Identification

Name
Terazosin
Accession Number
DB01162  (APRD00667)
Type
Small Molecule
Groups
Approved
Description

Terazosin is a selective alpha1-antagonist used for treatment of symptoms of benign prostatic hyperplasia (BPH). It also acts to lower blood pressure, so it is a drug of choice for men with hypertension and prostate enlargement. It works by blocking the action of adrenaline on smooth muscle of the bladder and the blood vessel walls.

Structure
Thumb
Synonyms
  • 1-(4-Amino-6,7-dimethoxy-2-quinazolinyl)-4-((tetrahydro-2-furanyl)carbonyl)piperazine
  • Terazosina
  • Terazosine
  • Térazosine
  • Terazosinum
External IDs
Abbott 45975
Product Ingredients
IngredientUNIICASInChI Key
Terazosin hydrochloride8QOP8Z995563074-08-8IWSWDOUXSCRCKW-UHFFFAOYSA-N
Terazosin hydrochloride hydrateD32S14F08270024-40-7MWYNOTLRCUQCKD-UHFFFAOYSA-N
Product Images
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
HytrinTablet10 mg/1OralAbbott1987-08-072008-03-31Us
HytrinCapsule, liquid filled2 mg/1OralPhysicians Total Care, Inc.1996-08-162010-12-31Us
HytrinTablet2 mgOralBgp Pharma Ulc1989-12-312016-02-19Canada
HytrinCapsule, liquid filled10 mg/1OralAbbott1994-12-142008-03-31Us
HytrinCapsule, liquid filled1 mg/1OralAbbott1994-12-142008-03-31Us
HytrinTablet2 mg/1OralAbbott1987-08-072008-03-31Us
HytrinTablet1 mgOralBgp Pharma Ulc1989-12-312016-02-19Canada
HytrinCapsule, liquid filled5 mg/1OralAbbott1994-12-142008-03-31Us
HytrinTablet5 mg/1OralAbbott1987-08-072008-03-31Us
HytrinTablet1 mg/1OralAbbott1987-08-072008-03-31Us
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo-terazosinTablet2 mgOralApotex Corporation1997-09-26Not applicableCanada
Apo-terazosinTablet10 mgOralApotex Corporation1997-09-26Not applicableCanada
Apo-terazosinTablet5 mgOralApotex Corporation1997-09-26Not applicableCanada
Apo-terazosinTablet1 mgOralApotex Corporation1997-09-26Not applicableCanada
Dom-terazosinTablet10 mgOralDominion Pharmacal2001-10-31Not applicableCanada
Dom-terazosinTablet1 mgOralDominion Pharmacal2001-10-31Not applicableCanada
Dom-terazosinTablet5 mgOralDominion Pharmacal2001-10-31Not applicableCanada
Dom-terazosinTablet2 mgOralDominion Pharmacal2001-10-31Not applicableCanada
Mylan-terazosinTablet10 mgOralMylan Pharmaceuticals2012-11-092016-06-28Canada
Mylan-terazosinTablet1 mgOralMylan Pharmaceuticals2012-11-092016-06-28Canada
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
Hytrin-7 Tabs 1mg-7 Tabs 2mg-14 Tabs 5mgTerazosin (1 mg) + Terazosin (2 mg) + Terazosin (5 mg)Kit; TabletOralAbbott1996-12-312006-10-17Canada
Hytrin-7 Tabs 1mg-7 Tabs 2mg-14 Tabs 5mgTerazosin (1 mg) + Terazosin (2 mg) + Terazosin (5 mg)Kit; TabletOralAbbott1996-12-312006-10-17Canada
Hytrin-7 Tabs 1mg-7 Tabs 2mg-14 Tabs 5mgTerazosin (1 mg) + Terazosin (2 mg) + Terazosin (5 mg)Kit; TabletOralAbbott1996-12-312006-10-17Canada
International/Other Brands
Blavin (Baliarda (Argentina)) / Flumarc (Raffo (Argentina)) / Fosfomic (Finadiet (Argentina)) / Heitrin (Abbott (Germany; discontinued)) / Hytrinex (Amdipharm (Sweden)) / Itrin (Keryos (Italy)) / Urodie (Keryos (Italy)) / Vicard (Amdipharm (Austria)) / Zayasel
Categories
UNII
8L5014XET7
CAS number
63590-64-7
Weight
Average: 387.4329
Monoisotopic: 387.190654313
Chemical Formula
C19H25N5O4
InChI Key
VCKUSRYTPJJLNI-UHFFFAOYSA-N
InChI
InChI=1S/C19H25N5O4/c1-26-15-10-12-13(11-16(15)27-2)21-19(22-17(12)20)24-7-5-23(6-8-24)18(25)14-4-3-9-28-14/h10-11,14H,3-9H2,1-2H3,(H2,20,21,22)
IUPAC Name
6,7-dimethoxy-2-[4-(oxolane-2-carbonyl)piperazin-1-yl]quinazolin-4-amine
SMILES
COC1=C(OC)C=C2C(N)=NC(=NC2=C1)N1CCN(CC1)C(=O)C1CCCO1

