诺美林草酸盐
- CAS号:141064-23-5
- 英文名:3-[4-(Hexyloxy)-1,2,5-thiadiazol-3-yl]-1,2,5,6-tetrahydro-1-methylpyridineoxalate
- 中文名:诺美林草酸盐
- CBNumber:CB12518809
- 分子式:C14H23N3OS.C2H2O4
- 分子量:371
- MOL File:141064-23-5.mol
- 熔点 :148-150℃
- 储存条件 :Desiccate at +4°C
- 溶解度 :DMF: 1.6 mg/ml; DMF:PBS (pH 7.2) (1:9): 0.1 mg/ml
- 形态 :Powder
- 颜色 :White to off-white
诺美林草酸盐性质、用途与生产工艺
- 生物活性 Xanomeline oxalate (LY246708 oxalate) 是一种有效的、选择性毒蕈碱受体激动剂 (SMRA)，可刺激体内的磷酸肌醇水解。 Xanomeline oxalate 可用于研究阿尔茨海默氏病。
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靶点
muscarinic receptor
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体外研究
Xanomeline stimulates phosphoinositide (PI) hydrolysis in the A9 L m1 cells.
Xanomeline inhibits [ 3 H]-pirenzepine ([ 3 H]-PZ) and [ 3 H]- oxotremorine -M ([ 3 H]-OXO-M) binding to rat brain with K i s of 7 and 3 nM, respectively. -
体内研究
Xanomeline robustly stimulates in vivo PI hydrolysis and the effect is blocked by muscarinic antagonists, demonstrating mediation by muscarinic receptors. In mice the ED 100 for Xanomeline-induced stimulation of [ 3 H]-IP accumulation is 54 μmole/kg in hippocampus. And in rats the ED 100 for Xanomeline-induced stimulation of [ 3 H]-IP accumulation is 8.1 μmole/kg in hippocampus.
Animal Model: Male CF1 mice weighing 18-20 g are injected [ 3 H]-myoinositol Dosage: 8.1-81 μmole/kg Administration: S.c. injections; 1 h prior to killing and 1 h after the administration Result: Increased accumulation in a dose-related manner up to 130%, 75%, 60% above lithium levels in hippocampus, cortex and neostriatum, respectively. And did not increase accumulation of [ 3 H]-IP in the brain stem. Induced salivation, tremor and hypothermia in mice with the ED 50 of 13.7±0.8 μmole/kg. Animal Model: Rats are injected [ 3 H]-myoinositol Dosage: 2.7-81 μmole/kg Administration: S.c. injections; 1 h prior to killing and 1 h after the administration Result: Increased [ 3 H]-IP formation dose dependently in hippocampus up to 221% above lithium control.
- 更新日期：2024/11/08
- 产品编号：HY-13410
- 产品名称：Xanomeline oxalate
- CAS编号：
- 包装：1 mg
- 价格：290元
- 更新日期：2024/11/08
- 产品编号：HY-13410
- 产品名称：诺美林草酸盐 Xanomeline oxalate
- CAS编号：141064-23-5
- 包装：5mg
- 价格：700元
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