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
相关类别
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
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
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
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
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
The α7 nicotinic acetylcholine receptor agonist tropisetron counteracts ultraviolet A-mediated oxidative stress in human dermal fibroblasts.
Agatha Stegemann et al.
Experimental dermatology, 25(12), 994-996 (2016-09-30)
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