N-Desmethylclozapine

SKU: orb1302043

描述

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.

研究领域

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

图片与验证

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关键属性

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CAS 号	6104-71-8
MW	312.8
纯度	99.83% (May vary between batches)
分子式	C₁₇H₁₇ClN₄
SMILES	Clc1ccc2N=c3ccccc3=C(Nc2c1)N1CCNCC1
靶点	Drug Metabolite,5-HT Receptor,AChR,Virus Protease,Opioid Receptor,Dopamine Receptor
溶解性	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)

生物活性

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靶点 IC50	5-HT2C:7.1 nM
体内	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 .
体外	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 .
动物研究	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 .

储存与操作

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储存	-20°C
有效期	12 months from date of receipt.
免责声明	For research use only

别名

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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

相似产品

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Tetramethylammonium perchlorate [orb2938894]
CAS 号：
2537-36-2
MW:
173.6
分子式：
C₄H₁₂ClNO₄
可选规格： 10 g, 25 g, 5 g
N-Desmethylclozapine [orb1221163]
纯度：
>98% (HPLC)
CAS 号：
6104-71-8
MW:
312.8
分子式：
C₁₇H₁₇ClN₄
可选规格： 5 mg, 10 mg, 25 mg, 50 mg, 100 mg, 200 mg, 500 mg, 1 g

质量保证

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化合物标识

PubChem CID

135409468 ↗

关键属性

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暂无计算属性。

实验方案信息

查看更多实验方案

纯度：	>98% (HPLC)
CAS 号：	6104-71-8
MW:	312.8
分子式：	C₁₇H₁₇ClN₄

N-Desmethylclozapine

描述

研究领域

图片与验证

关键属性

生物活性

储存与操作

别名

相似产品

Tetramethylammonium perchlorate [orb2938894]