Literature DB >> 11212102

Enkephalin analogues with 2',6'-dimethylphenylalanine replacing phenylalanine in position 4.

Y Sasaki1, M Hirabuki, A Ambo, H Ouchi, Y Yamamoto.   

Abstract

Four Leu-enkephalin (Enk) analogues containing 2',6'-dimethyphenylalanine (Dmp) in position 4 were prepared and tested for their receptor binding and biological activities. Among the analogues prepared, [2', 6'-dimethyltyrosine, D-Dmp4]Enk was found to be an antagonist toward mu and delta opioid receptors with pA2 values of 6.90 and 5.57, respectively.

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Year:  2001        PMID: 11212102     DOI: 10.1016/s0960-894x(00)00665-x

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  3 in total

1.  Bifunctional [2',6'-dimethyl-L-tyrosine1]endomorphin-2 analogues substituted at position 3 with alkylated phenylalanine derivatives yield potent mixed mu-agonist/delta-antagonist and dual mu-agonist/delta-agonist opioid ligands.

Authors:  Tingyou Li; Kimitaka Shiotani; Anna Miyazaki; Yuko Tsuda; Akihiro Ambo; Yusuke Sasaki; Yunden Jinsmaa; Ewa Marczak; Sharon D Bryant; Lawrence H Lazarus; Yoshio Okada
Journal:  J Med Chem       Date:  2007-05-12       Impact factor: 7.446

Review 2.  Developmental potential for endomorphin opioidmimetic drugs.

Authors:  Yoshio Okada; Yuko Tsuda; Severo Salvadori; Lawrence H Lazarus
Journal:  Int J Med Chem       Date:  2012-06-15

Review 3.  2',6'-dimethylphenylalanine: a useful aromatic amino Acid surrogate for tyr or phe residue in opioid peptides.

Authors:  Yusuke Sasaki; Akihiro Ambo
Journal:  Int J Med Chem       Date:  2012-04-04
  3 in total

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