采用反相高效液相色谱(RP-HPLC)与质谱(MS)联用技术对固相法化学合成七肽(H2N-PFNSLAI-COOH,M r 760.9)时出现的消旋产物进行了分析。根据弱疏水性合成七肽粗品特性,提出了充分利用吸附和分配双重保留机制的“早期吸附”概念,以此优化...采用反相高效液相色谱(RP-HPLC)与质谱(MS)联用技术对固相法化学合成七肽(H2N-PFNSLAI-COOH,M r 760.9)时出现的消旋产物进行了分析。根据弱疏水性合成七肽粗品特性,提出了充分利用吸附和分配双重保留机制的“早期吸附”概念,以此优化色谱条件得到4个峰形良好的色谱峰;质谱分析表明:4谱峰具有相同的m/z761.5[M+H]+值,对每一消旋产物进行在线多肽测序,并利用串联质谱(MSn)谱图叠加的方法,得到b轴和y轴两套片段信息,成功确定了合成七肽的4个消旋产物。展开更多
Endomorphin 1(EM 1) and its six analogs which were designed by rationally replacing the 2 /3 amino acid(Aa) of EM 1 were synthesized by using liquid phase peptides synthesis method to study their action of opiate rece...Endomorphin 1(EM 1) and its six analogs which were designed by rationally replacing the 2 /3 amino acid(Aa) of EM 1 were synthesized by using liquid phase peptides synthesis method to study their action of opiate receptor binding(AORB). The order of their affinity intensity for μ opiate receptor(MOR) was EM 1 >[ D Ala 2]EM 1 >[ D Pro 2]EM 1 > EM 1 >[ L Tyr 3]EM >[ L Pro 3]EM >EM The sequence of their selectivity for MOR is EM 1 >[ D Pro 2]EM 1 =[ L Tyr 3]EM >[ D Ala 2]EM 1 =[ L Pro 3]EM >EM The results showed that, comparatively speaking, the 2 Aa was more closely related to the selectivity of EM 1 while the 3 Aa to their affinity, though the different replacement changed the AORB of EM 1 dissimilarly.展开更多
文摘采用反相高效液相色谱(RP-HPLC)与质谱(MS)联用技术对固相法化学合成七肽(H2N-PFNSLAI-COOH,M r 760.9)时出现的消旋产物进行了分析。根据弱疏水性合成七肽粗品特性,提出了充分利用吸附和分配双重保留机制的“早期吸附”概念,以此优化色谱条件得到4个峰形良好的色谱峰;质谱分析表明:4谱峰具有相同的m/z761.5[M+H]+值,对每一消旋产物进行在线多肽测序,并利用串联质谱(MSn)谱图叠加的方法,得到b轴和y轴两套片段信息,成功确定了合成七肽的4个消旋产物。
文摘Endomorphin 1(EM 1) and its six analogs which were designed by rationally replacing the 2 /3 amino acid(Aa) of EM 1 were synthesized by using liquid phase peptides synthesis method to study their action of opiate receptor binding(AORB). The order of their affinity intensity for μ opiate receptor(MOR) was EM 1 >[ D Ala 2]EM 1 >[ D Pro 2]EM 1 > EM 1 >[ L Tyr 3]EM >[ L Pro 3]EM >EM The sequence of their selectivity for MOR is EM 1 >[ D Pro 2]EM 1 =[ L Tyr 3]EM >[ D Ala 2]EM 1 =[ L Pro 3]EM >EM The results showed that, comparatively speaking, the 2 Aa was more closely related to the selectivity of EM 1 while the 3 Aa to their affinity, though the different replacement changed the AORB of EM 1 dissimilarly.
