Clozapine 氯氮平

CAS 5786-21-0 MFCD00153785

化学结构图

5786-21-0
SMILES: CN1CCN(C2=Nc3cc(Cl)ccc3Nc3ccccc32)CC1

化学属性

Mol. FormulaC18H19ClN4
Mol. Weight326.83
Melting Point183.0 to 187.0 deg-C
TSCANo
Appearance 淡黄色结晶性粉末。熔点183-184℃。易溶于氯仿,溶于乙醇,几乎不溶于水。无臭,无味。
SolubilityDMSO 65 mg/mL Water <1 mg/mL Ethanol 32 mg/mL

别名和识别编码

Chemical NameClozapine
MDL NumberMFCD00153785
CAS Number5786-21-0
Synonym 5H-Dibenzo[b,e][1,4]diazepine, 8-chloro-11-(4-methyl-1-piperazinyl)- 8-CHLORO-11-(4-METHYL-1-PIPERAZINYL)-5H-DIBENZO[B,E]-[1,4]DIAZEPINE 8-Chloro-11-(4-methyl-1-piperazinyl)-5H-dibenzo(b,e)(1,4)diazepine 8-Chloro-11-(4-methyl-1-piperazinyl)-5H-dibenzo[b,e][1,4]-diazepine 8-Chloro-11-(4-methyl-1-piperazinyl)-5H-dibenzo[b,e][1,4]diazepine 8-Chloro-11-(4-methyl-1-piperazinyl)-5H-dibenzo[b,e][1,4]diazepine, HF-1854, Liponex 8-chloro-11-(4-methyl-1-piperazinyl)-5h-dibenzo(e)(1,4)diazepine 8-氯-11(4-甲基-1-哌嗪基)-5H-二苯并[B,E][1,4]二氮杂草 8-氯-11-(4-甲基-1-哌嗪基)-5H-二苯并[b,e][1,4]-二氮杂草 8-氯-11-(4-甲基-1-哌嗪基)-5H-二苯并[b,e][1,4]二氮杂卓 Asaleptin Azaleptine CLOZAPINE CLOZAPINE ATYPICAL NEUROLEPTIC CLOZARIL COLZARIL Clozapin Clozapine Clozaril {PubCh
PubChem Substance ID135398737
EC Number227-313-7
Merck Number2423
Chemical Name Translation氯氮平
Reaxys-RN764984
Wiswesser Line NotationT C676 BM INJ FG J- AT6N DNTJ D1
Beilstein Registry Number0764984
InChIInChI=1S/C18H19ClN4/c1-22-8-10-23(11-9-22)18-14-4-2-3-5-15(14)20-16-7-6-13(19)12-17(16)21-18/h2-7,12,20H,8-11H2,1H3
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分类

  • {SNA} Antagonists, Application Index, Approved Therapeutics/Drug Candidates, Bioactive Small Molecules, Biochemicals and Reagents, CI-CY, Cell Biology, Cell Signaling Enzymes, Cell Signaling and Neuroscience, Dopaminargics - Antagonists, Dopaminergics, Enzymes, Inhibitors, and Substrates, GPCR Modulators, GPCR Proteins, Modulators and Antibodies, Membrane Protein Biology Tools, Neuroscience, Neurotransmission, Neurotransmitters, Novartis, Proteins and Derivatives,
  • {SNA} Ana
  • {SNA} Antagonists, Application Index, Approved Therapeutics/Drug Candidates, Bioactive Small Molecule Alphabetical Index,
  • {SNA} Antagonists,
  • {SNA} Antagonists,

产品应用

  • 非典型抗精神病药,对 D4 多巴胺受体比对 D2 或 D3 多巴胺受体表现出更大的亲和性;在用典型抗精神病药无?效的患者中,对精神分裂症的阳性和阴性症状均表现出抗?精神病疗效。

