Tìm theo
Tasosartan
Các tên gọi khác (3) :
  • ANA-756
  • Tasosartan
  • WAY-ana-756
Thuốc Gốc
Small Molecule
CAS: 145733-36-4
ATC: C09CA05
CTHH: C23H21N7O
PTK: 411.4591
Tasosartan is a long-acting angiotensin II (AngII) receptor blocker. Its long duration of action has been attributed to its active metabolite enoltasosartan. It is used to treat patients with essential hypertension
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C23H21N7O
Phân tử khối
411.4591
Monoisotopic mass
411.180758329
InChI
InChI=1S/C23H21N7O/c1-14-18-11-12-21(31)30(23(18)25-15(2)24-14)13-16-7-9-17(10-8-16)19-5-3-4-6-20(19)22-26-28-29-27-22/h3-10H,11-13H2,1-2H3,(H,26,27,28,29)
InChI Key
InChIKey=ADXGNEYLLLSOAR-UHFFFAOYSA-N
IUPAC Name
2,4-dimethyl-8-({4-[2-(2H-1,2,3,4-tetrazol-5-yl)phenyl]phenyl}methyl)-5H,6H,7H,8H-pyrido[2,3-d]pyrimidin-7-one
Traditional IUPAC Name
tasosartan
SMILES
CC1=NC(C)=C2CCC(=O)N(CC3=CC=C(C=C3)C3=CC=CC=C3C3=NNN=N3)C2=N1
Độ hòa tan
3.25e-02 g/l
logP
4.18
logS
-4.1
pKa (strongest acidic)
7.4
pKa (Strongest Basic)
2.79
PSA
100.55 Å2
Refractivity
130.61 m3·mol-1
Polarizability
44.34 Å3
Rotatable Bond Count
4
H Bond Acceptor Count
6
H Bond Donor Count
1
Physiological Charge
0
Number of Rings
5
Bioavailability
1
Rule of Five
true
Dược Lực Học : By blocking the angiotensin II (AT1) receptor, the drug ultimately causes vasodilation, reduced secretion of vasopressin (ADH), reduced production and secretion of aldosterone, amongst other actions leading to the combined effect of a reduction of blood pressure.
Cơ Chế Tác Dụng : Tasosartan is a long-acting angiotensin II (AngII) receptor blocker. Its long duration of action has been attributed to its active metabolite enoltasosartan. It is used to treat patients with essential hypertension Tasosartan is a selective, potent, orally active and long-acting nonpeptide Angiotensin II type 1 (AT1) receptor antagonist. Tasosartan 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. Tasosartan 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 : Tasosartan is infrequently in the treatment of hypertension and heart failure.
Tương Tác Thuốc :
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01349
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=60919
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46504809
ChemSpider
http://www.chemspider.com/Chemical-Structure.54890.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=50040439
PharmGKB
http://www.pharmgkb.org/drug/PA164769057
Wikipedia
http://en.wikipedia.org/wiki/Tasosartan
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