In vitro antiplatelet activity of the carbinol analogue of ketoprofen, 3-(1-methyl-2-hydroxyethyl)-benzophenone

Arzneimittelforschung. 1996 Jul;46(7):691-3.

Abstract

3-(1-Methyl-2-hydroxyethyl)-benzophenone (F025) is a close structural analogue of ketoprofen, in which the carboxylic acid of ketoprofen is reduced to a carbinol moiety. The in vitro effects of F025 on platelet aggregation, cyclooxygenase and hypotonic NaCl-induced erythrocyte hemolysis were examined in comparison with those of ketoprofen. Although the inhibitory activity of F025 on collagen, arachidonic acid and ADP-induced platelet aggregation was between 2 and 20 times that of ketoprofen in healthy volunteers, guinea pigs, rabbits and rats, F025 had only one-tenth of the inhibitory action of ketoprofen on sheep seminal vesicle cyclooxygenase F025, but not ketoprofen, inhibited hypotonic NaCl-induced erythrocyte hemolysis in guinea pigs. The substantial antiplatelet activity of F025 may be due to membrane stabilization as well as to cyclooxygenase inhibition.

Publication types

  • Comparative Study

MeSH terms

  • Animals
  • Blood Platelets / drug effects
  • Blood Platelets / enzymology
  • Cyclooxygenase Inhibitors / pharmacology*
  • Guinea Pigs
  • Hemolysis / drug effects
  • Humans
  • Hypotonic Solutions
  • In Vitro Techniques
  • Male
  • Platelet Aggregation / drug effects
  • Platelet Aggregation Inhibitors / pharmacology*
  • Rabbits
  • Rats
  • Rats, Wistar
  • Sheep
  • Species Specificity

Substances

  • Cyclooxygenase Inhibitors
  • Hypotonic Solutions
  • Platelet Aggregation Inhibitors