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Interaction of prostaglandin D2 with prostacyclin, carbacyclin and the hydantoin prostaglandin, BW245C, in guinea-pig platelets.前列腺素D2与前列环素、卡前列环素及乙内酰脲前列腺素BW245C在豚鼠血小板中的相互作用。
Br J Pharmacol. 1985 May;85(1):285-90. doi: 10.1111/j.1476-5381.1985.tb08858.x.
2
Platelet and cardiovascular activity of the hydantoin BW245C, a potent prostaglandin analogue.海因类化合物BW245C（一种强效前列腺素类似物）的血小板及心血管活性
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3
The antagonism by BW A868C of PGD2 and BW245C activation of human platelet adenylate cyclase.BW A868C对前列腺素D2的拮抗作用以及BW245C对人血小板腺苷酸环化酶的激活作用。
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Different responsiveness of prostaglandin D2-sensitive systems to prostaglandin D2 and its analogues.前列腺素D2敏感系统对前列腺素D2及其类似物的不同反应性。
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A chemically stable analogue, 9 beta-methyl carbacyclin, with similar effects to epoprostenol (prostacyclin, PGI2) in man.一种化学性质稳定的类似物，9β-甲基卡前列环素，在人体内具有与依前列醇（前列环素，PGI2）相似的作用。
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Br J Pharmacol. 1985 Mar;84(3):595-607. doi: 10.1111/j.1476-5381.1985.tb16139.x.

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Prostaglandin D2 interacts at thromboxane receptor-sites on guinea-pig platelets.前列腺素D2在豚鼠血小板的血栓素受体位点上相互作用。
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The classification of prostaglandin DP-receptors in platelets and vasculature using BW A868C, a novel, selective and potent competitive antagonist.使用新型、选择性且强效的竞争性拮抗剂BW A868C对血小板和脉管系统中的前列腺素DP受体进行分类。
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本文引用的文献

1
Carbacyclin--a potent stable prostacyclin analogue for the inhibition of platelet aggregation.卡巴前列素——一种用于抑制血小板聚集的强效稳定前列环素类似物。
Prostaglandins. 1980 Apr;19(4):605-27. doi: 10.1016/s0090-6980(80)80010-4.
2
Platelet and cardiovascular activity of the hydantoin BW245C, a potent prostaglandin analogue.海因类化合物BW245C（一种强效前列腺素类似物）的血小板及心血管活性
Prostaglandins. 1983 Feb;25(2):205-23. doi: 10.1016/0090-6980(83)90105-3.
3
Ligand binding to thromboxane receptors on human platelets: correlation with biological activity.配体与人血小板上血栓素受体的结合：与生物活性的相关性。
Br J Pharmacol. 1983 Aug;79(4):953-64. doi: 10.1111/j.1476-5381.1983.tb10541.x.
4
Pharmacological and cardiovascular properties of a hydantoin derivative, BW 245 C, with high affinity and selectivity for PGD2 receptors.一种对前列地尔D2受体具有高亲和力和选择性的乙内酰脲衍生物BW 245 C的药理和心血管特性
Prostaglandins. 1983 Jan;25(1):13-28. doi: 10.1016/0090-6980(83)90131-4.
5
Desensitization of prostacyclin receptors in a neuronal hybrid cell line.神经元杂交细胞系中前列环素受体的脱敏作用
Br J Pharmacol. 1982 Sep;77(1):121-7. doi: 10.1111/j.1476-5381.1982.tb09277.x.
6
Inhibition of aggregation and stimulation of cyclic AMP generation in intact human platelets by the diterpene forskolin.二萜类药物福斯高林对完整人血小板聚集的抑制作用及环磷酸腺苷生成的刺激作用。
Mol Pharmacol. 1982 May;21(3):680-7.
7
Forskolin: unique diterpene activator of adenylate cyclase in membranes and in intact cells.福斯高林：膜及完整细胞中独特的腺苷酸环化酶二萜激活剂。
Proc Natl Acad Sci U S A. 1981 Jun;78(6):3363-7. doi: 10.1073/pnas.78.6.3363.
8
Prostaglandin D2 inhibits the aggregation of human platelets.前列腺素D2抑制人血小板的聚集。
Thromb Res. 1974 Sep;5(3):291-9. doi: 10.1016/0049-3848(74)90168-6.
9
Cyclic 3',5'-adenosine monophosphate in human blood platelets. II. Effect of N6-2'-o-dibutyryl cyclic 3',5'-adenosine monophosphate on platelet function.人血小板中的环3',5'-腺苷单磷酸。II. N6-2'-O-二丁酰环3',5'-腺苷单磷酸对血小板功能的影响。
J Clin Invest. 1971 Jan;50(1):131-41. doi: 10.1172/JCI106467.
10
Isomerization of prostaglandin H2 into prostaglandin D2 in the presence of serum albumin.在血清白蛋白存在的情况下，前列腺素H2异构化为前列腺素D2。
Biochim Biophys Acta. 1976 Apr 22;431(1):189-83. doi: 10.1016/0005-2760(76)90273-3.

前列腺素D2与前列环素、卡前列环素及乙内酰脲前列腺素BW245C在豚鼠血小板中的相互作用。

Interaction of prostaglandin D2 with prostacyclin, carbacyclin and the hydantoin prostaglandin, BW245C, in guinea-pig platelets.

作者信息

Hamid S, Whittle B J

出版信息

Br J Pharmacol. 1985 May;85(1):285-90. doi: 10.1111/j.1476-5381.1985.tb08858.x.

DOI:10.1111/j.1476-5381.1985.tb08858.x
PMID:2992652
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC1916783/
Abstract

The anti-aggregating actions of prostaglandin D2 (PGD2) have been compared to prostacyclin (PGI2), its stable analogue carbacyclin and a hydantoin prostaglandin, BW245C, in guinea-pig PGI2, carbacyclin and BW245C were potent inhibitors of ADP-induced aggregation in guinea-pig platelets, with ID50 values comparable to those obtained in human platelet-rich-plasma. In contrast, PGD2 acted as a weak and partial inhibitor in guinea-pig platelet aggregation, producing a bell-shaped dose-response relationship. PGD2 induced a dose-related antagonism of the inhibitory actions of BW245C, prostacyclin and carbacyclin on guinea-pig platelets. However, PGD2 did not antagonize the inhibitory actions of either forskolin or dibutyryl cyclic AMP on this platelet preparation. The results suggest a non-specific interaction of PGD2 with these prostanoid binding sites on guinea-pig platelets.

摘要

已将前列腺素D2（PGD2）的抗聚集作用与前列环素（PGI2）、其稳定类似物卡前列环素以及一种乙内酰脲前列腺素BW245C进行了比较。在豚鼠中，PGI2、卡前列环素和BW245C是ADP诱导的豚鼠血小板聚集的有效抑制剂，其半数抑制浓度（ID50）值与在富含血小板的人血浆中获得的值相当。相比之下，PGD2在豚鼠血小板聚集中起弱的部分抑制剂作用，产生钟形剂量反应关系。PGD2诱导了BW245C、前列环素和卡前列环素对豚鼠血小板抑制作用的剂量相关拮抗作用。然而，PGD2并不拮抗福斯可林或二丁酰环磷腺苷对该血小板制剂的抑制作用。结果表明PGD2与豚鼠血小板上的这些前列腺素结合位点存在非特异性相互作用。