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1
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.
2
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.
3
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。
Mol Pharmacol. 1993 Feb;43(2):302-12.
4
1-O-hexadecyl-2-metoxy-glycero-3-phosphatidylcholine--a methoxy ether lipid inhibiting platelet activating factor-induced platelet aggregation and neutrophil oxidative metabolism.1-O-十六烷基-2-甲氧基甘油-3-磷脂酰胆碱——一种抑制血小板活化因子诱导的血小板聚集和中性粒细胞氧化代谢的甲氧基醚脂质。
Biochem Pharmacol. 1995 May 26;49(11):1577-82. doi: 10.1016/0006-2952(95)00099-l.
5
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.
6
Pharmacological actions of Y-24180, a new specific antagonist of platelet activating factor (PAF): II. Interactions with PAF and benzodiazepine receptors.血小板活化因子（PAF）新型特异性拮抗剂Y-24180的药理作用：II. 与PAF及苯二氮䓬受体的相互作用
Prostaglandins. 1990 Dec;40(6):571-83. doi: 10.1016/0090-6980(90)90002-d.
7
CV 6209 is a non-competitive antagonist of platelet-activating factor receptors on guinea-pig resident peritoneal macrophages.CV 6209是豚鼠腹腔常驻巨噬细胞上血小板活化因子受体的非竞争性拮抗剂。
Clin Exp Pharmacol Physiol. 1989 Nov;16(11):813-20. doi: 10.1111/j.1440-1681.1989.tb01520.x.
8
Biochemical and pharmacological activities of SR 27417, a highly potent, long-acting platelet-activating factor receptor antagonist.SR 27417的生化和药理活性，一种高效、长效的血小板活化因子受体拮抗剂。
J Pharmacol Exp Ther. 1991 Oct;259(1):44-51.
9
Albumin inhibits platelet-activating factor (PAF)-induced responses in platelets and macrophages: implications for the biologically active form of PAF.白蛋白可抑制血小板活化因子（PAF）诱导的血小板和巨噬细胞反应：对PAF生物活性形式的影响。
Br J Pharmacol. 1992 Sep;107(1):73-7. doi: 10.1111/j.1476-5381.1992.tb14465.x.
10
Continuous binding of the PAF molecule to its receptor is necessary for the long-term aggregation of platelets.血小板的长期聚集需要PAF分子与其受体持续结合。
Am J Physiol. 1998 Jan;274(1):C47-57. doi: 10.1152/ajpcell.1998.274.1.C47.

引用本文的文献

1
Lysine trimethylation of EF-Tu mimics platelet-activating factor to initiate Pseudomonas aeruginosa pneumonia.EF-Tu 的赖氨酸三甲基化模拟血小板激活因子引发铜绿假单胞菌肺炎。
mBio. 2013 May 7;4(3):e00207-13. doi: 10.1128/mBio.00207-13.
2
Neutrophils stimulated with a variety of chemoattractants exhibit rapid activation of p21-activated kinases (Paks): separate signals are required for activation and inactivation of paks.用多种趋化因子刺激的中性粒细胞表现出p21激活激酶（Paks）的快速激活：Paks的激活和失活需要不同的信号。
Mol Cell Biol. 1998 Dec;18(12):7130-8. doi: 10.1128/MCB.18.12.7130.
3
Similar coronary vascular effects in the rat perfused heart of platelet-activating factor structural analogues with agonist and antagonist properties.在具有激动剂和拮抗剂特性的血小板活化因子结构类似物的大鼠灌注心脏中，有类似的冠状血管效应。
Br J Pharmacol. 1995 Nov;116(5):2359-64. doi: 10.1111/j.1476-5381.1995.tb15080.x.
4
Adenosine inhibits platelet-activating factor, but not tumour necrosis factor-alpha-induced priming of human neutrophils.腺苷可抑制血小板活化因子，但不能抑制肿瘤坏死因子-α诱导的人中性粒细胞的预激活。
Immunology. 1993 Jan;78(1):152-8.
5
Partial agonist effect of the platelet-activating factor receptor antagonists, WEB 2086 and WEB 2170, in the rat perfused heart.血小板活化因子受体拮抗剂WEB 2086和WEB 2170在大鼠离体灌注心脏中的部分激动剂效应。
Br J Pharmacol. 1993 Oct;110(2):645-50. doi: 10.1111/j.1476-5381.1993.tb13860.x.
6
Granulocyte and granulocyte-macrophage colony-stimulating factors exert differential effects on neutrophil platelet-activating factor generation and release.粒细胞和粒细胞巨噬细胞集落刺激因子对中性粒细胞血小板活化因子的产生和释放具有不同的作用。
Immunology. 1994 May;82(1):51-6.
7
Albumin inhibits platelet-activating factor (PAF)-induced responses in platelets and macrophages: implications for the biologically active form of PAF.白蛋白可抑制血小板活化因子（PAF）诱导的血小板和巨噬细胞反应：对PAF生物活性形式的影响。
Br J Pharmacol. 1992 Sep;107(1):73-7. doi: 10.1111/j.1476-5381.1992.tb14465.x.