Pharmacology

Indication

For the treatment of symptomatic BPH and mild to moderate hypertension.

Associated Conditions
Pharmacodynamics

Terazosin, classified as a quinazoline, is similar to doxazosin and prazosin. As an α-adrenergic blocking agent, terazosin is used to treat hypertension and BPH. Terazosin produces vasodilation and reduces peripheral resistance but in general has only a slight effect on cardiac output. The antihypertensive effect with chronic dosing is not usually accompanied by reflex tachycardia.

Mechanism of action

In general, α1-adrenergic receptors mediate contraction and hypertrophic growth of smooth muscle cells. α1-Receptors are 7-transmembrane domain receptors coupled to G proteins, Gq/11. Three α1-receptor subtypes, which share approximately 75% homology in their transmembrane domains, have been identified: α1A (chromosome 8), α1B (chromosome 5), and α1D (chromosome 20). Terazosin is the first α1-receptor antagonist to demonstrate selectivity for the α1A-receptor. All three receptor subtypes appear to be involved in maintaining vascular tone. The α1A-receptor maintains basal vascular tone while the α1B-receptor mediates the vasocontrictory effects of exogenous α1-agonists. Activation of α1-receptors activates Gq-proteins, which results in intracellular stimulation of phospholipases C, A2, and D. This results in mobilization of Ca2+ from intracellular stores, activation of mitogen-activated kinase and PI3 kinase pathways and subsequent vasoconstriction. Terozosin produces its pharmacological effects by inhibiting α1A-receptor activation. Inhibition of these receptors in the vasculature and prostate results in muscle relaxation, decreased blood pressure and improved urinary outflow in symptomatic benign prostatic hyperplasia.

TargetActionsOrganism
AAlpha-1A adrenergic receptor
antagonist
Human
AAlpha-1B adrenergic receptor
antagonist
Human
AAlpha-1D adrenergic receptor
antagonist
Human
UPotassium voltage-gated channel subfamily H member 2
inhibitor
Human
UPotassium voltage-gated channel subfamily H member 6
inhibitor
Human
UPotassium voltage-gated channel subfamily H member 7
inhibitor
Human
Absorption

Essentially completely absorbed in man (90% bioavailability).

Volume of distribution
Not Available
Protein binding

90-94%

Metabolism

Hepatic. One of the four metabolites identified (piperazine derivative of terazosin) has antihypertensive activity.

Route of elimination

Approximately 10% of an orally administered dose is excreted as parent drug in the urine and approximately 20% is excreted in the feces.

Half life

12 hours

Clearance
Not Available
Toxicity

LD50=259.3mg/kg (IV in mice)

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

Interactions

Drug Interactions
DrugInteraction
4-MethoxyamphetamineThe therapeutic efficacy of 4-Methoxyamphetamine can be decreased when used in combination with Terazosin.
AbediterolThe therapeutic efficacy of Abediterol can be decreased when used in combination with Terazosin.
AbemaciclibThe serum concentration of Abemaciclib can be increased when it is combined with Terazosin.
AcebutololThe serum concentration of Acebutolol can be increased when it is combined with Terazosin.
AceclofenacThe therapeutic efficacy of Terazosin can be decreased when used in combination with Aceclofenac.
AcemetacinThe therapeutic efficacy of Terazosin can be decreased when used in combination with Acemetacin.
AcepromazineTerazosin may increase the orthostatic hypotensive, hypotensive, and antihypertensive activities of Acepromazine.
AcetaminophenThe serum concentration of Acetaminophen can be increased when it is combined with Terazosin.
Acetylsalicylic acidThe serum concentration of Acetylsalicylic acid can be increased when it is combined with Terazosin.
AdrafinilThe therapeutic efficacy of Adrafinil can be decreased when used in combination with Terazosin.
Food Interactions
Not Available

