Biological Active Analogues of the Opioid Peptide Biphalin: Mixed 伪/尾3-Peptides

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• 作者：Adriano Mollica ; Francesco Pinnen ; Roberto Costante ; Marcello Locatelli ; Azzurra Stefanucci ; Stefano Pieretti ; Peg Davis ; Josephine Lai ; David Rankin ; Frank Porreca ; Victor J. Hruby
• 刊名：Journal of Medicinal Chemistry
• 出版年：2013
• 出版时间：April 25, 2013
• 年：2013
• 卷：56
• 期：8
• 页码：3419-3423
• 全文大小：278K
• 年卷期：v.56,no.8(April 25, 2013)
• ISSN：1520-4804

文摘

Natural residues of the dimeric opioid peptide Biphalin were replaced by the corresponding homo-尾³ amino acids. The derivative 1 containing h尾³ Phe in place of Phe showed good 渭- and 未-receptor affinities (K_i^未 = 0.72 nM; K_i^渭 = 1.1 nM) and antinociceptive activity in vivo together with an increased enzymatic stability in human plasma.