本文引用的文献

1
A modification of receptor theory.受体理论的一种修正。
Br J Pharmacol Chemother. 1956 Dec;11(4):379-93. doi: 10.1111/j.1476-5381.1956.tb00006.x.
2
Potent platelet stimulating activity of enantiomers of acetyl glyceryl ether phosphorylcholine and its methoxy analogues.乙酰甘油醚磷酸胆碱及其甲氧基类似物对映体的强效血小板刺激活性。
Biochem Biophys Res Commun. 1981 Mar 16;99(1):183-8. doi: 10.1016/0006-291x(81)91730-7.
3
The use of prostacyclin in the separation from plasma and washing of human platelets.前列环素在人血小板与血浆分离及洗涤中的应用。
Prostaglandins. 1982 Jun;23(6):929-45. doi: 10.1016/0090-6980(82)90135-6.
4
Activation of phospholipase C is dissociated from arachidonate metabolism during platelet shape change induced by thrombin or platelet-activating factor. Epinephrine does not induce phospholipase C activation or platelet shape change.在凝血酶或血小板激活因子诱导的血小板形态变化过程中，磷脂酶C的激活与花生四烯酸代谢相分离。肾上腺素不会诱导磷脂酶C激活或血小板形态变化。
J Biol Chem. 1984 Jul 10;259(13):8286-92.
5
Leukocyte-dependent histamine release from rabbit platelets. The role of IgE, basophils, and a platelet-activating factor.兔血小板中白细胞依赖性组胺释放。IgE、嗜碱性粒细胞和血小板激活因子的作用。
J Exp Med. 1972 Dec 1;136(6):1356-77. doi: 10.1084/jem.136.6.1356.
6
Intracellular calcium fluxes in human platelets.人类血小板中的细胞内钙通量
Eur J Biochem. 1985 Mar 1;147(2):421-7. doi: 10.1111/j.1432-1033.1985.tb08766.x.
7
Structural analogs of alkylacetylglycerophosphocholine inhibitory behavior on platelet activation.烷基乙酰甘油磷酸胆碱的结构类似物对血小板活化的抑制作用。
J Biol Chem. 1985 Oct 15;260(23):12710-4.
8
Fura-2 measurement of cytosolic free Ca2+ in monolayers and suspensions of various types of animal cells.用Fura-2测量各种动物细胞单层和悬浮液中的胞质游离Ca2+ 。
J Cell Biol. 1987 Nov;105(5):2145-55. doi: 10.1083/jcb.105.5.2145.
9
Staurosporine, a potent inhibitor of phospholipid/Ca++dependent protein kinase.星形孢菌素，一种磷脂/钙离子依赖性蛋白激酶的强效抑制剂。
Biochem Biophys Res Commun. 1986 Mar 13;135(2):397-402. doi: 10.1016/0006-291x(86)90008-2.
10
Perspectives in platelet-activating factor research.血小板活化因子研究的展望
Pharmacol Rev. 1987 Jun;39(2):97-145.

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。

1-O-hexadecyl-2-acetyl-sn-glycero-3-phospho (N,N,N trimethyl) hexanolamine: an analogue of platelet-activating factor with partial agonist activity.

作者信息

Grigoriadis G, Stewart A G

机构信息

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

出版信息

Br J Pharmacol. 1991 Sep;104(1):171-7. doi: 10.1111/j.1476-5381.1991.tb12403.x.

