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血小板活化因子(PAF)及其类似物的构效关系揭示了血小板和巨噬细胞上PAF受体之间的差异。

Structure-activity relationships for platelet-activating factor (PAF) and analogues reveal differences between PAF receptors on platelets and macrophages.

作者信息

Stewart A G, Grigoriadis G

机构信息

Department of Physiology, University of Melbourne, Parkville, Victoria, Australia.

出版信息

J Lipid Mediat. 1991 Nov;4(3):299-308.

PMID:1662547
Abstract

Analogues of PAF were examined for their potency in stimulating either platelet aggregation or macrophage superoxide anion generation. Modification of either the alkyl side-chain or the acetyl side-chain increased the relative potency of PAF analogues in macrophages, but all these compounds were more active in platelets. However, an analogue of PAF with an increased inter-ionic distance in the polar head group, hexanolamine PAF, showed a greater potency in macrophages than platelets. The latter compound also appeared to act as a partial agonist in both rabbit platelets and guinea-pig macrophages, but not in guinea-pig platelets. Differences in the rank order of potency of the PAF analogues in stimulating these cell elements suggest that platelet and macrophage PAF receptors differ.

摘要

研究了血小板活化因子(PAF)类似物刺激血小板聚集或巨噬细胞超氧阴离子生成的效力。烷基侧链或乙酰基侧链的修饰提高了PAF类似物在巨噬细胞中的相对效力,但所有这些化合物在血小板中更具活性。然而,一种在极性头部基团中离子间距离增加的PAF类似物,己醇胺PAF,在巨噬细胞中的效力比在血小板中更大。后一种化合物在兔血小板和豚鼠巨噬细胞中似乎也作为部分激动剂起作用,但在豚鼠血小板中不起作用。PAF类似物刺激这些细胞成分的效力排序差异表明血小板和巨噬细胞的PAF受体不同。

相似文献

1
Structure-activity relationships for platelet-activating factor (PAF) and analogues reveal differences between PAF receptors on platelets and macrophages.血小板活化因子(PAF)及其类似物的构效关系揭示了血小板和巨噬细胞上PAF受体之间的差异。
J Lipid Mediat. 1991 Nov;4(3):299-308.
2
1-O-hexadecyl-2-acetyl-sn-glycero-3-phospho (N,N,N trimethyl) hexanolamine: an analogue of platelet-activating factor with partial agonist activity.1-O-十六烷基-2-乙酰基-sn-甘油-3-磷酸(N,N,N-三甲基)己醇胺:一种具有部分激动剂活性的血小板活化因子类似物。
Br J Pharmacol. 1991 Sep;104(1):171-7. doi: 10.1111/j.1476-5381.1991.tb12403.x.
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PAF-agonistic and -antagonistic behaviour of new synthetic ether phospholipids. I. Studies on blood platelets in vitro.
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PAF receptor. 2. Quantitative hydrophobic contribution of the agonist's etheroxid chain.血小板活化因子受体。2. 激动剂醚氧化链的定量疏水贡献。
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Pharmacological characterization of a receptor for platelet-activating factor on guinea pig peritoneal macrophages using [3H]apafant, a selective and competitive platelet-activating factor antagonist: evidence that the noncompetitive behavior of apafant in functional studies relates to slow kinetics of dissociation.使用[3H]阿帕泛(一种选择性竞争性血小板活化因子拮抗剂)对豚鼠腹腔巨噬细胞上血小板活化因子受体进行药理学特性研究:阿帕泛在功能研究中的非竞争性行为与解离动力学缓慢有关的证据。
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High affinity specific binding sites for tritiated platelet-activating factor in canine platelet membranes: counterparts of platelet-activating factor receptors mediating platelet aggregation.犬血小板膜中氚标记血小板活化因子的高亲和力特异性结合位点:介导血小板聚集的血小板活化因子受体对应物。
Mol Pharmacol. 1988 Aug;34(2):145-51.
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Platelet-activating factor stimulation of tyrosine kinase and its relationship to phospholipase C in rabbit platelets: studies with genistein and monoclonal antibody to phosphotyrosine.血小板激活因子对兔血小板中酪氨酸激酶的刺激作用及其与磷脂酶C的关系:染料木黄酮和抗磷酸酪氨酸单克隆抗体的研究
Mol Pharmacol. 1990 Apr;37(4):519-25.
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Characterization of receptors for platelet-activating factor on platelets, polymorphonuclear leukocytes and macrophages.血小板、多形核白细胞和巨噬细胞上血小板活化因子受体的特性研究。
Br J Pharmacol. 1988 Aug;94(4):1225-33. doi: 10.1111/j.1476-5381.1988.tb11642.x.
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Equine peritoneal macrophage production of thromboxane and prostacyclin in response to platelet activating factor and its receptor antagonist SRI 63-441.马腹膜巨噬细胞对血小板活化因子及其受体拮抗剂SRI 63 - 441的反应中血栓素和前列环素的产生
Circ Shock. 1989 Jun;28(2):149-58.

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