677305-02-1
中文名称
S-Facinicline
英文名称
S-Facinicline
CAS
677305-02-1
分子式
C15H19ClN4O
分子量
306.791
MOL 文件
677305-02-1.mol
677305-02-1 结构式
基本信息
中文别名
化合物 RG3487 HYDROCHLORIDE 英文别名
RG3487S-Facinicline
RG3487 hydrochloride
Facinicline hydrochloride
物理化学性质
储存条件-20°C储存
溶解度DMSO: 125 mg/mL (407.44 mM); Methanol: 25 mg/mL (81.49 mM)
形态Solid
颜色White to off-white
常见问题列表
生物活性
Facinicline hydrochloride (RG3487 hydrochloride) 是具有口服活性的烟碱 α7 receptor 部分激动剂，对人nAChR 的 Ki 值为 6 nM。Facinicline hydrochloride (RG3487 hydrochloride) 可改善啮齿类动物的认知和感觉运动门控。Facinicline hydrochloride (RG3487 hydrochloride) 对5-HT3 受体 (拮抗剂)的Ki 值为 1.2 nM。靶点
|
5-HT 3 Receptor 1.2 nM (Ki) |
α7 6 nM (Ki) |
体外研究
Facinicline (RG3487) activates human α7 nAChRs with an EC
50
of 0.8 μM (oocytes) and 7.7 μM (QM7 cells).
Facinicline (RG3487) exhibits antagonist properties at the serotonin 3 receptor (IC
50
2.8 nM (oocytes), 32.7 nM (N1E-115 cells)).
体内研究
Facinicline (RG3487) improves object recognition memory in rats after acute [minimally effective dose (MED) 1.0 mg/kg p.o.] or repeated (10 day) administration at brain and plasma concentrations in the low-nanomolar range.
RG3487 (0.1–10 mg/kg p.o.) selectively enhances object recognition memory.
| Animal Model: | Male Sprague-Dawley rats. |
| Dosage: | 0.1-10 mg/kg (Pharmacokinetic Analysis). |
| Administration: | Orally. |
| Result: | The mean C max was typically observed between 0.5 and 4 h. |