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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Bibliografski detalji
Izdano u:Eur J Med Chem
Glavni autori: 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
Format: Artigo
Jezik:Inglês
Izdano: 2014
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Article
Online pristup: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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