107220-28-0
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
英文名稱
Cevimeline Hydrochloride Salt
CAS
107220-28-0
分子式
C10H18ClNOS
分子量
235.774
MOL 文件
107220-28-0.mol
更新日期
2024/12/31 09:16:58
107220-28-0 結(jié)構(gòu)式
基本信息
中文別名
西維美林-D4鹽酸鹽鹽 英文別名
SNK 508Fks 508
Snd 5008
Saligren
CeviMelin
rac-Cevimeline HCl
AF-102B hydrochloride
SNI-2011 hydrochloride
Cevimelin Hydrochloride
CEVIMELINE, HYDROCHLORIDE SALT
所屬類別
生物化工：激動劑抑制劑物理化學(xué)性質(zhì)
熔點195-197?C
儲存條件Inert atmosphere,Store in freezer, under -20°C
溶解度Water:50.0(Max Conc. mg/mL);212.07(Max Conc. mM)
形態(tài)結(jié)晶固體
顏色White to off-white
穩(wěn)定性吸濕性
安全數(shù)據(jù)
警示詞危險
危險性描述H301
毒性mouse,LD50,intravenous,33mg/kg (33mg/kg),United States Patent Document. Vol. #4855290,
常見問題列表
生物活性
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。靶點
Muscarinic M1 and M3 receptor
體外研究
In digested parotid cells, Cevimeline (0.1-100 μM) increases the intracellular Ca 2+ concentration.
體內(nèi)研究
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. |