Analysis for specific binding sites of endothelins

内皮素特异性结合位点分析

• 批准号: 03670107
• 负责人: NIWA Masami
• 金额: $ 1.28万
• 依托单位: Department of Pharmacology 2, Nagasaki University School of Medicine
• 依托单位国家: 日本
• 项目类别: Grant-in-Aid for General Scientific Research (C)
• 财政年份: 1991
• 资助国家: 日本
• 起止时间: 1991 至 1992
• 项目状态: 已结题
• 来源: https://kaken.nii.ac.jp/grant/KAKENHI-PROJECT-03670107/
• 关键词: endothelin receptors; receptor autoradiography; chemical cross-linking; rat brain; porcine spinal cord; human spinal cord; 定量的受容体オ-トラジオグラフ法; 受容体活性部位; エンドセリン

Specific binding sites for ^<125>I-endothelin-1 (^<125>I-ET-1) in the spinal cord were investigated using quantitative receptor autoradiographic and chemical cross-linking methods. The binding sites were highly concentrated in porcine and human spinal cord areas corresponding anatomically to the dorsal horn (Rexed's laminae I-III), an area around the central canal (lamina X) and the principal part of the intermediolateral nucleus (IMLp). The localization of the binding sites differed from those of ^<125>I-omega-conotoxin GVIA (^<125>I-CgTx) and ^<125>I-Bolton-Hunter substance P (^<125>I-BH-SP), with the exception that the IMLp shared ^<125>I-ET-1 with ^<125>I-CgTx and ^<125>I-BH-SP binding sites. Specific ^<125>I-ET-1 binding sites in the areas examined were characteristically single and of high affinity. There were no differences between the potencies of unlabeled ET family peptides, ET-1, ET-2, ET-3 and sarafotoxin S6b at inhibiting ^<125>I-ET-1 binding to the areas. Chemical cross-linking studies showed that ^<125>I-ET-1 AND ^<125>I-ET-3 mainly bound to a protein with molecular mass of 43 kDa in the porcine and human thoracic spinal cord membranes. The present finding shows the neuronal significance of this newly discovered peptide in the spinal cord.

用<125><125>定量受体放射自显影和化学交联方法研究了脊髓中^I-内皮素-1（^ I-ET-1）的特异性结合位点。结合位点高度集中在猪和人的脊髓区域对应的背角解剖（Rexed的板I-III），中央管周围的区域（板X）和中间外侧核（IMLp）的主要部分。结合位点的定位不同于^<125>I-omega-芋螺毒素GVIA（^<125>I-CgTx）和^<125>I-Bolton-Hunter物质P（^<125>I-BH-SP），除了IMLp<125>与^<125>I-CgTx和^<125>I-BH-SP共享^ I-ET-1结合位点。在<125>所检查的区域中的特异性^ I-ET-1结合位点具有特征性的单一和高亲和力。未标记的ET家族肽、ET-1、ET-2、ET-3和sarafotoxin S6 b在抑制^<125>I-ET-1与该区域结合方面的效力没有差异。化学交联研究表明，^<125>I-ET-1和^<125>I-ET-3主要与猪和人胸脊髓膜中分子量为43 kDa的蛋白质结合。目前的发现显示了这种新发现的肽在脊髓中的神经元意义。

项目成果

Masami Niwa: "Specific ^<125>Iーendothelin binding sites in the central nervous system" Clinical and Experimental HypertensionーTheory and Practice. A13. 799-806 (1991)

Masami Niwa：“中枢神经系统中的特定^ 125 I-内皮素结合位点”临床和实验高血压理论与实践A13（1991）。

Masami Niwa: "Specific ^<125>I-endothelin-1 binding sites in the central nervous system" Clinical and Experimental Hypertension. A13. 879-906 (1991)

Masami Niwa：“中枢神经系统中特定的^<125>I-内皮素-1结合位点”临床和实验性高血压。

Kohtaro Taniyama: "Involvement of cholinergic neuron in intestinal contraction by vasoactive intestinal contractor" European journal of Pharmacology. (1993)

Kohtaro Taniyama：“血管活性肠道承包商胆碱能神经元参与肠道收缩”欧洲药理学杂志。

Kimihiro Yamashita: "Increased production of endothelins in the hippocampus of stroke-prone spontaneous hypertensive rats..." Cellular and Molecular Neurobiology. 13. 15-23 (1993)

Kimihiro Yamashita：“易发生中风的自发性高血压大鼠海马内皮素的产生增加......”细胞和分子神经生物学。

Kimihiro Yamashita: "Increased production of endothelins in the hippocampus of stroke-prone" Cellular and Molecular Neurobiology. 13. 15-23 (1993)

Kimihiro Yamashita：“易发生中风的海马体内内皮素的产生增加”细胞和分子神经生物学。