中文名称: N-去甲基氯氮平
英文名称: N-Desmethylclozapine
CAS No: 6104-71-8
分子式: C17H17ClN4
分子量: 312.8
D11122 N-去甲基氯氮平 ≥98% (psaitong)
包装规格:
10mg 50mg 250mg in glass bottle
溶解性:
溶于(DMS:≥50mg/mL)
产品描述:

基本信息

产品编号:

D11122

产品名称:

N-Desmethylclozapine

CAS:

6104-71-8

 

储存条件

粉末

-20℃

四年

 

 

分子式:

C17H17ClN4

溶于液体

-80℃

6个月

分子量:

312.80

-20℃

1个月

化学名: 

N-Desmethylclozapine solution,1.0 mg/mL in methanol,ampule of 1mL,certified reference material

Solubility (25°C):

 

体外:

 

DMSO

 

Ethanol

 

Water

 

体内(现配现用):

 

1mg/ml表示微溶或不溶。

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。

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.

保存条件:
-20℃
UN码:
HazardClass:
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