STRUCTURE-ACTIVITY-RELATIONSHIPS OF ANALOGS OF HIGHLY POTENT OPIOID PEPTIDE BIPHALIN

被引:0
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作者
MISICKA, A
LIPKOWSKI, AW
HORVATH, R
DAVIS, P
PORRECA, F
YAMAMURA, HI
HRUBY, VJ
机构
[1] UNIV ARIZONA,DEPT PHARMACOL,TUCSON,AZ 85721
[2] WARSAW UNIV,DEPT CHEM,PL-02093 WARSAW,POLAND
[3] POLISH ACAD SCI,MED RES CTR,PL-00784 WARSAW,POLAND
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中图分类号
R5 [内科学];
学科分类号
1002 ; 100201 ;
摘要
For SAR study of biphalin [(Tyr-D-Ala-Gly-PheNH-)(2)] we have synthesized several analogues with modifications of amino acid residues in position 3 and 4. The introduction of halogenated phenylalanine residues in position 4 increases affinity to delta receptors. Introducing basic aromatic amino acid residues in position 4 resulted in decrease in affinity to mu receptors, but preserve affinity to delta receptors.
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页码:S131 / S132
页数:2
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