诺美林草酸盐

生物活性靶点体外研究体内研究诺美林草酸盐试剂级价格

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

诺美林草酸盐化学性质

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。
靶点

muscarinic receptor
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.