scholarly journals Identification of the hypertension drug niflumic acid as a glycine receptor inhibitor

2020 ◽  
Vol 10 (1) ◽  
Author(s):  
Daishi Ito ◽  
Yoshinori Kawazoe ◽  
Ayato Sato ◽  
Motonari Uesugi ◽  
Hiromi Hirata
Keyword(s):  
Glycine Receptor ◽  
Niflumic Acid ◽  
Receptor Inhibitor

scholarly journals Voltage-Dependent Inhibition of Glycine Receptor Channels by Niflumic Acid

2017 ◽  
Vol 10 ◽  
Author(s):  
Galyna Maleeva ◽  
Franck Peiretti ◽  
Boris S. Zhorov ◽  
Piotr Bregestovski
Keyword(s):  
Glycine Receptor ◽  
Niflumic Acid ◽  
Voltage Dependent ◽  
Dependent Inhibition

A Simple and Rapid Method to Determine GPIIb/IIIa-Receptor Inhibitor Activity in Whole Blood

1999 ◽  
Vol 19 (03) ◽  
pp. 134-138
Author(s):  
Gitta Kühnel ◽  
A. C. Matzdorff
Keyword(s):  
Flow Cytometry ◽  
Platelet Count ◽  
Blood Sample ◽  
Platelet Activation ◽  
Whole Blood ◽  
Receptor Occupancy ◽  
Aggregate Formation ◽  
Inhibitor Activity ◽  
Receptor Inhibitor

SummaryWe studied the effect of GPIIb/IIIa-inhibitors on platelet activation with flow cytometry in vitro. Citrated whole blood was incubated with increasing concentrations of three different GPIIb/IIIa-inhibitors (c7E3, DMP728, XJ757), then thrombin or ADP were added and after 1 min the sample was fixed. Samples without c7E3 but with 0.1 U/ml thrombin had a decrease in platelet count. Samples with increasing concentrations of c7E3 had a lesser or no decrease in platelet count. The two other inhibitors (DMP 725, XJ757) gave similar results. GPIIb/IIIa-inhibitors prevent aggregate formation and more single platelets remain in the blood sample. The agonist-induced decrease in platelet count correlates closely with the concentration of the GPIIb/IIIa inhibitor and receptor occupancy. This correlation may be used as a simple measure for inhibitor activity in whole blood.

Combined Thrombin and Platelet Inhibition Treatment for HIT Patients

1999 ◽  
Vol 19 (03) ◽  
pp. 128-133 ◽  
Author(s):  
B.E. Lewis ◽  
W. P. Jeske ◽  
F. Leya ◽  
Diane Wallis ◽  
M. Bakhos ◽  
...  
Keyword(s):  
Standard Dose ◽  
Combined Therapy ◽  
Platelet Inhibition ◽  
Thrombin Inhibitors ◽  
Thrombin Inhibitor ◽  
Heparin Induced Thrombocytopenia ◽  
Acute Thrombosis ◽  
Anti Platelet Drug ◽  
Receptor Inhibitor

SummaryDespite the use of potent anticoagulants such as r-hirudin and argatroban, the morbidity and mortality in heparin-induced thrombocytopenia (HIT) patients remains unacceptable. Data from our in vitro investigations show that thrombin inhibitors do not block platelet activation induced by heparin antibodies and heparin but that GPIIb/IIIa receptor inhibitors do block this process. We have treated four HIT positive patients with a combined therapy of thrombin inhibitor and GPIIb/IIIa receptor inhibitor when treatment with thrombin inhibitor alone failed to alleviate acute thrombosis. Combination therapies included r-hirudin (Refludan®) with tirofiban (Aggrastat®) and argatroban (Novastan®) with abciximab (ReoPro®). A reduced dose of the thrombin inhibitor was used with the standard dose of the anti-platelet drug. In all cases, there was no overt bleeding which required intervention, and all patients exhibited clinical improvement or full recovery. These case studies suggest that treatment of active thrombosis in HIT patients with adjunct GPIIb/IIIa receptor inhibitor therapy may be more effective than thrombin inhibitor treatment alone.

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