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Biochemical and pharmacological characterization of YM-60828, a newly synthesized and orally active inhibitor of human factor Xa.
TLDR
Results strongly suggest that YM-60828 will be a valuable orally active and potent anticoagulant agent showing potential antithrombotic activity.
Inhibition by aurintricarboxylic acid of von Willebrand factor binding to platelet GPIb, platelet retention, and thrombus formation in vivo
TLDR
Commercial aurintricarboxylic acid exhibited antithrombotic activity and caused a marked improvement in patency status following successful thrombolysis by t‐PA in electrically and copper coil‐induced thrombosis models, suggesting that specific inhibitors of the vWF‐GPIb interaction such as ATA may prove useful as antithromabotic agents.
Comparison of the anticoagulant and antithrombotic effects of YM-75466, a novel orally-active factor Xa inhibitor, and warfarin in mice.
TLDR
It is shown that YM-75466 has advantages over warfarin: i) rapid onset of anticoagulant activity, ii) wide therapeutic range, iii) little effect on bleeding and iv) lack of drug interaction with agents that interfere withwarfarin.
Clinical Pharmacokinetics and Pharmacodynamics of the Novel SGLT2 Inhibitor Ipragliflozin
TLDR
In single- and multiple-dose studies, the maximum plasma concentration and area under the plasma concentration-time curve (AUC) for ipragliflozin increased in a dose-dependent manner, and tubular concentration of free iprag liflozin is adequate to provide pharmacological activities.
Isolation and characterization of jararaca GPIb-BP, a snake venom antagonist specific to platelet glycoprotein Ib.
TLDR
The NH2-terminal amino acid sequences of the subunits revealed a high degree of homology with those of several Ca(2+)-dependent lectins, especially to those of two functionally opposite venom proteins, botrocetin (a vWF-modulator) and alboaggregin-B (a GPIb- modulator).
Complete Amino Acid Sequence and Identification of the Platelet Glycoprotein Ib-binding Site of Jararaca GPIb-BP, a Snake Venom Protein Isolated from Bothrops jararaca(*)
TLDR
The entire 142- and 123-residue amino acid sequences of the respective α and β subunits are presented and it is demonstrated that the platelet GPIb-binding site resides on the β and not on the α subunit based on an enzyme-linked immunosorbent assay using biotin-labeled jararaca GPIB-BP and competing ligands.
Comparative studies of an orally-active factor Xa inhibitor, YM-60828, with other antithrombotic agents in a rat model of arterial thrombosis.
TLDR
It is suggested that YM-60828 may be a promising antithrombotic agent for the treatment and prevention of arterial thrombosis which can be given by oral as well as intravenous administration.
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