11-(4-甲基哌嗪-1-基)-5H-二苯并[B,E] [1,4]二氮杂卓
氯氮平杂质(11-(4-methyl-1-piperazinyl)-5H-dibenzo(b,e)(1,4)diazepine)
CAS: 1977-07-7
化学式: C18H20N4
| 中文名 | 氯氮平杂质 |
| 英文名 | 11-(4-methyl-1-piperazinyl)-5H-dibenzo(b,e)(1,4)diazepine |
| 别名 | 去氯氮平 氯氮平杂质 去氯氯氮平 11-(4-甲基-1-哌嗪基)-5H-二苯并[B,E][1,4]二氮杂卓 11-(4-甲基哌嗪-1-基)-5H-二苯并[B,E] [1,4]二氮杂卓 |
| 英文别名 | Dechloroclozapine Dopamine serotonin antagonist-1 11-(4-Methylpiperazin-1-yl)-5H-dibenzo[b,e][1,4]diazepine 11-(4-methyl-1-piperazinyl)-5H-dibenzo(b,e)(1,4)diazepine 5H-Dibenzo[b,e][1,4]diazepine, 11-(4-methyl-1-piperazinyl)- |
| CAS | 1977-07-7 |
| 化学式 | C18H20N4 |
| 分子量 | 292.38 |
| 密度 | 1.22±0.1 g/cm3(Predicted) |
| 沸点 | 457.5±55.0 °C(Predicted) |
| 酸度系数 | 7.82±0.20(Predicted) |
| 存储条件 | Keep in dark place,Inert atmosphere,Room temperature |
| 体外研究 | Deschloroclozapine has greater potencies for DREADDs than previous agonists in vitro. Deschloroclozapine is a potent agonist for hM 3 Dq with an EC 50 =0.13 nM. Deschloroclozapine is also a potent agonist for hM 4 Di with an EC 50 =0.081 nM. Deschloroclozapine is a potent and selective agonist for hM 3 Dq and hM 4 Di, it does not display significant agonistic activity for any of the 318 tests wild-type GPCRs at <10 nM. |
| 体内研究 | Deschloroclozapine (100 μg/kg; i.v.) exhibits good brain concentration profiles and biostability. Pharmacokinetic studies confirmed that Deschloroclozapine is rapidly accumulated in mouse brains and monkey CSF, while its metabolites are negligible. Deschloroclozapine (1 μg/kg; i.p.) selectively and rapidly enhances neuronal activity via hM 3 Dq-DREADD in vivo, Deschloroclozapine can also be utilized for in vivo neuronal silencing by activating hM 4 Di, an inhibitory DREADD. Deschloroclozapine (1-100 μg/kg; i.v.) selectively induces hM 3 Dq-mediated metabolic activity. Deschloroclozapine (100 μg/kg; i.m.) selectively induces behavioral deficits in hM 4 Di-expressing monkeys. Animal Model: Macaque monkey; 2.8-8.0 kg; age 3-10 years Dosage: 10, 100, 1000, 10000 μg/kg Administration: I.v. bolus injection Result: Required the dose for 50% occupancy (ED 50 ) for Deschloroclozapine was 25 μg/kg. Animal Model: Macaque monkey; 2.8-8.0 kg; age 3-10 years Dosage: 100 μg/kg (Pharmacokinetic Analysis) Administration: I.v. injection Result: Provided a sufficient concentration of Deschloroclozapine by a low systemic dose of Deschloroclozapine to be available for hM 4 Di-DREADD binding in vivo for at least for 2 h without the production of metabolites in monkeys. Animal Model: Wild-type C57BL/6j mice; male; age >12 weeks Dosage: 100 μg/kg (Pharmacokinetic Analysis) Administration: I.p. administration Result: Diminished rapidly of Deschloroclozapine concentration and were undetectable at 2 h in either brain tissue or CSF. The amount of the desmethyl metabolite C21 in CSF was negligible. Animal Model: HM 3 Dq monkeys and non-DREADD monkeys Dosage: 1, 3, 100 μg/kg (Pharmacokinetic Analysis) Administration: I.v. injection Result: Increased of FDG uptaking after Deschloroclozapine administration occurred exclusively at the hM 3 Dq-positive area. Animal Model: Monkeys received multiple injections of an AAV-vector carrying hM 4 Di genes Dosage: 100 μg/kg (Pharmacokinetic Analysis) Administration: I.m. administration Result: Enabled a rapidly and reversibly-induced behavioral change through activating muscarinic-based DREADDs without significant side effects. |
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供应商列表
现货供应
产品名: Deschloroclozapine 去供应商网站查看 询盘CAS: 1977-07-7
产地: 上海
规格: D885042
价格: 10mg-159,50mg-553
库存: 7天内发货
电话: 13816333479/13918391375
手机: 13816333479/13918391375
电子邮件: wangrui@macklin.cn
QQ: 2885703204/285395191
微信: 19863730987/13918391375
现货供应
产品名: Deschloroclozapine 去供应商网站查看 询盘CAS: 1977-07-7
产地: 上海
规格: D885042
价格: 10mg-159,50mg-553
库存: 7天内发货
电话: 13816333479/13918391375
手机: 13816333479/13918391375
电子邮件: wangrui@macklin.cn
QQ: 2885703204/285395191
微信: 19863730987/13918391375
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