Autor: |
Anika, Lasota, Oliwia, Frączak, Anna, Leśniak, Adriana, Muchowska, Andrzej W, Lipkowski, Michał, Nowakowski, Andrzej, Ejchart, Aleksandra, Olma |
Rok vydání: |
2014 |
Předmět: |
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Zdroj: |
Journal of peptide science : an official publication of the European Peptide Society. 21(2) |
ISSN: |
1099-1387 |
Popis: |
New analogues of deltorphin I (DT I, Tyr-D-Ala-Phe-Asp-Val-Val-Gly-NH2 ), with the D-Ala residue in position 2 replaced by α-methyl-β-azido(amino, 1-pyrrolidinyl, 1-piperidinyl or 4-morpholinyl)alanine, were synthesized by a combination of solid-phase and solution methods. All ten new analogues were tested for receptor affinity and selectivity to μ- and δ-opioid receptors. The affinity of analogues containing (R) or (S)-α-methyl-β-azidoalanine in position 2 to δ-receptors strongly depended on the chirality of the α,α-disubstituted residue. Peptide II, containing (S)-α-methyl-β-azidoalanine in position 2, displayed excellent δ-receptor selectivity with its δ-receptor affinity being only three times lower than that of DT I. |
Databáze: |
OpenAIRE |
Externí odkaz: |
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