诺美林草酸盐
中文名称 | 诺美林草酸盐 |
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中文同义词 | 诺美林草酸盐;草酸占诺美林;呫诺美林草酸盐;化合物 T13353;占诺美林 草酸盐;XANOMELINE OXALATE 诺美林草酸盐 |
英文名称 | 3-[4-(Hexyloxy)-1,2,5-thiadiazol-3-yl]-1,2,5,6-tetrahydro-1-methylpyridineoxalate |
英文同义词 | 3-[4-(Hexyloxy)-1,2,5-thiadiazol-3-yl]-1,2,5,6-tetrahydro-1-methylpyridine ethanedioate (1:1);3-[4-(Hexyloxy)-1,2,5-thiadiazol-3-yl]-1,2,5,6-tetrahydro-1-methylpyridineoxalate;Xanomeline oxalate;3-(3-Hexyloxy-1,2,5-thiadiazol-4-yl)-1,2,5,6-tetrahydro-1-methylpyridine oxalate;Lumeron;LY246708;MEMCOR;LUMERON;LY246708 oxalate;Xanomeline oxalate salt |
CAS号 | 141064-23-5 |
分子式 | C14H23N3OS.C2H2O4 |
分子量 | 371 |
EINECS号 | |
相关类别 | 1 |
Mol文件 | 141064-23-5.mol |
结构式 | ![]() |
诺美林草酸盐 性质
熔点 | 148-150℃ |
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储存条件 | Desiccate at +4°C |
溶解度 | DMF:1.6mg/mL; DMF:PBS (pH 7.2) (1:9):0.1 mg/mL |
形态 | 粉末 |
颜色 | 白色至米白色 |
muscarinic receptor
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.
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. |
安全信息
更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
---|---|---|---|---|---|
2024/04/30 | HY-13410 | Xanomeline oxalate | 1 mg | 290元 | |
2024/04/30 | HY-13410 | 诺美林草酸盐 Xanomeline oxalate | 141064-23-5 | 10mM * 1mLin DMSO | 770元 |