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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Publicado no:Eur J Med Chem
Main Authors: 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
Formato: Artigo
Idioma:Inglês
Publicado em: 2014
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Article
Acesso em linha: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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