Drummond A H, Gordon J L
Br J Pharmacol. 1976 Apr;56(4):417-21. doi: 10.1111/j.1476-5381.1976.tb07452.x.
1 The uptake of 5-hydroxytryptamine (5-HT) by rat blood platelets in citrated plasma was linear for at most 10 s and was substantially complete within 3 minutes. 2 Adenosine 5'-diphosphate (ADP) was a potent inhibitor of 5-HT uptake (Ki=0.38 muM) and kinetic analysis revealed that the inhibition was not competitive. 3 Inhibition of 5-HT uptake by ADP was abolished in the presence of prostaglandin E1 and 2-n-amylthio-AMP, which also inhibit the stimulant actions of ADP on blood platelets. 4 It is concluded that ADP could inhibit 5-HT uptake by changing the Na+/K+ distribution across the cell membrane, and the biological significance of this is discussed.
1 在枸橼酸盐血浆中，大鼠血小板对5-羟色胺（5-HT）的摄取在至多10秒内呈线性，且在3分钟内基本完成。2 腺苷5'-二磷酸（ADP）是5-HT摄取的有效抑制剂（Ki = 0.38 μM），动力学分析表明该抑制作用并非竞争性的。3 在前列腺素E1和2-n-戊硫基-AMP存在的情况下，ADP对5-HT摄取的抑制作用被消除，这两种物质也抑制ADP对血小板的刺激作用。4 得出的结论是，ADP可能通过改变细胞膜上的Na+/K+分布来抑制5-HT摄取，并讨论了其生物学意义。
