In vitro antiplatelet activity of the carbinol analogue of ketoprofen, 3-(1-methyl-2-hydroxyethyl)-benzophenone.
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.
Oshima
K
K
Research Institute, Fuji Chemical Industries Co., Ltd., Toyama, Japan.
Hashizume
H
H
Miyamae
T
T
Morikawa
T
T
Hagiwara
M
M
D000818:Animals; D001792:Blood Platelets / Q000187:drug effects / Q000201:enzymology; D016861:Cyclooxygenase Inhibitors / Q000494:pharmacology*; D006168:Guinea Pigs; D006461:Hemolysis / Q000187:drug effects; D006801:Humans; D007038:Hypotonic Solutions; D066298:In Vitro Techniques; D008297:Male; D010974:Platelet Aggregation / Q000187:drug effects; D010975:Platelet Aggregation Inhibitors / Q000494:pharmacology*; D011817:Rabbits; D051381:Rats; D017208:Rats, Wistar; D012756:Sheep; D013045:Species Specificity
D016861:Cyclooxygenase Inhibitors; D007038:Hypotonic Solutions; D010975:Platelet Aggregation Inhibitors