ac-ryyrik-nh2

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 acti

Ac-RYYRIK-NH2 acetate is an agonist at nociceptin/orphanin FQ(noc/OFQ) receptors, affecting spontaneous locomotor activity. Ac-RYYRIK-NH2 acetate is a partial agonist on ORL1 transfected in CHO cells, antagonizes the stimulation of [35S]-GTPgammaS binding to G proteins by noc/OFQ in membranes and sections of rat brain.

Ac-RYYRIK-NH2 TFA acts as both a potent partial agonist for ORL1 when transfected in CHO cells (K d = 1.5 nM) and an endogenous ligand of ORL1. Moreover, it serves as a specific antagonist that inhibits G protein activation and competitively blocks the stimulation of [35S]-GTPγS binding to G proteins by nociceptin/orphanin FQ (noc/OFQ) in rat brain membranes and sections [1].