Carvisken
Decreten
Durapindol
Glauco-visken
Pectobloc
Pinbetol
Pindolol
Pindololum
Prinodolol
Pynastin
Visken
External Identifiers Not Available
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Dom-pindololtablet10 mgoralDominion Pharmacal1998-09-17Not applicableCanada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Dom-pindololtablet5 mgoralDominion Pharmacal1998-09-17Not applicableCanada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Dom-pindololtablet15 mgoralDominion Pharmacal1998-09-17Not applicableCanada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Gen-pindolol Tab 15mgtablet15 mgoralGenpharm Ulc1994-12-312010-08-04Canada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Mylan-pindololtablet5 mgoralMylan Pharmaceuticals Ulc1994-12-312012-10-19Canada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Mylan-pindololtablet10 mgoralMylan Pharmaceuticals Ulc1994-12-312012-10-19Canada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Nu-pindol Tab 10mgtablet10 mgoralNu Pharm Inc1990-12-312012-09-04Canada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Nu-pindol Tab 15mgtablet15 mgoralNu Pharm Inc1990-12-312012-09-04Canada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Nu-pindol Tab 5mgtablet5 mgoralNu Pharm Inc1990-12-312012-09-04Canada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Pindolol-10 Tab 10mgtablet10 mgoralPro Doc Limitee1989-12-31Not applicableCanada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Pindolol-15 Tab 15mgtablet15 mgoralPro Doc Limitee1989-12-312012-07-23Canada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Pindolol-5 Tab 5mgtablet5 mgoralPro Doc Limitee1989-12-31Not applicableCanada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
PMS-pindololtablet15 mgoralPharmascience Inc1998-05-28Not applicableCanada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
PMS-pindololtablet10 mgoralPharmascience Inc1998-05-28Not applicableCanada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
PMS-pindololtablet5 mgoralPharmascience Inc1998-05-28Not applicableCanada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Sandoz-pindololtablet15 mgoralSandoz Canada Incorporated2006-04-07Not applicableCanada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Sandoz-pindololtablet10 mgoralSandoz Canada Incorporated2006-04-07Not applicableCanada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Sandoz-pindololtablet5 mgoralSandoz Canada Incorporated2006-04-07Not applicableCanada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Syn-pindolol Tab 10mgtablet10 mgoralSyncare Pharmaceutical Inc.1989-12-311997-08-11Canada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Syn-pindolol Tab 15mgtablet15 mgoralSyncare Pharmaceutical Inc.1989-12-311997-08-11Canada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Syn-pindolol Tab 5mgtablet5 mgoralSyncare Pharmaceutical Inc.1989-12-311997-08-11Canada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Teva-pindololtablet5 mgoralTeva Canada Limited1990-12-31Not applicableCanada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Teva-pindololtablet15 mgoralTeva Canada Limited1990-12-31Not applicableCanada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Teva-pindololtablet10 mgoralTeva Canada Limited1990-12-31Not applicableCanada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Viskentablet5 mgoralTribute Pharmaceuticals Canada Inc1978-12-31Not applicableCanada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Viskentablet10 mgoralTribute Pharmaceuticals Canada Inc1978-12-31Not applicableCanada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Viskentablet15 mgoralTribute Pharmaceuticals Canada Inc1978-12-31Not applicableCanada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo-pindol Tab 10mgtablet10 mgoralApotex Inc1988-12-31Not applicableCanada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Apo-pindol Tab 15mgtablet15 mgoralApotex Inc1988-12-31Not applicableCanada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Apo-pindol Tab 5mgtablet5 mgoralApotex Inc1988-12-31Not applicableCanada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Pindololtablet5 mg/1oralMylan Pharmaceuticals Inc.1992-09-03Not applicableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Pindololtablet10 mg/1oralCarilion Materials Management1992-09-03Not applicableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Pindololtablet5 mg/1oralCarilion Materials Management1992-09-03Not applicableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Pindololtablet10 mg/1oralSun Pharmaceutical Industries, Inc.1994-01-27Not applicableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Pindololtablet10 mg/1oralNostrum Laboratories, Inc.2016-02-01Not applicableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Pindololtablet5 mg/1oralSun Pharmaceutical Industries, Inc.1994-01-27Not applicableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Pindololtablet5 mg/1oralNostrum Laboratories, Inc.2016-02-01Not applicableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Pindololtablet10 mg/1oralMylan Pharmaceuticals Inc.1992-09-03Not applicableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Over the Counter ProductsNot Available
International Brands
NameCompany
BetapindolNot Available
Blockin LNot Available
Blocklin LNot Available
CalviskenNot Available
DecretenNot Available
DurapindolNot Available
Glauco-ViskenNot Available
PectoblocNot Available
PinbetolNot Available
PrinodololNot Available
PynastinNot Available
ViskenNot Available
Brand mixtures
NameLabellerIngredients
Viskazide 10/25tabTribute Pharmaceuticals Canada Inc
Viskazide 10/50tabTribute Pharmaceuticals Canada Inc
SaltsNot Available
CategoriesNot Available
CAS number13523-86-9
WeightAverage: 248.3208
Monoisotopic: 248.152477894
Chemical FormulaC14H20N2O2
InChI KeyInChIKey=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
Taxonomy
DescriptionThis 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.
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassIndoles and derivatives
Sub ClassIndoles
Direct ParentIndoles
Alternative Parents
Substituents
  • Indole
  • Alkyl aryl ether
  • Benzenoid
  • Heteroaromatic compound
  • Pyrrole
  • Secondary alcohol
  • 1,2-aminoalcohol
  • Azacycle
  • Secondary amine
  • Ether
  • Secondary aliphatic amine
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Amine
  • Alcohol
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External DescriptorsNot Available
Pharmacology
IndicationFor the management of hypertension, edema, ventricular tachycardias, and atrial fibrillation.
PharmacodynamicsPindolol is a non-selective beta-adrenergic antagonist (beta-blocker) which possesses intrinsic sympathomimetic activity (ISA) in therapeutic dosage ranges but does not possess quinidine-like membrane stabilizing activity. Pindolol impairs AV node conduction and decreases sinus rate and may also increase plasma triglycerides and decrease HDL-cholesterol levels. Pindolol is nonpolar and hydrophobic, with low to moderate lipid solubility. Pindolol has little to no intrinsic sympathomimetic activity and, unlike some other beta-adrenergic blocking agents, pindolol has little direct myocardial depressant activity and does not have an anesthetic-like membrane-stabilizing action.
Mechanism of actionPindolol non-selectively blocks beta-1 adrenergic receptors mainly in the heart, inhibiting the effects of epinephrine and norepinephrine resulting in a decrease in heart rate and blood pressure. By binding beta-2 receptors in the juxtaglomerular apparatus, Pindolol inhibits the production of renin, thereby inhibiting angiotensin II and aldosterone production and therefore inhibits the vasoconstriction and water retention due to angiotensin II and aldosterone, respectively.
AbsorptionRapidly and reproducibly absorbed (bioavailability greater than 95%).
Volume of distribution
  • 2 L/kg
Protein binding40%
Metabolism

