Folia Pharmacologica Japonica
Online ISSN : 1347-8397
Print ISSN : 0015-5691
ISSN-L : 0015-5691
Anti-platelet actions of salicylates: In vivo, ex vivo and in vitro effects of choline salicylate
Osamu IRINOKiyoshi SAITOHKazumi OHKUBO
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1985 Volume 86 Issue 1 Pages 17-23

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Abstract
Effects of choline salicylate, sodium salicylate, choline chloride and acetylsalicylic acid on platelet aggregation in vivo, ex vivo and in vitro in mice were studied. These drugs all inhibited adenosine diphosphate (ADP)-induced respiratory depression, which is closely related to platelet aggregation in vivo, with choline salicylate showing the strongest inhibitory effect. Choline salicylate had a tendency to reduce the mortality of animals injected intravenously with endotoxin, but the other drugs had no such effect. The inhibitory effects of these drugs on ADP-induced platelet aggregation ex vivo were in the order of choline salicylate>acetylsalicylic acid ?? sodium salicylate>choline chlorides ?? no effect, and plasma concentrations of protein-unbound salicylic acid at 1 hr after oral administration of drugs were in the order of choline salicylate>acetylsalicylic acid ?? sodium salicylate. The in vitro effects of these drugs were in the order of choline salicylate ?? sodium salicylate>choline chloride ?? acetylsalicylic acid ?? no effect. Therefore, it was considered that salicylic acid played an important role on the in vivo, ex vivo and in vitro effects of choline salicylate and that choline increased plasma concentrations of salicylic acid and consequently enhanced the in vivo and ex vivo effects of salicylic acid. Furthermore, the ex vivo effects of choline salicylate were found when ADP-induced platelet aggregation was measured with platelet-rich plasma prepared from blood collected with heparin as anti-coagulant, but not when blood was collected with citrate. Thus, the possibility that the anti-platelet actions of salicylic acid may be due to the inhibition of metabolism of extracellular calcium in platelets during ADP-induced aggregation was suggested.
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