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新型香豆素衍生物8-一氯-3-β-二乙氨基乙基-4-甲基-7-乙氧基甲酰甲氧基香豆素在人体体内条件下缺乏抗血小板活性。

Lack of antiplatelet activity of the new coumarin derivative 8-monochloro-3-beta-diethylaminoethyl-4-methyl-7-ethoxy- carboxylmethoxycoumarin under in vivo conditions in man.

作者信息

Luzzatto G, Fabris F, Dal Bo Zanon R, Girolami A

出版信息

Arzneimittelforschung. 1986 Jun;36(6):972-3.

PMID:2943294
Abstract

Antiplatelet properties of AD 6 (8-monochloro-3-beta-diethylaminoethyl-4-methyl-7-ethoxy-carboxyl- methoxycoumarin) have been studied in vitro and in vivo. The drug showed a marked inhibitory effect on platelet aggregation, beta-thromboglobulin (beta TG) release and thromboxane B2 (TxB2) production in vitro. However, such effects were seen only in the presence of high concentrations of the drug (10(-3) and 10(-4) mol/l) and completely disappeared at lower concentrations. No effect was seen in vivo following oral administration of 300 mg of the drug in a small group of volunteers. It can be concluded that in vitro properties of the drug cannot be surmised without due caution to indicate its potential clinical use.

摘要

已在体外和体内研究了AD 6(8-氯-3-β-二乙氨基乙基-4-甲基-7-乙氧基-羧基-甲氧基香豆素)的抗血小板特性。该药物在体外对血小板聚集、β-血小板球蛋白(βTG)释放和血栓素B2(TxB2)生成显示出显著抑制作用。然而,此类作用仅在高浓度药物(10⁻³和10⁻⁴mol/L)存在时可见,在较低浓度时则完全消失。在一小群志愿者中口服300mg该药物后,在体内未观察到作用。可以得出结论,在没有充分谨慎考虑以表明其潜在临床用途的情况下,不能推测该药物的体外特性。

相似文献

1
Lack of antiplatelet activity of the new coumarin derivative 8-monochloro-3-beta-diethylaminoethyl-4-methyl-7-ethoxy- carboxylmethoxycoumarin under in vivo conditions in man.新型香豆素衍生物8-一氯-3-β-二乙氨基乙基-4-甲基-7-乙氧基甲酰甲氧基香豆素在人体体内条件下缺乏抗血小板活性。
Arzneimittelforschung. 1986 Jun;36(6):972-3.
2
Effects of 8-monochloro-3-beta-diethylaminoethyl-4-methyl-7-ethoxy carboxyl methoxy coumarin (AD6) on aggregation, arachidonic acid metabolism and thromboxane B2 formation in human platelets.8-氯-3-β-二乙氨基乙基-4-甲基-7-乙氧基羰基甲氧基香豆素(AD6)对人血小板聚集、花生四烯酸代谢及血栓素B2生成的影响
Pharmacol Res Commun. 1980 Apr;12(4):329-37. doi: 10.1016/s0031-6989(80)80089-0.
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AD6 (8-monochloro-3-beta-diethylamino-ethyl-4-methyl-7-ethoxycarbonyl-meth oxy coumarin) inhibits the release of arachidonic acid in human platelets stimulated by thrombin.
Thromb Res. 1987 Jul 1;47(1):15-24. doi: 10.1016/0049-3848(87)90236-2.
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[Studies on inhibition of platelet aggregation by carbocromen (author's transl)].卡波罗孟对血小板聚集的抑制作用研究(作者译)
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Action of AD6 (8-monochloro-3-beta-diethylaminoethyl-4-methyl-7-ethoxycarbonylmet hox y coumarin) on human platelets in vitro.
Naunyn Schmiedebergs Arch Pharmacol. 1986 Mar;332(3):305-10. doi: 10.1007/BF00504872.
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The effect of AD6 (8-monochloro-3-beta-diethylamino-ethyl-4-methyl-7-ethoxy- carbonylmethoxycoumarin) on washed human platelet aggregation induced by platelet activating factor (PAF) and epinephrine.AD6(8-一氯-3-β-二乙氨基乙基-4-甲基-7-乙氧羰基甲氧基香豆素)对血小板活化因子(PAF)和肾上腺素诱导的洗涤人血小板聚集的影响。
Eur J Pharmacol. 1986 Aug 22;128(1-2):119-27. doi: 10.1016/0014-2999(86)90565-0.
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Synthesis and in vitro inhibitory activity on human platelet aggregation of novel properly substituted 4-(1-piperazinyl)coumarins.新型适当取代的4-(1-哌嗪基)香豆素的合成及其对人血小板聚集的体外抑制活性
Eur J Med Chem. 2004 May;39(5):397-409. doi: 10.1016/j.ejmech.2003.12.010.
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Inhibition by AD6 (8-monochloro-3-beta-diethylaminoethyl-4-methyl-7-ethoxycarbonyl methoxy coumarin) of platelet aggregation in dog stenosed coronary artery.AD6(8-一氯-3-β-二乙氨基乙基-4-甲基-7-乙氧羰基甲氧基香豆素)对犬冠状动脉狭窄时血小板聚集的抑制作用。
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Coffee extracts inhibit platelet aggregation in vivo and in vitro.咖啡提取物在体内和体外均能抑制血小板聚集。
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[Quantitative method of measuring platelet ATP released in vitro in the presence of various aggregating agents].[在各种聚集剂存在下体外测量血小板释放ATP的定量方法]
Pathol Biol (Paris). 1984 Sep;32(7):772-8.

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