| 新型内皮素受体六肽拮抗剂的设计合成及其生物活性 |
| |
| 引用本文： | 梁远军,于文胜,刘克良,赵玉芬,费改顺,汪海. 新型内皮素受体六肽拮抗剂的设计合成及其生物活性[J]. 中国药物化学杂志, 2001, 11(2): 63-66 |
| |
| 作者姓名： | 梁远军 于文胜 刘克良 赵玉芬 费改顺 汪海 |
| |
| 作者单位： | 1. 军事医学科学院毒物药物研究所，
2. 清华大学化学系, |
| |
| 摘 要： | 以内皮素-1(endothelin-1,ET-1)羟基末端六肽(His-Leu-Asp-Ile-Ile-Trp)为模板,应用D型芳香性非天然氨基酸替代六肽结构中His残基进行结构设计,利用固相肽合成技术合成新型ET受体肽类拮抗剂,得到12个新六肽化合物,对所得化合物进行损坏抗ET-1收缩大鼠胸总动脉的活性研究,其中C-1,C-3,C-5,C-7,C-8,C-11等6个化合物在10^-9mol/L浓度水平表现出明显的拮抗活性.
|
| 关 键 词： | 内皮素A型受体 拮抗剂 非天然氨基酸 肽固相合成 BQ－485 主动脉平滑肌膜 |
| 文章编号： | 1005-0108(2001)02-0001-04 |
Syntheses andBioactivities of Endothelin Receptor Antagonist Hexapeptides |
| |
| LIANG Yuan-jun,Yu Wen-Sheng,LIU Ke-liang,ZHAO Yu-fen,FEI Gai-shun,WANG Hai. Syntheses andBioactivities of Endothelin Receptor Antagonist Hexapeptides[J]. Chinese Journal of Medicinal Chemistry, 2001, 11(2): 63-66 |
| |
| Authors: | LIANG Yuan-jun Yu Wen-Sheng LIU Ke-liang ZHAO Yu-fen FEI Gai-shun WANG Hai |
| |
| Affiliation: | LIANG Yuan jun 1,YU Wen sheng 2,LIU Ke liang 1,ZHAO Yu fen 2,FEI Gai shun 1,WANG Hai 1 |
| |
| Abstract: | Based on the structure of hexapeptide(His Leu Asp Ile Ile Trp,16 21) of the C terminal fragment of endothlin 1(ET 1),a series of novel hexapeptide analogues was synthesized using the solid phase peptide synthesis(SPPS) technology by the replacement of the residue His with D type of aromatic unusual amino acids.The introduction of D Phe derivatives in these peptidic ET antagonists resulted in potent ET antagonistic activity.The pectoral artery of the rat mainly contained ET A receptors and few ET B receptors.Six compounds of the twelve hexapeptides against ET 1 showed significant activity under the concentration on 10 -9 mol/L. |
| |
| Keywords: | ET A receptor antagonist unusual amino acid BQ 485 solid phase peptide synthesis aortic smooth muscle membrane |
| 本文献已被 CNKI 维普 万方数据 等数据库收录！ |
|
