Synthesis and biological evaluation of compact, conformationally constrained bifunctional opioid agonist – neurokinin-1 antagonist peptidomimetics

A reported mixed opioid agonist - neurokinin 1 receptor (NK1R) antagonist 4 (Dmt-D-Arg-Aba-Gly-(3’,5’-(CF(3))(2))NMe-benzyl) was modified to identify important features in both pharmacophores. The new dual ligands were tested in vitro and subsequently two compounds (lead structure 4 and one of the n...

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Vydáno v:Eur J Med Chem
Hlavní autoři: Guillemyn, Karel, Kleczkowska, Patrycia, Lesniak, Anna, Dyniewicz, Jolanta, Van der Poorten, Olivier, Van den Eynde, Isabelle, Keresztes, Attila, Varga, Eva, Lai, Josephine, Porreca, Frank, Chung, Nga N., Lemieux, Carole, Mika, Joanna, Rojewska, Ewelina, Makuch, Wioletta, Van Duppen, Joost, Przewlocka, Barbara, Broeck, Jozef Vanden, Lipkowski, Andrzej W., Schiller, Peter W., Tourwé, Dirk, Ballet, Steven
Médium: Artigo
Jazyk:Inglês
Vydáno: 2014
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Article
On-line přístup:https://ncbi.nlm.nih.gov/pmc/articles/PMC4336569/
https://ncbi.nlm.nih.gov/pubmed/25544687
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1016/j.ejmech.2014.12.033
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