Eprosartan

Identification

Summary

Eprosartan is an ARB used to treat hypertension, diabetic nephropathy, and congestive heart failure.

Brand Names
Teveten HCT
Generic Name
Eprosartan
DrugBank Accession Number
DB00876
Background

Eprosartan is an angiotensin II receptor antagonist used to treat hypertension. It performs 2 actions on the renin angiotensin system. By preventing the binding of angiotensin II to AT1, vascular smooth muscle relaxes and vasodilation occurs. By inhibiting norepinephrine production, blood pressure is further reduced.

Type
Small Molecule
Groups
Approved
Structure
Weight
Average: 424.513
Monoisotopic: 424.145677956
Chemical Formula
C23H24N2O4S
Synonyms
  • (E)-2-butyl-1-(p-carboxybenzyl)-α-2-thenylimidazole-5-acrylic acid
  • (E)-3-[2-n-butyl-1-{(4-carboxyphenyl)methyl}-1H-imidazol-5-yl]-2-(2-thienyl)methyl-2-propenoic acid
  • (E)-α{[2-butyl-1-[(4-carboxyphenyl)methyl]-1H-imidazole-5-yl]methylene}-2-thiopheneproprionic acid
  • Éprosartan
  • Eprosartan
  • Eprosartanum
External IDs
  • SK&F-108566
  • SKF 108566

Pharmacology

Indication

For the management of hypertension alone or in combination with other classes of antihypertensive agents. Also used as a first-line agent in the treatment of diabetic nephropathy, as well as a second-line agent in the treatment of congestive heart failure (only in those intolerant of ACE inhibitors).

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Associated Conditions
Indication TypeIndicationCombined Product DetailsApproval LevelAge GroupPatient CharacteristicsDose Form
Management ofCongestive heart failure••• •••••
Management ofDiabetic nephropathy••• •••••
Used in combination to manageHypertensionCombination Product in combination with: Hydrochlorothiazide (DB00999)•••••••••••••••••••••• ••••••• •••• •••••••••••
Adjunct therapy in management ofHypertension••••••••••••••••••
Management ofHypertension••••••••••••••••••
Contraindications & Blackbox Warnings
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Pharmacodynamics

Angiotensin II, the principal pressor agent of the renin-angiotensin system, is formed from angiotensin I in a reaction catalyzed by angiotensin-converting enzyme [kininase II]. It is responsible for effects such as vasoconstriction, stimulation of synthesis and release of aldosterone, cardiac stimulation, and renal reabsorption of sodium. Eprosartan selectively blocks the binding of angiotensin II to the AT1 receptor, which in turn leads to multiple effects including vasodilation, a reduction in the secretion of vasopressin, and reduction in the production and secretion of aldosterone. The resulting effect is a decrease in blood pressure.

Mechanism of action

Eprosartan blocks the vasoconstrictor and aldosterone-secreting effects of angiotensin II by selectively blocking the binding of angiotensin II to the AT1 receptor found in many tissues (e.g., vascular smooth muscle, adrenal gland). There is also an AT2 receptor found in many tissues but it is not known to be associated with cardiovascular homeostasis. Eprosartan does not exhibit any partial agonist activity at the AT1 receptor. Its affinity for the AT1 receptor is 1,000 times greater than for the AT2 receptor. In vitro binding studies indicate that eprosartan is a reversible, competitive inhibitor of the AT1 receptor. Eprosartan has also been shown to bind to AT1 receptors both presynaptically and synaptically. Its action on presynaptic AT1 receptors results in the inhibition of sympathetically stimulated noradrenaline release. Unlike ACE inhibitors, eprosartan and other ARBs do not interfere with response to bradykinins and substance P, which allows for the absence of adverse effects that are present in ACE inhibitors (eg. dry cough).

TargetActionsOrganism
AType-1 angiotensin II receptor
antagonist
Humans
Absorption

Absolute bioavailability following a single 300 mg oral dose of eprosartan is approximately 13%. Administering eprosartan with food delays absorption.

Volume of distribution

Not Available

Protein binding

Plasma protein binding of eprosartan is high (approximately 98%) and constant over the concentration range achieved with therapeutic doses.

