AR-R17779 hydrochloride 是一种有效和选择性的nAChR完全激动剂,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)通路减轻炎症。
产品描述
AR-R17779 hydrochloride is a potent and selective full agonist of nAChR, with K i s of 92 and 16000 nM for α7 and α4β2 subtype, respectively. AR-R17779 hydrochloride can improve learning and memory in rats which has the potential therapeutic use. AR-R17779 hydrochloride also has anxiolytic activity. AR-R17779 hydrochloride can reduce inflammation by activating antiinflammatory cholinergic (vagal) pathways [1] [2] [4].
体外活性
AR-R17779 is 5-fold more potent and 35000-fold more selective than (-)-nicotine at the α7 nicotinic receptor [1]. AR-R17779 (200 nM; 24 h) inhibits the LPS-induced TNF production in macrophages [4].
体内活性
AR-R17779 (1-5 mg/kg; i.p. twice a day for 7 d) improves arthritis, reduces synovial inflammation, delays onset of disease and protects against joint destruction [3]. 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 [2]. 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 [3] 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.
Cas No.
178419-42-6
分子式
C9H15ClN2O2
分子量
218.68
别名
AR-R 17779 hydrochloride
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years