Biological activity of fragments and analogues of the potent dimeric opioid peptide, biphalin

被引:41
作者
Lipkowski, AW [1 ]
Misicka, A
Davis, P
Stropova, D
Janders, J
Lachwa, M
Porreca, F
Yamamura, HI
Hruby, VJ
机构
[1] Univ Arizona, Dept Chem, Tucson, AZ 85721 USA
[2] Univ Arizona, Dept Pharmacol, Tucson, AZ 85721 USA
[3] Polish Acad Sci, Med Res Ctr, PL-02106 Warsaw, Poland
[4] Univ Warsaw, Dept Chem, PL-02093 Warsaw, Poland
关键词
D O I
10.1016/S0960-894X(99)00464-3
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
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. (C) 1999 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:2763 / 2766
页数:4
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