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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Pubblicato in:Eur J Med Chem
Autori principali: 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
Natura: Artigo
Lingua:Inglês
Pubblicazione: 2014
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Article
Accesso online: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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