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Antistasin, the first discovered naturally occurring direct Xa inhibitor Rivaroxaban, the first synthetic direct Xa inhibitor marketed as a drug Prior to the introduction of direct factor Xa inhibitors, vitamin K antagonists such as warfarin were the only oral anticoagulants for over 60 years, and together with heparin have been the main blood ...
Thrombin demonstrates a high level of allosteric regulation. [2] Allosterism in thrombin is regulated by the exosites 1 and 2 and the sodium binding site. A recent patent review has shown that the general consensus among researchers is that allosteric inhibitors may provide a more regulatable anticoagulant. [3]
Rivaroxaban. During the SAR development of rivaroxaban, researchers realized that adding a 5-chlorothiophene-2-carboxamide group to the oxazolidonine core could increase the potency by 200 fold, which had previously been too weak for medical use. In addition to this discovery, a clear preference for the (S)-configuration was confirmed.
Rivaroxaban bears a striking structural similarity to the antibiotic linezolid: both drugs share the same oxazolidinone-derived core structure. [39] Accordingly, rivaroxaban was studied for any possible antimicrobial effects and for the possibility of mitochondrial toxicity, which is a known complication of long-term linezolid use. [40]
Mechanism of class-switch recombination that allows isotype switching in activated B cells. Immunoglobulin class switching, also known as isotype switching, isotypic commutation or class-switch recombination (CSR), is a biological mechanism that changes a B cell's production of immunoglobulin from one type to another, such as from the isotype IgM to the isotype IgG. [1]
Acute use (1–3 days) yields a potency about 1.5× stronger than that of morphine and chronic use (7 days+) yields a potency about 2.5 to 5× that of morphine. Similarly, the effect of tramadol increases after consecutive dosing due to the accumulation of its active metabolite and an increase of the oral bioavailability in chronic use.
4-6 kDa Low-molecular-weight heparin ( LMWH ) is a class of anticoagulant medications . [ 1 ] They are used in the prevention of blood clots and, in the treatment of venous thromboembolism ( deep vein thrombosis and pulmonary embolism ), and the treatment of myocardial infarction .
[3] [4] Heparin is a blood anticoagulant that increases the activity of antithrombin. [5] It is used in the treatment of heart attacks and unstable angina. [3] It can be given intravenously or by injection under the skin. [3] Its anticoagulant properties make it useful to prevent blood clotting in blood specimen test tubes and kidney dialysis ...