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Endomorphin analogues with balanced affinity for bothμ- andδ-opioid receptors

Authors
Journal
Chinese Chemical Letters
1001-8417
Publisher
Elsevier
Publication Date
Volume
22
Issue
8
Identifiers
DOI: 10.1016/j.cclet.2011.01.035
Keywords
  • Endomorphin
  • Opioid
  • Analgesics

Abstract

Abstract Analogues of endomorphin and tripeptides modified at positions 4 and 3, respectively, with various phenylalanine analogues were synthesized and their affinities for opioid receptors were evaluated. Most of the peptides exhibited potent μ-receptor affinity and selectivity, among them, compound 7 (Dmt-Pro-Tmp-Tmp-NH 2) exhibited potent affinity for both μ- and δ-receptors ( K i μ = 0.47 nmol/L, K i δ = 1.63 nmol/L).

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