Design of mu selective opioid dipeptide antagonists

被引：23

作者：

Capasso, A

Amodeo, P

Balboni, G

Guerrini, R

Lazarus, LH

Temussi, PA

Salvadori, S

机构：

[1] UNIV NAPLES FEDERICO II,DIPARTIMENTO CHIM,I-80134 NAPLES,ITALY

[2] UNIV SALERNO,DIPARTIMENTO SCI FARMACEUT,I-84084 SALERNO,ITALY

[3] CNR,ICMIB,I-80072 ARCO,NAPLES,ITALY

[4] UNIV FERRARA,DIPARTIMENTO SCI FARMACEUT,I-44100 FERRARA,ITALY

[5] NIEHS,LMNI,RES TRIANGLE PK,NC 27709

来源：

FEBS LETTERS | 1997年 / 417卷 / 01期

关键词：

antagonism; peptide; opioid selectivity; conformation;

D O I：

10.1016/S0014-5793(97)01271-4

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

We have recently designed potent delta selective opioid antagonist dipeptides on the basis of a simple conformational analysis. Following a similar procedure me found a mu selective dipeptide antagonist, 2,6-dimethyl-Tyr-D-Phe-NH2. Although its selectivity is not as high as those of the quoted delta selective dipeptides it has good in vitro activity and looks very promising for further development since the 2,6-dimethyl-Tyr-D-Phe message, like the delta selective 2,6-dimethyl-Tyr-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid counterpart, seems able to impart antagonism to longer peptides. (C) 1997 Federation of European Biochemical Societies.

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收藏

页码：141 / 144

页数：4

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