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.
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