强效二聚体阿片肽双甲啡肽的片段及类似物的生物活性
Biological activity of fragments and analogues of the potent dimeric opioid peptide, biphalin.
作者信息
Lipkowski A W, Misicka A, Davis P, Stropova D, Janders J, Lachwa M, Porreca F, Yamamura H I, Hruby V J
机构信息
Department of Chemistry, University of Arizona, Tucson 85721, USA.
出版信息
Bioorg Med Chem Lett. 1999 Sep 20;9(18):2763-6. doi: 10.1016/s0960-894x(99)00464-3.
The synthesis and biological activity of two fragments of the very potent opioid peptide biphalin, showed that Tyr-D-Ala-Gly-Phe-NH-NH<-Phe is the minimal fragment necessary to express equal affinities and the same biological activity profile as the parent biphalin. The replacement of N'-Phe with other L- or D- lipophilic amino acids showed the possibility of modification of receptor efficacy of the analogues.
两种强效阿片样肽双丙氨肽片段的合成及生物活性表明，Tyr-D-Ala-Gly-Phe-NH-NH<-Phe是表达与母体双丙氨肽相同亲和力和相同生物活性谱所需的最小片段。用其他L-或D-亲脂性氨基酸取代N'-Phe显示了改变类似物受体效能的可能性。
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