References

Synthesis Reference

K. S. Keshava Murthy, Gamini Weeratunga, Tianhao Zhou, Bhaskar Reddy Guntoori, "Process for the manufacture of intermediates suitable to make doxazosin, terazosin, prazosin, tiodazosin and related antihypertensive medicines." U.S. Patent US5919931, issued September, 1986.

US5919931
General References
  1. Cushman WC, Ford CE, Cutler JA, Margolis KL, Davis BR, Grimm RH, Black HR, Hamilton BP, Holland J, Nwachuku C, Papademetriou V, Probstfield J, Wright JT Jr, Alderman MH, Weiss RJ, Piller L, Bettencourt J, Walsh SM: Success and predictors of blood pressure control in diverse North American settings: the antihypertensive and lipid-lowering treatment to prevent heart attack trial (ALLHAT). J Clin Hypertens (Greenwich). 2002 Nov-Dec;4(6):393-404. [PubMed:12461301]
External Links
Human Metabolome Database
HMDB0015293
KEGG Drug
D08569
KEGG Compound
C07127
PubChem Compound
5401
PubChem Substance
46509129
ChemSpider
5208
BindingDB
50033111
ChEBI
9445
ChEMBL
CHEMBL611
Therapeutic Targets Database
DAP000371
PharmGKB
PA451612
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Terazosin
ATC Codes
G04CA03 — Terazosin
AHFS Codes
  • 24:20.00 — Alpha-adrenergic Blocking Agents
FDA label
Download (1020 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
2Not Yet RecruitingPreventionCarotid Artery Stenosis1
2, 3CompletedTreatmentDisorder of Urinary Stent1
3CompletedPreventionAtherosclerosis / Cardiovascular Disease (CVD) / Coronary Heart Disease (CHD) / Diabetes Mellitus (DM) / High Blood Pressure (Hypertension) / High Cholesterol / Type 2 Diabetes Mellitus1
4CompletedPreventionNonvalvular Atrial Fibrillation1
4CompletedTreatmentHyperhidrosis1
4CompletedTreatmentProstatic Hyperplasia1
4WithdrawnTreatmentBenign Prostatic Hyperplasia (BPH)1
Not AvailableCompletedTreatmentAntidepressant Induced Excessive Sweating1
Not AvailableCompletedTreatmentHigh Blood Pressure (Hypertension) / Lower Urinary Tract Symptoms (LUTS)1
Not AvailableRecruitingPreventionCardiovascular Effects1
Not AvailableTerminatedTreatmentProstatic Hyperplasia / Urinary Retention1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
  • Advanced Pharmaceutical Services Inc.
  • Amerisource Health Services Corp.
  • Apotex Inc.
  • A-S Medication Solutions LLC
  • Cadista Pharmaceuticals Inc.
  • Cardinal Health
  • Comprehensive Consultant Services Inc.
  • Direct Dispensing Inc.
  • Dispensing Solutions
  • Diversified Healthcare Services Inc.
  • Golden State Medical Supply Inc.
  • H.J. Harkins Co. Inc.
  • Heartland Repack Services LLC
  • Intas Pharmaceuticals Ltd.
  • Ivax Pharmaceuticals
  • Kaiser Foundation Hospital
  • Major Pharmaceuticals
  • Mckesson Corp.
  • Murfreesboro Pharmaceutical Nursing Supply
  • Mylan
  • Nucare Pharmaceuticals Inc.
  • Palmetto Pharmaceuticals Inc.
  • PD-Rx Pharmaceuticals Inc.
  • Pharmaceutical Utilization Management Program VA Inc.
  • Physicians Total Care Inc.
  • Preferred Pharmaceuticals Inc.
  • Prepackage Specialists
  • Prepak Systems Inc.
  • Ranbaxy Laboratories
  • Rebel Distributors Corp.
  • Redpharm Drug
  • Remedy Repack
  • Resource Optimization and Innovation LLC
  • Sandoz
  • Southwood Pharmaceuticals
  • Teva Pharmaceutical Industries Ltd.
  • Torpharm Inc.
  • Tya Pharmaceuticals
  • UDL Laboratories
  • Va Cmop Dallas
  • Vangard Labs Inc.
Dosage forms
FormRouteStrength
TabletOral10 mg
Capsule, liquid filledOral1 mg/1
Capsule, liquid filledOral10 mg/1
Capsule, liquid filledOral2 mg/1
Capsule, liquid filledOral5 mg/1
TabletOral1 mg/1
TabletOral10 mg/1
TabletOral2 mg/1
TabletOral5 mg/1
Kit; tabletOral
CapsuleOral1 mg/1
CapsuleOral10 mg/1
CapsuleOral2 mg/1
CapsuleOral5 mg/1
TabletOral1 mg
TabletOral2 mg
TabletOral5 mg
Prices
Unit descriptionCostUnit
Hytrin 10 mg Tablet1.85USD tablet
Terazosin HCl 1 mg capsule1.67USD capsule
Terazosin HCl 10 mg capsule1.67USD capsule
Terazosin HCl 2 mg capsule1.67USD capsule
Terazosin HCl 5 mg capsule1.67USD capsule
Hytrin 5 mg Tablet1.26USD tablet
Hytrin 2 mg Tablet0.93USD tablet
Apo-Terazosin 10 mg Tablet0.92USD tablet
Novo-Terazosin 10 mg Tablet0.92USD tablet
Nu-Terazosin 10 mg Tablet0.92USD tablet
Pms-Terazosin 10 mg Tablet0.92USD tablet
Ratio-Terazosin 10 mg Tablet0.92USD tablet
Hytrin 1 mg Tablet0.73USD tablet
Apo-Terazosin 5 mg Tablet0.63USD tablet
Novo-Terazosin 5 mg Tablet0.63USD tablet
Nu-Terazosin 5 mg Tablet0.63USD tablet
Pms-Terazosin 5 mg Tablet0.63USD tablet
Ratio-Terazosin 5 mg Tablet0.63USD tablet
Apo-Terazosin 2 mg Tablet0.46USD tablet
Novo-Terazosin 2 mg Tablet0.46USD tablet
Nu-Terazosin 2 mg Tablet0.46USD tablet
Pms-Terazosin 2 mg Tablet0.46USD tablet
Ratio-Terazosin 2 mg Tablet0.46USD tablet
Apo-Terazosin 1 mg Tablet0.37USD tablet
Novo-Terazosin 1 mg Tablet0.37USD tablet
Nu-Terazosin 1 mg Tablet0.37USD tablet
Pms-Terazosin 1 mg Tablet0.37USD tablet
Ratio-Terazosin 1 mg Tablet0.37USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US5294615No1993-04-292013-04-29Us
US5212176No1993-06-292010-06-29Us

