货号 | 3661/50 |
别名 | (2R)-1-(Phenylmethyl)-N-[3-(spiro[i |
供应商 | Tocris |
生物活性 | Potent and selective NOP receptor antagonist (IC50 values are 0.27, 2500, 6700 and > 10000 nM for NOP, κ-,μ- and δ-receptors respectively). Inhibits nociceptin-induced stimulation of [35S]-GTPγS binding and Ca2+ mobilization in CHO cells in vitro and antagonizes NOP agonist-induced reduction in locomotor activity in vivo. Brain penetrant. |
运输条件 | Blue Ice |
存放说明 | -20℃ |
纯度 | >97 % |
计算分子量 | 506.51 |
分子式 | C27H35N3O2.2HCl |
可溶性/溶解性 | Soluble to 100 mM in water and to 100 mM in DMSO |
CAS号 | 475150-69-7 |
参考文献 | Fischettiet al (2009) Pharmacological characterization of the nociceptin/orphanin FQ receptor non peptide antagonist compound 24. Eur.J.Pharmacol. 614 50. PMID: 19445927. Liaoet al (2009) 1-Benzyl-N-[spiroisobenzofuran-1(3H),4'-piperidin-1-yl]propyl]pyrrolidine-2-carboxamide (compound 24) antagonizes NOP receptor-mediated potassium channel activation in rat periaqueductal gray slices. Eur.J.Pharmacol. 606 84. PMID: 19374842. Gotoet al (2006) Identification of a novel spiropiperidine opioid receptor-like 1 antagonist class by a focused library approach featuring 3D-pharmacophore similarity. J.Med.Chem. 49 847. PMID: 16451050. |