AT-121 是一种双功能伤害感受和 mu 阿片受体激动剂，Kis 分别为 3.67 和 16.49 nM。
| Cas No. | 2099681-31-7 |
| Canonical SMILES | CC(C)[C@@H]1CC[C@H](N2CCC3(C(N(CCNS(N)(=O)=O)CC4=C3C=CC=C4)=O)CC2)CC1 |
| 分子式 | C24H38N4O3S |
| 分子量 | 462.6 |
| 溶解度 | Chloroform: 10 mg/ml,DMF: miscible,DMSO: miscible,Ethanol: miscible,Ethanol:PBS (pH 7.2) (1:20): 50µ g/ml |
| 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 | AT-121 is a dual μ-opioid and nociceptin receptor partial agonist (Kis = 16.49 and 3.67 nM, respectively). It stimulates [35S]GTPγS binding to cell membranes expressing μ-opioid or nociceptin receptors (EC50s = 19.6 and 34.7 nM, respectively). AT-121 (0.003-0.03 mg/kg) decreases capsaicin-induced thermal allodynia without increasing scratching activity in rhesus monkeys in a dose-dependent manner. It lacks reinforcing effects, a marker of abuse potential, and reduces oxycodone, but not food pellet, reinforcement in a drug self-administration assay in rhesus monkeys when administered at doses ranging from 0.3 to 10 μg/kg per injection. AT-121 (0.01 or 0.03 mg/kg) does not induce hyperalgesia, a marker of tolerance development, in rhesus monkeys. |
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