Metabolism

Eprosartan is not metabolized by the cytochrome P450 system. It is mainly eliminated as unchanged drug. Less than 2% of an oral dose is excreted in the urine as a glucuronide.

Route of elimination

Not Available

Half-life

The terminal elimination half-life of eprosartan following oral administration is typically 5 to 9 hours.

Clearance

Not Available

Adverse Effects
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Toxicity

There was no mortality in rats and mice receiving oral doses of up to 3000 mg eprosartan/kg and in dogs receiving oral doses of up to 1000 mg eprosartan/kg.

Pathways
PathwayCategory
Eprosartan Action PathwayDrug action
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
DrugInteraction
AbaloparatideThe risk or severity of adverse effects can be increased when Eprosartan is combined with Abaloparatide.
AcebutololEprosartan may increase the hypotensive activities of Acebutolol.
AceclofenacThe risk or severity of renal failure, hyperkalemia, and hypertension can be increased when Eprosartan is combined with Aceclofenac.
AcemetacinThe risk or severity of renal failure, hyperkalemia, and hypertension can be increased when Eprosartan is combined with Acemetacin.
Acetylsalicylic acidThe risk or severity of renal failure, hyperkalemia, and hypertension can be increased when Eprosartan is combined with Acetylsalicylic acid.
Food Interactions
  • Take with or without food. The absorption is unaffected by food.

Products

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Product Ingredients
IngredientUNIICASInChI Key
Eprosartan mesylate8N2L1NX8S3144143-96-4DJSLTDBPKHORNY-XMMWENQYSA-N
Eprosartan mesylate dihydrate9G2HB74868197855-71-3HIUNDVRJXJGSGV-KMDBKMSFSA-N
Product Images
International/Other Brands
Eprozar (INTAS Pharmaceuticals) / Futuran (Merck) / Teveten
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
TevetenTablet600 mg/1OralAbbVie Inc.2010-05-242015-06-18US flag
TevetenTablet400 mgOralBgp Pharma Ulc2000-09-082023-09-18Canada flag
TevetenTablet400 mg/1OralKos Pharmaceuticals, Inc.2007-02-202007-02-20US flag
TevetenTablet400 mg/1OralAbbVie Inc.2010-05-242013-10-12US flag
TevetenTablet400 mg/1OralPhysicians Total Care, Inc.2003-04-302008-09-30US flag
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Eprosartan MesylateTablet, film coated600 mg/1OralMylan Pharmaceuticals Inc.2011-12-202019-03-31US flag
Eprosartan MesylateTablet, film coated400 mg/1OralMylan Pharmaceuticals Inc.2011-11-162011-06-15US flag
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
EPROSARTAN RAT COM600/12.5Eprosartan mesylate (600 mg) + Hydrochlorothiazide (12.5 mg)Tablet, film coatedOral2016-07-01Not applicableGermany flag
EPROSARTAN RAT COM600/12.5Eprosartan mesylate (600 mg) + Hydrochlorothiazide (12.5 mg)Tablet, film coatedOral2016-07-01Not applicableGermany flag
EPROSARTAN RAT COM600/12.5Eprosartan mesylate (600 mg) + Hydrochlorothiazide (12.5 mg)Tablet, film coatedOral2016-07-01Not applicableGermany flag
Teveten HCTEprosartan mesylate (600 mg/1) + Hydrochlorothiazide (12.5 mg/1)TabletOralKos Pharmaceuticals, Inc.2007-01-202007-01-20US flag
Teveten HCTEprosartan mesylate (600 mg/1) + Hydrochlorothiazide (12.5 mg/1)TabletOralPhysicians Total Care, Inc.2005-05-06Not applicableUS flag