Hepatic. In man, 35% to 40% is excreted unchanged in the urine and 60% to 65% is metabolized primarily to hydroxy-metabolites which are excreted as glucuronides and ethereal sulfates.

Route of eliminationPindolol undergoes extensive metabolism in animals and man. In man, 35% to 40% is excreted unchanged in the urine and 60% to 65% is metabolized primarily to hydroxy-metabolites which are excreted as glucuronides and ethereal sulfates. About 6% to 9% of an administered intravenous dose is excreted by the bile into the feces.
Half life3 to 4 hours
Clearance
  • 50-300 mL/min [cirrhotic patients]
ToxicityLD50=263 mg/kg (orally in rats). Signs of overdose include excessive bradycardia, cardiac failure, hypotension, and bronchospasm.
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
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 )
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
Dosage forms
FormRouteStrength
Tabletoral10 mg/1
Tabletoral5 mg/1
Tabletoral10 mg
Tabletoral15 mg
Tabletoral5 mg
Tabletoral
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.
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point171 °CPhysProp
water solubility7880 mg/LNot Available
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 RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Download (8.77 KB)
SpectraNot Available
References
Synthesis Reference

DrugSyn.org

US3471515
General ReferencesNot Available
External Links
ATC CodesC07AA03
AHFS Codes
  • 24:24.00
PDB EntriesNot Available
FDA labelNot Available
MSDSDownload (74.7 KB)
Interactions
Drug Interactions
Drug
AcepromazineAcepromazine may increase the hypotensive activities of Pindolol.
AcetylcholineThe risk or severity of adverse effects can be increased when Pindolol is combined with Acetylcholine.
AldesleukinThe risk or severity of adverse effects can be increased when Aldesleukin is combined with Pindolol.
AlfuzosinPindolol may increase the orthostatic hypotensive activities of Alfuzosin.
AmifostinePindolol may increase the hypotensive activities of Amifostine.
AmiodaroneAmiodarone may increase the bradycardic activities of Pindolol.
AripiprazoleThe serum concentration of Aripiprazole can be increased when it is combined with Pindolol.
BretyliumBretylium may increase the bradycardic activities of Pindolol.
BrimonidineBrimonidine may increase the antihypertensive activities of Pindolol.
BupivacaineThe serum concentration of Bupivacaine can be increased when it is combined with Pindolol.
BupropionThe serum concentration of Pindolol can be increased when it is combined with Bupropion.
ButabarbitalThe serum concentration of Pindolol can be decreased when it is combined with Butabarbital.
ButethalThe serum concentration of Pindolol can be decreased when it is combined with Butethal.
CabergolinePindolol may increase the vasoconstricting activities of Cabergoline.
CarbacholThe risk or severity of adverse effects can be increased when Pindolol is combined with Carbachol.
CeritinibPindolol may increase the bradycardic activities of Ceritinib.
ChloroquineThe metabolism of Pindolol can be decreased when combined with Chloroquine.
ChlorpropamidePindolol may increase the hypoglycemic activities of Chlorpropamide.
DiazoxideDiazoxide may increase the hypotensive activities of Pindolol.
DigoxinPindolol may increase the bradycardic activities of Digoxin.
DipivefrinDipivefrin may increase the atrioventricular blocking (AV block) activities of Pindolol.
DipyridamoleDipyridamole may increase the bradycardic activities of Pindolol.
DisopyramideDisopyramide may increase the bradycardic activities of Pindolol.
DronedaroneDronedarone may increase the bradycardic activities of Pindolol.
DuloxetinePindolol may increase the orthostatic hypotensive activities of Duloxetine.
EsmololEsmolol may increase the bradycardic activities of Pindolol.
FingolimodPindolol may increase the bradycardic activities of Fingolimod.
