The effect of the ETA receptor antagonist FR 139317 on 125I-ET-1 binding to the atherosclerotic human coronary artery.

机译：ETA受体拮抗剂FR 139317对125I -ET-1与动脉粥样硬化人冠状动脉结合的影响。

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1. The distribution of [125I]-endothelin (ET-1) binding sites on atherosclerotic human epicardial coronary arteries has been studied by in vitro receptor autoradiography. 2. [125I]-ET-1 binding was to the tunica media and regions of neovascularization. 3. Competition studies were carried out in the presence of ET-1 and the ETA receptor antagonist, FR 139317. The IC50 values for ET-1 at the tunica media and regions of neovascularization were similar (mean +/- s.e.mean of n = 4 patients, 2.5 +/- 0.9 nM and 2.9 +/- 0.9 nM, respectively) whereas IC50 values for FR 139317 at regions of neovascularization (607 +/- 34 nM) were significantly higher than those of the tunica media (12.6 +/- 2.4 nM) (P < 0.0001). 4. These results indicate that ETA receptors are present on the tunica media of the diseased human coronary artery whereas a different ET receptor subtype exists at regions of neovascularization.

机译：1.已通过体外受体放射自显影研究了[125I]-内皮素（ET-1）结合位点在动脉粥样硬化人心外膜冠状动脉上的分布。 2. [125I] -ET-1与中膜和新生血管形成区域结合。 3.在存在ET-1和ETA受体拮抗剂FR 139317的情况下进行了竞争研究。在中膜和新生血管形成区域，ET-1的IC50值相似（平均值+/- s n = 4例患者，分别为2.5 +/- 0.9 nM和2.9 +/- 0.9 nM），而新血管形成区域的FR 139317的IC50值（607 +/- 34 nM）显着高于中膜（12.6 + / -2.4 nM）（P <0.0001）。 4.这些结果表明，在患病的人冠状动脉的中膜介质上存在ETA受体，而在新血管形成区域存在不同的ET受体亚型。

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期刊名称 British Journal of Pharmacology and Chemotherapy
作者
M. R. Dashwood; S. P. Allen; T. N. Luu; J. R. Muddle;
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年(卷),期 1994(112),2
年度 1994
页码 386–389
总页数 4
原文格式 PDF
正文语种
中图分类药学;
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7. The effect of the ETA receptor antagonist, FR 139317, on [125I]-ET-1 binding to the atherosclerotic human coronary artery. [O] . Dashwood, M. R., Allen, S. P., Luu, T. N., 1994

机译：ETA受体拮抗剂FR 139317对[125I] -ET-1与动脉粥样硬化人冠状动脉结合的影响。
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The effect of the ETA receptor antagonist FR 139317 on 125I-ET-1 binding to the atherosclerotic human coronary artery.

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