Details
Stereochemistry | ACHIRAL |
Molecular Formula | C14H15NO5S2 |
Molecular Weight | 341.403 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
OC(=O)COC1=CC=C(CCNS(=O)(=O)C2=CC=CC=C2)S1
InChI
InChIKey=ISSKMEQROMFEHL-UHFFFAOYSA-N
InChI=1S/C14H15NO5S2/c16-13(17)10-20-14-7-6-11(21-14)8-9-15-22(18,19)12-4-2-1-3-5-12/h1-7,15H,8-10H2,(H,16,17)
Linotroban is a potent and selective thromboxane (TXA2) receptor antagonist. It is known as a novel antithrombotic agent. Linotroban ingestion reduced significantly the thrombus volume. The coagulation, as measured by fibrin deposition and FPA plasma levels, was not significantly affected by Linotroban. It appears that the thromboxane A2 receptor antagonist linotroban reduces the thrombotic response by primarily impairing the platelet function at arterial blood flow conditions, and particularly at high wall shear rates. Linotroban had been in phase II clinical trial for the treatment of thrombosis. But this research was discontinued.
Originator
Approval Year
PubMed
Title | Date | PubMed |
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HN-11500--a novel thromboxane A2 receptor antagonist with antithrombotic activity in humans at arterial blood flow conditions. | 1994 Jan |
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Role of ADP and thromboxanes in human thrombus formation in ex vivo models. | 1997 |
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Thromboxane A2 does not mediate angiotensin II-dependent nonischemic peripheral vasoconstriction in healthy men: a pilot study. | 1997 Feb |
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Cisplatin-induced renal effects and thromboxane A2 receptor blockade. | 1997 Oct |
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Effects of the novel thromboxane (TXA2) receptor antagonist linotroban on inulin and para-aminohippuric acid clearances in the conscious male and female rat. | 1997 Sep |
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Determination of efficacy of linotroban by inducing a reduction of renal inulin/para-aminohippuric acid clearances with the thromboxane A2 mimetic U-46619 in the conscious female rat. | 2000 Sep |
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[Design, synthesis of novel N, N'-bis-(halogenophenyl)-4- methoxybenzene-1, 3-disulfonamides and evaluation of their anti-platelet aggregation activity]. | 2015 Feb |
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NCI_THESAURUS |
C29750
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100000082318
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C086833
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C66016
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ACTIVE MOIETY