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)273 °CPhysProp
water solubility29.7mg/mLNot Available
logP1Not Available
Predicted Properties
PropertyValueSource
Water Solubility1.5 mg/mLALOGPS
logP1.12ALOGPS
logP1.18ChemAxon
logS-2.4ALOGPS
pKa (Strongest Acidic)19.93ChemAxon
pKa (Strongest Basic)7.24ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count8ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area103.04 Å2ChemAxon
Rotatable Bond Count4ChemAxon
Refractivity105.18 m3·mol-1ChemAxon
Polarizability41.26 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+1.0
Blood Brain Barrier+0.9646
Caco-2 permeable+0.8868
P-glycoprotein substrateSubstrate0.698
P-glycoprotein inhibitor INon-inhibitor0.5666
P-glycoprotein inhibitor IINon-inhibitor0.8619
Renal organic cation transporterNon-inhibitor0.6319
CYP450 2C9 substrateNon-substrate0.8864
CYP450 2D6 substrateNon-substrate0.8032
CYP450 3A4 substrateSubstrate0.7753
CYP450 1A2 substrateNon-inhibitor0.9046
CYP450 2C9 inhibitorNon-inhibitor0.9435
CYP450 2D6 inhibitorNon-inhibitor0.9628
CYP450 2C19 inhibitorNon-inhibitor0.9492
CYP450 3A4 inhibitorNon-inhibitor0.7905
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.901
Ames testNon AMES toxic0.5943
CarcinogenicityNon-carcinogens0.906
BiodegradationNot ready biodegradable0.9785
Rat acute toxicity2.2262 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.8368
hERG inhibition (predictor II)Inhibitor0.8204
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
MS/MS Spectrum - , positiveLC-MS/MSsplash10-000i-0049000000-86650e3e374df663aa35
MS/MS Spectrum - , positiveLC-MS/MSsplash10-000i-0059000000-ca9adf5daab9e5e9b6e7
MS/MS Spectrum - , positiveLC-MS/MSsplash10-000e-1292000000-9081c5bb64e8d096db78

