ChemicalBook
English   Japanese   Germany   Korea

网站主页 >> CAS数据库列表 >> 氯氮平杂质

氯氮平杂质

生物活性 靶点 体外研究 体内研究

氯氮平杂质, 1977-07-7, 结构式
氯氮平杂质
CAS号:
1977-07-7
英文名:
11-(4-methyl-1-piperazinyl)-5H-dibenzo(b,e)(1,4)diazepine
英文别名:
Dechloroclozapine;Dopamine serotonin antagonist-1;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
中文名:
氯氮平杂质
中文别名:
去氯氮平;去氯氯氮平;11-(4-甲基-1-哌嗪基)-5H-二苯并(B,E)(1,4)二氮卓;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
CBNumber:
CB21316359
分子式:
C18H20N4
分子量:
292.38
MOL File:
1977-07-7.mol

氯氮平杂质化学性质

沸点:
457.5±55.0 °C(Predicted)
密度:
1.22±0.1 g/cm3(Predicted)
储存条件:
Keep in dark place,Inert atmosphere,Room temperature
溶解度:
DMSO : ≥ 83.3 mg/mL (284.90 mM)
酸度系数(pKa):
7.82±0.20(Predicted)
形态:
solid
颜色:
Yellow
安全信息

氯氮平杂质性质、用途与生产工艺

生物活性

Deschloroclozapine 是有效的，高亲和力的，选择性的，代谢稳定的基于毒蕈碱的 DREADDs 的激动剂。Deschloroclozapine 抑制 [3H] 苄基喹啉基 (QNB) 与 hM3Dq 和 hM4Di 的结合，Ki 值分别为 6.3 和 4.2 nM。据报道 Deschloroclozapine 在小鼠和非人类灵长类动物中都有多种用途。

靶点

Ki: 6.3 nM (hM 3 Dq), 4.2 nM (hM 4 Di)

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.

氯氮平杂质 上下游产品信息

上游原料

下游产品

氯氮平杂质 生产厂家

全球有 31家供应商   氯氮平杂质国内生产厂家
供应商联系电话电子邮件国家产品数优势度
上海贺康生物技术有限公司 18939837085 youchemicals@gmail.com 中国 1813 55
上海毕得医药科技股份有限公司 400-1647117 15221909166 product02@bidepharm.com 中国 41438 60
深圳振强生物技术有限公司 0755-0755-66853366 13670046396 sales@chem-strong.com 中国 17982 56
杭州宇昊化工科技有限公司 0571-82693216 info@yuhaochemical.com 中国 2031 58
上海超岚化工科技中心 QQ:65489617 15618227136 info@SuperLan-chem.com 中国 9445 58
湖北扬信医药科技有限公司 15374522761 3003392093@qq.com 中国 7851 55
江苏艾康生物医药研发有限公司 025-66113011 18112977050 cb6@aikonchem.com 中国 15495 58
TargetMol Chemicals Inc. +1-781-999-5354 +1-00000000000 marketing@targetmol.com 美国 19892 58
ChemeGen 中国 18818260767 sales@chemegen.com 中国 11289 58
上海凯为化学科技有限公司 021-58461859 15821823057 service@aiviche.com 中国 49323 58
上海弘渠生物医药科技有限公司 88888888888 hongquchem@qq.com 中国 5132 58
卡托研究化学公司 020-81215950 4000-868-328 customer@uwalab.com 美国 10413 58
郑州汇聚化工有限公司 0371-53736046 13393710386 2853979814@qq.com 中国 10003 58
安耐吉化学&3A（安徽泽升科技有限公司） 021-58432009 400-005-6266 marketing1@energy-chemical.com 中国 44894 58
天津普西唐生物医药科技有限公司 010-60605840 15801484223 psaitong@jm-bio.com 中国 29834 58
常州翔龙医药科技有限公司 18661161657 yaoxiangqiu2021@163.com 中国 10066 58
上海皓鸿生物医药科技有限公司 400-8210725 4008210725 malulu@leyan.com 中国 39997 58
深圳摩科生化科技有限公司 18274848843 3001006472@qq.com 中国 8620 58
TargetMol中国（陶术生物） 4008200310 marketing@tsbiochem.com 中国 24131 58
合肥合药生物科技有限公司 181-55150309 18155150309 waimaobu@hepharma.cn 中国 2896 58
金克隆（北京）生物技术有限公司 400-910-1997 17560619001 3243204476@qq.com 中国 9962 58
上海捷世凯生物科技有限公司 021-57520305 15801958784 lihua@jskchem.com 中国 49036 58
湖北省德奥化研医药科技有限责任公司 18502726233 3641133981@qq.com 中国 9293 58
Aladdin Scientific Corporation +1-833-552-7181 sales@aladdinsci.com 美国 52927 58
LEAPCHEM CO., LTD. +86-852-30606658 market18@leapchem.com 中国 43348 58
 

1977-07-7, 氯氮平杂质 相关搜索:

拉米地坦杂质7 拉米地坦杂质3 拉米地坦 (2S,3R)-2-(2,4-二氟苯基)-3-甲基-2-[(1H-1,2,4-三唑-1-基)甲基]环氧乙烷 拉米地坦杂质4 (6-氨基吡啶-2-基)(1-甲基哌啶-4-基)甲酮 拉米地坦杂质5 果糖二丙酮 拉米地坦杂质6 依度沙班杂质EDBZP 拉米地坦杂质1
  • 杂质对照品
  • 11-(4-甲基-1-哌嗪基)-5H-二苯并(B,E)(1,4)二氮卓
  • 去氯氮平
  • 11-(4-甲基哌嗪-1-基)-5H-二苯并[B,E] [1,4]二氮杂卓
  • 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
  • 1977-07-7
  • inhibit,Inhibitor,Muscarinic acetylcholine receptor,hM4Di,Deschloroclozapine,hM3Dq,muscarinic-based,mAChR,DREADDs
  • Dopamine serotonin antagonist-1
  • 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
  • 5H-Dibenzo[b,e][1,4]diazepine, 11-(4-methyl-1-piperazinyl)-
  • Dechloroclozapine
  • 11-(4-Methylpiperazin-1-yl)-5H-dibenzo[b,e][1,4]diazepine
Copyright 2016 © ChemicalBook. All rights reserved