FloctafenineThe risk or severity of adverse effects can be increased when Floctafenine is combined with Pindolol.
HeptabarbitalThe serum concentration of Pindolol can be decreased when it is combined with Heptabarbital.
HexobarbitalThe serum concentration of Pindolol can be decreased when it is combined with Hexobarbital.
InfliximabInfliximab may decrease the antihypertensive activities of Pindolol.
IvabradinePindolol may increase the bradycardic activities of Ivabradine.
LacosamidePindolol may increase the atrioventricular blocking (AV block) activities of Lacosamide.
LevodopaPindolol may increase the orthostatic hypotensive activities of Levodopa.
LidocaineThe serum concentration of Lidocaine can be increased when it is combined with Pindolol.
MepivacaineThe serum concentration of Mepivacaine can be increased when it is combined with Pindolol.
MethacholineThe risk or severity of adverse effects can be increased when Pindolol is combined with Methacholine.
MethohexitalThe serum concentration of Pindolol can be decreased when it is combined with Methohexital.
MethylphenidateMethylphenidate may decrease the antihypertensive activities of Pindolol.
MidodrinePindolol may increase the bradycardic activities of Midodrine.
MolsidomineMolsidomine may increase the hypotensive activities of Pindolol.
MoxonidineMoxonidine may increase the hypotensive activities of Pindolol.
NicorandilNicorandil may increase the hypotensive activities of Pindolol.
NifedipineNifedipine may increase the hypotensive activities of Pindolol.
ObinutuzumabPindolol may increase the hypotensive activities of Obinutuzumab.
OctreotideOctreotide may increase the bradycardic activities of Pindolol.
OrciprenalinePindolol may decrease the activities of Orciprenaline.
ParoxetineThe serum concentration of Pindolol can be increased when it is combined with Paroxetine.
PentobarbitalThe serum concentration of Pindolol can be decreased when it is combined with Pentobarbital.
PentoxifyllinePentoxifylline may increase the hypotensive activities of Pindolol.
PhenelzinePhenelzine may increase the orthostatic hypotensive activities of Pindolol.
PrazosinPindolol may increase the orthostatic hypotensive activities of Prazosin.
PrimidoneThe serum concentration of Pindolol can be decreased when it is combined with Primidone.
PropafenoneThe serum concentration of Pindolol can be increased when it is combined with Propafenone.
QuinineQuinine may increase the hypotensive activities of Pindolol.
RegorafenibRegorafenib may increase the bradycardic activities of Pindolol.
ReserpineReserpine may increase the hypotensive activities of Pindolol.
RisperidonePindolol may increase the hypotensive activities of Risperidone.
RituximabPindolol may increase the hypotensive activities of Rituximab.
RivastigmineRivastigmine may increase the bradycardic activities of Pindolol.
RuxolitinibRuxolitinib may increase the bradycardic activities of Pindolol.
SecobarbitalThe serum concentration of Pindolol can be decreased when it is combined with Secobarbital.
SufentanilSufentanil may increase the bradycardic activities of Pindolol.
TacrineTacrine may increase the bradycardic activities of Pindolol.
TadalafilTadalafil may increase the antihypertensive activities of Pindolol.
TheophyllinePindolol may decrease the activities of Theophylline.
TofacitinibTofacitinib may increase the bradycardic activities of Pindolol.
TranylcypromineTranylcypromine may increase the orthostatic hypotensive activities of Pindolol.
TreprostinilTreprostinil may increase the hypotensive activities of Pindolol.
ValsartanThe risk or severity of adverse effects can be increased when Valsartan is combined with Pindolol.
VardenafilVardenafil may increase the antihypertensive activities of Pindolol.
YohimbineYohimbine may decrease the antihypertensive activities of Pindolol.
Food Interactions
  • Magnesium, potassium and zinc needs increased.
  • Take without regard to meals. Avoid alcohol.

