Forasartan
Identification
- Name
- Forasartan
- Accession Number
- DB01342
- Description
Forasartan, a specific angiotensin II antagonist, is used alone or with other antihypertensive agents to treat hypertension. Forasartan competes with angiotensin II for binding at the AT1 receptor subtype. As angiotensin II is a vasoconstrictor which also stimulates the synthesis and release of aldosterone, blockage of its effects results in a decreases in systemic vascular resistance.
- Type
- Small Molecule
- Groups
- Experimental
- Structure
Structure for Forasartan (DB01342)
- Weight
- Average: 416.522
Monoisotopic: 416.243692936 - Chemical Formula
- C23H28N8
- Synonyms
- forasartán
- External IDs
- SC-52458
Pharmacology
- Indication
For the treatment of hypertension.
- Contraindications & Blackbox Warnings
Learn about our commercial Contraindications & Blackbox Warnings data.
Learn More- Pharmacodynamics
Forasartan, a specific angiotensin II antagonist, is used alone or with other antihypertensive agents to treat hypertension. By inhibiting angiotensin II receptors, this drug leads to a decrease in sodium reabsorption (which decreases water content of blood) and a decrease in vasoconstriction. Combined, this has the effect of lowering blood pressure.
- Mechanism of action
Forasartan competes with angiotensin II for binding at the AT1 receptor subtype. As angiotensin II is a vasoconstrictor which also stimulates the synthesis and release of aldosterone, blockage of its effects results in a decreases in systemic vascular resistance. Also, since angiotensin causes vasoconstriction, the inhibition of this receptor decreases vasoconstriction, which consequently also decreases vascular resistnace.
Target Actions Organism AType-1 angiotensin II receptor antagonistHumans - Absorption
- Not Available
- Volume of distribution
- Not Available
- Protein binding
- Not Available
- Metabolism
- Not Available
- Route of elimination
- Not Available
- Half-life
- Not Available
- Clearance
- Not Available
- Adverse Effects
Learn about our commercial Adverse Effects data.
Learn More- Toxicity
- Not Available
- Affected organisms
- Humans and other mammals
- Pathways
Pathway Category Forasartan Action Pathway Drug 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.
Drug Interaction Unlock Additional DataAcebutolol The risk or severity of hyperkalemia can be increased when Acebutolol is combined with Forasartan. Aceclofenac The risk or severity of renal failure, hyperkalemia, and hypertension can be increased when Forasartan is combined with Aceclofenac. Acemetacin The risk or severity of renal failure, hyperkalemia, and hypertension can be increased when Forasartan is combined with Acemetacin. Acetylsalicylic acid The risk or severity of renal failure, hyperkalemia, and hypertension can be increased when Forasartan is combined with Acetylsalicylic acid. Alclofenac The risk or severity of renal failure, hyperkalemia, and hypertension can be increased when Forasartan is combined with Alclofenac. Aliskiren The risk or severity of hyperkalemia can be increased when Aliskiren is combined with Forasartan. Alogliptin The risk or severity of angioedema can be increased when Forasartan is combined with Alogliptin. Alteplase The risk or severity of angioedema can be increased when Alteplase is combined with Forasartan. Amiloride The risk or severity of hyperkalemia can be increased when Forasartan is combined with Amiloride. Aminophenazone The risk or severity of renal failure, hyperkalemia, and hypertension can be increased when Forasartan is combined with Aminophenazone. Additional Data Available- Extended DescriptionExtended Description
Extended description of the mechanism of action and particular properties of each drug interaction.
Learn more - Severity
- Evidence Level
- ActionAction
An effect category for each drug interaction. Know how this interaction affects the subject drug.
Learn more
- Food Interactions
- Not Available
Products
Categories
- Drug Categories
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as phenylpyridines. These are polycyclic aromatic compounds containing a benzene ring linked to a pyridine ring through a CC or CN bond.
