Ac-RYYRIK-NH2-Get quote

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Ac-RYYRIK-NH2 is a potent and partial agonist on ORL1 transfected in CHO cells (Kd=1.5 nM) and behaves as a endogenous ligand of ORL1. Ac-RYYRIK-NH2 is a specific antagonist for the activation of G protein and competitively antagonizes the stimulation of [35S]-GTPgS binding to G proteins by nociceptin/orphanin FQ (noc/OFQ) in membranes and sections of rat brain[1].—Neuroscience-Neuromodulation–C44H70N14O9—-[1]H Berger, et al. 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. 1999 Feb;126(3):555-8.|[2]H Berger, et al. The nociceptin/orphanin FQ receptor ligand acetyl-RYYRIK-amide exhibits antagonistic and agonistic properties.Peptides. 2000 Jul;21(7):1131-9.|[3]C T Dooley, et al. Binding and in vitro activities of peptides with high affinity for the nociceptin/orphanin FQ receptor, ORL1. J Pharmacol Exp Ther. 1997 Nov;283(2):735-41.–200959-48-4–939.11—-O=C([R][Y][Y][R]([K])(N)I)C–Neurological Disease–10 mM in DMSO–Opioid Receptor–NOP Receptor/ORL1–GPCR/G Protein;Neuronal Signaling–Peptides