((+/-)-順式-2-甲基螺[1,3-氧硫雜環(huán)戊烷-5,3'-奎寧環(huán)]鹽酸半水合物
| 中文名稱 | ((+/-)-順式-2-甲基螺[1,3-氧硫雜環(huán)戊烷-5,3'-奎寧環(huán)]鹽酸半水合物 |
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| 中文同義詞 | 西維美林-D4鹽酸鹽鹽;((+/-)-順式-2-甲基螺[1,3-氧硫雜環(huán)戊烷-5,3'-奎寧環(huán)]鹽酸半水合物;REL-(2R,3'R)-2-甲基-1'-氮雜螺[[1,3]氧硫雜環(huán)戊烷-5,3'-雙環(huán)[2.2.2]辛烷]鹽酸鹽;CEVIMELINE HYDROCHLORIDE,M1 AND M3 RECEPTOR激動劑 |
| 英文名稱 | Cevimeline Hydrochloride Salt |
| 英文同義詞 | 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號 | 107220-28-0 |
| 分子式 | C10H18ClNOS |
| 分子量 | 235.77402 |
| EINECS號 | |
| 相關類別 | Heterocycles;Intermediates & Fine Chemicals;Neurochemicals;Pharmaceuticals;API |
| Mol文件 | 107220-28-0.mol |
| 結構式 | ![((+/-)-順式-2-甲基螺[1,3-氧硫雜環(huán)戊烷-5,3'-奎寧環(huán)]鹽酸半水合物 結構式](CAS/GIF/107220-28-0.gif) |
((+/-)-順式-2-甲基螺[1,3-氧硫雜環(huán)戊烷-5,3'-奎寧環(huán)]鹽酸半水合物 性質
| 熔點 | 195-197?C |
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| 儲存條件 | Inert atmosphere,Store in freezer, under -20°C |
| 溶解度 | 水：50.0（最大濃度 mg/mL）；212.07（最大濃度 mM） |
| 形態(tài) | 結晶固體 |
| 顏色 | 白色至米白色 |
| 穩(wěn)定性 | 吸濕性 |
Cevimeline hydrochloride (AF102B hydrochloride) 是一種乙酰膽堿的奎尼丁衍生物，也是一種選擇性的和口服活性的毒蕈堿型 M1 和 M3 受體激動劑。Cevimeline hydrochloride 可刺激唾液腺分泌，并可用作口干癥的一種催涎劑。Cevimeline hydrochloride 可穿過血腦屏障。
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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