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.
CB2R激动剂, 其化学式为C25H28N6O3S,分子量为508.6 g mol。作为一种高效且具有选择性的CB2R激动剂,该化合物表现出在医疗研究中应用的潜力。其结构包含吡咯并[2,3-b]吡啶-3-胺环,与CB2受体的结合力强。在体外试验中,这种化合物的EC50值为22 nM,体现了其高度选择性。