相关文献及参考

  • [2]. Zhukovskaya NL, et al. Clozapine downregulates 5-hydroxytryptamine6 (5-HT6) and upregulates 5-HT7 receptors in HeLa cells. Neurosci Lett. 2000 Jul 21;288(3):236-40.
  • [3]. Moreno JL, et al. Persistent effects of chronic clozapine on the cellular and behavioral responses to LSD in mice. Psychopharmacology (Berl). 2013 Jan;225(1):217-26.
  • [4]. Zorn SH, et al. Clozapine is a potent and selective muscarinic M4 receptor agonist. Eur J Pharmacol. 1994 Nov 15;269(3):R1-2.
  • [1]. Seeman P, et al. Clozapine, a fast-off-D2 antipsychotic. ACS Chem Neurosci. 2014 Jan 15;5(1):24-9.
  • [1]. Seeman P, et al. Clozapine, a fast-off-D2 antipsychotic. ACS Chem Neurosci. 2014 Jan 15;5(1):24-9.
  • [2]. Zhukovskaya NL, et al. Clozapine downregulates 5-hydroxytryptamine6 (5-HT6) and upregulates 5-HT7 receptors in HeLa cells. Neurosci Lett. 2000 Jul 21;288(3):236-40.
  • [3]. Moreno JL, et al. Persistent effects of chronic clozapine on the cellular and behavi

安全信息

WGK Germany3
GHS Symbol
Precautionary statements
  • P201 Obtain special instructions before use. 使用前获取专门指示。
  • P202 Do not handle until all safety precautions have been read and understood. 已阅读并理解所有的安全预防措施之前,切勿操作。
  • P203
  • P264 Wash hands thoroughly after handling. 处理后要彻底洗净双手。
  • P270 Do not eat, drink or smoke when using this product. 使用本产品时不要吃东西,喝水或吸烟。
  • P280 Wear protective gloves/protective clothing/eye protection/face protection. 戴防护手套/防护服/眼睛的保护物/面部保护物。
  • P281 Use personal protective equipment as required. 使用所需的个人防护装备。
  • P301+P310
  • P301+P310+P330
  • P301+P316
  • P302+P350
  • P302+P352+P332+P313+P362+P364
  • P305+P351+P338
  • P305+P351+P338+P337+P313
  • P308+P313
  • P318
  • P321 Specific treatment (see … on this label). 具体治疗(见本标签上的)。
  • P330 Rinse mouth. 漱口
  • P332+P313
  • P337+P313
  • P362 Take off contaminated clothing and wash before reuse. 脱掉污染的衣服,清洗后方可重新使用
  • P405 Store locked up. 上锁保管。
  • P501 Dispose of contents/container to..… 处理内容物/容器.....
Hazard statements
  • H301 Toxic if swallowed 吞食有毒
  • H341 Suspected of causing genetic defects 怀疑导致遗传性缺陷
  • H361 Suspected of damaging fertility or the unborn child 怀疑对生育能力或未出生婴儿造成伤害
Signal word Danger
RTECSHP1750000
Hazard Codes Xn Xn,Xi Xi
Safety Statements
  • S36/37 Wear suitable protective clothing and gloves 穿戴适当的防护服和手套;
  • S26 In case of contact with eyes, rinse immediately with plenty of water and seek medical advice 眼睛接触后,立即用大量水冲洗并征求医生意见;
  • S60 This material and its container must be disposed of as hazardous waste 该物质及其容器必须作为危险废物处置;
Risk Statements
  • R36/37/38 Irritating to eyes, respiratory system and skin 对眼睛、呼吸系统和皮肤有刺激性
  • R22 Harmful if swallowed 吞咽有害
  • R68 Possible risk of irreversible effects 可能有不可挽回的作用的危险
  • R63 Possible risk of harm to the unborn child 可能危害未出生婴儿
Packing GroupIII
UN Number UN 2811 6.1/PG 3 UN2811 2811
Hazard Class6.1
Storage condition 储存温度-20°C 储存温度2-8℃
TYPE OF TEST            : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE       : Oral
SPECIES OBSERVED        : Human - man
DOSE/DURATION           : 270 mg/kg/6W-I
TOXIC EFFECTS :
   Lungs, Thorax, or Respiration - structural or functional change in trachea
   or bronchi
   Gastrointestinal - hypermotility, diarrhea
   Blood - agranulocytosis
REFERENCE :
   AMDIBO Annales de Medecine Interne.  (Masson Abonnements, B.P.22, F-41354
   Vineuil Cedex, France) V.120-    1969-  Volume(issue)/page/year:
   144,494,1993

