Peripherally acting enkephalin analogs. 2. Polar tri-and tetrapeptides

…, LA Lowe, G Mills, PY Sang, DSA Simpkin…

文献索引：Hardy, George W.; Lowe, Lawrence A.; Mills, Gail; Sang, Pang Yih; Simpkin, Dean S. A.; et al. Journal of Medicinal Chemistry, 1989 , vol. 32, # 5 p. 1108 - 1118

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被引用次数: 22

摘要

The design, synthesis, and biological activity of a series of DArgZ-enkephalin-derived tetrapeptide amides and tripeptide aralkylamides are reported. These polar analogues were designed to be excluded from the central nervous system with their action thus limited to peripheral opioid receptors. The effects of the nature of the aromatic ring, aryl ring substitution, and aralkylamine chain length on activity were investigated; in a number of ...