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.
(Modifications: Arg-1 = N-terminal Ac, Lys-6 = C-terminal amide)
|Storage||Desiccate at -20°C|
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.
Preparing Stock Solutions
The following data is based on the product molecular weight 939.12. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||1.06 mL||5.32 mL||10.65 mL|
|5 mM||0.21 mL||1.06 mL||2.13 mL|
|10 mM||0.11 mL||0.53 mL||1.06 mL|
|50 mM||0.02 mL||0.11 mL||0.21 mL|
References are publications that support the products' biological activity.
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, NOP, Receptors, NOP, Receptors, Tocris Bioscience
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