SB-612111

SB-612111 is a novel and potent opiate receptor-like orphan receptor (ORL-1) antagonist with a high affinity for hORL-1 (K_i=0.33 nM). SB-612111 exhibits selectivity for μ-,?κ- and?δ-receptors with K_i values of?57.6 nM, 160.5 nM and 2109 nM, respecticely. SB-612111 effectively antagonizes the pronociceptive action of Nociceptin (HY-P0183) in an acute pain model^[1].
IC50 & Target: Ki: 0.33 nM (hORL-1)
Ki: 57.6 nM (μ-receptor); 160.5 nM (κ-receptor); 2109 nM (δ-receptor)^[1] In Vivo: SB-612111 (intravenous?injection; 0.6-10 nmol/mouse) antagonize nociceptin-induced thermal hyperalgesia in a dose-dependent manner with an ED₅₀ of 0.62 mg/kg^[1].
SB-612111 (intravenous?injection; 0.1-5 mg/kg) causes a significant inhibition of the carrageenan-induced reduction in paw withdrawal latencies in rat, however, untreated paw are uneffected^[1].