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关于甲氯芬那酸钠药理活性的机制

On the mechanism of the pharmacologic activity of meclofenamate sodium.

作者信息

McLean J R, Gluckman M I

出版信息

Arzneimittelforschung. 1983;33(4A):627-31.

PMID:6603853
Abstract

N-(2,6-Dichloro-m-tolyl)anthranilic acid, sodium salt (meclofenamate sodium, Meclomen), the sodium salt of meclofenamic acid, has anti-inflammatory activity both in animal models and in clinical use. This activity is believed to be due in large part to the ability of the drug to inhibit the synthesis of prostaglandins by inhibiting arachidonic acid cyclo-oxygenase. Further, there is evidence that meclofenamic acid directly antagonizes the actions of prostaglandins at receptor sites. In addition, meclofenamic acid may also inhibit arachidonic acid lipoxygenase, resulting in decreased synthesis of leukotrienes, known mediators involved in the inflammatory process.

摘要

N-(2,6-二氯间甲苯基)邻氨基苯甲酸的钠盐(甲氯芬那酸钠,甲氯灭酸),具有抗炎活性,在动物模型和临床应用中均有体现。人们认为这种活性很大程度上归因于该药物通过抑制花生四烯酸环氧化酶来抑制前列腺素合成的能力。此外,有证据表明甲氯芬那酸可在受体部位直接拮抗前列腺素的作用。另外,甲氯芬那酸还可能抑制花生四烯酸脂氧合酶,从而减少白三烯的合成,白三烯是炎症过程中已知的介质。

相似文献

1
On the mechanism of the pharmacologic activity of meclofenamate sodium.关于甲氯芬那酸钠药理活性的机制
Arzneimittelforschung. 1983;33(4A):627-31.
2
Effects of meclofenamate on the renal actions of mannitol infusion in conscious rabbits. Evidence for osmotic control of renal prostaglandin synthesis?甲氯芬那酸对清醒兔静脉输注甘露醇时肾脏作用的影响。肾前列腺素合成受渗透压调控的证据?
Adv Prostaglandin Thromboxane Res. 1980;7:1039-45.
3
Structure-activity relationships in a series of anti-inflammatory N-arylanthranilic acids.一系列抗炎N-芳基邻氨基苯甲酸的构效关系
Arzneimittelforschung. 1983;33(4A):621-7.
4
Pharmacology, pharmacokinetics, and therapeutic use of meclofenamate sodium.甲氯芬那酸钠的药理学、药代动力学及治疗用途。
Clin J Pain. 1991;7 Suppl 1:S44-8.
5
Meclofenamate sodium in the treatment of post-traumatic edema. Report of a controlled double-blind study.甲氯芬那酸钠治疗创伤后水肿。一项对照双盲研究报告。
Arzneimittelforschung. 1983;33(4A):663-7.
6
Effect of meclomen on production and action of human interferon alpha.美洛昔康对人α干扰素产生及作用的影响。
Acta Virol. 1990 Feb;34(1):27-36.
7
The effect of meclofenamate on renal blood flow in the unanesthetized dog: relation to renal prostaglandins and sodium balance.甲氯芬那酸对未麻醉犬肾血流量的影响:与肾前列腺素和钠平衡的关系。
J Pharmacol Exp Ther. 1980 Jul;214(1):1-4.
8
Meclofenamate sodium in the treatment of degenerative joint disease of the hand (Heberden nodes).甲氯芬那酸钠治疗手部退行性关节病(赫伯登结节)。
Arzneimittelforschung. 1983;33(4A):656-9.
9
Effect of indomethacin and sodium meclofenamate on the renal concentrating defect in experimental enterococcal pyelonephritis in rats.吲哚美辛和甲氯芬那酸钠对大鼠实验性肠球菌性肾盂肾炎肾浓缩功能缺陷的影响。
J Lab Clin Med. 1976 Dec;88(6):958-64.
10
Study of the mechanisms of action of sodium meclofenamic acid (Meclomen) a "double inhibitor" of the arachidonic acid cascade.甲氯芬那酸钠(甲氯灭酸)——一种花生四烯酸级联反应的“双重抑制剂”的作用机制研究
J Med. 1994;25(6):371-82.

引用本文的文献

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Significance of Multiple Bioactivation Pathways for Meclofenamate as Revealed through Modeling and Reaction Kinetics.通过建模和反应动力学揭示甲氯芬那酸的多种生物活化途径的意义。
Drug Metab Dispos. 2021 Feb;49(2):133-141. doi: 10.1124/dmd.120.000254. Epub 2020 Nov 25.
2
Inhibition by fenamates of calcium influx and proliferation of human lymphocytes.非甾体抗炎芬那酸盐对人淋巴细胞钙内流和增殖的抑制作用。
Br J Pharmacol. 1996 Oct;119(3):487-94. doi: 10.1111/j.1476-5381.1996.tb15698.x.
3
A double-blind, placebo controlled, cross-over comparison of the analgesic effect of ibuprofen 400 mg and 800 mg on laser-induced pain.
布洛芬400毫克和800毫克对激光诱导疼痛镇痛作用的双盲、安慰剂对照、交叉比较。
Br J Clin Pharmacol. 1990 Nov;30(5):711-5. doi: 10.1111/j.1365-2125.1990.tb03840.x.
4
Receptors involved in mechanical responses to catecholamines in the circular muscle of guinea-pig stomach treated with meclofenamate.用甲氯芬那酸处理的豚鼠胃环形肌中参与对儿茶酚胺机械反应的受体。
Br J Pharmacol. 1990 Dec;101(4):809-14. doi: 10.1111/j.1476-5381.1990.tb14162.x.