| 名称 | N-Desmethylclozapine |
| 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. |
| 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]. |
| 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]. |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | DMSO : 125 mg/mL (399.62 mM), Sonication is recommended.
Ethanol : 30 mg/mL (95.91 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (6.39 mM), Sonication is recommended.
|
| 关键字 | δ-opioid receptor | VirusProtease | Virus Protease | OpioidReceptor | Opioid Receptor | N-Desmethylclozapine | NDesmethylclozapine | N Desmethylclozapine | Muscarinic acetylcholine receptor | mAChR | Inhibitor | inhibit | DrugMetabolite | Drug Metabolite | DopamineReceptor | Dopamine Receptor | D4 | 5HTReceptor | 5-HT2C | 5HT Receptor |
| 相关产品 | Mitotane | Cefaclor monohydrate | Urethane | Alverine citrate | Arecoline | Dapoxetine hydrochloride | Adenine | N,N-Dicyclohexylcarbodiimide | 1,8-Cineole | L-Lysine | Thymidine | Phenytoin sodium |
| 相关库 | 抑制剂库 | 经典已知活性库 | 已知活性化合物库 | 抗阿尔茨海默症化合物库 | 抗病毒库 | GPCR靶点分子库 | 膜蛋白靶向化合物库 | 神经退行性疾病化合物库 | 药物功能重定位化合物库 | 疼痛相关化合物库 | 抗癌临床化合物库 | 抗癌药物库 |