Categories

ATC Codes
C09DA02 — Eprosartan and diureticsC09CA02 — Eprosartan
Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
This compound belongs to the class of organic compounds known as benzoic acids. These are organic Compounds containing a benzene ring which bears at least one carboxyl group.
Kingdom
Organic compounds
Super Class
Benzenoids
Class
Benzene and substituted derivatives
Sub Class
Benzoic acids and derivatives
Direct Parent
Benzoic acids
Alternative Parents
Imidazolyl carboxylic acids and derivatives / Benzoyl derivatives / 1,2,5-trisubstituted imidazoles / N-substituted imidazoles / Dicarboxylic acids and derivatives / Thiophenes / Heteroaromatic compounds / Carboxylic acids / Azacyclic compounds / Organopnictogen compounds
show 4 more
Substituents
1,2,5-trisubstituted-imidazole / Aromatic heteromonocyclic compound / Azacycle / Azole / Benzoic acid / Benzoyl / Carbonyl group / Carboxylic acid / Carboxylic acid derivative / Dicarboxylic acid or derivatives
show 14 more
Molecular Framework
Aromatic heteromonocyclic compounds
External Descriptors
imidazoles, thiophenes, dicarboxylic acid (CHEBI:4814)
Affected organisms
  • Humans and other mammals

Chemical Identifiers

UNII
2KH13Z0S0Y
CAS number
133040-01-4
InChI Key
OROAFUQRIXKEMV-LDADJPATSA-N
InChI
InChI=1S/C23H24N2O4S/c1-2-3-6-21-24-14-19(12-18(23(28)29)13-20-5-4-11-30-20)25(21)15-16-7-9-17(10-8-16)22(26)27/h4-5,7-12,14H,2-3,6,13,15H2,1H3,(H,26,27)(H,28,29)/b18-12+
IUPAC Name
4-({2-butyl-5-[(1E)-2-carboxy-2-[(thiophen-2-yl)methyl]eth-1-en-1-yl]-1H-imidazol-1-yl}methyl)benzoic acid
SMILES
CCCCC1=NC=C(\C=C(/CC2=CC=CS2)C(O)=O)N1CC1=CC=C(C=C1)C(O)=O

References

Synthesis Reference

Richard T. Matsuoka, Peng Liu, "Process for preparing eprosartan using regioselective protection of 2,4-disubstituted-imidazole intermediates." U.S. Patent US6294675, issued June, 1992.

US6294675
General References
  1. Ruilope L, Jager B, Prichard B: Eprosartan versus enalapril in elderly patients with hypertension: a double-blind, randomized trial. Blood Press. 2001;10(4):223-9. [Article]
  2. Hedner T: The clinical profile of the angiotensin II receptor blocker eprosartan. J Hypertens Suppl. 2002 Jun;20(5):S33-8. [Article]
  3. Puig JG, Lopez MA, Bueso TS, Bernardino JI, Jimenez RT: Clinical profile of eprosartan. Cardiovasc Drugs Ther. 2002 Dec;16(6):543-9. [Article]
  4. Ruilope L, Jager B: Eprosartan for the treatment of hypertension. Expert Opin Pharmacother. 2003 Jan;4(1):107-14. [Article]
  5. de la Sierra A, Ram CV: Introduction: The pharmacological profile of eprosartan--implications for cerebrovascular and cardiovascular risk reduction. Curr Med Res Opin. 2007 Nov;23 Suppl 5:S1-3. doi: 10.1185/030079907X260692. [Article]
  6. Blankestijn PJ, Rupp H: Clinical profile of eprosartan: a different angiotensin II receptor blocker. Cardiovasc Hematol Agents Med Chem. 2008 Oct;6(4):253-7. [Article]
  7. FDA Approved Drug Products: Teveten HCT (eprosartan mesylate/hydrochlorothiazide) oral tablets [Link]
Human Metabolome Database
HMDB0015014
KEGG Drug
D04040
KEGG Compound
C07467
PubChem Compound
5281037
PubChem Substance
46506765
ChemSpider
4444504
BindingDB
50011977
RxNav
83515
ChEBI
4814
ChEMBL
CHEMBL813
ZINC
ZINC000029319828
Therapeutic Targets Database
DAP001367
PharmGKB
PA449481
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
PDRhealth
PDRhealth Drug Page
Wikipedia
Eprosartan
FDA label
Download (1.09 MB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4CompletedNot AvailableHealthy Volunteers (HV)1
4CompletedNot AvailableHypertension, Essential Hypertension1
4CompletedTreatmentCoronavirus Disease 2019 (COVID‑19)1
4RecruitingTreatmentCardiovascular Disease (CVD) / Type 2 Diabetes Mellitus1
4SuspendedPreventionCoronavirus Disease 2019 (COVID‑19) / Hypertension1

