Ontology highlight
ABSTRACT:
SUBMITTER: Betti C
PROVIDER: S-EPMC4677362 | biostudies-literature | 2015 Dec
REPOSITORIES: biostudies-literature
Betti Cecilia C Starnowska Joanna J Mika Joanna J Dyniewicz Jolanta J Frankiewicz Lukasz L Novoa Alexandre A Bochynska Marta M Keresztes Attila A Kosson Piotr P Makuch Wioletta W Van Duppen Joost J Chung Nga N NN Vanden Broeck Jozef J Lipkowski Andrzej W AW Schiller Peter W PW Janssens Frans F Ceusters Marc M Sommen François F Meert Theo T Przewlocka Barbara B Tourwé Dirk D Ballet Steven S
ACS medicinal chemistry letters 20151031 12
Herein, the synthesis and biological evaluation of dual opioid agonists-neurokinin 1 receptor (NK1R) antagonists is described. In these multitarget ligands, the two pharmacophores do not overlap, and this allowed maintaining high NK1R affinity and antagonist potency in compounds 12 and 13. Although the fusion of the two ligands resulted in slightly diminished opioid agonism at the μ- and δ-opioid receptors (MOR and DOR, respectively), as compared to the opioid parent peptide, balanced MOR/DOR ac ...[more]