Gray S J, Heptinstall S
Eur J Pharmacol. 1985 Aug 15;114(2):129-37. doi: 10.1016/0014-2999(85)90620-x.
The effects of prostaglandin E2 (PGE2) and an antihypertensive PGE2 analogue, CL 115,347 (d,l-15-deoxy-16-hydroxy-16 (alpha/beta)-vinyl prostaglandin E2 methyl ester), were examined on human blood platelet behaviour in platelet-rich plasma (PRP) and in whole blood (WB). The effects on baseline tone of isolated human carotid arterial strips were also examined. PGE2 had a biphasic effect on platelet behaviour, potentiating ADP- and collagen-induced aggregation at low concentrations (10(-8)-10(-6) M) and inhibiting aggregation at higher concentrations (10(-5) M). In contrast, low concentrations of CL 115,347 (10(-9)-10(-5) M) had no effect on platelet aggregation and higher concentrations (10(-4) M) potentiated ADP- and collagen-induced aggregation. The effects of PGE2 and CL 115,347 on adrenaline-induced aggregation were different to those of the other aggregating agents since only inhibition of platelet aggregation was observed. In the presence of PGI2 (10(-9)-10(-8) M) however, PGE2 (10(-8)-10(-6) M) was able to potentiate both ADP- and adrenaline-induced aggregation. Results obtained in WB were similar to those obtained in PRP. Both PGE2 and CL 115,347 contracted isolated human carotid arterial strips in a dose-dependent manner, with PGE2 being approximately 20 times more potent than its synthetic analogue. These results indicate that CL 115,347 is less potent than PGE2 in its effects on human blood platelet behaviour and vascular contractility in vitro.
研究了前列腺素E2（PGE2）和一种抗高血压的PGE2类似物CL 115,347（d，l-15-脱氧-16-羟基-16（α/β）-乙烯基前列腺素E2甲酯）对富血小板血浆（PRP）和全血（WB）中人体血小板行为的影响。还研究了它们对离体人颈动脉条基线张力的影响。PGE2对血小板行为有双相作用，低浓度（10^(-8)-10^(-6)M）时增强ADP和胶原诱导的聚集，高浓度（10^(-5)M）时抑制聚集。相比之下，低浓度的CL 115,347（10^(-9)-10^(-5)M）对血小板聚集无影响，高浓度（10^(-4)M）时增强ADP和胶原诱导的聚集。PGE2和CL 115,347对肾上腺素诱导的聚集的影响与其他聚集剂不同，因为仅观察到对血小板聚集的抑制作用。然而，在存在前列环素（PGI2，10^(-9)-10^(-8)M）的情况下，PGE2（10^(-8)-10^(-6)M）能够增强ADP和肾上腺素诱导的聚集。在WB中获得的结果与在PRP中获得的结果相似。PGE2和CL 115,347均以剂量依赖的方式使离体人颈动脉条收缩，PGE2的效力约为其合成类似物的20倍。这些结果表明，CL 115,347在体外对人体血小板行为和血管收缩性的影响方面比PGE2效力更低。
