Influence of the antianginal drug trapidil and its derivative AR 12463 on arachidonic acid liberation and thromboxane formation in thrombin-stimulated platelets.
The 5,7-disubstituted s-triazolo(1,5-a)pyrimidines (TPs) trapidil and AR 12463 inhibited the thrombin-induced Thromboxane (TX) formation in washed human platelets in a concentration-dependent manner (Ic50:trapidil 410 mumol/l and AR 12463 9 mumol/l). The arachidonic acid (AA) liberation measured in parallel was unchanged or only reduced to a small extent. The present study shows that the inhibition of TX formation by trapidil and AR 12463 is independent of AA liberation of platelets.
Block
H U
HU
Department of Pharmacology and Toxicology, Martin Luther University Halle-Wittenberg, GDR.
Dunemann
A
A
Niebisch
M
M
Mest
H J
HJ
D000959:Antihypertensive Agents / Q000494:pharmacology*; D001095:Arachidonic Acids / Q000097:blood*; D001792:Blood Platelets / Q000187:drug effects / Q000502:physiology*; D006801:Humans; D066298:In Vitro Techniques; D007700:Kinetics; D011743:Pyrimidines / Q000494:pharmacology*; D013917:Thrombin / Q000502:physiology*; D013931:Thromboxanes / Q000096:biosynthesis / Q000097:blood*; D014192:Trapidil / Q000031:analogs & derivatives / Q000494:pharmacology*
D000959:Antihypertensive Agents; D001095:Arachidonic Acids; D011743:Pyrimidines; D013931:Thromboxanes; D013917:Thrombin; D014192:Trapidil; C053729:AR 12463