N-Desmethylclozapine

SKU: orb1302043

Description

N-Desmethylclozapine is a bioactive metabolite of clozapine, functioning as a potent 5-HT2C receptor antagonist (IC50: 7.1 nM), a dopamine D4 receptor antagonist, and a δ-opioid receptor agonist. It is a valuable research tool for investigating neuropsychiatric disorders and receptor pharmacology in both in vitro and in vivo experimental models.

Research Area

Infectious Disease & Virology, Metabolism Research, Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 6104-71-8
• MW: 312.8
• Purity: 99.83% (May vary between batches)
• Formula: C₁₇H₁₇ClN₄
• SMILES: Clc1ccc2N=c3ccccc3=C(Nc2c1)N1CCNCC1
• Target: Virus Protease,Drug Metabolite,5-HT Receptor,Dopamine Receptor,Opioid Receptor,AChR
• Solubility: DMSO:125 mg/mL (399.62 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (6.39 mM);Ethanol:30 mg/mL (95.91 mM)

Bioactivity

• Target IC50:
  5-HT2C:7.1 nM
• In Vivo:
  NDMC (3-30mg/kg) decreased exploratory locomotor activity in a dose-dependent manner, and the reduced locomotor activity was significantly antagonized by scopolamine at doses of 0.1 and 0.3mg/kg. NDMC (10-30mg/kg) dose-dependently increased prepulse inhibition (PPI) in DBA/2J mice .
• In Vitro:
  N-desmethylclozapine antagonized 5-HT-stimulated phosphoinositide hydrolysis with IC50 values of 29.4 nM . N-desmethylclozapine exhibited slight agonistic effects on the M1 mAChR and agonistic properties at the 5-HT1A receptor in the cerebral cortex and hippocampus. This compound also behaved as an agonist at the δ-opioid receptor in the cerebral cortex and the striatum . Muscarinic agonist activity of N-desmethylclozapine was higher than that of clozapine, higher in excitatory neurons than in inhibitory neurons, sensitive to pirenzepine, and partially masked when co-applied with clozapine .
• Animal Research:
  Exploratory locomotor activity was monitored as described previously. Animals were habituated to the experimental room for at least 60 min before testing. Oxotremorine (0.01, 0.03, 0.1 mg/kg, s.c.), NDMC (3, 10, 30 mg/kg, s.c.), xanomeline (0.3, 1, 3 mg/kg, s.c.), or scopolamine (0.1, 0.3, 1 mg/kg, s.c.) was administered. Scopolamine (0.1, 0.3 mg/kg, s.c.) was injected 30 min before the administration of test agents in antagonism studies. Animals were placed in plastic cages (22.5D×33.8 W×14.0H cm) immediately after the administration of test agents in the antagonism studies, and exploratory locomotor activity was measured during a 60 min observation period using an infrared motion detector system .

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

5HTReceptor, 5-HT2C, 5HT Receptor, DrugMetabolite, Dopamine Receptor, Drug Metabolite, DopamineReceptor, Desmethylclozapine, D4, Inhibitor, Normethylclozapine, Norclozapine, Muscarinic acetylcholine receptor, N Desmethylclozapine, inhibit, NDesmethylclozapine, N-Desmethylclozapine, mAChR, Opioid Receptor, OpioidReceptor, δ-opioid receptor, Virus Protease, VirusProtease

Compound Identifiers

PubChem CID

135409468