| 取代P物质类似物的合成及生物活性 |
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| 引用本文： | 陆一安,朱应麒,檀东平,邹冈.取代P物质类似物的合成及生物活性[J].中国生物化学与分子生物学报,1986,2(5):23-28. |
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| 作者姓名： | 陆一安 朱应麒 檀东平 邹冈 |
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| 作者单位： | 中国科学院上海药物研究所，中国科学院上海药物研究所，中国科学院上海药物研究所，中国科学院上海药物研究所 研究生 |
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| 摘 要： | 使用固相法合成含有不同D-型氨基酸取代的八个P物质类似物。纯化采用凝胶过滤,硅胶柱层或反相高效液相色谱。化合物的SP样作用及拮抗SP样作用在离体豚鼠迴肠纵行肌上进行了试验。所有化合物都显示了不同程度的拮抗作用。其中化合物A-58D-Arg~1,D-Phe~5,D-Trp~(7,9),Leu~(11)]SP拮抗活性最高。它拮抗SP样作用的剂量比率(EC_(50)之比)在10~(-6)M时为24,在3×10~(-6)M时为52.2。
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| 关 键 词： | P物质 激动剂 拮抗剂 |
| 收稿时间： | 1986-10-20 |
SYNTHESIS AND BIOLOGICAL ACTIVITIES OF SUBSTANCE P ANTAGONISTS |
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| Lu,Yi-An Zhe,Ying-QiTan,Dong-Ping Zou,Gang.SYNTHESIS AND BIOLOGICAL ACTIVITIES OF SUBSTANCE P ANTAGONISTS[J].Chinese Journal of Biochemistry and Molecular Biology,1986,2(5):23-28. |
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| Authors: | Lu Yi-An Zhe Ying-QiTan Dong-Ping Zou Gang |
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| Institution: | (Shanghai Institute of Materia Medica,Academia Sinica |
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| Abstract: | Eight analogs of substance P (SP) containing various D-Amino Acid modifications were synthesised by the solid phase method,purified by gel filtration,silica chromatography combined with reversed phase HPLC.The agonist and antagonist activities of SP were assayed on the isolated guinea pig ileum.All analogs showed antagonistic activity with different degree.D-Arg1,D-Phe5,D-Trp7.9,Leu11]SP (A-58) is the most potent atagonist of the analogs with a dose ratio of 24.0 at 10-6M and 52.5 at 3×10-6M respectively. |
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| Keywords: | Substance P Agonists Antagonists |
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