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血小板活化因子拮抗剂BN 50730治疗角叉菜胶诱导的关节炎

Treatment of carrageenan induced arthritis by the platelet activating factor antagonist BN 50730.

作者信息

Hilliquin P, Natour J, Aissa J, Guinot P, Laoussadi S, Benveniste J, Menkes C J, Arnoux B

机构信息

Service de Rhumatologie A, Hôpital Cochin, Paris, France.

出版信息

Ann Rheum Dis. 1995 Feb;54(2):140-3. doi: 10.1136/ard.54.2.140.

DOI:10.1136/ard.54.2.140
PMID:7702404
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC1005539/
Abstract

OBJECTIVE

To evaluate the role of platelet activating factor (PAF) in the early stage of arthritis.

METHODS

Arthritis was induced in rabbits by weekly intra-articular injections of carrageenan. A PAF receptor antagonist, BN 50730, was used as a preventive or curative agent.

RESULTS

BN 50730 was able partially to prevent the development of arthritis, and was also active on established arthritis. The joint arthritis scores of BN treated animals were significantly lower than those of the non-treated animals. The blood concentrations of PAF, PAF bound to lipoproteins (lipo-PAF), and its precursor, lyso-PAF, were not correlated with clinical variations.

CONCLUSIONS

The present data demonstrate a therapeutic action of a PAF antagonist in experimental arthritis and suggest a critical role for PAF during the early stage of arthritis.

摘要

目的

评估血小板活化因子(PAF)在关节炎早期的作用。

方法

通过每周向兔关节腔内注射角叉菜胶诱导关节炎。使用PAF受体拮抗剂BN 50730作为预防或治疗药物。

结果

BN 50730能够部分预防关节炎的发展,对已形成的关节炎也有作用。接受BN治疗的动物的关节关节炎评分显著低于未治疗的动物。PAF、与脂蛋白结合的PAF(脂蛋白-PAF)及其前体溶血-PAF的血药浓度与临床变化无关。

结论

目前的数据证明了PAF拮抗剂在实验性关节炎中的治疗作用,并提示PAF在关节炎早期起关键作用。

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1
Treatment of carrageenan induced arthritis by the platelet activating factor antagonist BN 50730.血小板活化因子拮抗剂BN 50730治疗角叉菜胶诱导的关节炎
Ann Rheum Dis. 1995 Feb;54(2):140-3. doi: 10.1136/ard.54.2.140.
2
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Involvement of platelet-activating factor and tumour necrosis factor in the pathogenesis of joint inflammation in rabbits.血小板活化因子和肿瘤坏死因子在兔关节炎症发病机制中的作用。
Clin Exp Immunol. 1992 May;88(2):318-23. doi: 10.1111/j.1365-2249.1992.tb03080.x.
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A double blind, placebo controlled study of a platelet activating factor antagonist in patients with rheumatoid arthritis.一项针对类风湿性关节炎患者的血小板活化因子拮抗剂的双盲、安慰剂对照研究。
J Rheumatol. 1998 Aug;25(8):1502-7.
6
New trends in PAF antagonist research: a new series of potent hetrapazine-derived PAF antagonists.血小板活化因子拮抗剂研究的新趋势:一系列新型强效的六氮杂茚衍生的血小板活化因子拮抗剂。
Agents Actions. 1991 Jan;32(1-2):34-6. doi: 10.1007/BF01983304.
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Long-lasting inhibitory activity of the hetrazepinic BN 50730 on exudation and cellular alterations evoked by PAF and LPS.海曲氮平BN 50730对PAF和LPS诱发的渗出及细胞改变的持久抑制活性。
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Inhibitory effect of new PAF antagonists on PAF-induced rabbit platelet aggregation in vitro and ex vivo.新型血小板活化因子拮抗剂对血小板活化因子诱导的兔血小板体外及体内聚集的抑制作用
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Formation of a highly stable complex between BN 50730 [tetrahydro-4,7,8,10 methyl-1(chloro-2 phenyl)-6 (methoxy-4 phenyl-carbamoyl)-9 pyrido [4',3'-4,5] thieno [3,2-f] triazolo-1,2,4 [4,3-a] diazepine-1,4] and the platelet-activating factor receptor in rabbit platelet membranes.BN 50730[四氢-4,7,8,10-甲基-1-(氯-2-苯基)-6-(甲氧基-4-苯基-氨基甲酰基)-9-吡啶并[4',3'-4,5]噻吩并[3,2-f]三唑并-1,2,4[4,3-a]二氮杂卓-1,4]与兔血小板膜中血小板活化因子受体形成高度稳定的复合物。
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Effect of BN 50727 on pathological findings and tissue platelet activating factor levels during ileal ischemia in newborn piglets.BN 50727对新生仔猪回肠缺血期间病理结果及组织血小板活化因子水平的影响。
J Pediatr Surg. 1996 Dec;31(12):1675-9. doi: 10.1016/s0022-3468(96)90046-9.

引用本文的文献

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Neurochem Res. 2000 May;25(5):613-9. doi: 10.1023/a:1007550801444.

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Biosynthetic labelling of platelet activating factor from radioactive acetate by stimulated platelets.受刺激血小板利用放射性乙酸对血小板激活因子进行生物合成标记
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Human neutrophil-derived platelet activating factor.人中性粒细胞源性血小板活化因子
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Release of 1-O-alkylglyceryl 3-phosphorylcholine, O-deacetyl platelet-activating factor, from leukocytes: chemical ionization mass spectrometry of phospholipids.1-O-烷基甘油基3-磷酸胆碱(O-脱乙酰基血小板活化因子)从白细胞中的释放:磷脂的化学电离质谱分析
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Biosynthesis of Paf-acether (platelet-activating factor). VII. Precursors of Paf-acether and acetyl-transferase activity in human leukocytes.血小板激活因子(Paf-乙酰醚)的生物合成。VII. 人白细胞中血小板激活因子的前体和乙酰转移酶活性
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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。
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Antigenic release of paf-acether and beta-glucuronidase from alveolar macrophages of asthmatics.哮喘患者肺泡巨噬细胞中血小板活化因子乙酰水解酶和β-葡萄糖醛酸酶的抗原性释放
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Inhibition of transmembrane movement and metabolism of platelet activating factor (PAF-acether) by a specific antagonist, BN 52021.一种特异性拮抗剂BN 52021对血小板活化因子(PAF-乙醚)跨膜转运和代谢的抑制作用
Biochem Biophys Res Commun. 1985 Oct 30;132(2):460-6. doi: 10.1016/0006-291x(85)91156-8.
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Influence of SK&F 95587 and BN 50730 on bronchoconstrictor responses in the cat.SK&F 95587和BN 50730对猫支气管收缩反应的影响。
J Pharmacol Exp Ther. 1990 Dec;255(3):1320-7.
9
Presence of paf-acether in rheumatic diseases.风湿性疾病中血小板活化因子乙酰醚的存在。
Ann Rheum Dis. 1992 Jan;51(1):29-31. doi: 10.1136/ard.51.1.29.
10
Paf-acether acetylhydrolase activity is increased in patients with rheumatic diseases.风湿性疾病患者的血小板活化因子乙酰水解酶活性增加。
Scand J Rheumatol. 1992;21(4):161-4. doi: 10.3109/03009749209099215.