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Ac-RYYRIK-NH2 acetate is a potent and partial agonist on ORL1 transfected in CHO cells (Kd = 1.5 nM). 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.