SIB 1553A hydrochloride
| 中文名称 | SIB 1553A hydrochloride |
|---|---|
| 中文同义词 | 化合物 T16881;SIB-1553A 盐酸盐;SIB 1553A HYDROCHLORIDE,NACHR激动剂;4-((2-(1-甲基吡咯烷-2-基)乙基)硫代)苯酚 盐酸盐 |
| 英文名称 | SIB 1553A hydrochloride |
| 英文同义词 | SIB 1553A hydrochloride;4-[2-(1-methylpyrrolidin-2-yl)ethylsulfanyl]phenol:hydrochloride;SIB 1553A Hyrdrochloride;(±)-4-[[2-(1-Methyl-2-pyrrolidinyl)ethyl]thio]phenol hydrochloride;4-[2-(1-methylpyrrolidin-2-yl)ethylsulfanyl]phenol;SIB 1553A,SIB1553A;SIB 1553A hydrochloride, nAChR agonist;4-((2-(1-Methylpyrrolidin-2-yl)ethyl)thio)phenol hydrochloride |
| CAS号 | 191611-89-9 |
| 分子式 | C13H20ClNOS |
| 分子量 | 273.82 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 191611-89-9.mol |
| 结构式 |  |
SIB 1553A hydrochloride 性质
| 熔点 | 149-151°C |
|---|---|
| 储存条件 | Hygroscopic, Refrigerator, under inert atmosphere |
| 溶解度 | DMSO（少许）、水（少许） |
| 形态 | 固体 |
| 颜色 | 白色至类白色 |
| 水溶解性 | Soluble to 100 mM in water |
SIB-1553A 是一种口服生物有效的烟碱乙酰胆碱受体 (nAChRs) 激动剂，对含有 nAChRs 的 β4 亚单位具有选择性。SIB-1553A 也是一种选择性配体神经元 nAChR 配体。SIB-1553A 是一种认知增强剂，对阿尔茨海默病和其他认知障碍的症状研究具有潜在的研究潜力。
SIB-1553A displaces the binding of
[H]
nicotine (NIC) to the rat brain nAChRs with an IC
50
value of 110 nM.
In calcium flux assays, SIB-1553A (0.1-5 μM), shows a greater selectivity for beta4-subunit containing recombinant hnAChRs (alpha2beta4, alpha3beta4 and alpha4beta4) vs. beta2-subunit containing nAChRs (alpha4beta2 and alpha3beta2) both in terms of efficacy and potency.
SIB-1553A (1-40 mg/kg; s.c.) produces dose-dependent increases in ACh levels.
| Animal Model: | Male Sprague-Dawley rats (200-250 g) |
| Dosage: | 1, 2, 4, 10, 20 and 40 mg/kg |
| Administration: | s.c. |
| Result: | Induced hippocampal ACh release. |