Pharmacoeconomics

Manufacturers
  • Abbott laboratories
Packagers
  • Abbott Laboratories Ltd.
  • BTA Pharmaceuticals
  • Irvs Pharmacy and Sickroom Supply
  • Physicians Total Care Inc.
  • Solvay Pharmaceuticals
Dosage Forms
FormRouteStrength
TabletOral
TabletOral735.80 mg
Tablet, film coatedOral
Tablet, film coatedOral400 mg/1
Tablet, film coatedOral600 mg/1
Tablet, coatedOral600 mg
TabletOral400 mg
TabletOral400 mg/1
TabletOral600 mg
TabletOral600 mg/1
Tablet, film coatedOral
Tablet, film coatedOral400 mg
TabletOral
Tablet, film coatedOral600 mg
TabletOral300 mg
Tablet, coatedOral
TabletOral200 MG
TabletOral600.00 mg
Prices
Unit descriptionCostUnit
Teveten hct 600-12.5 mg tablet3.52USD tablet
Teveten hct 600-25 mg tablet3.42USD tablet
Teveten 600 mg tablet3.19USD tablet
Teveten 400 mg tablet2.83USD tablet
Teveten 400 mg tiltab1.24USD tablet
Teveten 600 mg Tablet1.18USD tablet
Teveten 400 mg Tablet0.79USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
US5656650No1997-08-122014-08-12US flag
US5185351No1993-02-092010-02-09US flag
CA2250395No2005-09-062017-03-26Canada flag
CA2115170No2004-05-252012-08-12Canada flag

