Saprisartan

Các tên gọi khác (4 ) :

GR-138950
GR-138950C
Saprisartan
Saprisartan potassium

Thuốc Gốc

Small Molecule

CAS: 146623-69-0

CTHH: C₂₅H₂₂BrF₃N₄O₄S

PTK: 611.431

Saprisartan is an AT1 receptor antagonist. It is based on medications of losartan's prototypical chemical structure. The mode of (functional) AT1 receptor antagonism has been characterized as insurmountable/noncompetitive for saprisartan. It is very likely that slow dissociation kinetics from the AT1 receptor underlie insurmountable antagonism.(10579749)

Nhận Dạng Quốc Tế & Đặc Tính Hóa Học

Công thức hóa học

C₂₅H₂₂BrF₃N₄O₄S

Phân tử khối

611.431

Monoisotopic mass

610.049723164

InChI

InChI=1S/C25H22BrF3N4O4S/c1-2-19-31-21(14-8-9-14)22(24(30)34)33(19)12-13-7-10-18-16(11-13)20(26)23(37-18)15-5-3-4-6-17(15)32-38(35,36)25(27,28)29/h3-7,10-11,14,32H,2,8-9,12H2,1H3,(H2,30,34)

InChI Key

InChIKey=DUEWVPTZCSAMNB-UHFFFAOYSA-N

IUPAC Name

1-({3-bromo-2-[2-(trifluoromethane)sulfonamidophenyl]-1-benzofuran-5-yl}methyl)-4-cyclopropyl-2-ethyl-1H-imidazole-5-carboxamide

Traditional IUPAC Name

3-{[3-bromo-2-(2-trifluoromethanesulfonamidophenyl)-1-benzofuran-5-yl]methyl}-5-cyclopropyl-2-ethylimidazole-4-carboxamide

SMILES

CCC1=NC(C2CC2)=C(N1CC1=CC2=C(OC(=C2Br)C2=CC=CC=C2NS(=O)(=O)C(F)(F)F)C=C1)C(N)=O

Độ hòa tan

1.51e-02 g/l

logP

3.35

logS

-4.6

pKa (strongest acidic)

2.27

pKa (Strongest Basic)

5.18

PSA

120.22 Å²

Refractivity

137.15 m³·mol^-1

Polarizability

54.2 Å³

Rotatable Bond Count

H Bond Acceptor Count

H Bond Donor Count

Physiological Charge

-1

Number of Rings

Bioavailability

MDDR-Like Rule

true

Dược Lực Học : By inhibiting the angiotensin II receptor, this drug leades to a decrease in sodium reabsorption and a decrease in vasoconstriction. This has the combined effect of decreasing blood pressure.

Cơ Chế Tác Dụng : Saprisartan is an AT1 receptor antagonist. It is based on medications of losartan's prototypical chemical structure. The mode of (functional) AT1 receptor antagonism has been characterized as insurmountable/noncompetitive for saprisartan. It is very likely that slow dissociation kinetics from the AT1 receptor underlie insurmountable antagonism.(10579749) Saprisartan is a selective, potent, orally active and long-acting nonpeptide Angiotensin II type 1 (AT1) receptor antagonist. Saprisartan blocks the renin-angiotensin-aldosterone system (RAAS) at the level of the AT1 receptor that mediates most, if not all, of the important actions of Ang II. Saprisartan binds reversibly to the AT1 receptors in vascular smooth muscle and the adrenal gland. As angiotensin II is a vasoconstrictor, which also stimulates the synthesis and release of aldosterone, blockage of its effects results in decreases in systemic vascular resistance. AT1 receptor antagonists avoid the nonspecificity of the Ang I converting enzyme (ACE) inhibitors.

Chỉ Định : Saprisartan is used in the treatment of hypertension and heart failure.

Tương Tác Thuốc :

Amiloride Increased risk of hyperkalemia
Lithium The ARB increases serum levels of lithium
Potassium Increased risk of hyperkalemia
Triamterene Increased risk of hyperkalemia

Tài Liệu Tham Khảo Thêm

drugbank

http://www.drugbank.ca/drugs/DB01347

PubChem Compound

http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=60921

PubChem Substance

http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46508176

ChemSpider

http://www.chemspider.com/Chemical-Structure.54892.html

PharmGKB

http://www.pharmgkb.org/drug/PA164746338

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