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Updated: Feb 15, 2026

Turbidimetry on Human Washed Platelets: The Effect of the Pannexin1-inhibitor Brilliant Blue FCF on Collagen-induced Aggregation
Published on: April 6, 2017
Design, synthesis and evaluation of 1,4-benzodioxine derivatives as novel platelet aggregation inhibitors
Zhouling Xie1, Lulu Zhao2, Xue Ding3
1School of Biological & Medical Engineering, Hefei University of Technology, Hefei, Anhui 230009, PR China.
Aim:
To find novel platelet aggregation inhibitors, two new series of 1,4-benzodioxine derivatives were synthesized and screened for the ability to inhibit platelet aggregation.
Materials & Methods:
The synthesized compounds were evaluated for antiplatelet aggregation activity using human blood platelet and GPIIb/IIIa antagonistic activity.
Results:
Compound 9-2p showed significant antiplatelet activity with the IC50 values of 41.7 and 22.2 μM induced by ADP and thrombin, respectively, more potent than that of LX2421. Compound 9-2p exhibited GPIIb/IIIa antagonistic activity with the IC50 value of 2.3 μM, as potent as RGDs. In vivo study showed that 9-2p displayed remarkable antithrombotic activity, more effective than LX2421, but less effective than tirofiban.
Conclusion:
Compound 9-2p showed moderate antiplatelet activity and antithrombotic activity, which could be further optimized based on the target of GPIIb/IIIa.
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