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

• Autorzy: Berezowska I. , Lemieux C. , Chung N.N. , Zelent B. , Schiller P.W.
• Języki publikacji: EN

Abstrakty

EN

Dansylated analogues of the potent and selective u opioid peptide agonist [Dmt1]DALDA (H-Dmt-D-Arg-Phe-Lys-NH2; Dmt = 2',6'-dimethyltyrosine) were pre­pared either by substitution of Nε-dansyl-a,β-diaminopropionic acid or Nε-dansyl- lysine for Lys4 , or by attachment of a dansyl group to the C-terminal carboxamide function via a linker. All three analogues displayed high u agonist potency in vitro and the C-terminally dansylated one retained significant u 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.

Słowa kluczowe

EN

fluorescence quantum yield; opioid peptide; fluorescence parameter; in vitro; opioid activity; fluorescence spectroscopy

• Wydawca: -
• Czasopismo: Acta Biochimica Polonica
• Rocznik: 2004
• Tom: 51
• Numer: 1
• Opis fizyczny: p.107-113,ref.

Twórcy

autor

Berezowska I.

• Clinical Research Institute of Montreal, 110 Pine Avenue West, Montreal, Quebec, Canada

autor

Lemieux C.

autor

Chung N.N.

autor

Zelent B.

autor

Schiller P.W.

Bibliografia

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