Mutulis F K, Mutule I E, Maurops G Kh, Sekatsis I P, Grigor'eva V D
Bioorg Khim. 1985 Sep;11(9):1276-8.
[Adpoc-Glu(N3)6, (Met-N3)11] substance P-(6-11)-peptide was reacted with diamines H2N(CH2) nNH2 (n = 3-10, 12) to give cyclopeptides. Subsequent careful cleavage of the Adpoc group leads to the formation of compounds of type cyclo-[H-Glu-Phe-Phe-Gly-Leu-Met-NH-(CH2) n-NH-] X HCl. The substances produce a specific two-phase myotropic effect in experiments on isolated guinea pig ileum. The compounds where n is 3, 7, 12 exhibit also a hypotensive activity when assayed on anaesthetized rats.
将[Adpoc-Glu(N3)6, (Met-N3)11]P物质-(6 - 11)-肽与二胺H2N(CH2)nNH2(n = 3 - 10, 12)反应,得到环肽。随后小心裂解Adpoc基团,形成环-[H-Glu-Phe-Phe-Gly-Leu-Met-NH-(CH2)n-NH-]型化合物盐酸盐。在豚鼠离体回肠实验中,这些物质产生特定的双相肌otropic效应。当在麻醉大鼠上进行测定时,n为3、7、12的化合物还表现出降压活性。