Repozytorium
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Kolekcje
Inne
Synthesis, biological activity and resistance to proteolytic digestion of new cyclic dermorphin/deltorphin analogues.
Autorzy
Rok wydania
2013
Czasopismo
European Journal of Medicinal Chemistry
Numer woluminu
63
Strony
457-467
DOI
10.1016/j.ejmech.2013.02.019
Kolekcja
Język
Angielski
Typ publikacji
Artykuł
A series of novel cyclic ureidopeptides, analogues of dermorphine/deltorphine tetrapeptide, were synthesized by solid phase peptide synthesis and/or in solution. The antinociceptive activity of N-substituted amides 1–10 was evaluated using hot-plate and tail-flick tests. Analogue 1 showed significant, stronger than morphine, antinociceptive effect after systemic applications. All analogues were also tested for their in vitro resistance to proteolysis by means of mass spectroscopy and it was found that all substituted amides 1–10 showed full stability during incubation with large excess of chymotrypsin and pepsin. Compound 1 is a lead molecule for further evaluation.
Słowa kluczowe
Cyclic opioid peptides, Peptide synthesis, Dermorphin/deltorphin analogues, Antinociceptive effect, Stability to proteolytic enzymes
Adres publiczny
http://dx.doi.org/10.1016/j.ejmech.2013.02.019
Strona internetowa wydawcy
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