Powder: -20°C for 3 years
In solvent: -80°C for 2 years
N-Desmethylclozapine is an antagonist of serotonin (5-HT) receptor subtype 5-HT2C (IC50: 7.1 nM). It also is an antagonist at dopamine D4 receptors, an agonist at δ-opioid receptors.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
5 mg | In stock | $ 71.00 | |
10 mg | In stock | $ 126.00 | |
25 mg | In stock | $ 274.00 | |
50 mg | In stock | $ 433.00 | |
100 mg | In stock | $ 700.00 |
Description | N-Desmethylclozapine is an antagonist of serotonin (5-HT) receptor subtype 5-HT2C (IC50: 7.1 nM). It also is an antagonist at dopamine D4 receptors, an agonist at δ-opioid receptors. |
Targets&IC50 | 5-HT2C:7.1 nM |
In vitro | N-desmethylclozapine antagonized 5-HT-stimulated phosphoinositide hydrolysis with IC50 values of 29.4 nM [1]. 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 [2]. 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 [3]. |
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 [4]. |
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 [4]. |
Synonyms | Norclozapine, Normethylclozapine, Desmethylclozapine |
Molecular Weight | 312.8 |
Formula | C17H17ClN4 |
CAS No. | 6104-71-8 |
Powder: -20°C for 3 years
In solvent: -80°C for 2 years
DMSO: 30 mg/mL
Ethanol: 30 mg/mL
( < 1 mg/ml refers to the product slightly soluble or insoluble )
You can also refer to dose conversion for different animals. More
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N-Desmethylclozapine 6104-71-8 Endocrinology/Hormones GPCR/G Protein Metabolism Microbiology/Virology Neuroscience Dopamine Receptor Virus Protease 5-HT Receptor Opioid Receptor Drug Metabolite AChR Norclozapine N Desmethylclozapine inhibit Normethylclozapine NDesmethylclozapine Desmethylclozapine Inhibitor mAChR Muscarinic acetylcholine receptor inhibitor