- Kingdom
- Organic compounds
- Super Class
- Organoheterocyclic compounds
- Class
- Pyridines and derivatives
- Sub Class
- Phenylpyridines
- Direct Parent
- Phenylpyridines
- Alternative Parents
- Phenyltetrazoles and derivatives / Benzene and substituted derivatives / Triazoles / Heteroaromatic compounds / Azacyclic compounds / Organopnictogen compounds / Organonitrogen compounds / Hydrocarbon derivatives
- Substituents
- 1,2,4-triazole / 2-phenylpyridine / Aromatic heteromonocyclic compound / Azacycle / Azole / Benzenoid / Heteroaromatic compound / Hydrocarbon derivative / Monocyclic benzene moiety / Organic nitrogen compound
- Molecular Framework
- Aromatic heteromonocyclic compounds
- External Descriptors
- Not Available
Chemical Identifiers
- UNII
- 065F7WPT0B
- CAS number
- 145216-43-9
- InChI Key
- YONOBYIBNBCDSJ-UHFFFAOYSA-N
- InChI
- InChI=1S/C23H28N8/c1-3-5-11-21-25-22(12-6-4-2)31(28-21)16-17-13-14-20(24-15-17)18-9-7-8-10-19(18)23-26-29-30-27-23/h7-10,13-15H,3-6,11-12,16H2,1-2H3,(H,26,27,29,30)
- IUPAC Name
- 5-[(dibutyl-1H-1,2,4-triazol-1-yl)methyl]-2-[2-(2H-1,2,3,4-tetrazol-5-yl)phenyl]pyridine
- SMILES
- CCCCC1=NN(CC2=CN=C(C=C2)C2=CC=CC=C2C2=NNN=N2)C(CCCC)=N1
References
- General References
- Not Available
- External Links
- Human Metabolome Database
- HMDB0015434
- KEGG Drug
- D04243
- PubChem Compound
- 132706
- PubChem Substance
- 46505698
- ChemSpider
- 117146
- BindingDB
- 50049209
- ChEBI
- 141552
- ChEMBL
- CHEMBL315021
- ZINC
- ZINC000005139136
- Therapeutic Targets Database
- DAP001256
- PharmGKB
- PA164776845
- Wikipedia
- Forasartan
Clinical Trials
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
- Not Available
- Prices
- Not Available
- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
- Not Available
- Predicted Properties
Property Value Source Water Solubility 0.00667 mg/mL ALOGPS logP 4.51 ALOGPS logP 5.89 ChemAxon logS -4.8 ALOGPS pKa (Strongest Acidic) 7.35 ChemAxon pKa (Strongest Basic) 3.99 ChemAxon Physiological Charge 0 ChemAxon Hydrogen Acceptor Count 6 ChemAxon Hydrogen Donor Count 1 ChemAxon Polar Surface Area 98.06 Å2 ChemAxon Rotatable Bond Count 10 ChemAxon Refractivity 145.44 m3·mol-1 ChemAxon Polarizability 46.79 Å3 ChemAxon Number of Rings 4 ChemAxon Bioavailability 1 ChemAxon Rule of Five No ChemAxon Ghose Filter No ChemAxon Veber's Rule No ChemAxon MDDR-like Rule Yes ChemAxon - Predicted ADMET Features
Property Value Probability Human Intestinal Absorption + 1.0 Blood Brain Barrier + 0.9069 Caco-2 permeable + 0.5 P-glycoprotein substrate Substrate 0.615 P-glycoprotein inhibitor I Non-inhibitor 0.6612 P-glycoprotein inhibitor II Non-inhibitor 0.8805 Renal organic cation transporter Inhibitor 0.5228 CYP450 2C9 substrate Non-substrate 0.7854 CYP450 2D6 substrate Non-substrate 0.831 CYP450 3A4 substrate Non-substrate 0.5512 CYP450 1A2 substrate Non-inhibitor 0.64 CYP450 2C9 inhibitor Non-inhibitor 0.5115 CYP450 2D6 inhibitor Non-inhibitor 0.7168 CYP450 2C19 inhibitor Inhibitor 0.7661 CYP450 3A4 inhibitor Inhibitor 0.6576 CYP450 inhibitory promiscuity High CYP Inhibitory Promiscuity 0.7192 Ames test Non AMES toxic 0.5233 Carcinogenicity Non-carcinogens 0.8243 Biodegradation Not ready biodegradable 0.9969 Rat acute toxicity 2.7970 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.6462 hERG inhibition (predictor II) Non-inhibitor 0.546
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Spectrum Spectrum Type Splash Key Predicted GC-MS Spectrum - GC-MS Predicted GC-MS Not Available Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS Not Available
Targets
- 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
- Tokunaga R, Kushiku K, Yamada K, Yamada H, Furukawa T: Possible involvement of calcium-calmodulin pathways in the positive chronotropic response to angiotensin II on the canine cardiac sympathetic ganglia. Jpn J Pharmacol. 2001 Aug;86(4):381-9. [PubMed:11569611]
- Usune S, Furukawa T: Effects of SC-52458, a new nonpeptide angiotensin II receptor antagonist, on increase in cytoplasmic Ca2+ concentrations and contraction induced by angiotensin II and K(+)-depolarization in guinea-pig taenia coli. Gen Pharmacol. 1996 Oct;27(7):1179-85. [PubMed:8981065]
- Hagmann M, Nussberger J, Naudin RB, Burns TS, Karim A, Waeber B, Brunner HR: SC-52458, an orally active angiotensin II-receptor antagonist: inhibition of blood pressure response to angiotensin II challenges and pharmacokinetics in normal volunteers. J Cardiovasc Pharmacol. 1997 Apr;29(4):444-50. [PubMed:9156352]
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
Drug created on June 30, 2007 12:11 / Updated on June 12, 2020 10:51
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