141064-23-5
141064-23-5 結(jié)構(gòu)式
基本信息
諾美林草酸鹽
呫諾美林草酸鹽
LY246708 oxalate
Xanomeline oxalate
Xanomeline oxalate salt
LY246708
MEMCOR
LUMERON
3-(3-Hexyloxy-1,2,5-thiadiazol-4-yl)-1,2,5,6-tetrahydro-1-methylpyridine oxalate
3-[4-(Hexyloxy)-1,2,5-thiadiazol-3-yl]-1,2,5,6-tetrahydro-1-methylpyridineoxalate
3-[4-(Hexyloxy)-1,2,5-thiadiazol-3-yl]-1,2,5,6-tetrahydro-1-methylpyridine ethanedioate (1:1)
物理化學(xué)性質(zhì)
常見(jiàn)問(wèn)題列表
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. |