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当前内皮素受体分类:是时候重新考虑了?

The current endothelin receptor classification: time for reconsideration?

作者信息

Bax W A, Saxena P R

机构信息

Department of Pharmacology, Cardiovascular Research Institute COEUR, Faculty of Medicine and Health Sciences, Eramus University Rotterdam, The Netherlands.

出版信息

Trends Pharmacol Sci. 1994 Oct;15(10):379-86. doi: 10.1016/0165-6147(94)90159-7.

DOI:10.1016/0165-6147(94)90159-7
PMID:7809954
Abstract

The possible involvement of endothelins in a variety of diseases has attracted the attention of many pharmacologists in search of a novel therapeutic approach. The rapid development of endothelin research has resulted in the molecular characterization and pharmacological recognition of ETA and ETB receptors, and in the development of compounds selective for these receptors. However, the characterization of receptors in various assays has shown that a number of effects are mediated by receptors that do not fit the present criteria for ETA or ETB receptors. In this article, Willem Bax and Pramod Saxena address endothelin receptors in general, and atypical receptors in particular.

摘要

内皮素可能参与多种疾病,这吸引了许多药理学家的关注,他们致力于寻找新的治疗方法。内皮素研究的迅速发展,促成了ETA和ETB受体的分子特性鉴定和药理学识别,以及针对这些受体的选择性化合物的开发。然而,各种实验中的受体特性鉴定表明,许多效应是由不符合目前ETA或ETB受体标准的受体介导的。在本文中,威廉·巴克斯和普拉莫德·萨克森纳探讨了一般意义上的内皮素受体,特别是非典型受体。

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1
The current endothelin receptor classification: time for reconsideration?当前内皮素受体分类:是时候重新考虑了?
Trends Pharmacol Sci. 1994 Oct;15(10):379-86. doi: 10.1016/0165-6147(94)90159-7.
2
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Use of the endothelin antagonists BQ-123 and PD 142893 to reveal three endothelin receptors mediating smooth muscle contraction and the release of EDRF.使用内皮素拮抗剂BQ - 123和PD 142893揭示三种介导平滑肌收缩和内皮舒张因子释放的内皮素受体。
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In vitro biological profile of a highly potent novel endothelin (ET) antagonist BQ-123 selective for the ETA receptor.一种对ETA受体具有选择性的高效新型内皮素(ET)拮抗剂BQ-123的体外生物学特性
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Endothelin-1 and the regulation of vascular tone.内皮素-1与血管张力的调节
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Reversal of established responses to endothelin-1 in vivo and in vitro by the endothelin receptor antagonists, BQ-123 and PD 145065.内皮素受体拮抗剂BQ - 123和PD 145065在体内和体外对已建立的内皮素 - 1反应的逆转作用。
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Hybrid peptides constructed from RES-701-1, an endothelin B receptor antagonist, and endothelin; binding selectivity for endothelin receptors and their pharmacological activity.由内皮素B受体拮抗剂RES-701-1和内皮素构建的杂合肽;对内皮素受体的结合选择性及其药理活性。
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ETA and ETB receptors mediate contraction to endothelin-1 in renal artery of aging SHR. Effects of FR139317 and bosentan.ETA和ETB受体介导衰老自发性高血压大鼠肾动脉对内皮素-1的收缩反应。FR139317和波生坦的作用。
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Biochem Biophys Res Commun. 1993 Oct 15;196(1):209-15. doi: 10.1006/bbrc.1993.2236.

引用本文的文献

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Agonist-dependent modulation of arterial endothelinA receptor function.激动剂依赖调节动脉内皮素 A 受体功能。
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Dual Roles for Endothelin-B Receptors in Modulating Adjuvant-Induced Inflammatory Hyperalgesia in Rats.内皮素-B受体在调节大鼠佐剂诱导的炎性痛觉过敏中的双重作用
Open Pain J. 2009;2:30-40. doi: 10.2174/1876386300902010030.
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[D-Val22]big ET-1[16-38] inhibits endothelin-converting enzyme activity: a promising concept in the prevention of cerebral vasospasm.
[D-缬氨酸22]大内皮素-1[16-38]抑制内皮素转化酶活性:预防脑血管痉挛的一个有前景的概念。
Neurosurg Rev. 2003 May;26(2):125-32. doi: 10.1007/s10143-002-0242-9. Epub 2002 Nov 19.
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Endothelin-1 inhibits TNF alpha-induced iNOS expression in 3T3-F442A adipocytes.内皮素-1抑制肿瘤坏死因子α诱导的3T3-F442A脂肪细胞中诱导型一氧化氮合酶的表达。
Br J Pharmacol. 2003 Jul;139(5):935-44. doi: 10.1038/sj.bjp.0705325.
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Endothelin-1 binding to endothelin receptors in the rat anterior pituitary gland: possible formation of an ETA-ETB receptor heterodimer.内皮素-1与大鼠垂体前叶中的内皮素受体结合:可能形成ETA-ETB受体异二聚体。
Cell Mol Neurobiol. 2002 Apr;22(2):207-26. doi: 10.1023/a:1019822107048.
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Evidence that ET-1, but not ET-3 and S6b, ET(A)-receptor mediated contractions in isolated rat mesenteric arteries are modulated by co-activation of ET(B) receptors.有证据表明,在离体大鼠肠系膜动脉中,ET-1(而非ET-3和S6b)通过ET(A)受体介导的收缩作用受ET(B)受体的共同激活调节。
Br J Pharmacol. 2001 Jul;133(6):927-35. doi: 10.1038/sj.bjp.0704135.
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Differential modulation of endothelin ligand-induced contraction in isolated tracheae from endothelin B (ET(B)) receptor knockout mice.内皮素B(ET(B))受体基因敲除小鼠离体气管中内皮素配体诱导收缩的差异调节
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