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)248-250 °C (mesylate form)Not Available
water solubilityInsoluble (mesylate form)Not Available
logP3.9Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.00866 mg/mLALOGPS
logP3.57ALOGPS
logP3.75Chemaxon
logS-4.7ALOGPS
pKa (Strongest Acidic)3.47Chemaxon
pKa (Strongest Basic)6.67Chemaxon
Physiological Charge-2Chemaxon
Hydrogen Acceptor Count5Chemaxon
Hydrogen Donor Count2Chemaxon
Polar Surface Area92.42 Å2Chemaxon
Rotatable Bond Count10Chemaxon
Refractivity117.02 m3·mol-1Chemaxon
Polarizability45.37 Å3Chemaxon
Number of Rings3Chemaxon
Bioavailability1Chemaxon
Rule of FiveYesChemaxon
Ghose FilterYesChemaxon
Veber's RuleNoChemaxon
MDDR-like RuleYesChemaxon
Predicted ADMET Features
PropertyValueProbability
Human Intestinal Absorption+0.9863
Blood Brain Barrier-0.6931
Caco-2 permeable-0.6261
P-glycoprotein substrateSubstrate0.8011
P-glycoprotein inhibitor INon-inhibitor0.8577
P-glycoprotein inhibitor IINon-inhibitor0.9574
Renal organic cation transporterNon-inhibitor0.7673
CYP450 2C9 substrateNon-substrate0.7897
CYP450 2D6 substrateNon-substrate0.9116
CYP450 3A4 substrateNon-substrate0.7557
CYP450 1A2 substrateNon-inhibitor0.5798
CYP450 2C9 inhibitorNon-inhibitor0.6617
CYP450 2D6 inhibitorNon-inhibitor0.8325
CYP450 2C19 inhibitorNon-inhibitor0.6234
CYP450 3A4 inhibitorNon-inhibitor0.6086
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.644
Ames testNon AMES toxic0.7313
CarcinogenicityNon-carcinogens0.9454
BiodegradationNot ready biodegradable0.6117
Rat acute toxicity2.4288 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9464
hERG inhibition (predictor II)Non-inhibitor0.8827
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-MSsplash10-0570-3319300000-aac3fe556775bf3acc88
LC-MS/MS Spectrum - LC-ESI-ITFT , negativeLC-MS/MSsplash10-004i-0009000000-fa421ee23b907968b800
LC-MS/MS Spectrum - LC-ESI-ITFT , negativeLC-MS/MSsplash10-00di-0002900000-694c481f9555295f9426
LC-MS/MS Spectrum - LC-ESI-ITFT , negativeLC-MS/MSsplash10-004u-0289000000-647b9ea41a7a812dea66
LC-MS/MS Spectrum - LC-ESI-ITFT , negativeLC-MS/MSsplash10-00kg-0290000000-08e189bdaeb9c6af3b4f
LC-MS/MS Spectrum - LC-ESI-ITFT , negativeLC-MS/MSsplash10-014j-1290000000-e8207e65f017389d706f
LC-MS/MS Spectrum - LC-ESI-ITFT , negativeLC-MS/MSsplash10-00lr-9260000000-7b844b75045cf89e145e
LC-MS/MS Spectrum - LC-ESI-ITFT , negativeLC-MS/MSsplash10-001i-9100000000-f49fc8384f38dc7b6e3b
LC-MS/MS Spectrum - LC-ESI-ITFT , negativeLC-MS/MSsplash10-00di-0002900000-e62e6d74d830487d0954
LC-MS/MS Spectrum - LC-ESI-ITFT , negativeLC-MS/MSsplash10-002u-0198000000-d571b7bcdbe9e3f7e69f
LC-MS/MS Spectrum - LC-ESI-ITFT , negativeLC-MS/MSsplash10-00kp-0290000000-0b7c3fe664812ce51596
LC-MS/MS Spectrum - LC-ESI-ITFT , negativeLC-MS/MSsplash10-014j-1090000000-85f4ee357273ee0268c0
LC-MS/MS Spectrum - LC-ESI-ITFT , negativeLC-MS/MSsplash10-001i-9240000000-8ed6c4fadafd173a2579
LC-MS/MS Spectrum - LC-ESI-ITFT , negativeLC-MS/MSsplash10-001i-9400000000-81bd0b20c45458b1bdec
LC-MS/MS Spectrum - LC-ESI-ITFT , negativeLC-MS/MSsplash10-004i-0009000000-0333ac2f95788dceda2c
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-0a4l-0196300000-c2476723863e5584d7e8
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-004i-0000900000-a93af7ff9cf5786971d0
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-056r-0171900000-4a8d34412967af4cbf35
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-052r-1971000000-ee85641cdce897ab6693
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-052r-1920000000-282ecc38e7c0c6cbefef
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-0a4i-1900000000-1a109162fa90e4ce7932
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-0a4i-2900000000-54946c90c1dfdf5eb21e
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-004i-0000900000-f33c4c2419ad566fa726
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-056r-1172900000-e0852717bfa6c5f8f0cd
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-052r-1970000000-fed4d418faa53031f6ca
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-052r-1920000000-2ddeec1f39e95c27109d
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-0a4r-1910000000-2953fc7d89567648d5ea
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-0a4i-1900000000-1e52f8edbad114f026d5
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-0a4l-0196300000-e398b1a8add5df82164b
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSsplash10-004i-0000900000-47670e6d690e26131521
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSsplash10-00dj-2035900000-ea938a8888c44bdf608a
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSsplash10-056r-0002900000-8871b707ac586d510fa5
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSsplash10-005i-1019000000-4761a310585bc7053c07
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSsplash10-05mo-5916200000-b96804b88b805ad72e95
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSsplash10-0a5d-1469000000-ed1b1ec735fa70396845
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]-219.3919135
predicted
DarkChem Lite v0.1.0
[M-H]-223.3712135
predicted
DarkChem Lite v0.1.0
[M-H]-194.71751
predicted
DeepCCS 1.0 (2019)
[M+H]+217.3415135
predicted
DarkChem Lite v0.1.0
[M+H]+220.5128135
predicted
DarkChem Lite v0.1.0
[M+H]+197.07552
predicted
DeepCCS 1.0 (2019)
[M+Na]+216.6577135
predicted
DarkChem Lite v0.1.0
[M+Na]+221.0652135
predicted
DarkChem Lite v0.1.0
[M+Na]+203.21538
predicted
DeepCCS 1.0 (2019)

