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N-Desmethylclozapine (Desmethylclozapine) 是非典型抗精神病药 Clozapine 的主要活性代谢产物。它是血清素受体亚型 5-HT2C 的拮抗剂,IC50值为7.1 nM。 它也是多巴胺 D4 受体的拮抗剂和δ-阿片受体的激动剂。


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N-Desmethylclozapine (Desmethylclozapine) 是非典型抗精神病药 Clozapine 的主要活性代谢产物。它是血清素受体亚型 5-HT2C 的拮抗剂,IC50值为7.1 nM。 它也是多巴胺 D4 受体的拮抗剂和δ-阿片受体的激动剂。
| 规格 | 价格 | 库存 | 数量 |
|---|---|---|---|
| 1 mg | ¥ 155 | In stock | |
| 5 mg | ¥ 353 | In stock | |
| 10 mg | ¥ 597 | In stock | |
| 25 mg | ¥ 1,360 | In stock | |
| 50 mg | ¥ 2,150 | In stock | |
| 100 mg | ¥ 3,110 | In stock | |
| 200 mg | ¥ 4,380 | In stock | |
| 1 mL x 10 mM (in DMSO) | ¥ 437 | In stock |
N-Desmethylclozapine 相关产品
| 产品描述 | 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. |
| 靶点活性 | 5-HT2C:7.1 nM |
| 体外活性 | 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]. |
| 体内活性 | 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]. |
| 动物实验 | 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]. |
| 别名 | N-去甲基氯氮平, Normethylclozapine, Norclozapine, Desmethylclozapine |
| 分子量 | 312.8 |
| 分子式 | C17H17ClN4 |
| CAS No. | 6104-71-8 |
| Smiles | Clc1ccc2N=c3ccccc3=C(Nc2c1)N1CCNCC1 |
| 密度 | 1.38g/cm3 |
| 颜色 | Yellow |
| 物理性状 | Solid |
| 存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||||||||||||||||||||||
| 溶解度信息 | DMSO: 50 mg/mL (159.85 mM), Sonication is recommended. Ethanol: 30 mg/mL (95.91 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||||||||||||
溶液配制表 | |||||||||||||||||||||||||||||||||||||||||
Ethanol/DMSO
DMSO
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