Name | N-desmethylclozapine |
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Synonyms |
3-chloro-6-piperazin-1-yl-5H-benzo[b][1,4]benzodiazepine
Normethylclozapine BzATP triethylammonium salt Desmethylclozapine EINECS 200-659-6 Demethylclozapine N-Demethylclozapine MFCD00210189 N-desmethyl clozapine Norclozapine |
Description | N-Desmethylclozapine is a dengue virus inhibitor, and an agonist of δ-opioid receptor. |
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Related Catalog | |
In Vitro | The IC50s 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[1]. 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[2]. 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[3]. 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[5]. |
In Vivo | 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[4]. |
References |
Density | 1.38g/cm3 |
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Boiling Point | 490.1ºC at 760 mmHg |
Melting Point | 120-125°C |
Molecular Formula | C17H17ClN4 |
Molecular Weight | 312.79700 |
Flash Point | 250.2ºC |
Exact Mass | 312.11400 |
PSA | 39.66000 |
LogP | 3.22080 |
Index of Refraction | 1.709 |
Storage condition | Store at RT |
Symbol |
GHS02, GHS06, GHS08 |
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Signal Word | Danger |
Hazard Statements | H225-H301 + H311 + H331-H370 |
Precautionary Statements | P210-P260-P280-P301 + P310-P311 |
Personal Protective Equipment | dust mask type N95 (US);Eyeshields;Gloves |
Hazard Codes | Xn |
Risk Phrases | 20/22-36/37/38 |
Safety Phrases | S22-S36-S45 |
RIDADR | 3249 |
WGK Germany | 3 |
Packaging Group | III |
Hazard Class | 6.1(b) |
HS Code | 2933990090 |
Precursor 7 | |
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DownStream 0 |
HS Code | 2933990090 |
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Summary | 2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0% |