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Forasartan

Forasartan structure

Forasartan 

structure
  • CAS No:

    145216-43-9

  • Formula:

    C23H28N8

  • Chemical Name:

    Forasartan

  • Synonyms:

    Pyridine,5-[(3,5-dibutyl-1H-1,2,4-triazol-1-yl)methyl]-2-[2-(2H-tetrazol-5-yl)phenyl]-;Pyridine,5-[(3,5-dibutyl-1H-1,2,4-triazol-1-yl)methyl]-2-[2-(1H-tetrazol-5-yl)phenyl]-;5-[(3,5-Dibutyl-1H-1,2,4-triazol-1-yl)methyl]-2-[2-(2H-tetrazol-5-yl)phenyl]pyridine;SC 52458;Forasartan

Description

Solid


Forasartan is a member of the class of pyridines that is pyridine which is substituted at positions 2 and 5 by o-(tetrazol-5-yl)phenyl and (3,5-dibutyl-1,2,4-triazol-1-yl)methyl groups, respectively. It is a nonpeptide antagonist of angiotensin II, type 1 (AT1) receptors, used for the treatment of hypertension. It has a role as an angiotensin receptor antagonist and an antihypertensive agent. It is a member of tetrazoles, a member of pyridines, a member of triazoles and a member of benzenes.|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.|Forasartan is a nonpeptide angiotensin II receptor antagonist with antihypertensive activity. Forasartan selectively competes with angiotensin II for the binding of the angiotensin II (AT1) receptor subtype 1 in vascular smooth muscle, thereby blocking angiotensin II-mediated vasoconstriction resulting in vascular dilatation. In addition, the antagonistic effect on AT1 in the adrenal gland, prevents angiotensin II-induced stimulation of aldosterone synthesis and secretion by the adrenal cortex. This blocks the effects of aldosterone leading to an increase in sodium excretion and water and eventually a reduction in plasma volume and blood pressure.

Forasartan Basic Attributes

416.52200

416.52

065F7WPT0B

DTXSID70162942

C65749

Characteristics

98.06000

4.25370

1.26g/cm3

681.6ºC at 760mmHg

366ºC

1.668

6.67e-03 g/L

1.96E-18mmHg at 25°C

Drug Information

For the treatment of hypertension.

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.

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.

5-((3,5-dibutyl-1H-1,2,4-triazol-1-yl)methyl)-2-(2-(1H-tetrazol-5-ylphenyl))pyridine

Computed Properties

Molecular Weight:416.5
XLogP3:4.9
Hydrogen Bond Donor Count:1
Hydrogen Bond Acceptor Count:6
Rotatable Bond Count:10
Exact Mass:416.24369293
Monoisotopic Mass:416.24369293
Topological Polar Surface Area:98.1
Heavy Atom Count:31
Complexity:520
Covalently-Bonded Unit Count:1
Compound Is Canonicalized:Yes

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