Loading…

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...

Full description

Saved in:
Bibliographic Details
Published in:European journal of pharmacology 1998-02, Vol.344 (1), p.45-48
Main Authors: Muck, Stephanie, Weber, Artur-Aron, Schrör, Karsten
Format: Article
Language:English
Subjects:
Citations: Items that this one cites
Items that cite this one
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
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.
ISSN:0014-2999
1879-0712
DOI:10.1016/S0014-2999(97)01612-9