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

被引:0
|
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
关键词
D O I
暂无
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.
引用
收藏
页码:S131 / S132
页数:2
相关论文
共 50 条
  • [41] STRUCTURE-ACTIVITY-RELATIONSHIPS AMONG DAUNORUBICIN AND ADRIAMYCIN ANALOGS
    HENRY, DW
    ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 1977, 174 (SEP): : 67 - 67
  • [42] STRUCTURE-ACTIVITY-RELATIONSHIPS OF RGH-6643 ANALOGS
    ZOLYOMI, G
    BIRKASFAIGL, E
    HASKO, T
    KOLTAI, E
    ANDRASI, F
    BERZSENYI, P
    EZER, E
    NAKAMURA, M
    EUROPEAN JOURNAL OF PHARMACOLOGY, 1990, 183 (02) : 599 - 599
  • [43] Crystal structure of biphalin sulfate: A multireceptor opioid peptide
    Flippen-Anderson, JL
    Deschamps, JR
    George, C
    Hruby, VJ
    Misicka, A
    Lipkowski, AW
    JOURNAL OF PEPTIDE RESEARCH, 2002, 59 (03): : 123 - 133
  • [44] NEW POTENT PROLYL ENDOPEPTIDASE INHIBITORS - SYNTHESIS AND STRUCTURE-ACTIVITY-RELATIONSHIPS OF INDAN AND TETRALIN DERIVATIVES AND THEIR ANALOGS
    TANAKA, Y
    NIWA, S
    NISHIOKA, H
    YAMANAKA, T
    TORIZUKA, M
    YOSHINAGA, K
    KOBAYASHI, N
    IKEDA, Y
    ARAI, H
    JOURNAL OF MEDICINAL CHEMISTRY, 1994, 37 (13) : 2071 - 2078
  • [45] SYNTHESES, RESOLUTION AND STRUCTURE-ACTIVITY-RELATIONSHIPS OF POTENT ACETYLCHOLINESTERASE INHIBITORS - 8-CARBA-PHYSOSTIGMINE ANALOGS
    CHEN, YL
    NIELSEN, J
    HEDBERG, K
    DUNAISKIS, A
    JONES, S
    RUSSO, L
    JOHNSON, J
    IVES, J
    LISTON, D
    ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 1991, 202 : 143 - MEDI
  • [46] PEPTIDE QUANTITATIVE STRUCTURE-ACTIVITY-RELATIONSHIPS, A MULTIVARIATE APPROACH
    HELLBERG, S
    SJOSTROM, M
    SKAGERBERG, B
    WOLD, S
    JOURNAL OF MEDICINAL CHEMISTRY, 1987, 30 (07) : 1126 - 1135
  • [47] Modifications of the 4,4′-residues and SAR studies of biphalin, a highly potent opioid receptor active peptide
    Li, GG
    Haq, W
    Xiang, L
    Lou, BS
    Hughes, R
    De Leon, IA
    Davis, P
    Gillespie, TJ
    Romanowski, M
    Zhu, XY
    Misicka, A
    Lipkowski, AW
    Porreca, F
    Davis, TP
    Yamamura, HI
    O'Brien, DF
    Hruby, VJ
    BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1998, 8 (05) : 555 - 560
  • [48] STRUCTURE-ACTIVITY-RELATIONSHIPS OF ILLUDINS - ANALOGS WITH IMPROVED THERAPEUTIC INDEX
    MCMORRIS, TC
    KELNER, MJ
    WANG, W
    ESTES, LA
    MONTOYA, MA
    TAETLE, R
    JOURNAL OF ORGANIC CHEMISTRY, 1992, 57 (25): : 6876 - 6883
  • [49] SYNTHESIS AND STRUCTURE-ACTIVITY-RELATIONSHIPS (SAR) OF NOVEL FENTANYL ANALOGS
    HUANG, BS
    TERRELL, R
    KUDZMA, L
    SEVERNAK, S
    DEUTSCHE, KH
    ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 1987, 193 : 28 - MEDI
  • [50] STRUCTURE-ACTIVITY-RELATIONSHIPS FOR TUMOR RADIOSENSITIZATION BY ANALOGS OF NICOTINAMIDE AND BENZAMIDE
    BROWN, JM
    LEMMON, MJ
    HORSMAN, MR
    LEE, WW
    INTERNATIONAL JOURNAL OF RADIATION BIOLOGY, 1991, 59 (03) : 739 - 748