Taxonomy

Description
This compound belongs to the class of organic compounds known as n-arylpiperazines. These are organic compounds containing a piperazine ring where the nitrogen ring atom carries an aryl group.
Kingdom
Organic compounds
Super Class
Organoheterocyclic compounds
Class
Diazinanes
Sub Class
Piperazines
Direct Parent
N-arylpiperazines
Alternative Parents
Quinazolinamines / Anisoles / Dialkylarylamines / Alkyl aryl ethers / Aminopyrimidines and derivatives / Imidolactams / Tetrahydrofurans / Tertiary carboxylic acid amides / Heteroaromatic compounds / Amino acids and derivatives
show 8 more
Substituents
N-arylpiperazine / Quinazolinamine / Diazanaphthalene / Quinazoline / Anisole / Dialkylarylamine / Alkyl aryl ether / Aminopyrimidine / Pyrimidine / Imidolactam
show 22 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
primary amino compound, furans, quinazolines, piperazines (CHEBI:9445)

Targets

Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Antagonist
General Function
Protein heterodimerization activity
Specific Function
This alpha-adrenergic receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. Its effect is mediated by G(q) and G(11) prot...
Gene Name
ADRA1A
Uniprot ID
P35348
Uniprot Name
Alpha-1A adrenergic receptor
Molecular Weight
51486.005 Da
References
  1. Chapple CR: Medical therapy and quality of life. Eur Urol. 1998;34 Suppl 2:10-7; discussion 46. [PubMed:9732824]
  2. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
  3. Lee E, Lee C: Clinical comparison of selective and non-selective alpha 1A-adrenoreceptor antagonists in benign prostatic hyperplasia: studies on tamsulosin in a fixed dose and terazosin in increasing doses. Br J Urol. 1997 Oct;80(4):606-11. [PubMed:9352700]
  4. Michel MC, Grubbel B, Taguchi K, Verfurth F, Otto T, Kropfl D: Drugs for treatment of benign prostatic hyperplasia: affinity comparison at cloned alpha 1-adrenoceptor subtypes and in human prostate. J Auton Pharmacol. 1996 Feb;16(1):21-8. [PubMed:8736427]
  5. Na YJ, Guo YL, Gu FL: Clinical comparison of selective and non-selective alpha 1A-adrenoceptor antagonists for bladder outlet obstruction associated with benign prostatic hyperplasia: studies on tamsulosin and terazosin in Chinese patients. The Chinese Tamsulosin Study Group. J Med. 1998;29(5-6):289-304. [PubMed:10503165]
  6. Roehrborn CG, Schwinn DA: Alpha1-adrenergic receptors and their inhibitors in lower urinary tract symptoms and benign prostatic hyperplasia. J Urol. 2004 Mar;171(3):1029-35. [PubMed:14767264]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Antagonist
General Function
Protein heterodimerization activity
Specific Function
This alpha-adrenergic receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. Its effect is mediated by G(q) and G(11) prot...
Gene Name
ADRA1B
Uniprot ID
P35368
Uniprot Name
Alpha-1B adrenergic receptor
Molecular Weight
56835.375 Da
References
  1. Boyle P, Robertson C, Manski R, Padley RJ, Roehrborn CG: Meta-analysis of randomized trials of terazosin in the treatment of benign prostatic hyperplasia. Urology. 2001 Nov;58(5):717-22. [PubMed:11711348]
  2. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
  3. Simpson P: Stimulation of hypertrophy of cultured neonatal rat heart cells through an alpha 1-adrenergic receptor and induction of beating through an alpha 1- and beta 1-adrenergic receptor interaction. Evidence for independent regulation of growth and beating. Circ Res. 1985 Jun;56(6):884-94. [PubMed:2988814]
