Inhibition of thromboxane A2 production by trapidil and trapidil derivatives in the arachidonic acid-injected rat.
Trapidil and four selected 5,7-disubstituted s-triazolo (1,5-a)pyrimidine derivatives (AR 12456, AR 12463, AR 12464, AR 12465) which have already been shown to possess inhibitory effects on arachidonic acid(AA)-induced aggregation and thromboxane A2(TXA2) formation in human and rabbit platelets in vitro diminished the AA-stimulated TXA2 production in murine blood in vivo. The inhibitory effects of the derivatives were generally stronger than those of trapidil. The strongest inhibitor of TXA2 formation was the derivative AR 12456. These in vivo results correspond well with our previous in vitro findings.
Heinroth-Hoffmann
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I
Department of Pharmacology and Toxicology, Martin Luther University, Halle, GDR.
Hauser
A
A
Mest
H J
HJ
D015105:3',5'-Cyclic-AMP Phosphodiesterases / Q000037:antagonists & inhibitors*; D000818:Animals; D016718:Arachidonic Acid; D001095:Arachidonic Acids / Q000494:pharmacology*; D008297:Male; D010975:Platelet Aggregation Inhibitors / Q000494:pharmacology; D011743:Pyrimidines / Q000494:pharmacology*; D051381:Rats; D011919:Rats, Inbred Strains; D013928:Thromboxane A2 / Q000096:biosynthesis*; D014192:Trapidil / Q000031:analogs & derivatives / Q000494:pharmacology*
D001095:Arachidonic Acids; D010975:Platelet Aggregation Inhibitors; D011743:Pyrimidines; C046930:AR 12456; D016718:Arachidonic Acid; D013928:Thromboxane A2; D015105:3',5'-Cyclic-AMP Phosphodiesterases; D014192:Trapidil