前列环素类似物刺激兔和人红细胞中受体介导的环磷酸腺苷（cAMP）合成及三磷酸腺苷（ATP）释放。
Prostacyclin analogs stimulate receptor-mediated cAMP synthesis and ATP release from rabbit and human erythrocytes.
作者信息
Sprague Randy S, Bowles Elizabeth A, Hanson Madelyn S, DuFaux Eileen A, Sridharan Meera, Adderley Shaquria, Ellsworth Mary L, Stephenson Alan H
机构信息
Department of Pharmacological and Physiological Science, Saint Louis University, School of Medicine, St. Louis, Missouri 63104, USA.
出版信息
Microcirculation. 2008 Jul;15(5):461-71. doi: 10.1080/10739680701833804.
OBJECTIVES
The purpose of this study was to establish that the prostacyclin (PGI(2)) receptor (IP receptor) is present on rabbit and human erythrocytes and that its activation stimulates cyclic adenosine monophosphate (cAMP) synthesis and adenosine triphosphate (ATP) release.
METHODS
The effect of incubation of erythrocytes with the active PGI(2) analogs, iloprost or UT-15C, on cAMP levels and ATP release was determined in the absence and presence of the IP receptor antagonist, CAY10441. Western analysis was used to determine the presence of the IP receptor on isolated membranes. To establish that effects of PGI(2) analogs were not due to prostaglandin E(2)(PGE(2)) receptor activation, the effect of PGE(2) on cAMP levels and ATP release was determined.
RESULTS
Rabbit and human erythrocytes possess IP receptors. Iloprost and UT-15C stimulated increases in cAMP and ATP release that were prevented by the IP receptor antagonist, CAY10441. PGE(2) did not stimulate cAMP accumulation or ATP release and did not inhibit iloprost-induced increases in cAMP.
CONCLUSIONS
This study establishes that the IP receptor is present on rabbit and human erythrocytes and that its activation results in increases in cAMP and ATP release. These results suggest a novel mechanism by which PGI(2) and its active analogs, when administered pharmacologically, could produce vasodilation.
目的
本研究旨在证实前列环素（PGI₂）受体（IP受体）存在于兔和人的红细胞上，且其激活可刺激环磷酸腺苷（cAMP）合成及三磷酸腺苷（ATP）释放。
方法
在有无IP受体拮抗剂CAY10441的情况下，测定活性PGI₂类似物依洛前列素或UT - 15C与红细胞孵育对cAMP水平和ATP释放的影响。采用蛋白质免疫印迹分析来确定分离膜上IP受体的存在情况。为证实PGI₂类似物的作用并非由于前列腺素E₂（PGE₂）受体激活所致，测定了PGE₂对cAMP水平和ATP释放的影响。
结果
兔和人的红细胞均具有IP受体。依洛前列素和UT - 15C刺激cAMP增加及ATP释放，而这被IP受体拮抗剂CAY10441所阻断。PGE₂未刺激cAMP积累或ATP释放，且不抑制依洛前列素诱导的cAMP增加。
结论
本研究证实IP受体存在于兔和人的红细胞上，且其激活导致cAMP增加及ATP释放。这些结果提示了一种新机制，通过该机制，PGI₂及其活性类似物在药理给药时可产生血管舒张作用。
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