中文名称: | N-去甲基氯氮平 | ||||
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英文名称: | N-Desmethylclozapine | ||||
别名: | N-去甲基氯氮平 Norclozapine; Desmethylclozapine; Normethylclozapine | ||||
CAS No: | 6104-71-8 | 分子式: | C17H17ClN4 | 分子量: | 312.8 |
CAS No: | 6104-71-8 | ||||
分子式: | C17H17ClN4 | ||||
分子量: | 312.8 |
基本信息
产品编号: |
D11122 |
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产品名称: |
N-Desmethylclozapine |
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CAS: |
6104-71-8 |
储存条件 |
粉末 |
-20℃ |
四年 |
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分子式: |
溶于液体 |
-80℃ |
6个月 |
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分子量: |
312.80 |
-20℃ |
1个月 |
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化学名: |
N-Desmethylclozapine solution,1.0 mg/mL in methanol,ampule of 1mL,certified reference material |
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Solubility (25°C): |
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体外:
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DMSO |
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Ethanol |
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Water |
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体内(现配现用): |
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<1mg/ml表示微溶或不溶。 |
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普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。 |
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请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;⼀旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 |
制备储备液
浓度
溶液体积 质量 |
1mg |
5mg |
10mg |
1mM |
3.1969mL |
15.9847mL |
31.9693mL |
5mM |
0.6394mL |
3.1969mL |
6.3939mL |
10mM |
0.3197mL |
1.5985mL |
3.1969mL |
生物活性
产品描述 |
一种非典型抗精神病药 Clozapine 的主要活性代谢产物。N-Desmethylclozapine 是一种有效的、变构的部分 M1 受体激动剂 (EC50=115nM)能通过 M1 受体激活增强海马 N-methyl-d-aspartate (NMDA) 受体电流。N-Desmethylclozapine 也是 δ-opioid 激动剂。 |
靶点 |
EC50:115nM (M1 receptors)δ-opioid |
体外研究 |
The brain penetrant metabolite N-desmethylclozapine preferentially bound to M1 muscarinic receptors with an IC50 of 55nM and was a more potent partial agonist (EC50,115nM and 50% of acetylcholine response) at this receptor than clozapine.N-desmethylclozapine exhibits slight agonistic effects on the M1 mAChR,and agonistic properties at the 5-HT1A receptor in the cerebral cortex and hippocampus.This compound also behaves as an agonist at the δ-opioid receptor in the cerebral cortex and striatum.N-desmethylclozapine (3μM) greatly decreases the outward current in excitatory neurons,but not in inhibitory neurons.In excitatory neurons,N-desmethylclozapine alone is more effective than either clozapine alone or the combination of clozapine and N-desmethylclozapine.The effect of N-desmethylclozapine in excitatory neurons is significantly suppressed by 0.1μM pirenzepine and 1μM atropine.N-desmethylclozapine,but not clozapine,suppressed K+channels via M1 receptors in excitatory cells.N-desmethylclozapine leads to a decrease in TxB2 levels under unstimulated conditions as well as under TSST-1 stimulation.Clozapine,N-desmethylclozapine and CPZ possibly act on neurotransmitter systems via modulation of TxA2 or TxB2 production.The IC50s of N-desmethylclozapine,fluoxetine hydrochloride,and salmeterol xinafoate in Huh-7 cells infected with DENV-2 are 1μM,0.38μM,and 0.67μM,respectively.The levels of NS3 are reduced in cells treated with all three inhibitors compared to DMSO treatment,suggesting that the inhibitors act at a stage prior to viral protein translation.N-Desmethylclozapinetreated cells show a >75% reduction in negative-strand RNA levels. |
体内研究 |
N-desmethylclozapine in rat and human at M2 and M4 mAChRs underlying presynaptic modulation of GABA and glutamate release,respectively.In particular,N-desmethylclozapine maybe a M2 mAChR antagonist in the rat but has no activity at this receptor in human neocortex.However,N-desmethylclozapine has an agonistic effect at M4 mAChR in the human but no such effect in the rat neocortex. |
本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液,使用的计算公式为:
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为:C1V1 = C2V2 ( 输入 输出 )