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1
Interaction of the Paf antagonist WEB 2086 and its hetrazepine analogues with human platelets and endothelial cells.血小板活化因子拮抗剂WEB 2086及其杂氮䓬类似物与人类血小板和内皮细胞的相互作用。
Br J Pharmacol. 1989 Oct;98(2):653-61. doi: 10.1111/j.1476-5381.1989.tb12640.x.
2
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.
3
Structure-activity relationships and effects of platelet-activating factor antagonists in the hetrazepine series.海曲替平系列中血小板活化因子拮抗剂的构效关系及作用
Int Arch Allergy Appl Immunol. 1989;88(1-2):82-7. doi: 10.1159/000234754.
4
The benzodiazepine receptor ligands RO 5-4864 and RO 15-1788 do not block the inhibition of PAF-induced platelet aggregation seen with the hetrazepine WEB2086.苯二氮䓬受体配体RO 5-4864和RO 15-1788不会阻断用海曲替林WEB2086观察到的对PAF诱导的血小板聚集的抑制作用。
Biochem Biophys Res Commun. 1989 Apr 14;160(1):263-7. doi: 10.1016/0006-291x(89)91650-1.
5
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.
6
Inhibition of PAF-induced platelet aggregation by WEB 2086 'in-vitro', an antagonist to the receptor for platelet-activating factor, in bovine.血小板激活因子受体拮抗剂WEB 2086在体外对牛体内PAF诱导的血小板聚集的抑制作用。
Zentralbl Veterinarmed A. 1996 Sep;43(7):399-413. doi: 10.1111/j.1439-0442.1996.tb00468.x.
7
Comparison of three paf-acether receptor antagonist ginkgolides.三种血小板活化因子乙酰水解酶受体拮抗剂银杏内酯的比较。
Eur J Pharmacol. 1988 Jul 26;152(1-2):101-10. doi: 10.1016/0014-2999(88)90840-0.
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
[3H]WEB 2086 labels platelet activating factor receptors in guinea pig and human lung.[3H]WEB 2086标记豚鼠和人肺中的血小板活化因子受体。
Eur J Pharmacol. 1989 Oct 10;169(2-3):313-6. doi: 10.1016/0014-2999(89)90029-0.
10
BN 52021 displaces [3H]paf-acether from, and inhibits its binding to intact human platelets.BN 52021 可从完整的人血小板中置换出 [3H] 血小板活化因子，并抑制其与之结合。
Eur J Pharmacol. 1987 Oct 27;142(3):331-41. doi: 10.1016/0014-2999(87)90071-9.

引用本文的文献

1
Effect of a platelet-activating factor (PAF) receptor antagonist on hyperacute xenograft rejection; evaluation in a pig kidney-human blood xenoperfusion model.血小板活化因子（PAF）受体拮抗剂对超急性异种移植排斥反应的影响；在猪肾-人血异种灌注模型中的评估。
Clin Exp Immunol. 1998 Jul;113(1):136-44. doi: 10.1046/j.1365-2249.1998.00634.x.
2
The effect of inhibitors of platelet aggregation on the metabolism of platelet-activating factor (PAF) in washed rabbit platelets.血小板聚集抑制剂对洗涤兔血小板中血小板活化因子（PAF）代谢的影响。
Lipids. 1991 Dec;26(12):1011-4. doi: 10.1007/BF02536493.
3
PAF. A review of its effects, antagonists and possible future clinical implications (Part II).血小板活化因子。其作用、拮抗剂及未来可能的临床意义综述（第二部分）
Drugs. 1991 Aug;42(2):174-204. doi: 10.2165/00003495-199142020-00002.

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Some quantitative uses of drug antagonists.药物拮抗剂的一些定量应用。
Br J Pharmacol Chemother. 1959 Mar;14(1):48-58. doi: 10.1111/j.1476-5381.1959.tb00928.x.
2
Background and present status of research on platelet-activating factor (PAF-acether).血小板活化因子（PAF-乙酰醚）的研究背景与现状
Ann N Y Acad Sci. 1981;370:119-37. doi: 10.1111/j.1749-6632.1981.tb29727.x.
3
Specific binding by human polymorphonuclear leucocytes of the immunological mediator 1-O-hexadecyl/octadecyl-2-acetyl-sn-glycero-3-phosphorylcholine.免疫介质1-O-十六烷基/十八烷基-2-乙酰基-sn-甘油-3-磷酸胆碱与人多形核白细胞的特异性结合
Immunology. 1983 Jan;48(1):141-9.
4
Inhibition by ticlopidine of Paf-acether-induced in vitro aggregation of rabbit and human platelets.噻氯匹定对血小板活化因子诱导的兔和人血小板体外聚集的抑制作用。
Thromb Res. 1984 Jun 15;34(6):463-71. doi: 10.1016/0049-3848(84)90251-2.
5
The actions of Paf-acether (platelet-activating factor) on guinea-pig isolated heart preparations.血小板激活因子对豚鼠离体心脏标本的作用。
Br J Pharmacol. 1983 Sep;80(1):81-3. doi: 10.1111/j.1476-5381.1983.tb11052.x.
6
CV-3988 - a specific antagonist of platelet activating factor (PAF).CV - 3988——一种血小板活化因子（PAF）的特异性拮抗剂。
Life Sci. 1983 Apr 25;32(17):1975-82. doi: 10.1016/0024-3205(83)90049-8.
7
Specific binding of phospholipid platelet-activating factor by human platelets.人血小板对磷脂血小板活化因子的特异性结合。
J Immunol. 1982 Oct;129(4):1637-41.
8
Platelet-activating factor-induced aggregation of human platelets specifically inhibited by triazolobenzodiazepines.三唑并苯二氮䓬类药物特异性抑制血小板活化因子诱导的人血小板聚集。
Science. 1984 Dec 21;226(4681):1454-6. doi: 10.1126/science.6150550.
9
Culture of human endothelial cells derived from umbilical veins. Identification by morphologic and immunologic criteria.源自脐静脉的人内皮细胞培养。通过形态学和免疫学标准进行鉴定。
J Clin Invest. 1973 Nov;52(11):2745-56. doi: 10.1172/JCI107470.
10
Preparation of suspensions of washed platelets from humans.人洗涤血小板悬液的制备。
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血小板活化因子拮抗剂WEB 2086及其杂氮䓬类似物与人类血小板和内皮细胞的相互作用。

