Ac-RYYRIK-NH2 (TFA)-Get quote

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Ac-RYYRIK-NH2 TFA 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–C46H71F3N14O11—-[1]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.|[2]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.|[3]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.—-1053.13—-OC(C(F)(F)F)=O.OC(C=C1)=CC=C1C[C@@H](C(N[C@@H](CCCNC(N)=N)C(N[C@@H]([C@@H](C)CC)C(N[C@H](C(N)=O)CCCCN)=O)=O)=O)NC([C@@H](NC([C@@H](NC(C)=O)CCCNC(N)=N)=O)CC2=CC=C(C=C2)O)=O–Neurological Disease–10 mM in DMSO–Opioid Receptor–NOP Receptor/ORL1–GPCR/G Protein;Neuronal Signaling–Peptides