Details
Stereochemistry | ACHIRAL |
Molecular Formula | C12H12N2O3.ClH |
Molecular Weight | 268.696 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
Cl.OC(=O)C1=CC=C(OCCN2C=CN=C2)C=C1
InChI
InChIKey=PVKDFUXBDJPRGU-UHFFFAOYSA-N
InChI=1S/C12H12N2O3.ClH/c15-12(16)10-1-3-11(4-2-10)17-8-7-14-6-5-13-9-14;/h1-6,9H,7-8H2,(H,15,16);1H
Molecular Formula | ClH |
Molecular Weight | 36.461 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
Molecular Formula | C12H12N2O3 |
Molecular Weight | 232.2353 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
Dazoxiben is a selective inhibitor of thromboxane synthetase (IC50 3 nM), an enzyme that converts the endo-peroxide PGH2 into thromboxane A2, which is a potent vasoconstrictor and platelet aggregating agent. Dazoxiben has demonstrated efficacy in some clinical trial for the treatment of Raynaud's syndrome, an ischaemic condition manifested by the pallor of affected digits. In subsequent studies, however, no significant effect of dazoxiben was found. Dazoxiben was also evaluated in patients with sepsis, adult respiratory distress syndrome, stable angina, and other conditions.
Approval Year
PubMed
Title | Date | PubMed |
---|---|---|
UK-37, 248, a novel, selective thromboxane synthetase inhibitor with platelet anti-aggregatory and anti-thrombotic activity. | 1981 Jul 1-15 |
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[(1H-imidazol-1-yl)methyl]- and [(3-pyridinyl)methyl]pyrroles as thromboxane synthetase inhibitors. | 1989 Apr |
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The mechanism of anti-thrombotic, thrombolytic and fibrinolytic actions of camonagrel--a new thromboxane synthase inhibitor. | 1995 |
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Effects of the selective inhibition of platelet thromboxane synthesis on the platelet-subendothelium interaction. | 2002 Dec |
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Prostaglandin endoperoxides and thromboxane A2 activate the same receptor isoforms in human platelets. | 2002 Jan |
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Sexual dimorphism in prostanoid-potentiated vascular contraction: roles of endothelium and ovarian steroids. | 2002 Nov |
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Role of contaminating platelets in thromboxane synthesis in primary cultures of human umbilical vein endothelial cells. | 2002 Sep |
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Study of the mechanisms involved in the bradykinin-induced contraction of the pig iris sphincter muscle in vitro. | 2003 Jan 1 |
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Effects of camonagrel, a selective inhibitor of platelet thromboxane synthase, on the platelet-subendothelium interaction. | 2003 Sep |
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Role of platelet microparticles in the production of thromboxane by rabbit pulmonary artery. | 2004 Feb |
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Role of endothelin-1 and thromboxane A2 in the pulmonary hypertension induced by heparin-protamine interaction in anesthetized dogs. | 2004 Jan |
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BK2 but not BK1 receptors mediating contractile response in human umbilical arteries: role of thromboxane A2. | 2004 May |
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Mechanisms underlying ATP-induced endothelium-dependent contractions in the SHR aorta. | 2007 Feb 5 |
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The calcium ionophore A23187 induces endothelium-dependent contractions in femoral arteries from rats with streptozotocin-induced diabetes. | 2007 Mar |
|
Estrogen potentiates constrictor prostanoid function in female rat aorta by upregulation of cyclooxygenase-2 and thromboxane pathway expression. | 2008 Jun |
Substance Class |
Chemical
Created
by
admin
on
Edited
Fri Dec 15 14:59:06 GMT 2023
by
admin
on
Fri Dec 15 14:59:06 GMT 2023
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Record UNII |
G5AI939LWF
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Record Status |
Validated (UNII)
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Record Version |
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74226-22-5
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DTXSID40225215
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53000
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C169879
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CHEMBL267473
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G5AI939LWF
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DBSALT002937
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ACTIVE MOIETY |