Antithrombotic and thrombolytic efficacy of YM-254890, a Gq/11 inhibitor, in a rat model of arterial thrombosis

被引：35

作者：

Kawasaki, T

Taniguchi, M

Moritani, Y

Hayashi, K

Saito, T

Takasaki, J

Nagai, K

Inagaki, O

Shikama, H

机构：

[1] Yamanouchi Pharmaceut Co Ltd, Pharmacol Labs, Cardiovasc Dis Res, Inst Drug Discovery Res, Tsukuba, Ibaraki 3058585, Japan

[2] Yamanouchi Pharmaceut Co Ltd, Inst Drug Discovery Res, Chem Labs, Tsukuba, Ibaraki 3058585, Japan

[3] Yamanouchi Pharmaceut Co Ltd, Inst Drug Discovery Res, Mol Med Labs, Tsukuba, Ibaraki 3058585, Japan

[4] Yamanouchi Pharmaceut Co Ltd, Inst Drug Discovery Res, Microbiol Labs, Tokyo, Japan

来源：

THROMBOSIS AND HAEMOSTASIS | 2003年 / 90卷 / 03期

关键词：

YM-254890; a G(q/11) inhibitor; thrombosis; thrombolysis; rat;

D O I：

10.1160/TH03-02-0115

中图分类号：

R5 [内科学];

学科分类号：

1002 ; 100201 ;

摘要：

We examined the antithrombotic and thrombolytic effects of the G(q/11) inhibitor YM-254890 in an electrically-induced carotid artery thrombosis model in rats. YM-254890 dose-dependently inhibited ex vivo ADP-induced platelet aggregation after i.v. bolus injection. In the thrombosis study, YM-254890 dose-dependently prolonged time to occlusion at doses of 3 and 10 mug/kg i.v. and decreased occlusion rate at 10 mug/kg i.v. In the thrombolysis study, YM-254890 at 30 mug/kg i.v. shortened the time to reperfusion and prevented reocclusion after thrombolysis with a modified tissue-type plasminogen activator. YM-254890, at 10 mug/kg and more, significantly improved carotid patency status after thrombolysis. However, at 30 mug/kg and more,YM-254890 decreased systemic blood pressure. These results suggest that YM-254890 may be effective for treating G(q)-mediated diseases, and that YM-254890 is a useful tool for investigating the biological roles of G(q/11).

引用

页码：406 / 413

页数：8

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