| 强啡肽A－（1－13）类似物的合成及生物活性 |
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| 引用本文： | 陈亚利,钟明鼐,聂忠贞,董玉轩. 强啡肽A－（1－13）类似物的合成及生物活性[J]. 药学学报, 1995, 0(12) |
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| 作者姓名： | 陈亚利 钟明鼐 聂忠贞 董玉轩 |
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| 作者单位： | 南京军区总医院临床分子生物学实验室，中国人民解放军药物化学研究所 |
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| 摘 要： | 用固相多肽合成方法，合成了强啡肽Ａ－（１－１３）（Ｉ）及其类似物［Ａｌａ８，Ｄ－Ｐｒｏ１０］－ＤＹＮＡ－（１－１３）－ＮＨ２（ＩＩ）和［Ｄ－Ａｌａ２，Ａｌａ８，Ｄ－Ｐｒｏ１０］－ＤＹＮＡ－（１－１３）－ＮＨ２（ＩＩＩ），并对其进行了镇痛活性试验和ＭＶＤ及ＲＶＤ试验。结果表明，合成产物均有镇痛活性，其中类似物ＩＩＩ的镇痛活性是１的３．６倍，ＲＶＤ试验活性比１强１３５倍，比已知的ｋ－受体强激动剂Ｕ５００４８８强１１倍。
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| 关 键 词： | 强啡肽A－（1－13），阿片活性，固相多肽合成 |
SYNTHESISANDBIOLOICAL ACTIVITY OF DYNORPHINA- (1- 13)A NA LOGS |
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| YLChen,MNZhong,ZZNieandYXDong. SYNTHESISANDBIOLOICAL ACTIVITY OF DYNORPHINA- (1- 13)A NA LOGS[J]. Acta pharmaceutica Sinica, 1995, 0(12) |
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| Authors: | YLChen MNZhong ZZNieandYXDong |
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| Abstract: | Dynorphin A-(1-13)(I) and its two analogs were synthesized by solid- phase method. Full y-protected pe pt ides were cl eaved from the resi n w ithHF.The three prod ucts were purified and their analgesis activity (antiwrithing response in mouse) and receptor affinity in mouse vas deferens (MVD)and rabbit vas deferens(RVD)were measured. The biological and pharmacologi-cal results showed that the repldcefment of Gla2,Ile8 and Pro10by D- Ala2, Ala8and D-Pro10caused an increase in analgesic activity , receptor affin ity and selectivity. In analgesia and RVD assay, its activity is 2. 6 times and 1 35 times respectively higher than dynorphin A-(1-13). The structure-activity relationshipe were briefly discussed. |
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| Keywords: | Dynorphin A-(1-13) Peptides synthesis Opioid activity |
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