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首页> 外文期刊>Autonomic neuroscience: basic & clinical >Cardiovascular effects of centrally applied endothelin-1 1-31 and its relationship to endothelin-1 1-21 in rats.
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Cardiovascular effects of centrally applied endothelin-1 1-31 and its relationship to endothelin-1 1-21 in rats.

机译：大鼠中央应用内皮素1 1-31的心血管效应及其与内皮素1 1-21的关系。

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摘要

Endothelin-1(1-31) (ET-1(1-31)) is a novel member of the endothelin family, which comprises 31 amino acids and derived from the selective hydrolysis of big ET-1 by chymase. Although ET-1(1-31) has been reported to be involved in biological effects via direct or indirect (converting to ET-1(1-21)) mechanisms, the cardiovascular effects of central ET-1(1-31) are not fully identified. The present study was designed to comparatively investigate the cardiovascular effects of intracerebroventricular (icv) application of ET-1(1-31) or ET-1(1-21) in anesthetized rats. Injection (icv) of ET-1(1-31) (500 pmol) produced a biphasic blood pressure response: an initial increase (from 118+/-8 to 138+/-14 mmHg, P<0.05) followed by a sustained decrease in BP (from 118+/-8 to 58+/-9 mmHg, P<0.05), which was very similar to BP response to icv injection of big ET-1 (500 pmol) or ET-1(1-21) (25 pmol)(.) The cardiovascular effects of icv injection of ET-1(1-31) or ET-1(1-21) were completely antagonized by ET(A) receptor antagonist BQ123 but not ET(B) receptor antagonist BQ788. Furthermore, pretreatment with ET converting enzyme inhibitor phosphoramidon (10 nmol) abolished the cardiovascular effects evoked by icv injection of ET-1(1-31) or big ET-1. In conclusion, the current data showed that central ET-1(1-31) produced the similar cardiovascular effects as those of central ET-1(1-21), and suggesting that the central cardiovascular effects of ET-1(1-31) resulted from it converting to ET-1(1-21) and then activating ET(A) receptors.
机译：内皮素-1（1-31）（ET-1（1-31））是内皮素家族的一个新成员，它包含31个氨基酸，是由糜酶选择性水解大ET-1衍生而来的。尽管据报道ET-1（1-31）通过直接或间接（转换为ET-1（1-21））机制参与生物学效应，但中枢ET-1（1-31）的心血管效应是尚未完全确定。本研究旨在比较研究麻醉大鼠的ET-1（1-31）或ET-1（1-21）对脑室内（icv）的心血管作用。注射（icv）ET-1（1-31）（500 pmol）产生双相血压反应：最初升高（从118 +/- 8 mmHg增加到138 +/- 14 mmHg，P <0.05），然后持续升高血压下降（从118 +/- 8降至58 +/- 9 mmHg，P <0.05），与icv注射大ET-1（500 pmol）或ET-1（1-21）的BP反应非常相似）（25 pmol）（。）ET（A）受体拮抗剂BQ123完全拮抗icv注射ET-1（1-31）或ET-1（1-21）的心血管作用拮抗剂BQ788。此外，用ET转换酶抑制剂磷酰胺（10 nmol）进行的预处理消除了通过icv注射ET-1（1-31）或大ET-1引起的心血管效应。总之，目前的数据表明，中枢ET-1（1-31）产生的心血管效应与中枢ET-1（1-21）相似，这表明ET-1（1-31）的中枢心血管效应）是由于它转化为ET-1（1-21）然后激活了ET（A）受体。

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