SML2049
AR-R17779 盐酸盐
≥97% (HPLC)
别名:
(-)-AR-R 13489 HCl, (-)-AR-R13489 HCl, (-)-螺[1-氮杂双环[2.2.2]辛烷-3,5′;-噁唑烷]-2′-酮盐酸盐；(3S)-螺[1-氮杂双环[2.2.2]辛烷-3,5′-噁唑烷]-2′-酮盐酸盐, (S)-AR-R 13489 HCl, (S)-AR-R13489 HCl, AR-R 17779 HCl
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关于此项目
经验公式（希尔记法）:
C9H14N2O2 · HCl
化学文摘社编号:
分子量:
218.68
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
InChI
1S/C9H14N2O2.ClH/c12-8-10-5-9(13-8)6-11-3-1-7(9)2-4-11;/h7H,1-6H2,(H,10,12);1H/t9-;/m0./s1
SMILES string
O=C1O[C@@]2(CN1)CN3CCC2CC3.Cl
InChI key
XGLBLUBBDSJBIU-FVGYRXGTSA-N
assay
≥97% (HPLC)
form
powder
optical activity
[α]/D -59 to -69°, c = 1.0 in methanol
storage condition
desiccated
color
white to beige
solubility
H2O: 2 mg/mL, clear
storage temp.
−20°C
Biochem/physiol Actions
AR-R17779是一种靶向α7 nAChR的烟碱型乙酰胆碱受体α7完全激动剂，具有高亲和力（对于5 nM α-BTX，Ki为92 nM/rat α7；对于3 nM (-)-烟碱，Ki为16 μM/rat α4β2）和高选择性（EC50 = 6.2/10/12.7 μM采用人/大鼠/猴 α7 nAChR-爪蟾卵母细胞通过全细胞电压钳，采用人α4β2-, α3β4-, α3β2-, α3β2α5-表达卵母细胞对乙酰胆碱没有拮抗活性，采用大鼠5HT3a表达卵母细胞对5-HT没有拮抗活性）。AR-R17779在体内具有改善大鼠（1-20 mg / kg s.c）和小鼠（1-20 mg / kg ip.p.）认知的功效并被广泛用于研究其他α7 nAChR依赖性生理功能。
在体内具有改善认知功效的选择性高亲和力烟碱型乙酰胆碱受体α7（α7 nAChR）完全激动剂
signalword
Danger
hcodes
Hazard Classifications
Eye Dam. 1 - Skin Irrit. 2 - STOT SE 3
target_organs
Respiratory system
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
G Mullen et al.
Journal of medicinal chemistry, 43(22), 4045-4050 (2000-11-07)
Neuronal nicotinic acetylcholine receptors are members of the ligand-gated ion channel receptor superfamily and may play important roles in modulating neurotransmission, cognition, sensory gating, and anxiety. Because of its distribution and abundance in the CNS, the alpha 7 nicotinic receptor
Lei Zhao et al.
Toxicological sciences : an official journal of the Society of Toxicology, 153(1), 103-111 (2016-06-23)
Maternal cigarette smoke is the major risk of sudden infant death syndrome (SIDS). A depressed ventilatory response to hypoxia (HVR) and hypercapnia (HCVR) is thought to be responsible for the pathogenesis of SIDS and the carotid body is critically involved
R L Papke et al.
Bioorganic & medicinal chemistry letters, 14(8), 1849-1853 (2004-03-31)
Nicotinic receptors containing alpha7 subunits are widely distributed in the central nervous system and are thought to be involved in a number of functions. However, it has been difficult to study alpha7-containing receptors in vivo because of a paucity of
Aya Watanabe et al.
Atherosclerosis, 244, 113-120 (2015-11-28)
Activation of vagal nerve suppresses inflammatory responses through activation of α7 nicotinic acetylcholine receptor (nAchR). We sought to determine whether AR-R17779, a selective agonist of α7nAchR, affects the development of abdominal aortic aneurysm (AAA). AAA was induced by topical application
F A Koopman et al.
Oral diseases, 21(7), 858-865 (2015-06-23)
Activation of the cholinergic anti-inflammatory pathway (CAP) has been shown to reduce inflammation in animal models, while abrogation of the pathway increases inflammation. We investigated whether modulation of CAP influences inflammation in the non-obese diabetic (NOD) mouse model for Sjögren's
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