AR-R17779 HYDROCHLORIDE
| 中文名称 | AR-R17779 HYDROCHLORIDE |
|---|---|
| 中文同义词 | 化合物 T21857;AR-R17779 盐酸盐 |
| 英文名称 | AR-R 17779 hydrochloride |
| 英文同义词 | AR-R 17779 hydrochloride, >=98%;(3S)-Spiro[1-azabicyclo[2.2.2]octane-3,5'-oxazolidine]-2'-one hydrochloride;AR-R17779 Hydrochloride >=97% (HPLC) |
| CAS号 | 178419-42-6 |
| 分子式 | C9H15ClN2O2 |
| 分子量 | 218.68 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 178419-42-6.mol |
| 结构式 |  |
AR-R17779 HYDROCHLORIDE 性质
| 储存条件 | -20°C |
|---|---|
| 溶解度 | <10.93mg/ml，溶于 DMSO； <21.87mg/ml，在水中 |
| 形态 | 粉末 |
| 颜色 | 白色至米色 |
| 旋光性 (optical activity) | [α]/D -59 to -69°, c = 1.0 in methanol |
AR-R17779 hydrochloride 是一种有效和选择性的 nAChR 全激动剂，对 α7 和 α4β2 亚型的 Ki 直分别为 92 和 16000 nM。AR-R17779 hydrochloride 可以改善大鼠的学习和记忆能力。AR-R17779 hydrochloride 也具有抗焦虑活性。AR-R17779 hydrochloride 可通过激活抗炎胆碱能（迷走神经）途径减轻炎症。
IC50: 92 nM (α7-nAChR)
AR-R17779 is 5-fold more potent and 35000-fold more selective than (-)-nicotine for the α7 nicotinic receptor.
AR-R17779 (200 nM; 24 h) inhibits the LPS-induced TNF production in macrophages.
AR-R17779 (1-5 mg/kg; i.p. twice a day for 7 d) ameliorates arthritis, reduces synovial inflammation, delays onset of disease and protects against joint destruction.
AR-R17779 (1-10 mg/kg; s.c. for 3 weeks) improves learning in two radial-arm maze tasks and reverses working memory impairment caused by fimbria-fornix sections in rats.
| Animal Model: | Male DBA/1 mice (8-10 weeks) were subjected to unilateral cervical vagotomy or sham surgery, after which arthritis was induced with type II collagen |
| Dosage: | 1, 2.5, 5 mg/kg |
| Administration: | I.p. twice daily from day 20 until day 26 |
| Result: |
Ameliorated arthritis and delayed onset of disease.
Reduced erosive disease, cartilage degradation and synovial inflammation. Reduced TNFα levels in plasma and synovial tissue. |