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Identification
Name Forasartan
Accession Number DB01342
Type small molecule
Groups approved
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.
Structure Thumb
Download: MOL | SDF | SMILES | InChI
Display: 2D Structure | 3D Structure
Synonyms Not Available
Brand names Not Available
Brand name mixtures Not Available
Categories
  • Antihypertensive Agents
  • Angiotensin II Receptor Antagonists
CAS number 145216-43-9
Weight Average: 416.522
Monoisotopic: 416.243692936
Chemical Formula C23H28N8
InChI Key InChIKey=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)
Plain Text
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=CC=C(N=C2)C2=C(C=CC=C2)C2=NNN=N2)C(CCCC)=N1
Plain Text
Mass Spec Not Available
Taxonomy
Kingdom Organic
Classes
  • Phenyltetrazoles and Derivatives
Substructures
  • Triazoles
  • Pyridines and Derivatives
  • Benzene and Derivatives
  • Tetrazoles
  • Phenyltetrazoles and Derivatives
  • Heterocyclic compounds
  • Aromatic compounds
  • Imines
  • Cyanamides
Pharmacology
Indication For the treatment of hypertension.
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.
Absorption Not Available
Volume of distribution Not Available
Protein binding Not Available
Metabolism
Route of elimination Not Available
Half life Not Available
Clearance Not Available
Toxicity Not Available
Affected organisms
  • Humans and other mammals
Pathways Not Available
Pharmacoeconomics
Manufacturers Not Available
Packagers Not Available
Dosage forms Not Available
Prices Not Available
Patents Not Available
Properties
State solid
Melting point Not Available
Experimental Properties Not Available
Predicted Properties
Property Value Source
water solubility 6.67e-03 g/l ALOGPS
logP 4.51 ALOGPS
logP 5.89 ChemAxon Molconvert
logS -4.80 ALOGPS
pKa ChemAxon Molconvert
hydrogen acceptor count 6 ChemAxon Molconvert
hydrogen donor count 1 ChemAxon Molconvert
polar surface area 98.06 ChemAxon Molconvert
rotatable bond count 10 ChemAxon Molconvert
refractivity 145.44 ChemAxon Molconvert
polarizability 46.79 ChemAxon Molconvert
References
Synthesis Reference Not Available
General Reference Not Available
External Links
Resource Link
PubChem Compound 132706 Link_out
PubChem Substance 46505698 Link_out
ChemSpider 117146 Link_out
BindingDB 50049209 Link_out
Therapeutic Targets Database DAP001256 Link_out
Drug Product Database 0 Link_out
ATC Codes Not Available
AHFS Codes Not Available
PDB Entries Not Available
FDA label Not Available
MSDS Not Available
Interactions
Drug Interactions Not Available
Food Interactions Not Available
Targets

1. Type-1 angiotensin II receptor

Pharmacological action: yes
Actions: antagonist

Receptor for angiotensin II. Mediates its action by association with G proteins that activate a phosphatidylinositol- calcium second messenger system

Organism class: human
UniProt ID: P30556 Link_out
Gene: AGTR1 Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

References:
  1. 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
  2. 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
  3. 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
  4. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. Pubmed
Comments
Drug created on June 30, 2007 12:11 / Updated on November 10, 2010 13:48

This project is supported by Genome Alberta & Genome Canada, a not-for-profit organization that is leading Canada's national genomics strategy with $600 million in funding from the federal government. This project is also supported in part by GenomeQuest, Inc., an enterprise genomic information company serving the life science community.