Identification

Name
Pindolol
Accession Number
DB00960  (APRD00678)
Type
Small Molecule
Groups
Approved, Investigational
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
  • Pindololum
External IDs
BRN 1536506 / CCRIS 9215 / DL-LB-46 / HSDB 6539 / LB 46 / LB-46
Product Images
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Pindolol-10 Tab 10mgTablet10 mgOralPro Doc Limitee1989-12-31Not applicableCanada
Pindolol-15 Tab 15mgTablet15 mgOralPro Doc Limitee1989-12-312012-07-23Canada
Pindolol-5 Tab 5mgTablet5 mgOralPro Doc Limitee1989-12-31Not applicableCanada
ViskenTablet5 mgOralTribute Pharmaceuticals1978-12-31Not applicableCanada
ViskenTablet10 mgOralTribute Pharmaceuticals1978-12-31Not applicableCanada
ViskenTablet10 mg/1OralNovartis2006-10-31Not applicableUs
ViskenTablet15 mgOralTribute Pharmaceuticals1978-12-312017-07-13Canada
ViskenTablet5 mg/1OralNovartis2006-10-31Not applicableUs
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo-pindol Tab 10mgTablet10 mgOralApotex Corporation1988-12-31Not applicableCanada
Apo-pindol Tab 15mgTablet15 mgOralApotex Corporation1988-12-31Not applicableCanada
Apo-pindol Tab 5mgTablet5 mgOralApotex Corporation1988-12-31Not applicableCanada
Dom-pindololTablet5 mgOralDominion Pharmacal1998-09-17Not applicableCanada
Dom-pindololTablet15 mgOralDominion Pharmacal1998-09-17Not applicableCanada
Dom-pindololTablet10 mgOralDominion Pharmacal1998-09-17Not applicableCanada
Gen-pindolol Tab 15mgTablet15 mgOralGenpharm Ulc1994-12-312010-08-04Canada
Mylan-pindololTablet5 mgOralMylan Pharmaceuticals1994-12-312012-10-19Canada
Mylan-pindololTablet10 mgOralMylan Pharmaceuticals1994-12-312012-10-19Canada
Nu-pindol Tab 10mgTablet10 mgOralNu Pharm Inc1990-12-312012-09-04Canada
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
Viskazide 10/25tabPindolol (10 mg) + Hydrochlorothiazide (25 mg)TabletOralTribute Pharmaceuticals1983-12-31Not applicableCanada
Viskazide 10/50tabPindolol (10 mg) + Hydrochlorothiazide (50 mg)TabletOralTribute Pharmaceuticals1983-12-31Not applicableCanada
International/Other Brands
Betapindol / Blockin L / Blocklin L / Calvisken / Decreten / Durapindol / Glauco-Visken / Pectobloc / Pinbetol / Prinodolol / Pynastin / Visken
Categories
UNII
BJ4HF6IU1D
CAS number
13523-86-9
Weight
Average: 248.3208
Monoisotopic: 248.152477894
Chemical Formula
C14H20N2O2
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

Pharmacology

Indication

For the management of hypertension, edema, ventricular tachycardias, and atrial fibrillation.

Associated Conditions
Pharmacodynamics

Pindolol 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 action

Pindolol 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.

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

Rapidly and reproducibly absorbed (bioavailability greater than 95%).

Volume of distribution
  • 2 L/kg
Protein binding

40%

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 elimination

Pindolol 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 life

3 to 4 hours

Clearance
  • 50-300 mL/min [cirrhotic patients]
Toxicity

LD50=263 mg/kg (orally in rats). Signs of overdose include excessive bradycardia, cardiac failure, hypotension, and bronchospasm.

