178419-42-6
中文名稱
AR-R17779 HYDROCHLORIDE
英文名稱
AR-R 17779 hydrochloride
CAS
178419-42-6
分子式
C9H14N2O2.HCl
分子量
218.68
MOL 文件
178419-42-6.mol
178419-42-6 結(jié)構(gòu)式
基本信息
英文別名
AR-R 17779 hydrochloride, >=98%AR-R17779 Hydrochloride >=97% (HPLC)
(3S)-Spiro[1-azabicyclo[2.2.2]octane-3,5'-oxazolidine]-2'-one hydrochloride
物理化學(xué)性質(zhì)
儲存條件-20°C
溶解度<10.93mg/ml in DMSO; <21.87mg/ml in H2O
形態(tài)粉末
顏色白色至米色
旋光性 (optical activity)[α]/D -59 to -69°, c = 1.0 in methanol
常見問題列表
生物活性
AR-R17779 hydrochloride 是一種有效和選擇性的 nAChR 全激動劑，對 α7 和 α4β2 亞型的 Ki 直分別為 92 和 16000 nM。AR-R17779 hydrochloride 可以改善大鼠的學(xué)習(xí)和記憶能力。AR-R17779 hydrochloride 也具有抗焦慮活性。AR-R17779 hydrochloride 可通過激活抗炎膽堿能（迷走神經(jīng)）途徑減輕炎癥。靶點
IC50: 92 nM (α7-nAChR)
體外研究
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.
體內(nèi)研究
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. |