178419-42-6

178419-42-6 structure

Name: AR-R17779 hydrochloride
Chemical Name: (2S)-2'H-Spiro[4-azabicyclo[2.2.2]octane-2,5'-[1,3]oxazolidin]-2'-one hydrochloride (1:1)
CAS Number: 178419-42-6
Molecular Formula: C₉H₁₅ClN₂O₂
Molecular Weight: 218.681
Catalog: Signaling Pathways Membrane Transporter/Ion Channel nAChR
Create Date: 2018-07-06 00:05:03
Modify Date: 2024-01-13 16:39:47
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].

Name	(2S)-2'H-Spiro[4-azabicyclo[2.2.2]octane-2,5'-[1,3]oxazolidin]-2'-one hydrochloride (1:1)
Synonyms	Spiro[1-azabicyclo[2.2.2]octane-3,5'-oxazolidin]-2'-one, (3S)-, hydrochloride (1:1) (2S)-2'H-Spiro[4-azabicyclo[2.2.2]octane-2,5'-[1,3]oxazolidin]-2'-one hydrochloride (1:1)

Description	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].
Related Catalog	Signaling Pathways >> Membrane Transporter/Ion Channel >> nAChR Signaling Pathways >> Neuronal Signaling >> nAChR Research Areas >> Neurological Disease
Target	IC50: 92 nM (α7-nAChR)[1]
In Vitro	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: 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.
References	[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):4045-50. [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.

Molecular Formula	C₉H₁₅ClN₂O₂
Molecular Weight	218.681
Exact Mass	218.082199

Hazard Codes	C

178419-42-6	178419-47-1
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