NORCLOZAPINE
N-Desmethyl Clozapine
CAS: 6104-71-8
Molecular Formula: C17H17ClN4
NORCLOZAPINE - Names and Identifiers
NORCLOZAPINE - Physico-chemical Properties
| Molecular Formula | C17H17ClN4 |
| Molar Mass | 312.8 |
| Density | 1.38±0.1 g/cm3(Predicted) |
| Melting Point | 120-125°C |
| Boling Point | 502.6±60.0 °C(Predicted) |
| Flash Point | 9℃ |
| Solubility | Chloroform (Slightly), DMSO, Methanol (Slightly) |
| Appearance | Yellow solid. |
| Color | Light Yellow to Yellow |
| pKa | 8.49±0.10(Predicted) |
| Storage Condition | Store at RT |
| Physical and Chemical Properties | Bioactive N-Desmethylclozapine are the main active metabolites of atypical antipsychotic Clozapine. N-Desmethylclozapine is an effective, allosteric partial M1 receptor agonist (EC50=115 nM), which can enhance hippocampal N-methyl-d-aspartate (NMDA) receptor current through M1 receptor activation. N-Desmethylclozapine are also δ-opioid agonists. |
NORCLOZAPINE - Risk and Safety
| Risk Codes | R20/22 - Harmful by inhalation and if swallowed. R36/37/38 - Irritating to eyes, respiratory system and skin. R39/23/24/25 - R23/24/25 - Toxic by inhalation, in contact with skin and if swallowed. R11 - Highly Flammable |
| Safety Description | S22 - Do not breathe dust. S36 - Wear suitable protective clothing. S45 - In case of accident or if you feel unwell, seek medical advice immediately (show the label whenever possible.) S36/37 - Wear suitable protective clothing and gloves. S16 - Keep away from sources of ignition. S7 - Keep container tightly closed. |
| UN IDs | 3249 |
| WGK Germany | 3 |
| Hazard Class | 6.1(b) |
| Packing Group | III |
NORCLOZAPINE - Upstream Downstream Industry
NORCLOZAPINE - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 3.197 ml | 15.985 ml | 31.969 ml |
| 5 mM | 0.639 ml | 3.197 ml | 6.394 ml |
| 10 mM | 0.32 ml | 1.598 ml | 3.197 ml |
| 5 mM | 0.064 ml | 0.32 ml | 0.639 ml |
Last Update：2024-01-02 23:10:35
NORCLOZAPINE - Uses and synthesis methods
Target
EC50: 115 nM (M1 receptors)
δ-opioid
in vitro studies
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.
In vivo studies
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.
Last Update：2024-04-09 21:04:16
Supplier List
Spot supply
Product Name: Clozapine Impurity 3(Clozapine EP Impurity C) Visit Supplier Webpage Request for quotationCAS: 6104-71-8
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Spot supply
Product Name: Clozapine Impurity 3(Clozapine EP Impurity C) Visit Supplier Webpage Request for quotationCAS: 6104-71-8
Tel: 0714-3999186
Email: 2853786052@qq.com
Mobile: 86+15671228036
QQ: 2853786052
Wechat: 15671228036
Spot supply
Product Name: N-Desmethyl Clozapine Visit Supplier Webpage Request for quotationCAS: 6104-71-8
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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Raw Materials for NORCLOZAPINE