Synthesis and biological activity of nociceptin/orphanin FQ analogues substituted in position 7 or 11 with Calpha,alpha-dialkylated amino acids.

@article{Arduin2007SynthesisAB,
  title={Synthesis and biological activity of nociceptin/orphanin FQ analogues substituted in position 7 or 11 with Calpha,alpha-dialkylated amino acids.},
  author={Marika Arduin and Barbara Spagnolo and Girolamo Calo and Renzo Guerrini and Giacomo Carr{\'a} and Carmela Fischetti and Claudio Trapella and Erika Marzola and John N. McDonald and D G Lambert and Domenico Regoli and S. Portaluppi F. Salvadori},
  journal={Bioorganic & medicinal chemistry},
  year={2007},
  volume={15 13},
  pages={
          4434-43
        }
}
Previous structure-activity and NMR studies on nociceptin/orphanin FQ (N/OFQ) demonstrated that Aib substitution of Ala(7) and/or Ala(11) increases the peptide potency through an alpha helix structure induction mechanism. On these bases we synthesised and evaluated pharmacologically in the mouse vas deferens assay a series of N/OFQ-NH(2) analogues substituted in position 7 and 11 with Calpha,alpha-disubstituted cyclic, linear and branched amino acids. None of the 20 novel N/OFQ analogues… CONTINUE READING

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