Tìm theo
Ridogrel
Các tên gọi khác (3) :
  • R-68070
  • Ridogrel
  • Ridogrelum
platelet aggregation inhibitors, gastrointestinal agents, enzyme inhibitors, thrombolytic agents
Thuốc Gốc
Small Molecule
CAS: 110140-89-1
CTHH: C18H17F3N2O3
PTK: 366.3344
Ridogrel is a dual action drug useful for the prevention of systemic thrombo-embolism and as an adjunctive agent to thrombolytic therapy in acute myocardial infarction. However, there currently are no clinical indications for preferential use of ridogrel over aspirin.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C18H17F3N2O3
Phân tử khối
366.3344
Monoisotopic mass
366.119127035
InChI
InChI=1S/C18H17F3N2O3/c19-18(20,21)15-7-3-5-13(11-15)17(14-6-4-9-22-12-14)23-26-10-2-1-8-16(24)25/h3-7,9,11-12H,1-2,8,10H2,(H,24,25)/b23-17+
InChI Key
InChIKey=GLLPUTYLZIKEGF-HAVVHWLPSA-N
IUPAC Name
5-{[(E)-{pyridin-3-yl[3-(trifluoromethyl)phenyl]methylidene}amino]oxy}pentanoic acid
Traditional IUPAC Name
ridogrel
SMILES
OC(=O)CCCCO\N=C(\C1=CN=CC=C1)C1=CC(=CC=C1)C(F)(F)F
Độ hòa tan
8.39e-03 g/l
logP
4.3
logS
-4.6
pKa (strongest acidic)
3.5
pKa (Strongest Basic)
4.26
PSA
71.78 Å2
Refractivity
88.89 m3·mol-1
Polarizability
34.94 Å3
Rotatable Bond Count
9
H Bond Acceptor Count
5
H Bond Donor Count
1
Physiological Charge
-1
Number of Rings
2
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Ridogrel, a combined thromboxane synthase inhibitor and receptor antagonist, is used with streptokinase as an adjunctive therapy to reduce the formation and size of blood clots. Blood clots can cause ischemic cardiac events (heart attacks). Ridogrel has the dual property of inhibiting the synthesis of thromboxane and blocking the receptors of thromboxane/prostaglandin/endoperoxides. It has been shown to accelerate the speed of recanalization and to delay or prevent reocclusion during systemic thrombolysis with tissue plasminogen activator (streptokinase). Ridogrel is a more potent antiplatelet agent than aspirin and might offer an advantage over aspirin as an adjunct to thrombolysis in patients suffering from acute myocardial infarction. While aspirin inhibits cyclooxygenase, the enzyme responsible for producing thromboxane, ridogrel inhibits thromboxane synthesis directly. A recent comparison between aspirin and ridogrel in as adjunct to thrombolysis in patients with acute myocardial infarction demonstrated that ridogrel is not superior to aspirin in enhancing the fibrinolytic efficacy of streptokinase but might be more effective in preventing new ischemic events. Clinical experience with this drug is still relatively limited.
Cơ Chế Tác Dụng : Ridogrel is a dual action drug useful for the prevention of systemic thrombo-embolism and as an adjunctive agent to thrombolytic therapy in acute myocardial infarction. However, there currently are no clinical indications for preferential use of ridogrel over aspirin. Ridogrel inhibits thromboxane A2 synthase and also blocks the thromboxane A2/prostaglandin endoperoxide receptors. Thromboxane synthetase produces thromboxane in platelets. Thromboxane is a vasoconstrictor and facilitates the clumping of platelets. Therefore by inhibiting the production and promotion of thromboxane, thrombolysis is enhanced.
Dược Động Học :
▧ Absorption :
Rapidly absorbed after oral administration (30-60 min)
▧ Protein binding :
Approximately 60% bound to plasma proteins
Chỉ Định : Used as an adjunctive therapy to induce thrombolysis in patients suffering acute myocardial infarction.
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01207
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=5362391
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46506774
ChemSpider
http://www.chemspider.com/Chemical-Structure.4515025.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=50003795
PharmGKB
http://www.pharmgkb.org/drug/PA164746413
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