Synthesis and Biological Activity of [MeTyr^1,MeArg^7,D-Leu^8]-Dynorphin A(1-9)-NHEt and [D-Cys^2-Cys^5,MeArg^7,D-Leu^8]-Dynorphin A(1-9)-NH_2

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The opioid activities of [MeTyr^1]-Dyn(1-7)-NH_2,[MeTyr^1,D-Leu^8]-Dyn(1-8)-NH_2,[MeTyr^1,D-Leu^8]-Dyn(1-9)-NH_2,[MeTyr^1,D-Leu^8]-Dyn(1-10)-NH_2,[MeTyr^1,D-Leu^8]Dyn(1-11)-NH_2,and [MeTyr^1,D-Leu^<8,12>]-Dyn(1-13)-NH_2 were examined in the bioassays (guinea pig ileum, mouse vas deferens and rabbit vas deferens). Because [MeTyr^1,D-Leu^8]-Dyn(1-9)-NH_2 showed the most potent opioid activity of the peptides tested, the biological activities of two kinds of Dyn(1-9) analogues, [MeTyr^1,MeArg^7,D-Leu^8]-Dyn(1-9)-NHEt and [D-Cys^2-Cys^5,MeArg^7,D-Leu^8]-Dyn(1-9)-NH_2 were determined and compared with those of [MeTyr^1,MeArg^7,D-Leu^8]-Dyn(1-8)-NHEt and [D-Cys^2-Cys^5,MeArg^7,D-Leu^8]-Dyn(1-8)-NHEt in the three bioassays, in the receptor binding assays, and in the mouse tail pinch test after subcutaneous administration. The results suggest that the extension of the C-terminal in the peptide chain of [MeArg^7,D-Leu^8]-Dyn(1-8)-NH_2 analogues by Arg is ineffective for increasing the κ-opioid activities, κ-receptor selectivity and/or analgesic effects of the peptides.
社団法人日本薬学会の論文
1990-08-25