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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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
References are publications that support the biological activity of the product.
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, Ac-RYYRIK-NH2 supplier, High, affinity, NOP, ligands, Nociceptin, Receptors, ORL1, OP4, Opioid, 1239, Tocris Bioscience
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Peptides Involved in Appetite Modulation Scientific Review
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Peripheral sensitization is the reduction in the threshold of excitability of sensory neurons that results in an augmented response to a given external stimulus. This poster outlines the excitatory and inhibitory signaling pathways involved in modulation of peripheral sensitization. The role of ion channels, GPCRs, neurotrophins, and cytokines in sensory neurons are also described.