Tìm theo
Phenindione
Các tên gọi khác (9 ) :
  • 2-Phenyl-1,3-diketohydrindene
  • 2-Phenyl-1,3-indandione
  • 2-Phenyl-1,3(2H)-indenedione
  • Fenindiona
  • Fenindione
  • Phenindion
  • Phénindione
  • Phenindionum
  • PID
Thuốc tác dụng lên quá trình đông máu
Thuốc Gốc
Small Molecule
CAS: 83-12-5
ATC: B01AA02
CTHH: C15H10O2
PTK: 222.2387
An indandione that has been used as an anticoagulant. Phenindione has actions similar to warfarin, but it is now rarely employed because of its higher incidence of severe adverse effects. (From Martindale, The Extra Pharmacopoeia, 30th ed, p234)
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C15H10O2
Phân tử khối
222.2387
Monoisotopic mass
222.068079564
InChI
InChI=1S/C15H10O2/c16-14-11-8-4-5-9-12(11)15(17)13(14)10-6-2-1-3-7-10/h1-9,13H
InChI Key
InChIKey=NFBAXHOPROOJAW-UHFFFAOYSA-N
IUPAC Name
2-phenyl-2,3-dihydro-1H-indene-1,3-dione
Traditional IUPAC Name
phenindione
SMILES
O=C1C(C(=O)C2=CC=CC=C12)C1=CC=CC=C1
Độ tan chảy
150 °C
Độ hòa tan
27 mg/L (at 20 °C)
logP
2.90
logS
-4
pKa (strongest acidic)
4.88
pKa (Strongest Basic)
-7.5
PSA
34.14 Å2
Refractivity
65.23 m3·mol-1
Polarizability
23.24 Å3
Rotatable Bond Count
1
H Bond Acceptor Count
2
H Bond Donor Count
0
Physiological Charge
-1
Number of Rings
3
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Phenindione thins the blood by antagonizing vitamin K which is required for the production of clotting factors in the liver. Anticoagulants such as Phenindione have no direct effect on an established thrombus, nor do they reverse ischemic tissue damage (damage caused by an inadequate blood supply to an organ or part of the body). However, once a thrombus has occurred, the goal of anticoagulant treatment is to prevent further extension of the formed clot and prevent secondary thromboembolic complications which may result in serious and possibly fatal sequelae. Phenindione has actions similar to warfarin, but it is now rarely employed because of its higer incidence of severe adverse effects.
Cơ Chế Tác Dụng : An indandione that has been used as an anticoagulant. Phenindione has actions similar to warfarin, but it is now rarely employed because of its higher incidence of severe adverse effects. (From Martindale, The Extra Pharmacopoeia, 30th ed, p234) Phenindione inhibits vitamin K reductase, resulting in depletion of the reduced form of vitamin K (vitamin KH2). As vitamin K is a cofactor for the carboxylation of glutamate residues on the N-terminal regions of vitamin K-dependent proteins, this limits the gamma-carboxylation and subsequent activation of the vitamin K-dependent coagulant proteins. The synthesis of vitamin K-dependent coagulation factors II, VII, IX, and X and anticoagulant proteins C and S is inhibited. Depression of three of the four vitamin K-dependent coagulation factors (factors II, VII, and X) results in decreased prothrombin levels and a decrease in the amount of thrombin generated and bound to fibrin. This reduces the thrombogenicity of clots.
Dược Động Học :
▧ Absorption :
Absorbed slowly from the gastrointestinal tract.
▧ Protein binding :
88%
▧ Metabolism :
Hepatic.
▧ Half Life :
5-10 hours
Độc Tính : Oral, mouse: LD50 = 175 mg/kg; Oral, rat: LD50 = 163 mg/kg.
Chỉ Định : For the treatment of pulmonary embolism, cardiomyopathy, atrial fibrillation and flutter, cerebral embolism, mural thrombosis, and thrombophili. Also used for anticoagulant prophylaxis.
Dữ Kiện Thương Mại
Nhà Sản Xuất
  • Công ty : Sigma
    Sản phẩm biệt dược : Dindevan
  • Công ty : Souriree
    Sản phẩm biệt dược : Fenindion
  • Công ty : Goldshield
    Sản phẩm biệt dược : Phenindione
  • Công ty : Cooper
    Sản phẩm biệt dược : Soluthrombine
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00498
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=4760
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46505018
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07584
ChemSpider
http://www.chemspider.com/Chemical-Structure.4596.html
PharmGKB
http://www.pharmgkb.org/drug/PA164784031
Wikipedia
http://en.wikipedia.org/wiki/Phenindione
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