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N-Desmethylclozapine

Catalog No. T5158 CAS 6104-71-8

Synonyms: Desmethylclozapine, Normethylclozapine, Norclozapine

N-Desmethylclozapine (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.

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N-Desmethylclozapine, CAS 6104-71-8

Pack Size	Availability	Price/USD
1 mg	In stock	$ 34.00
5 mg	In stock	$ 71.00
10 mg	In stock	$ 126.00
25 mg	In stock	$ 273.00
50 mg	In stock	$ 433.00
100 mg	In stock	$ 638.00
1 mL * 10 mM (in DMSO)	In stock	$ 94.00

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Purity: 98.45%

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Storage & Solubility Information

Description	N-Desmethylclozapine (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	Desmethylclozapine, Normethylclozapine, Norclozapine
Molecular Weight	312.8
Formula	C17H17ClN4
CAS No.	6104-71-8

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 50 mg/mL (159.85 mM)

Ethanol: 30 mg/mL

References and Literature

1. Kuoppamäki M, et al. Clozapine and N-desmethylclozapine are potent 5-HT1C receptor antagonists. Eur J Pharmacol. 1993 Apr 15;245(2):179-82. 2. Odagaki Y, et al. Comparative analysis of pharmacological properties of xanomeline and N-desmethylclozapine in rat brain membranes. J Psychopharmacol. 2016 Sep;30(9):896-912. 3. Sugawara Y, et al. Electrophysiological evidence showing muscarinic agonist-antagonist activities of N-desmethylclozapine using hippocampal excitatory and inhibitory neurons. Brain Res. 2016 Jul 1;1642:255-262. 4. Maehara S, et al. Behavioral effects of N-desmethylclozapine on locomotor activity and sensorimotor gating function in mice-Possible involvement of muscarinic receptors. Brain Res. 2011 Oct 18;1418:111-9. 6. Medigeshi GR, et al. N-Desmethylclozapine, Fluoxetine and Salmeterol inhibit post-entry stages of dengue virus life-cycle. Antimicrob Agents Chemother. 2016 Aug 29.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Anti-Neurodegenerative Disease Compound Library Anti-Cancer Clinical Compound Library Anti-Cancer Drug Library GPCR Compound Library Drug Repurposing Compound Library Anti-Infection Compound Library Serotonin Receptor-Targeted Compound Library NO PAINS Compound Library Target-Focused Phenotypic Screening Library

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Keywords

N-Desmethylclozapine 6104-71-8 Endocrinology/Hormones GPCR/G Protein Metabolism Microbiology/Virology Neuroscience Drug Metabolite AChR Virus Protease Dopamine Receptor 5-HT Receptor Opioid Receptor N Desmethylclozapine inhibit NDesmethylclozapine Desmethylclozapine Inhibitor Normethylclozapine mAChR Norclozapine Muscarinic acetylcholine receptor inhibitor

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