FORASARTAN

Details

Stereochemistry	ACHIRAL
Molecular Formula	C23H28N8
Molecular Weight	416.522
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CCCCC1=NN(CC2=CN=C(C=C2)C3=CC=CC=C3C4=NN=NN4)C(CCCC)=N1

InChI

InChIKey=YONOBYIBNBCDSJ-UHFFFAOYSA-N

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)

HIDE SMILES / InChI

Description
Sources: https://www.ncbi.nlm.nih.gov/pubmed/9156352 | https://www.ncbi.nlm.nih.gov/pubmed/7505365

Forasartan (also known as SC-52458) was developed as an orally active, competitive angiotensin (Ang) II subtype 1 (AT1)-receptor antagonist for the treatment of hypertension. Forasartan competes with angiotensin II for binding at the AT1 receptor subtype. It is known that angiotensin II is a vasoconstrictor and stimulates the synthesis and release of aldosterone, and blockage of its effects results in a decrease in systemic vascular resistance. Information about the further development of forasartan is not available.

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Type-1 angiotensin II receptor 41 Target ID: P30556 Gene ID: 185.0 Gene Symbol: AGTR1 Target Organism: Homo sapiens (Human) Sources: https://www.ncbi.nlm.nih.gov/pubmed/8981065 \| https://www.ncbi.nlm.nih.gov/pubmed/9156352	Antagonist 2849

PubMed

Title	Date	PubMed
[Bee (Apis mellifera, Hymenoptera: Apoidea) visitation to cantaloupe Cucumis melo (Cucurvitaceae) flowers in Panama].	2007-06	19069779
Non-peptide angiotensin II receptor antagonists: chemical feature based pharmacophore identification.	2003-02-27	12593652
Inositol(1,4,5)trisphosphate signal triggers a receptor-mediated ATP release.	2002-05-03	12054523
Possible involvement of calcium-calmodulin pathways in the positive chronotropic response to angiotensin II on the canine cardiac sympathetic ganglia.	2001-08	11569611
Upregulation of immunoreactive angiotensin II release and angiotensinogen mRNA expression by high-frequency preganglionic stimulation at the canine cardiac sympathetic ganglia.	2001-01-19	11139482
Elucidation of the insurmountable nature of an angiotensin receptor antagonist, SC-54629.	1995-01	7838120
Pharmacology of SC-52458, an orally active, nonpeptide angiotensin AT1 receptor antagonist.	1993-10	7505365

Sample Use Guides

In Vivo Use Guide

two groups of eight healthy men ingested placebo or increasing single oral doses (10, 25, and 50 mg or 100, 150, and 200 mg) of SC-52458 (FORASARTAN).

Route of Administration: Oral

Name

Type

Language

FORASARTAN

Official Name

English

SC-52458

Preferred Name

English

forasartan [INN]

Common Name

English

FORASARTAN [USAN]

Common Name

English

Forasartan [WHO-DD]

Common Name

English

5-[(3,5-Dibutyl-1H-1,2,4-triazol-1-yl)methyl]-2-(O-1H-tetrazol-5-ylphenyl)pyridine

Common Name

English

PYRIDINE, 5-((3,5-DIBUTYL-1H-1,2,4-TRIAZOL-1-YL)METHYL)-2-(2-(1H-TETRAZOL-5-YL)PHENYL)-

Systematic Name

English

Classification Tree Code System Code

NCI_THESAURUS

C66930