DOI:10.1111/j.1476-5381.1991.tb12403.x
PMID:1664761
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC1908285/
Abstract
  1. During studies of the role of platelet-activating factor (PAF) in macrophage superoxide anion generation (O2(-1], we identified an agonist action of the putative PAF receptor antagonist 1-O-hexadecyl-2-acetyl-sn-glycero-3-phospho (N,N,N-trimethyl) hexanolamine (hexanolamine PAF) in guinea-pig macrophages. The 1-O-octadecyl form of this compound has specific antagonist actions at PAF receptors. 2. The agonist properties of hexanolamine PAF were examined in rabbit washed platelets (aggregation) and in guinea-pig peritoneal macrophages (O2- generation). 3. Hexanolamine PAF induced significant platelet aggregation (50% of the PAF maximum). However, the omission of bovine serum albumin (BSA) from the Tyrode buffer resulted in a diminution of the response of washed platelets during storage for 24 h at 4 degrees C (7% of PAF maximum), whereas the maximum response to PAF was unaffected by storage for this period, irrespective of the presence of BSA. 4. Platelet aggregation induced by hexanolamine PAF was not accompanied by a detectable increase in intracellular calcium [Ca2+]i, whereas the aggregation response to PAF was preceded by a large rise in [Ca2+]i. 5. Hexanolamine PAF induced O2- generation in adherent macrophages, with a maximum response 45% of that to PAF. Hexanolamine PAF (100 nM), at a concentration equi-effective with PAF (1 nM) for stimulation of O2- generation in macrophages, induced an increase in [Ca2+]i which was significantly less than that induced by PAF. 6. PAF concentration-response curves were constructed in platelets or macrophages following pretreatment with hexanolamine PAF (0.1 and 1 microM). The interaction between PAF and the putative partial agonist (hexanolamine PAF) had the characteristics expected of a partial agonist interacting with a full agonist.7. Platelet aggregation induced by hexanolamine PAF was antagonized non-competitively by the PAF receptor antagonist, WEB 2086, whereas antagonism of PAF-induced aggregation by WEB 2086 was competitive. Macrophage 2- generation induced by hexanolamine PAF or PAF was antagonized by WEB 2086.8. These data indicate that hexanolamine PAF is a partial agonist at PAF receptors in macrophages and platelets. The inability of hexanolamine PAF to increase [Ca2+]i in platelets suggests that PAF receptors may be coupled to platelet aggregation by both Ca2 +-dependent and -independent pathways.
摘要
  1. 在研究血小板活化因子（PAF）在巨噬细胞超氧阴离子生成（O₂⁻）中的作用时，我们在豚鼠巨噬细胞中鉴定出了假定的PAF受体拮抗剂1 - O - 十六烷基 - 2 - 乙酰 - sn - 甘油 - 3 - 磷酸（N，N，N - 三甲基）己醇胺（己醇胺PAF）的激动剂作用。该化合物的1 - O - 十八烷基形式在PAF受体上具有特异性拮抗剂作用。2. 在兔洗涤血小板（聚集）和豚鼠腹腔巨噬细胞（O₂⁻生成）中检测了己醇胺PAF的激动剂特性。3. 己醇胺PAF诱导显著的血小板聚集（达到PAF最大聚集量的50%）。然而，在Tyrode缓冲液中省略牛血清白蛋白（BSA）会导致洗涤后的血小板在4℃储存24小时期间反应减弱（为PAF最大聚集量的7%），而在此期间PAF的最大反应不受储存影响，无论是否存在BSA。4. 己醇胺PAF诱导的血小板聚集并未伴随细胞内钙[Ca²⁺]i的可检测增加，而对PAF的聚集反应之前[Ca²⁺]i会大幅升高。5. 己醇胺PAF诱导贴壁巨噬细胞产生O₂⁻，最大反应为PAF的45%。在刺激巨噬细胞产生O₂⁻方面，己醇胺PAF（100 nM）的浓度与PAF（1 nM）等效，但其诱导的[Ca²⁺]i增加明显小于PAF诱导的增加。6. 在血小板或巨噬细胞中，用己醇胺PAF（0.1和1 μM）预处理后构建了PAF浓度 - 反应曲线。PAF与假定的部分激动剂（己醇胺PAF）之间的相互作用具有部分激动剂与完全激动剂相互作用的预期特征。7. 己醇胺PAF诱导的血小板聚集被PAF受体拮抗剂WEB 2086非竞争性拮抗，而WEB 2086对PAF诱导的聚集的拮抗是竞争性的。己醇胺PAF或PAF诱导的巨噬细胞O₂⁻生成被WEB 2086拮抗。8. 这些数据表明己醇胺PAF是巨噬细胞和血小板中PAF受体的部分激动剂。己醇胺PAF不能增加血小板中的[Ca²⁺]i，这表明PAF受体可能通过钙依赖性和非依赖性途径与血小板聚集偶联。