  4. Vincent J, Dachman W, Blaschke TF, Hoffman BB: Pharmacological tolerance to alpha 1-adrenergic receptor antagonism mediated by terazosin in humans. J Clin Invest. 1992 Nov;90(5):1763-8. [PubMed:1358918]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Antagonist
General Function
Alpha1-adrenergic receptor activity
Specific Function
This alpha-adrenergic receptor mediates its effect through the influx of extracellular calcium.
Gene Name
ADRA1D
Uniprot ID
P25100
Uniprot Name
Alpha-1D adrenergic receptor
Molecular Weight
60462.205 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]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Voltage-gated potassium channel activity involved in ventricular cardiac muscle cell action potential repolarization
Specific Function
Pore-forming (alpha) subunit of voltage-gated inwardly rectifying potassium channel. Channel properties are modulated by cAMP and subunit assembly. Mediates the rapidly activating component of the ...
Gene Name
KCNH2
Uniprot ID
Q12809
Uniprot Name
Potassium voltage-gated channel subfamily H member 2
Molecular Weight
126653.52 Da
References
  1. Thomas D, Wimmer AB, Wu K, Hammerling BC, Ficker EK, Kuryshev YA, Kiehn J, Katus HA, Schoels W, Karle CA: Inhibition of human ether-a-go-go-related gene potassium channels by alpha 1-adrenoceptor antagonists prazosin, doxazosin, and terazosin. Naunyn Schmiedebergs Arch Pharmacol. 2004 May;369(5):462-72. Epub 2004 Apr 20. [PubMed:15098086]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Voltage-gated potassium channel activity
Specific Function
Pore-forming (alpha) subunit of voltage-gated potassium channel. Elicits a slowly activating, rectifying current (By similarity). Channel properties may be modulated by cAMP and subunit assembly.
Gene Name
KCNH6
Uniprot ID
Q9H252
Uniprot Name
Potassium voltage-gated channel subfamily H member 6
Molecular Weight
109923.705 Da
References
  1. Thomas D, Wimmer AB, Wu K, Hammerling BC, Ficker EK, Kuryshev YA, Kiehn J, Katus HA, Schoels W, Karle CA: Inhibition of human ether-a-go-go-related gene potassium channels by alpha 1-adrenoceptor antagonists prazosin, doxazosin, and terazosin. Naunyn Schmiedebergs Arch Pharmacol. 2004 May;369(5):462-72. Epub 2004 Apr 20. [PubMed:15098086]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Voltage-gated potassium channel activity
Specific Function
Pore-forming (alpha) subunit of voltage-gated potassium channel. Channel properties may be modulated by cAMP and subunit assembly.
Gene Name
KCNH7
Uniprot ID
Q9NS40
Uniprot Name
Potassium voltage-gated channel subfamily H member 7
Molecular Weight
134998.525 Da
References
  1. Thomas D, Wimmer AB, Wu K, Hammerling BC, Ficker EK, Kuryshev YA, Kiehn J, Katus HA, Schoels W, Karle CA: Inhibition of human ether-a-go-go-related gene potassium channels by alpha 1-adrenoceptor antagonists prazosin, doxazosin, and terazosin. Naunyn Schmiedebergs Arch Pharmacol. 2004 May;369(5):462-72. Epub 2004 Apr 20. [PubMed:15098086]

Transporters

Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
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. Takara K, Sakaeda T, Kakumoto M, Tanigawara Y, Kobayashi H, Okumura K, Ohnishi N, Yokoyama T: Effects of alpha-adrenoceptor antagonist doxazosin on MDR1-mediated multidrug resistance and transcellular transport. Oncol Res. 2009;17(11-12):527-33. [PubMed:19806783]

Drug created on June 13, 2005 07:24 / Updated on November 12, 2018 07:41