1. GPCR/G Protein
    Neuronal Signaling
    Metabolic Enzyme/Protease
    Anti-infection
  2. mAChR
    Opioid Receptor
    Drug Metabolite
    Virus Protease
  3. N-Desmethylclozapine

N-Desmethylclozapine (Synonyms: Norclozapine; Desmethylclozapine; Normethylclozapine)

Cat. No.: HY-G0021 Purity: 99.72%
Handling Instructions

N-Desmethylclozapine is a major active metabolite of the atypical antipsychotic drug Clozapine. N-Desmethylclozapine is a potent, allosteric and partial M1 receptors agonist (EC50=115 nM) and is able to potentiate hippocampal N-methyl-d-aspartate (NMDA) receptor currents through M1 receptor activation. N-Desmethylclozapine is also a δ-opioid agonist.

For research use only. We do not sell to patients.

N-Desmethylclozapine Chemical Structure

N-Desmethylclozapine Chemical Structure

CAS No. : 6104-71-8

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 106 In-stock
Estimated Time of Arrival: December 31
5 mg USD 96 In-stock
Estimated Time of Arrival: December 31
10 mg USD 168 In-stock
Estimated Time of Arrival: December 31
25 mg USD 360 In-stock
Estimated Time of Arrival: December 31
50 mg   Get quote  
100 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

N-Desmethylclozapine is a major active metabolite of the atypical antipsychotic drug Clozapine. N-Desmethylclozapine is a potent, allosteric and partial M1 receptors agonist (EC50=115 nM) and is able to potentiate hippocampal N-methyl-d-aspartate (NMDA) receptor currents through M1 receptor activation. N-Desmethylclozapine is also a δ-opioid agonist[1][2].

IC50 & Target

EC50: 115 nM (M1 receptors)[1]
δ-opioid[2]

In Vitro

The brain penetrant metabolite N-desmethylclozapine preferentially bound to M1 muscarinic receptors with an IC50 of 55 nM and was a more potent partial agonist (EC50, 115 nM and 50% of acetylcholine response) at this receptor than clozapine[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].
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[6].

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].

Molecular Weight

312.80

Formula

C₁₇H₁₇ClN₄

CAS No.

6104-71-8

SMILES

ClC1=CC=C2C(N=C(N3CCNCC3)C4=CC=CC=C4N2)=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 50 mg/mL (159.85 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (7.99 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (7.99 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

N-DesmethylclozapineNorclozapineDesmethylclozapineNormethylclozapinemAChROpioid ReceptorDrug MetaboliteVirus ProteaseMuscarinic acetylcholine receptorInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product name

 

Salutation

Applicant name *

 

Email address *

Phone number *

 

Organization name *

Country or Region *

 

Requested quantity *

Remarks

Bulk Inquiry

Inquiry Information

Product name:
N-Desmethylclozapine
Cat. No.:
HY-G0021
Quantity:
MCE Japan Authorized Agent: