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2004 | 51 | 1 | 107-113
Article title

Dansylated analogues of the opioid peptide [Dmt1]DALDA: in vitro activity profiles and fluorescence parameters.

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EN
Abstracts
EN
Dansylated analogues of the potent and selective μ opioid peptide agonist [Dmt1]DALDA (H-Dmt-D-Arg-Phe-Lys-NH2; Dmt = 2',6'-dimethyltyrosine) were prepared either by substitution of Nβ-dansyl-α,β-diaminopropionic acid or Nε-dansyllysine for Lys4, or by attachment of a dansyl group to the C-terminal carboxamide function via a linker. All three analogues displayed high μ agonist potency in vitro and the C-terminally dansylated one retained significant μ receptor selectivity. The three analogues showed interesting differences in their fluorescence emission maxima and quantum yields, indicating that the dansyl group in two of them was engaged in intramolecular hydrophobic interactions. These dansylated [Dmt1]DALDA analogues represent valuable tools for binding studies, cellular uptake and intracellular distribution studies, and tissue distribution studies.
Year
Volume
51
Issue
1
Pages
107-113
Physical description
Dates
published
2004
received
2003-10-31
revised
2004-02-10
accepted
2004-02-20
References
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Document Type
Publication order reference
YADDA identifier
bwmeta1.element.bwnjournal-article-abpv51i1p107kz
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