Cat. No. 1239
Biological ActivityHigh 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.
(Modifications: Arg-1 = N-terminal Ac, Lys-6 = C-terminal amide)
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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. PMID: 10188961.
Berger et al (1999) Acetyl-RYYRIK-NH2, a nociceptin/orphanin FQ (noc/OFQ) receptor ligand, exhibits properties of an antagonist and agonist as well. Regul.Pept. 80 122. PMID: 10998548.
Dooley et 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. PMID: 9353393.
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Keywords: Ac-RYYRIK-NH2, supplier, High, affinity, NOP, ligands, Nociceptin, Receptors, ORL1, OP4, Opioid, Tocris Bioscience, NOP Receptor Ligand products
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