Takada A, Takada Y
Department of Physiology, Hamamatsu University School of Medicine.
Nihon Rinsho. 1992 Feb;50(2):315-8.
Endothelins are a family of three peptides that act as local hormones in all mammalian species. They were found to inhibit rabbit and dog platelet aggregation in vivo, whereas no effect was observed in vitro. In order to investigate the possible interaction between endothelins and human platelet serotonergic receptors, their effect on the platelet aggregation, induced by serotonin, was studied. Endothelin-1, -2 and -3 had a dual action for platelet aggregation induced by serotonin. When added simultaneously to serotonin endothelins aggregatory response to this amine was potentiated. On the contrary, preincubation of platelet suspension with endothelins resulted in a concentration-dependent inhibition of serotonin-promoted platelet response. Moreover, endothelin-1 inhibited serotonergic amplification of epinephrine-induced aggregation of platelets. It is proposed that endothelins bind to the platelet membrane and interact with serotonergic receptors and/or G proteins. The diverse effect of eodothelins on serotonin-induced aggregation of platelets may be due to stimulation of protein kinase C.
内皮素是一族由三种肽组成的物质，在所有哺乳动物物种中作为局部激素发挥作用。研究发现，它们在体内可抑制兔和犬的血小板聚集，而在体外未观察到这种作用。为了研究内皮素与人类血小板血清素能受体之间可能存在的相互作用，研究了它们对血清素诱导的血小板聚集的影响。内皮素-1、-2和-3对血清素诱导的血小板聚集具有双重作用。当与血清素同时添加时，内皮素对这种胺的聚集反应会增强。相反，将血小板悬液与内皮素预孵育会导致血清素促进的血小板反应呈浓度依赖性抑制。此外，内皮素-1抑制了肾上腺素诱导的血小板聚集的血清素能放大作用。有人提出，内皮素与血小板膜结合并与血清素能受体和/或G蛋白相互作用。内皮素对血清素诱导的血小板聚集的不同作用可能是由于蛋白激酶C的刺激。