Interaction of the Paf antagonist WEB 2086 and its hetrazepine analogues with human platelets and endothelial cells.

作者信息

Korth R, Hirafuji M, Keraly C L, Delautier D, Bidault J, Benveniste J

机构信息

INSERM U 200, Université Paris-Sud, Clamart, France.

出版信息

Br J Pharmacol. 1989 Oct;98(2):653-61. doi: 10.1111/j.1476-5381.1989.tb12640.x.

DOI:10.1111/j.1476-5381.1989.tb12640.x
PMID:2555017
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC1854736/
Abstract
  1. Intact platelets and confluent human umbilical vein endothelial cells bound [3H]-Paf-acether (platelet activating factor, [3H]-Paf) at 20 degrees C in the presence of 0.25% (w/v) bovine serum albumin (BSA). 2. [3H]-Paf binding to platelets was inhibited in a concentration-dependent manner by WEB 2086. An excess of WEB 2086 indicated the presence of specific, saturable Paf binding which reached a maximum of 28.3 +/- 3.7 fmol [3H]-Paf per 5 x 10(7) platelets. In platelets, different hetrazepines (WEB 2098, 2105, but not 2118) also inhibited [3H]-Paf binding in a concentration-dependent manner. 3. WEB 2086 partially displaced platelet-bound [3H]-Paf in a concentration-dependent manner reaching a plateau at 400 nM WEB 2086. No further displacement was observed when WEB 2086 and an excess of unlabelled Paf were added together. 4. The hetrazepines inhibited platelet aggregation. Platelet aggregation IC50 values correlated well with the IC50 values of the hetrazepines against [3H]-Paf binding (r2 = 0.99). WEB 2086 shifted the Paf dose-response curve rightwards in a parallel manner. Tested against platelet aggregation the pA2 obtained for WEB 2086 was 7.9. 5. WEB 2086 inhibited [3H]-Paf binding to endothelial cells in a concentration-dependent manner. WEB 2086 also inhibited the Paf-mediated cytosolic calcium increase in endothelial cells with an IC50 value of 23.1 +/- 10.4 nM as compared with an IC50 of 21.6 +/- 10.4 nM WEB 2086 for platelet aggregation. 6. These results demonstrate an inhibition of [3H]-Paf binding to platelets and endothelial cells by different hetrazepines, most probably at the Paf receptor level.
摘要

  1. 在20℃、存在0.25%（w/v）牛血清白蛋白（BSA）的条件下，完整血小板和汇合的人脐静脉内皮细胞能结合[3H] - 血小板活化因子（[3H] - Paf）。

  2. WEB 2086以浓度依赖的方式抑制[3H] - Paf与血小板的结合。过量的WEB 2086表明存在特异性、可饱和的Paf结合，每5×10（7）个血小板中[3H] - Paf的最大结合量达到28.3±3.7 fmol。在血小板中，不同的吲唑类化合物（WEB 2098、2105，但不包括2118）也以浓度依赖的方式抑制[3H] - Paf的结合。

  3. WEB 2086以浓度依赖的方式部分置换血小板结合的[3H] - Paf，在400 nM WEB 2086时达到平台期。当同时加入WEB 2086和过量未标记的Paf时，未观察到进一步的置换。

  4. 吲唑类化合物抑制血小板聚集。血小板聚集的IC50值与吲唑类化合物对[3H] - Paf结合的IC50值相关性良好（r2 = 0.99）。WEB 2086使Paf剂量反应曲线平行右移。针对血小板聚集进行测试，得到的WEB 2086的pA2为7.9。

  5. WEB 2086以浓度依赖的方式抑制[3H] - Paf与内皮细胞的结合。WEB 2086还抑制内皮细胞中Paf介导的胞质钙增加，IC50值为23.1±10.4 nM，而其对血小板聚集的IC50值为21.6±10.4 nM。

  6. 这些结果表明不同的吲唑类化合物抑制[3H] - Paf与血小板和内皮细胞的结合，最可能是在Paf受体水平。