sb-612111

SB-612111 is a novel and potent human opiate receptor-like orphan receptor (ORL-1) antagonist with a high affinity for hORL-1 (Ki=0.33 nM). SB-612111 exhibits selectivity for μ-, κ- and δ-receptors with Ki values of 57.6 nM, 160.5 nM and 2109 nM, respecticely. SB-612111 effectively antagonizes the pronociceptive action of Nociceptin in an acute pain model[1]. [1]. Paola F Zaratin, et al. Modification of Nociception and Morphine Tolerance by the Selective Opiate Receptor-Like Orphan Receptor Antagonist (-)-cis-1-methyl-7-[[4-(2,6-dichlorophenyl)piperidin-1-yl]methyl]-6,7,8,9-tetrahydro-5H-benzocyclohepten-5-ol (SB-612111).J Pharmacol Exp Ther. 2004 Feb;308(2):454-61.

NOP receptor antagonist

SB-612111 hydrochloride 是一种高效的、新型的阿片受体孤儿受体 (ORL-1) 拮抗剂，对 hORL-1 具有较高的亲和力，Ki 值为 0.33 nM。SB-612111 hydrochloride 能够作用于 μ-receptor (Ki: 57.6 nM)，κ-receptor (Ki: 160.5 nM) 和 δ-receptor (Ki: 2109 nM)。SB-612111 hydrochloride 能有效拮抗 Nociceptin 在急性疼痛模型中的造成的痛觉作用。