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Purity: ≥98%
Norclozapine (ACP-104; NDMC; ACP104; N-Desmethylclozapine) is a major active metabolite of the atypical antipsychotic drug clozapine. It functions as a mild partial agonist at the D2 and D3 receptors, just like aripiprazole and bifeprunox, in contrast to clozapine, which lacks this intrinsic activity. It is a dopamine/muscarinic/5-HT2A inverse agonist that may be used to treat schizophrenia. N-desmethylclozapine functions as both an agonist and an inhibitor of the dengue virus receptor.
| Targets |
δ Opioid Receptor/DOR; mAChR1
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|---|---|
| ln Vitro |
N-desmethylclozapine, a brain penetrant metabolite, was found to bind to M1 muscarinic receptors preferentially, with an IC50 of 55 nM. Compared to clozapine, it was a more potent partial agonist at this receptor, with an EC50 of 115 nM and 50% of acetylcholine response[1].
N-desmethylclozapine has agonistic characteristics at the 5-HT1A receptor in the cerebral cortex and hippocampus, as well as mild agonistic effects on the M1 mAChR. Additionally, this substance exhibits agonistic behavior at the δ-opioid receptor located in the striatum and cerebral cortex[2]. N-desmethylclozapine (3 μM) significantly reduces excitatory neurons' outward current, but not that of inhibitory neurons. When it comes to excitatory neurons, N-desmethylclozapine works better on its own than it does when combined with clozapine or taken alone. One microgram of atropine and 0.1 microgram of pirenzepine both considerably reduce the effects of N-desmethylclozapine on excitatory neurons. In excitatory cells, K125 channels were inhibited by N-desmethylclozapine but not by clozapine via M1 receptors[3]. N-desmethylclozapine causes TxB2 levels to drop both in response to TSST-1 stimulation and in unstimulated conditions. The production of TxA2 or TxB2 may be modulated by clozapine, N-desmethylclozapine, and CPZ, potentially affecting neurotransmitter systems[5]. N-desmethylclozapine, fluoxetine hydrochloride, and salmeterol xinafoate have IC50 values of 1 μM, 0.38 μM, and 0.67 μM in Huh-7 cells infected with DENV-2, respectively. When cells treated with all three inhibitors are compared to those treated with DMSO, the levels of NS3 are lower, indicating that the inhibitors function at a stage before the translation of viral proteins. Negative-strand RNA levels are reduced by >75% in cells treated with N-desmethylclozapine[6]. |
| ln Vivo |
N-desmethylclozapine underlies presynaptic modulation of glutamate release and GABA in humans and rats at M2 and M4 mAChRs, respectively. N-desmethylclozapine, for example, may be an M2 mAChR antagonist in rats, but it is not active at this receptor in the human neocortex. On the other hand, N-desmethylclozapine does not have an agonistic effect at M4 mAChR in the rat neocortex[4].
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| References |
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| Molecular Formula |
C17H17CLN4
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|---|---|
| Molecular Weight |
312.797
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| Exact Mass |
312.11
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| Elemental Analysis |
C, 65.28; H, 5.48; Cl, 11.33; N, 17.91
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| CAS # |
6104-71-8
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| Related CAS # |
N-Desmethylclozapine-d8; 1189888-77-4; N-Desmethylclozapine-d8 hydrochloride; 2705402-91-9
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| Appearance |
Solid powder
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| SMILES |
C1CN(CCN1)C2=NC3=C(C=CC(=C3)Cl)NC4=CC=CC=C42
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| InChi Key |
JNNOSTQEZICQQP-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H17ClN4/c18-12-5-6-15-16(11-12)21-17(22-9-7-19-8-10-22)13-3-1-2-4-14(13)20-15/h1-6,11,19-20H,7-10H2
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| Chemical Name |
3-chloro-6-piperazin-1-yl-11H-benzo[b][1,4]benzodiazepine
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| Synonyms |
AZD-5991; AZD-5991 S-enantiomer; AZD 5991 S-enantiomer.
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ≥ 50 mg/mL (~159.9 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.99 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (7.99 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.1969 mL | 15.9847 mL | 31.9693 mL | |
| 5 mM | 0.6394 mL | 3.1969 mL | 6.3939 mL | |
| 10 mM | 0.3197 mL | 1.5985 mL | 3.1969 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT00628420 | Completed | Drug: ACP-104 Drug: Placebo |
Schizophrenia | University of Texas Southwestern Medical Center |
January 2005 | Phase 1 |
| NCT00490516 | Completed | Drug: ACP-104 Drug: Placebo |
Schizophrenia | ACADIA Pharmaceuticals Inc. | June 2007 | Phase 2 |
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