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血小板激活因子拮抗剂CV-3988的活性表征

Characterization of the activity of a platelet activating factor antagonist, CV-3988.

作者信息

Hayashi M, Kimura J, Oh-Ishi S, Tsushima S, Nomura H

机构信息

Department of Pharmacology, School of Pharmaceutical Sciences, Kitasato University, Tokyo, Japan.

出版信息

Jpn J Pharmacol. 1987 Jun;44(2):127-34. doi: 10.1254/jjp.44.127.

DOI:10.1254/jjp.44.127
PMID:2888915
Abstract

CV-3988 inhibited the vascular permeability increase induced by C16-PAF and C18-PAF in rat skin in a dose-dependent manner. The inhibition was shown to be specific and competitive with PAF on its receptor by the following observations: parallel shift of the dose-response curve; crossing of double reciprocal plots on the intersection of the ordinate; and no inhibition on other autacoids such as bradykinin, histamine, 5-hydroxytryptamine and LTC4. PAF-induced blood pressure fall in rats was also suppressed by pretreatment with CV-3988 selectively.

摘要

CV - 3988以剂量依赖性方式抑制C16 - PAF和C18 - PAF诱导的大鼠皮肤血管通透性增加。通过以下观察结果表明这种抑制是特异性的,并且在其受体上与PAF具有竞争性:剂量 - 反应曲线的平行移动;双倒数图在纵坐标交点处交叉;对其他自分泌物质如缓激肽、组胺、5 - 羟色胺和LTC4没有抑制作用。用CV - 3988预处理也选择性地抑制了PAF诱导的大鼠血压下降。

相似文献

1
Characterization of the activity of a platelet activating factor antagonist, CV-3988.血小板激活因子拮抗剂CV-3988的活性表征
Jpn J Pharmacol. 1987 Jun;44(2):127-34. doi: 10.1254/jjp.44.127.
2
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trans-2,5-Bis-(3,4,5-trimethoxyphenyl)tetrahydrofuran. An orally active specific and competitive receptor antagonist of platelet activating factor.反式-2,5-双-(3,4,5-三甲氧基苯基)四氢呋喃。一种口服活性的血小板活化因子特异性竞争性受体拮抗剂。
J Biol Chem. 1985 Dec 15;260(29):15639-45.
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