5H-Dibenzo[b,e][1,4]diazepine, 11-(4-methyl-1-piperazinyl)-
11-(4-methyl-1-piperazinyl)-5H-dibenzo(b,e)(1,4)diazepine
CAS: 1977-07-7
Molecular Formula: C18H20N4
5H-Dibenzo[b,e][1,4]diazepine, 11-(4-methyl-1-piperazinyl)- - Names and Identifiers
5H-Dibenzo[b,e][1,4]diazepine, 11-(4-methyl-1-piperazinyl)- - Physico-chemical Properties
| Molecular Formula | C18H20N4 |
| Molar Mass | 292.38 |
| Density | 1.22±0.1 g/cm3(Predicted) |
| Boling Point | 457.5±55.0 °C(Predicted) |
| pKa | 7.82±0.20(Predicted) |
| Storage Condition | Keep in dark place,Inert atmosphere,Room temperature |
| Use | This product is for scientific research only and shall not be used for other purposes. |
| In vitro study | 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. |
| In vivo study | 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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Product Name: Clozapine Impurity 11 Visit Supplier Webpage Request for quotationCAS: 1977-07-7
Tel: 0714-3999186
Email: 2853786052@qq.com
Mobile: 86+15671228036
QQ: 2853786052
Wechat: 15671228036
Product Name: 11-(4-methyl-1-piperazinyl)-5H-dibenzo(b,e)(1,4)diazepine Visit Supplier Webpage Request for quotation
CAS: 1977-07-7
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
CAS: 1977-07-7
Tel: 18301782025
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Mobile: 18021002903
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Wechat: 18301782025
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