Ac-RYYRIK-NH2 TFA 

Ac-RYYRIK-NH2 TFA is a potent and partial agonist on ORL1 transfected in CHO cells (K_d=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].

Kd: 1.5 nM (ORL1 in CHO cells)^[1]

Ac-RYYRIK-NH2 TFA (intracerebroventricularly (i.c.v.)) inhibits spontaneous locomotor activity in mice with an ID₅₀ of 0.07 nmol. Co-administration of noc/OFQ and Ac-RYYRIK-NH2 lead to additive effects in Male Swiss mice^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

1053.13

C₄₆H₇₁F₃N₁₄O₁₁

Ac-RYYRIK-NH2

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Please store the product under the recommended conditions in the Certificate of Analysis.

• [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.  [Content Brief]

  [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.  [Content Brief]

  [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.  [Content Brief]