Irino O, Saitoh K, Ohkubo K
Nihon Yakurigaku Zasshi. 1985 Jul;86(1):17-23. doi: 10.1254/fpj.86.17.
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 greater than acetylsalicylic acid congruent to sodium salicylate greater than choline chloride congruent to 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 greater than acetylsalicylic acid congruent to sodium salicylate. The in vitro effects of these drugs were in the order of choline salicylate congruent to sodium salicylate greater than choline chloride congruent to acetylsalicylic acid congruent to 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.(ABSTRACT TRUNCATED AT 250 WORDS)
研究了胆碱水杨酸酯、水杨酸钠、氯化胆碱和乙酰水杨酸对小鼠体内、体外和离体血小板聚集的影响。这些药物均抑制二磷酸腺苷(ADP)诱导的呼吸抑制,而呼吸抑制与体内血小板聚集密切相关,其中胆碱水杨酸酯的抑制作用最强。胆碱水杨酸酯有降低静脉注射内毒素动物死亡率的趋势,但其他药物无此作用。这些药物对体外ADP诱导的血小板聚集的抑制作用顺序为:胆碱水杨酸酯>乙酰水杨酸≈水杨酸钠>氯化胆碱≈无作用,口服药物1小时后血浆中游离水杨酸的浓度顺序为:胆碱水杨酸酯>乙酰水杨酸≈水杨酸钠。这些药物的体外作用顺序为:胆碱水杨酸酯≈水杨酸钠>氯化胆碱>乙酰水杨酸≈无作用。因此,认为水杨酸在胆碱水杨酸酯的体内、体外和离体作用中起重要作用,胆碱可增加水杨酸的血浆浓度,从而增强水杨酸的体内和体外作用。此外,当用肝素作为抗凝剂采集的血液制备富含血小板的血浆来测定ADP诱导的血小板聚集时,发现了胆碱水杨酸酯的体外作用,但用柠檬酸盐采集血液时则未发现。(摘要截短于250字)