| Description | R121919 (NBI30775) is a potent small molecule adrenocorticotropic hormone-releasing factor receptor 1 (CRF1) receptor antagonist with antidepressant and anxiolytic activity that inhibits the CRF1 receptor, the CRF2 receptor, and the CRF-binding proteins. |
| In vitro | R121919是一种强效的小分子CRF1受体拮抗剂，对CRF1受体具有高亲和力，其Ki值在2-5 nM范围内。值得注意的是，其在CRF2受体、CRF结合蛋白和其他70种受体类型上的活性均弱1000倍以上[2]。 |
| In vivo | 在大鼠中，R121919显示出对抗压力的肾上腺皮质激素(restraint stress)反应中的促肾上腺皮质激素和皮质醇的剂量依赖性降低。当剂量为10 mg/kg时，R121919使得促肾上腺皮质激素和皮质醇的血浆浓度分别降低了9%和25%[2]。此外，R121919在小鼠中表现出具有陡峭剂量-反应曲线的抗焦虑效果，从而降低了焦虑水平。该化合物的一些细胞内靶点包括如GR（糖皮质激素受体）、MR（矿物皮质激素受体）、BAG-1（Bcl-2相关athanogene-1）、以及AP-1（激活蛋白1）等分子[1]。 |
| Target activity | CRF1 receptor:2-5 nM (Ki) |
| Synonyms | NBI30775 |
| molecular weight | 380.53 |
| Molecular formula | C22H32N6 |
| CAS | 195055-03-9 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility | DMSO: 5 mg/mL (13.14 mM), Sonication is recommended. Ethanol: 80 mg/mL (210.23 mM), Sonication is recommended. |
| References | 1. Post A, et al. Identification of molecules potentially involved in mediating the in vivo actions of the corticotropin-releasing hormone receptor 1 antagonist, NBI30775 (R121919). Psychopharmacology (Berl). 2005 Jun;180(1):150-8. 2. Gutman DA, et al. The corticotropin-releasing factor1 receptor antagonist R121919 attenuates the behavioral and endocrine responses to stress. J Pharmacol Exp Ther. 2003 Feb;304(2):874-80. |