[The effect of trapidil and the trapidil derivative AR 12463 on blood pressure and thromboxane formation in spontaneously hypertensive rats].
The trapidil derivative AR 12463 has a much more stronger inhibiting effect than trapidil on different atherosclerotic parameters of the cell cultures obtained from normal intima and fatty streaks of human aorta, on thromboxane (TX) formation and on the aggregation of human platelets in vitro, and on the activity of phosphodiesterase. In addition to these present results, AR 12463 reduced significantly the mean arterial blood pressure of spontaneously hypertensive rats (at a dosage of 20 mg/kg/d administered orally for 2 weeks) in contrast to the same dosage of trapidil. Simultaneously, TX formation is significantly reduced in serum by 48% in aorta thoracica by 29%, and in aorta abdominalis by 19%. Due to these properties, AR 12463 seems to be suitable for a therapeutic and prophylactic strategy in chronic ischemic diseases.
Taube
C
C
Institut für Pharmakologie und Toxikologie, Bereichs Medizin, Martin-Luther-Universität Halle-Wittenberg.
Steinborn
C
C
Mest
H J
HJ
D015121:6-Ketoprostaglandin F1 alpha / Q000097:blood; D000818:Animals; D001794:Blood Pressure / Q000187:drug effects*; D006339:Heart Rate / Q000187:drug effects; D008297:Male; D011743:Pyrimidines / Q000494:pharmacology*; D051381:Rats; D011918:Rats, Inbred SHR; D013929:Thromboxane B2 / Q000096:biosynthesis*; D014192:Trapidil / Q000031:analogs & derivatives / Q000494:pharmacology*
D011743:Pyrimidines; D013929:Thromboxane B2; D015121:6-Ketoprostaglandin F1 alpha; D014192:Trapidil; C053729:AR 12463
Zur Wirkung von Trapidil und Trapidilderivat AR 12463 auf Blutdruck und Thromboxanbildung spontanhypertoner Ratten.