((+/-)-顺式-2-甲基螺[1,3-氧硫杂环戊烷-5,3'-奎宁环]盐酸半水合物
| 中文名称 | ((+/-)-顺式-2-甲基螺[1,3-氧硫杂环戊烷-5,3'-奎宁环]盐酸半水合物 |
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| 中文同义词 | 西维美林-D4盐酸盐盐 |
| 英文名称 | Cevimeline Hydrochloride Salt |
| 英文同义词 | CEVIMELINE, HYDROCHLORIDE SALT;Fks 508;Saligren;Snd 5008;cis-2-Methylspiro[1,3-oxathiolane-5,3'-quinuclidine]hydrochloride;(2'R,3R)-rel-2'-Methyl- spiro[1-azabicyclo[2.2.2]octane-3,5'-[1,3]oxathiolane] hydrochloride;SNK 508;CeviMelin |
| CAS号 | 107220-28-0 |
| 分子式 | C10H18ClNOS |
| 分子量 | 235.77402 |
| EINECS号 | |
| 相关类别 | Heterocycles;Intermediates & Fine Chemicals;Neurochemicals;Pharmaceuticals;API |
| Mol文件 | 107220-28-0.mol |
| 结构式 | ![((+/-)-顺式-2-甲基螺[1,3-氧硫杂环戊烷-5,3'-奎宁环]盐酸半水合物 结构式](CAS/GIF/107220-28-0.gif) |
((+/-)-顺式-2-甲基螺[1,3-氧硫杂环戊烷-5,3'-奎宁环]盐酸半水合物 性质
| 熔点 | 195-197?C |
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| 储存条件 | Inert atmosphere,Store in freezer, under -20°C |
| 溶解度 | 水：50.0（最大浓度 mg/mL）；212.07（最大浓度 mM） |
| 形态 | 结晶固体 |
| 稳定性 | 吸湿性 |
Cevimeline hydrochloride (AF102B hydrochloride) 是一种乙酰胆碱的奎尼丁衍生物，也是一种选择性的和口服活性的毒蕈碱型 M1 和 M3 受体激动剂。Cevimeline hydrochloride 可刺激唾液腺分泌，并可用作口干症的一种催涎剂。Cevimeline hydrochloride 可穿过血脑屏障。
Muscarinic M1 and M3 receptor
In digested parotid cells, Cevimeline (0.1-100 μM) increases the intracellular Ca 2+ concentration.
Cevimeline (0.008-0.016 mg/kg; intraperitoneal injection; male Wistar rats) treatment shows slowly increasing and lasting salivation, and increased blood flow increment in the parotid gland and pressor response. Cevimeline inhibits angiotensin II-induced water intake and neuronal activity in the subfornical organ at 0.016 mg/kg.
| Animal Model: | Male Wistar rats (8-week-old) injected with angiotensin-II |
| Dosage: | 0.008 mg/kg, 0.016 mg/kg |
| Administration: | Intraperitoneal injection |
| Result: | Showed slowly increasing and lasting salivation, and increased blood flow increment in the parotid gland and pressor response. |
安全信息
| 毒性 | mouse,LD50,intravenous,33mg/kg (33mg/kg),United States Patent Document. Vol. #4855290, |
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