SR 17018 是一种 mu-阿片受体 (MOR) 激动剂，与 GTPγS 结合，EC50 为 97 nM。
| Cas No. | 2134602-45-0 |
| 化学名 | 5,6-dichloro-1-[1-[(4-chlorophenyl)methyl]-4-piperidinyl]-1,3-dihydro-2H-benzimidazol-2-one |
| Canonical SMILES | ClC(C=C1)=CC=C1CN2CCC(N3C(NC4=C3C=C(Cl)C(Cl)=C4)=O)CC2 |
| 分子式 | C19H18Cl3N3O |
| 分子量 | 410.7 |
| 溶解度 | DMF: 1 mg/ml,DMSO: 1 mg/ml,DMSO:PBS (pH 7.2) (1:2): 0.33 mg/ml,Ethanol: slightly soluble |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | SR 17018 is an orally bioavailable and brain-penetrant agonist of μ-opioid receptors. It is functionally selective for G protein-coupled receptor signaling (EC50 = 97 nM for GTPγS binding in CHO cells expressing μ-opioid receptors) over β-arrestin 2 recruitment (EC50 = >10,000 nM) at the μ-opioid receptor. SR 17018 increases latency to withdraw in the hot plate and warm water tail-flick assay (ED50s = 6.9 and 7.7 mg/kg, respectively) without inducing respiratory depression in mice when administered at doses up to 48 mg/kg. SR 17018 was designed for this biased agonism at the μ-opioid receptor to potentially widen the therapeutic window and reduce adverse effects of μ-opioid receptors, such as respiratory depression. |
