| Bioactivity | AR-R17779 hydrochloride is a potent and selective full agonist of nAChR, with Kis of 92 and 16000 nM for α7 and α4β2 subtype, respectively. AR-R17779 hydrochloride can improve learning and memory in rats. AR-R17779 hydrochloride also has anxiolytic activity. AR-R17779 hydrochloride can reduce inflammation by activating antiinflammatory cholinergic (vagal) pathways[1][2][4]. |
| Target | IC50: 92 nM (α7-nAChR) |
| Invitro | AR-R17779 is 5-fold more potent and 35000-fold more selective than (-)-nicotine for the α7 nicotinic receptor[1].AR-R17779 (200 nM; 24 h) inhibits the LPS-induced TNF production in macrophages[4]. |
| In Vivo | 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[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: |
| Name | AR-R17779 hydrochloride |
| CAS | 178419-42-6 |
| Formula | C9H15ClN2O2 |
| Molar Mass | 218.68 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Mullen G, et, al. (-)-Spiro[1-azabicyclo[2.2.2]octane-3,5'-oxazolidin-2'-one], a conformationally restricted analogue of acetylcholine, is a highly selective full agonist at the alpha 7 nicotinic acetylcholine receptor. J Med Chem. 2000 Nov 2;43(22):4045- [2]. Levin ED, et, al. AR-R17779, and alpha7 nicotinic agonist, improves learning and memory in rats. Behav Pharmacol. 1999 Nov;10(6-7):675-80. [3]. Maanen MA, et, al. Stimulation of nicotinic acetylcholine receptors attenuates collagen-induced arthritis in mice. Arthritis Rheum. 2009 Jan;60(1):114-22. [4]. Lopes F, et, al. Involvement of Mast Cells in α7 Nicotinic Receptor Agonist Exacerbation of Freund's Complete Adjuvant-Induced Monoarthritis in Mice. |
AR-R17779 hydrochloride
CAS: 178419-42-6 F: C9H15ClN2O2 W: 218.68
AR-R17779 hydrochloride is a potent and selective full agonist of nAChR, with Kis of 92 and 16000 nM for α7 and α4β2
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