Catalog Number: 1239
Biological Activity
High affinity ligand for the NOP site (Ki = 1.5 nM). Antagonizes nociceptin-stimulated GTP binding in rat brain and the chronotropic effect of nociceptin on rat cardiomyocytes. However, displays potent agonist properties in vivo, inhibiting locomotor activity in mice.
Technical Data
  • M.Wt:
  • Formula:
  • Sequence:

    (Modifications: Arg-1 = N-terminal Ac, Lys-6 = C-terminal amide)

  • Storage:
    Desiccate at -20°C
  • CAS No:
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Background References
  1. Antagonism by acetyl-RYYRIK-NH2 of G protein activation in rat brain preparations and of chronotropic effect on rat cardiomyocytes evoked by nociceptin/orphanin FQ.
    Berger et al.
    Br.J.Pharmacol., 1999;126:555
  2. Acetyl-RYYRIK-NH2, a nociceptin/orphanin FQ (noc/OFQ) receptor ligand, exhibits properties of an antagonist and agonist as well.
    Berger et al.
    Regul.Pept., 1999;80:122
  3. Binding and in vitro activities of peptides with high affinity for the nociceptin/orphanin FQ receptor, ORL1.
    Dooley et al.
    J.Pharmacol.Exp.Ther., 1997;283:735

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