Affected organisms
  • Humans and other mammals
Pathways
PathwayCategory
Pindolol Action PathwayDrug action
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteraction
(R)-warfarinThe risk or severity of adverse effects can be increased when Pindolol is combined with (R)-warfarin.
(S)-WarfarinThe risk or severity of adverse effects can be increased when Pindolol is combined with (S)-Warfarin.
1,10-Phenanthroline1,10-Phenanthroline may increase the bradycardic activities of Pindolol.
2,5-Dimethoxy-4-ethylamphetamineThe risk or severity of serotonin syndrome can be increased when Pindolol is combined with 2,5-Dimethoxy-4-ethylamphetamine.
2,5-Dimethoxy-4-ethylthioamphetamineThe risk or severity of serotonin syndrome can be increased when Pindolol is combined with 2,5-Dimethoxy-4-ethylthioamphetamine.
3-isobutyl-1-methyl-7H-xanthineThe risk or severity of adverse effects can be increased when Pindolol is combined with 3-isobutyl-1-methyl-7H-xanthine.
3,4-MethylenedioxyamphetamineThe risk or severity of serotonin syndrome can be increased when Pindolol is combined with 3,4-Methylenedioxyamphetamine.
4-Bromo-2,5-dimethoxyamphetamineThe risk or severity of serotonin syndrome can be increased when Pindolol is combined with 4-Bromo-2,5-dimethoxyamphetamine.
4-hydroxycoumarinThe risk or severity of adverse effects can be increased when Pindolol is combined with 4-hydroxycoumarin.
4-MethoxyamphetamineThe therapeutic efficacy of 4-Methoxyamphetamine can be decreased when used in combination with Pindolol.
Food Interactions
  • Magnesium, potassium and zinc needs increased.
  • Take without regard to meals. Avoid alcohol.

References

Synthesis Reference
US3471515
General References
Not Available
External Links
Human Metabolome Database
HMDB0015095
KEGG Drug
D00513
KEGG Compound
C07445
PubChem Compound
4828
PubChem Substance
46508362
ChemSpider
4662
BindingDB
50019443
ChEBI
8214
ChEMBL
CHEMBL500
Therapeutic Targets Database
DAP000025
PharmGKB
PA450966
IUPHAR
91
Guide to Pharmacology
GtP Drug Page
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
PDRhealth
PDRhealth Drug Page
Wikipedia
Pindolol
ATC Codes
C07AA03 — PindololC07CA03 — Pindolol and other diuretics
AHFS Codes
  • 24:24.00 — Beta-adrenergic Blocking Agents
MSDS
Download (74.7 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1CompletedBasic ScienceAmphetamine-Related Disorders / Moods Disorders / Substance-Related Disorders1
1Unknown StatusTreatmentHealthy Volunteers1
2CompletedTreatmentAntidepressant Treatment Response / Major Depressive Disorder (MDD)1
2, 3TerminatedTreatmentUnipolar Depression1
Not AvailableCompletedBasic ScienceHealthy Volunteers1
Not AvailableTerminatedTreatmentHigh Blood Pressure (Hypertension) / Microvascular Angina1
Not AvailableTerminatedTreatmentMajor Depressive Disorder (MDD)1

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
TabletOral10 mg
TabletOral15 mg
TabletOral5 mg
TabletOral
TabletOral10 mg/1
TabletOral5 mg/1
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 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 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-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-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

Taxonomy

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
Indole / Alkyl aryl ether / Benzenoid / Pyrrole / Heteroaromatic compound / Secondary alcohol / 1,2-aminoalcohol / Azacycle / Secondary amine / Ether
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
indoles, secondary amine (CHEBI:8214)

Targets

Kind
Protein
Organism
Human
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. [PubMed:11752352]
  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:14608456]
  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:1687398]
  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:2148726]
  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:8884690]
  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:2907348]
Kind
Protein
Organism
Human
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. [PubMed:16574446]
  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:1666931]
  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:1678274]
  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:1687398]
  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:1979630]
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Antagonist
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. [PubMed:10088139]
  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:10331108]
  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:10432475]
  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:10435400]
  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:10490909]
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Other/unknown
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. [PubMed:10727715]
  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:2512511]
  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:2664084]
  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:3141589]
  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:7944828]
Kind
Protein
Organism
Human
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. 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. [PubMed:1682311]

Enzymes

Kind
Protein
Organism
Human
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. 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. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
  2. 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. [PubMed:1472073]
  3. 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. [PubMed:1675413]

Drug created on June 13, 2005 07:24 / Updated on November 17, 2018 04:48