Papamuri

Rivaroxaban, 5-chloro-N-[[(5S)-2-oxo-3-[4-(3-oxomorpholin-4-yl)phenyl]-1,3-oxazolidin-5-yl]methyl]thiophene-2 -carboxamide, he aukati ngota iti-iti o te tauwehe Xa he mea whakakoi i tetahi waahi nui i roto i te ara whakakoi toto ka puta mai te whakatipuranga te thrombin me te hanganga o te toka. Ka herea e Rivaroxaban ki te Tyr288 i roto i te pute S1 o te tauwehe Xa na roto i te taunekeneke a Tyr288 me te whakakapi maota o te wahanga chlorothiophene. Ka taea te whakakore i te aukati (koff = 5x10-3s-1), tere (kon = 1.7x107 mol/L-1 s-1), me te ahua o te kukū (Ki = 0.4 nmol/L). I tenei wa kei te akohia a Rivaroxaban mo te maimoatanga o te VTE, te aukati i nga kaupapa cardiovascular i roto i nga turoro me te mate pukupuku o te mate, te aukati i te whiu i roto i nga turoro me te fibrillation atrial.

Tohutoro

Ko Elisabeth Perzborn, Susanne Roehrig, Alexander Straub, Dagmar Kubitza, Wolfgang Mueck, me Volker Laux. Rivaroxaban: he aukati hou a-waha Xa. Arterioscler Thromb Vasc Biol 2010; 30(3): 376-381

Whakaahuatanga

Rivaroxaban (BAY 59-7939) he tino kaha，whiriwhiri me te tika Factor Xa (FXa) inhibitor, te whakatutuki i te painga kaha i roto i te kaha anti-FXa (IC50 0.7 nM; Ki 0.4 nM).

In Vitro

Ko te Rivaroxaban (BAY 59-7939) he aukati-waha, he tika tonu te Factor Xa (FXa) i roto i te whakawhanaketanga mo te aukati me te maimoatanga o te thrombosis arterial me te venous. Ko Rivaroxaban te whakataetae i te FXa tangata (Ki 0.4 nM) me te> 10 000-fold nui ake te whiriwhiringa atu mo etahi atu porotease serine; ka aukati hoki i te mahi prothrombinase (IC50 2.1 nM). Rivaroxaban inhibits endogenous FXa more potently in human and rabbit plasma (IC50 21 nM) than rat plasma (IC50 290 nM). E whakaatu ana i nga paanga anticoagulant i roto i te plasma tangata, te ruarua o te wa prothrombin (PT) me te whakahohe i te wa thromboplastin wahanga i te 0.23 me te 0.69μM, ia.

Ko te Rivaroxaban (BAY 59-7939) he kaha me te whiriwhiri, te aukati FXa tika me te pai o te mahi vivo me te pai o te koiora o te waha. Rivaroxaban (BAY 59-7939), e whakahaeretia ana e te iv bolus i mua i te whakauru o te thrombus, ka whakaiti i te hanganga o te thrombus (ED50 0.1 mg / kg), te whakakore i te FXa, me te whakaroa i te horopeta PT i runga i te whakawhirinaki. Ko te PT me te FXa e pa ana ki te ED50 (te pikinga 1.8 me te 32% te aukati, ia). I te 0.3 mg/kg (te horopeta e tata ana ki te aukati i te hanganga o te thrombus), ka whakaroahia e Rivaroxaban te PT (3.2).±0.5-fold) me te aukati i te mahi FXa (65±3%).

Rokiroki

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