11-(4-methyl-1-piperazinyl)-5H-dibenzo(b,e)(1,4)diazepine
- Product Name
- 11-(4-methyl-1-piperazinyl)-5H-dibenzo(b,e)(1,4)diazepine
- CAS No.
- 1977-07-7
- Chemical Name
- 11-(4-methyl-1-piperazinyl)-5H-dibenzo(b,e)(1,4)diazepine
- Synonyms
- Dechloroclozapine;Dopamine serotonin antagonist-1;Deschloroclozapine, 10 mM in DMSO;(4-Methyl-1-piperazinyl)-5h-dibenzo(b,e)(1,4)diazepine;11-(4-methyl-1-piperazinyl)-5H-dibenzo(b,e)(1,4)diazepine;11-(4-Methylpiperazin-1-yl)-5H-dibenzo[b,e][1,4]diazepine;5H-Dibenzo[b,e][1,4]diazepine, 11-(4-methyl-1-piperazinyl)-;inhibit,Inhibitor,Muscarinic acetylcholine receptor,hM4Di,Deschloroclozapine,hM3Dq,muscarinic-based,mAChR,DREADDs;11-(4-Methylpiperazin-1-yl)-5H-dibenzo[b,e][1,4]diazepineQ: What is 11-(4-Methylpiperazin-1-yl)-5H-dibenzo[b,e][1,4]diazepine Q: What is the CAS Number of 11-(4-Methylpiperazin-1-yl)-5H-dibenzo[b,e][1,4]diazepine
- CBNumber
- CB21316359
- Molecular Formula
- C18H20N4
- Formula Weight
- 292.38
- MOL File
- 1977-07-7.mol
11-(4-methyl-1-piperazinyl)-5H-dibenzo(b,e)(1,4)diazepine Property
- Boiling point:
- 457.5±55.0 °C(Predicted)
- Density
- 1.22±0.1 g/cm3(Predicted)
- storage temp.
- Keep in dark place,Inert atmosphere,Room temperature
- solubility
- DMSO : ≥ 83.3 mg/mL (284.90 mM)
- pka
- 7.82±0.20(Predicted)
- form
- solid
- color
- Yellow
N-Bromosuccinimide Price
- Product number
- CS-M3647
- Product name
- Deschloroclozapine
- Purity
- 99.79%
- Packaging
- 10mg
- Price
- $100
- Updated
- 2021/12/16
- Product number
- CS-M3647
- Product name
- Deschloroclozapine
- Purity
- 99.79%
- Packaging
- 50mg
- Price
- $350
- Updated
- 2021/12/16
- Product number
- CHM0997406
- Product name
- 11-(4-METHYL-1-PIPERAZINYL)-5H-DIBENZO(B,E)(1,4)DIAZEPINE
- Purity
- 95.00%
- Packaging
- 5MG
- Price
- $496.91
- Updated
- 2021/12/16
- Product number
- CS-M3647
- Product name
- Deschloroclozapine
- Purity
- 99.79%
- Packaging
- 100mg
- Price
- $550
- Updated
- 2021/12/16
- Product number
- CD11170784
- Product name
- 11-(4-Methylpiperazin-1-yl)-5H-dibenzo[b,e][1,4]diazepine
- Purity
- 97%
- Packaging
- 50mg
- Price
- $289
- Updated
- 2021/12/16
11-(4-methyl-1-piperazinyl)-5H-dibenzo(b,e)(1,4)diazepine Chemical Properties,Usage,Production
Biological Activity
Deschloroclozapine is a potent, high-affinity, selective, metabolically stable agonist of muscarinic-based DREADDs.
Synthesis
109-01-3
5814-41-5
1977-07-7
General procedure for the synthesis of 11-(4-methylpiperazin-1-yl)-5H-dibenzo[b,E][1,4]diazepin-11-one from N-methylpiperazine and 5,10-dihydro-11H-dibenzo[b,e][1,4]diazepin-11-one: 5,10-dihydro-11H-dibenzo[b,e][1,4]diazepin-11-one (105 mg , 0.5 mmol) was placed in a 50 mL round bottom flask. N,N-dimethylaniline (36.3 mg, 0.3 mmol) was added sequentially. An appropriate amount of super-dry trichlorophosphorus and a magnetic stirrer were added and the mixture was stirred under reflux conditions for 12 h at 130°C under nitrogen protection. Upon completion of the reaction, the excess phosphorous trichloride was removed by distillation. Subsequently, the reaction was terminated by adding an appropriate amount of N-methylpiperazine and continued stirring for 12 hours. The progress of the reaction was monitored by thin layer chromatography (TLC). The reaction mixture was extracted with ethyl acetate (3 x 70 mL) and washed sequentially with water. The organic layers were combined and dried by adding anhydrous Na2SO4. After filtration, the residue was concentrated. Purification by column chromatography (eluent: dichloromethane/methanol = 25:1) afforded 110 mg of the target product 11-(4-methylpiperazin-1-yl)-5H-dibenzo[b,E][1,4]diazepine in 75% yield.
in vitro
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.
b>
target
Ki: 6.3 nM (hM 3 Dq), 4.2 nM (hM 4 Di)
storage
Room temperature
References
[1] Patent: CN108586364, 2018, A. Location in patent: Paragraph 0150; 0151; 0152
11-(4-methyl-1-piperazinyl)-5H-dibenzo(b,e)(1,4)diazepine Preparation Products And Raw materials
Raw materials
Preparation Products
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View Lastest Price from 11-(4-methyl-1-piperazinyl)-5H-dibenzo(b,e)(1,4)diazepine manufacturers
- Product
- Dopamine serotonin antagonist-1 1977-07-7
- Price
- US $2.00-5.00/kg
- Min. Order
- 1kg
- Purity
- 99%
- Supply Ability
- 100kg
- Release date
- 2025-06-23