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 |
|
| [(1H-imidazol-1-yl)methyl]- and [(3-pyridinyl)methyl]pyrroles as thromboxane synthetase inhibitors. | 1989 Apr |
|
| Effects of the selective inhibition of platelet thromboxane synthesis on the platelet-subendothelium interaction. | 2002 Dec |
|
| Cyclooxygenase contracting factors and altered pulmonary vascular responses in chronically hypoxic newborn pigs. | 2002 Jan |
|
| Role of contaminating platelets in thromboxane synthesis in primary cultures of human umbilical vein endothelial cells. | 2002 Sep |
|
| Effects of camonagrel, a selective inhibitor of platelet thromboxane synthase, on the platelet-subendothelium interaction. | 2003 Sep |
|
| Chronic AT(1) receptor blockade alters mechanisms mediating responses to hypoxia in rat skeletal muscle resistance arteries. | 2004 Aug |
|
| Role of platelet microparticles in the production of thromboxane by rabbit pulmonary artery. | 2004 Feb |
|
| Attenuation of lipopolysaccharide-induced hyperreactivity of human internal mammary arteries by melatonin. | 2004 Sep |
|
| In SHR aorta, calcium ionophore A-23187 releases prostacyclin and thromboxane A2 as endothelium-derived contracting factors. | 2006 Nov |
|
| Mechanisms underlying ATP-induced endothelium-dependent contractions in the SHR aorta. | 2007 Feb 5 |
|
| The calcium ionophore A23187 induces endothelium-dependent contractions in femoral arteries from rats with streptozotocin-induced diabetes. | 2007 Mar |
|
| Effect of inhibitors of arachidonic acid conversion in platelets on thrombin-fibrinogen interaction and thrombin tolerance. | 2007 Oct |
|
| Oral vasodilators for primary Raynaud's phenomenon. | 2008 Apr 16 |
|
| Roles of IL-6-gp130 Signaling in Vascular Inflammation. | 2008 Aug |
|
| 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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