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| 固相法合成心肌兴奋肽及其类似物 | |
| 引用本文： | 刘文,王德心,鲁桂琛,韩济生,柴松海,范镭. 固相法合成心肌兴奋肽及其类似物[J]. 药学学报, 1988, 0(4) |
| 作者姓名： | 刘文 王德心 鲁桂琛 韩济生 柴松海 范镭 |
| 作者单位： | 中国医学科学院药物研究所，中国医学科学院药物研究所，中国医学科学院药物研究所，北京医科大学生理教研室，北京医科大学生理教研室，北京医科大学生理教研室 北京，北京，北京 |
| 摘 要： | 用Boc-和Tos-基团分别保护氨基和侧链胍基,以1%交联度聚苯乙烯二苯甲氨基树脂为载体,用DCC固相法合成肽,HF断裂肽树脂键和去除侧链保护基团,粗产物经高效液相层析纯化,合成了心肌兴奋肽Phe-Met-Arg-Phe-NH_2及其类似物Phe-Pro-Arg-Phe-NH_2,并观察了此二种肽对大鼠血压和心率的影响。 |
| 关 键 词： | 心肌兴奋肽 固相法合成多肽 氟化氢裂解 阿片样物质 |
SOLID PHASE PEPTIDE SYNTHESIS OF CARDIOEXCITATORY PEPTIDE AND ITS ANALOG |
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| W Liu,DX Wang,GS Lu,JS Han,SH Chai and L Fan. SOLID PHASE PEPTIDE SYNTHESIS OF CARDIOEXCITATORY PEPTIDE AND ITS ANALOG[J]. Acta pharmaceutica Sinica, 1988, 0(4) | |
| Authors: | W Liu DX Wang GS Lu JS Han SH Chai L Fan |
| Affiliation: | W Liu,DX Wang,GS Lu,JS Han~*,SH Chai and L Fan~* |
| Abstract: | Cordioexeitatory peptide (Phe-Met-Arg-Phe-NH_2, FMRF-NH_2) and its analog (Phe-Pro-Arg-Phe-NH_2, FPRF-NH2) were synthesized by a solid phase procedure on a benzhydrylamine resin. Boo-amino acids and Boc-Arg(Tos) were used. The course of the synthesis was monitored by quantitative ninhydrin analysis. Following cleavage by the 90% HF method the peptides were purified by reverse phase HPLC. The overall yields of homogeneous isolated peptides from the first amino acid were 36% and 37%, respectively. It was found that the cleavage of Tos from Arg is related to temperature. The efficacy of FMRF-NH_2 and FPRF-NH_2 as antagonists to the opioid peptide D-Ala~2, Leu~5 enkephalin was tested, using changes in mean arterial blood pressure and heart rate as indices. Results indicate that the former is more potent than the latter. |
| Keywords: | Cardioexcitatory peptide Solid phase peptide synthesis HF cleavage Opioid |
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