Targets

1. Beta-1 adrenergic receptor

Kind: Protein

Organism: Human

Pharmacological action: yes

Actions: partial agonist

Components

Name UniProt ID Details
Beta-1 adrenergic receptor P08588 Details

References:

  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. Pubmed
  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. Pubmed
  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. Pubmed
  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. Pubmed
  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. Pubmed
  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. Pubmed

2. Beta-2 adrenergic receptor

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: partial agonist

Components

Name UniProt ID Details
Beta-2 adrenergic receptor P07550 Details

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. Pubmed
  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. Pubmed
  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. Pubmed
  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. Pubmed
  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. Pubmed
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. Pubmed

3. 5-hydroxytryptamine receptor 1A

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: antagonist

Components

Name UniProt ID Details
5-hydroxytryptamine receptor 1A P08908 Details

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. Pubmed
  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. Pubmed
  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. Pubmed
  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. Pubmed
  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. Pubmed
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. Pubmed

4. 5-hydroxytryptamine receptor 1B

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: other/unknown

Components

Name UniProt ID Details
5-hydroxytryptamine receptor 1B P28222 Details

References:

  1. Dawson LA, Nguyen HQ: The role of 5-HT and 5-HT 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. Pubmed
  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. Pubmed
  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. Pubmed
  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. Pubmed
  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. Pubmed

Enzymes

1. Cytochrome P450 2D6

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: substrate inhibitor inducer

Components

Name UniProt ID Details
Cytochrome P450 2D6 P10635 Details

References:

  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed

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Drug created on June 13, 2005 07:24 / Updated on October 08, 2013 14:25