Synthesis, structure-activity relationship of nociceptin and its fragments  

作　　者：Shouliang Dong Tao Wang Qiang Chen Rui Wang 

机构地区：[1]Lanzhou Univ, Sch Life Sci, Dept Biochem & Mol Biol, Lanzhou 730000, Peoples R China

出　　处：《Chinese Science Bulletin》1999年第18期1655-1659,共5页

摘　　要：Nociceptin (NC) and its 4 fragments have been synthesized by solid phase peptide synthesis. Their hypotensive activity and mechanism, MVD assay and structure-activity relationship have been investigated. Results show that NC(1-13)NH2 is the smallest fragment that shares the same activity with NC. The truncation of C-terminal not only leads the decreaseNociceptin (NC) and its 4 fragments have been synthesized by solid phase peptide synthesis. Their hypotensive activity and mechanism, MVD assay and structure-activity relationship have been investigated. Results show that NC(1–13)NH2 is the smallest fragment that shares the same activity with NC. The truncation of C-terminal not only leads the decrease of receptor affinity but also the changes of receptor selectivity. The entire sequence may not be required for the full activity since NC(1–13)NH2 is as active as NC. Arg-Lys at the 12–13 position of C-terminal plays an important role in the activity of NC. The hypotensive activity of NC does not antagonize the hypertensive activity of renin-angiotensin system.

关 键 词：NOCICEPTIN solid phase PEPTIDE SYNTHESIS HYPOTENSIVE activity STRUCTURE-ACTIVITY relationship. 

分 类 号：R544.1[医药卫生—心血管疾病]