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编 号:F153194
分子式:C16H25N3O5S
分子量:371.45
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10mM*1mL in DMSO
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1mg
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5mg
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10mg
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50mg
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100mg
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生物活性:
Xanomeline oxalate (LY246708 oxalate) is a potent and selective muscarinic receptor agonist (SMRA) and stimulates phosphoinositide hydrolysis in vivo. Xanomeline oxalate can be used for the research of Alzheimer’s disease.

体内研究:
Xanomeline oxalate 强烈刺激体内 PI 水解,并且该作用被毒蕈碱拮抗剂阻断,表明由毒蕈碱受体介导。在小鼠中,Xanomeline oxalate 诱导的海马体中 [3H]-IP 积累的 ED100 在为 54 μMole/kg。在大鼠中,Xanomeline oxalate 诱导的海马体中 [3H]-IP 积累的 ED100 为 8.1 μMole/kg。Animal Model:Male CF1 mice weighing 18-20 g are injected [3H]-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 [3H]-IP in the brain stem.Induced salivation, tremor and hypothermia in mice with the ED50 of 13.7±0.8 μmole/kg.
Animal Model:Rats are injected [3H]-myoinositol
Dosage:2.7-81 μmole/kg
Administration:S.c. injections; 1 h prior to killing and 1 h after the administration
Result:Increased [3H]-IP formation dose dependently in hippocampus up to 221% above lithium control.

体外研究:
Xanomeline oxalate 刺激 A9 L m1 细胞中的磷酸肌醇 (PI) 水解。 Xanomeline oxalate 抑制[3H]-pirenzepine ([3H]-PZ) 和[3H]-oxotremorine-M ([3H]-OXO-M) 结合大鼠大脑的 Ki 分别为 7 和 3 nM。
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