6104-71-8
基本信息
N-去甲氯氮平
氯氮平EP杂质C
N-去甲基氯氮平
N-去甲基氣氮平
氯羟喹杂质C(EP)
氯氮平杂质C(EP)
去甲氯氮平溶液,100PPM
8-氯-11-(1-哌嗪基)-5H-二苯并[B,E] [1,4]吡喃
8-氯-11-(1-哌嗪基)-5H-二苯并[B,E] [1,4]二氮杂卓
物理化学性质
| 熔点 | 120-125°C |
| 沸点 | 502.6±60.0 °C(Predicted) |
| 密度 | 1.38±0.1 g/cm3(Predicted) |
| 闪点 | 9℃ |
| 储存条件 | Store at RT |
| 溶解度 | 可溶于氯仿（少许）、DMSO、甲醇（少许） |
| 酸度系数(pKa) | 8.49±0.10(Predicted) |
| 形态 | 黄色固体 |
| 颜色 | 淡黄色至黄色 |
| CAS 数据库 | 6104-71-8(CAS DataBase Reference) |
安全数据
| 危险性符号(GHS) |  GHS07 |
| 警示词 | 警告 |
| 危险性描述 | H302+H332-H315-H319-H335 |
| 防范说明 | P261-P264-P301+P312-P302+P352-P304+P340+P312-P305+P351+P338 |
| 危险品标志 | Xn,T,F |
| 危险品标志 | Xn |
| 危险类别码 | 20/22-36/37/38-39/23/24/25-23/24/25-11 |
| 危险类别码 | R20/22-R36/37/38 |
| 安全说明 | 22-36-45-36/37-16-7 |
| 安全说明 | S22-S36-S45 |
| 危险品运输编号 | 3249 |
| WGK Germany | 3 |
| WGK Germany | 3 |
| 危险等级 | 6.1(b) |
| 包装类别 | III |
知名试剂公司产品信息
常见问题列表
EC50: 115 nM (M1 receptors)
δ-opioid
The brain penetrant metabolite N-desmethylclozapine preferentially bound to M1 muscarinic receptors with an IC
50
of 55 nM and was a more potent partial agonist (EC
50
, 115 nM 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 (3 μM) 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 0.1 μM pirenzepine and 1 μM 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 IC
50
s of N-desmethylclozapine, fluoxetine hydrochloride, and salmeterol xinafoate in Huh-7 cells infected with DENV-2 are 1 μM, 0.38 μM, and 0.67 μM, 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-Desmethylclozapine-treated cells show a >75% reduction in negative-strand RNA levels.
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.