AR-R17779 hydrochloride is a potent, selective full agonist of the nAChR, demonstrating K i values of 92 nM for the α7 subtype and 16,000 nM for the α4β2 subtype. It is noted for its ability to enhance learning and memory in rats, suggesting potential therapeutic applications. Additionally, this compound exhibits anxiolytic properties and can mitigate inflammation by activating anti-inflammatory cholinergic (vagal) pathways [1] [2] [4].

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].

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.