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Ac-RYYRIK-NH2
Biological Activity:
High
affinity ligand for the ORL1 site (Ki = 1.5 nM).
Antagonises 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.
Dooleyet al (1997) Binding and in vitro activities of
peptides with high affinity for the nociceptin/orphanin FQ receptor, ORL1.
J.Pharmacol.Exp.Ther. 283 735. Berger et al (1999)
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. Br.J.Pharmacol. 126 555. Bergeret
al (1999) Acetyl-RYYRIK-NH2, a nociceptin/orphanin FQ (noc/OFQ)
receptor ligand, exhibits properties of an antagonist and agonist as well.
Regul.Peptides 80 122.