Targets

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Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Antagonist
General Function
Protein heterodimerization activity
Specific Function
Receptor for angiotensin II. Mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system.
Gene Name
AGTR1
Uniprot ID
P30556
Uniprot Name
Type-1 angiotensin II receptor
Molecular Weight
41060.53 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. Heusser K, Vitkovsky J, Schmieder RE, Schobel HP: AT1 antagonism by eprosartan lowers heart rate variability and baroreflex gain. Auton Neurosci. 2003 Aug 29;107(1):45-51. [Article]
  3. Gremmler B, Kunert M, Schleiting H, Ulbricht LJ: Improvement of cardiac output in patients with severe heart failure by use of ACE-inhibitors combined with the AT1-antagonist eprosartan. Eur J Heart Fail. 2000 Jun;2(2):183-7. [Article]
  4. Suzuki G, Mishima T, Tanhehco EJ, Sharov VG, Todor A, Rostogi S, Gupta RC, Chaudhry PA, Anagnostopoulos PV, Nass O, Goldstein S, Sabbah HN: Effects of the AT1-receptor antagonist eprosartan on the progression of left ventricular dysfunction in dogs with heart failure. Br J Pharmacol. 2003 Jan;138(2):301-9. [Article]
  5. Ilson BE, Martin DE, Boike SC, Jorkasky DK: The effects of eprosartan, an angiotensin II AT1 receptor antagonist, on uric acid excretion in patients with mild to moderate essential hypertension. J Clin Pharmacol. 1998 May;38(5):437-41. [Article]
  6. Nap A, Mathy MJ, Balt JC, Pfaffendorf M, van Zwieten PA: Pre- and postsynaptic inhibitory potencies of the angiotensin AT1 receptor antagonists eprosartan and candesartan. Eur J Pharmacol. 2003 May 23;469(1-3):117-24. [Article]
  7. Hedner T: The clinical profile of the angiotensin II receptor blocker eprosartan. J Hypertens Suppl. 2002 Jun;20(5):S33-8. [Article]
  8. Puig JG, Lopez MA, Bueso TS, Bernardino JI, Jimenez RT: Clinical profile of eprosartan. Cardiovasc Drugs Ther. 2002 Dec;16(6):543-9. [Article]
  9. Ruilope L, Jager B: Eprosartan for the treatment of hypertension. Expert Opin Pharmacother. 2003 Jan;4(1):107-14. [Article]
  10. de la Sierra A, Ram CV: Introduction: The pharmacological profile of eprosartan--implications for cerebrovascular and cardiovascular risk reduction. Curr Med Res Opin. 2007 Nov;23 Suppl 5:S1-3. doi: 10.1185/030079907X260692. [Article]
  11. Murdoch DR, McDonagh TA, Farmer R, Morton JJ, McMurray JJ, Dargie HJ: ADEPT: Addition of the AT1 receptor antagonist eprosartan to ACE inhibitor therapy in chronic heart failure trial: hemodynamic and neurohormonal effects. Am Heart J. 2001 May;141(5):800-7. [Article]

Transporters

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inducer
General Function
Organic anion transmembrane transporter activity
Specific Function
Mediates hepatobiliary excretion of numerous organic anions. May function as a cellular cisplatin transporter.
Gene Name
ABCC2
Uniprot ID
Q92887
Uniprot Name
Canalicular multispecific organic anion transporter 1
Molecular Weight
174205.64 Da
References
  1. Weiss J, Sauer A, Divac N, Herzog M, Schwedhelm E, Boger RH, Haefeli WE, Benndorf RA: Interaction of angiotensin receptor type 1 blockers with ATP-binding cassette transporters. Biopharm Drug Dispos. 2010 Mar;31(2-3):150-61. doi: 10.1002/bdd.699. [Article]

Drug created at June 13, 2005 13:24 / Updated at March 18, 2024 16:48