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Effects of terbogrel on platelet function and prostaglandin endoperoxide transfer
The present study describes the platelet-inhibitory effects of terbogrel (5-hexenoic acid, 6-[3-[[(cyanoamino)[(1,1-dimethylethyl)amino]methylene]amino]phenyl]-6-(3-pyridinyl)-, ( ϵ)-), a novel combined thromboxane A 2 synthase inhibitor and thromboxane A 2 receptor antagonist. Terbogrel concentrati...
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Published in: | European journal of pharmacology 1998-02, Vol.344 (1), p.45-48 |
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Main Authors: | , , |
Format: | Article |
Language: | English |
Subjects: | |
Citations: | Items that this one cites Items that cite this one |
Online Access: | Get full text |
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Summary: | The present study describes the platelet-inhibitory effects of terbogrel (5-hexenoic acid, 6-[3-[[(cyanoamino)[(1,1-dimethylethyl)amino]methylene]amino]phenyl]-6-(3-pyridinyl)-, (
ϵ)-), a novel combined thromboxane A
2 synthase inhibitor and thromboxane A
2 receptor antagonist. Terbogrel concentration-dependently inhibited collagen (0.6
μg/ml)- and U46619 (11
α,9
α-epoxymethano-15(
S)-hydroxy-prosta-5
Z,13
E-dienoic acid) (1
μM)-induced aggregation and thromboxane synthesis of washed human platelets. In this system, terbogrel exhibited an equipotent (IC
50 of about 10 nM) activity as thromboxane A
2 synthase inhibitor and thromboxane A
2 receptor antagonist. In addition, the compound favoured prostacyclin synthesis in cultured vascular smooth muscle cells by increasing the transfer of platelet-derived prostaglandin endoperoxides. Terbogrel appears to be a compound with an equipotent molar potency as thromboxane A
2 synthase inhibitor and receptor antagonist. |
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ISSN: | 0014-2999 1879-0712 |
DOI: | 10.1016/S0014-2999(97)01612-9 |