TYPE OF TEST            : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE       : Oral
SPECIES OBSERVED        : Rodent - rat
DOSE/DURATION           : 251 mg/kg
TOXIC EFFECTS :
   Details of toxic effects not reported other than lethal dose value
REFERENCE :
   KSRNAM Kiso to Rinsho.  Clinical Report.  (Yubunsha Co., Ltd., 1-5, Kanda
   Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan)  V.1-    1960-
   Volume(issue)/page/year: 7,667,1973

TYPE OF TEST            : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE       : Subcutaneous
SPECIES OBSERVED        : Rodent - rat
DOSE/DURATION           : 240 mg/kg
TOXIC EFFECTS :
   Behavioral - altered sleep time (including change in righting reflex)
   Behavioral - convulsions or effect on seizure threshold
   Lungs, Thorax, or Respiration - respiratory depression
REFERENCE :
   KSRNAM Kiso to Rinsho.  Clinical Report.  (Yubunsha Co., Ltd., 1-5, Kanda
   Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan)  V.1-    1960-
   Volume(issue)/page/year: 7,667,1973

TYPE OF TEST            : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE       : Subcutaneous
SPECIES OBSERVED        : Rodent - mouse
DOSE/DURATION           : 194 mg/kg
TOXIC EFFECTS :
   Behavioral - somnolence (general depressed activity)
   Behavioral - convulsions or effect on seizure threshold
   Behavioral - excitement
REFERENCE :

{ha

TYPE OF TEST            : Sex chromosome loss and nondisjunction
ROUTE OF EXPOSURE       : Oral
TEST SYSTEM             : Insect - Drosophila melanogaster
DOSE/DURATION           : 2 mg/2D
REFERENCE :
   SOGEBZ Soviet Genetics.  English translation of GNKAA5.  (Plenum Pub. Corp.,
   233 Spring St., New York, NY 10013)  V.2-    1966- Volume(issue)/page/year:
   11,718,1975

TYPE OF TEST            : Cytogenetic analysis
TEST SYSTEM             : Human Lymphocyte
DOSE/DURATION           : 10 mg/L
REFERENCE :
   HUGEDQ Human Genetics.  (Springer-Verlag New York, Inc., Service Center, 44
   Hartz Way, Secaucus, NJ 07094)  V.31-    1976-  Volume(issue)/page/year:
   38,77,1977

TYPE OF TEST            : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE       : Oral
SPECIES OBSERVED        : Rodent - rat
DOSE                    : 24 mg/kg
SEX/DURATION            : female 9-14 day(s) after conception
TOXIC EFFECTS :
   Reproductive - Fertility - pre-implantation mortality (e.g. reduction in
   number of implants per female; total number of implants per corpora lutea)
   Reproductive - Specific Developmental Abnormalities - musculoskeletal system
   Reproductive - Effects on Newborn - weaning or lactation index (e.g., #
   alive at weaning per # alive at day 4)
REFERENCE :
   KSRNAM Kiso to Rinsho.  Clinical Report.  (Yubunsha Co., Ltd., 1-5, Kanda
   Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan)  V.1-    1960-
   Volume(issue)/page/year: 7,696,1973

TYPE OF TEST            : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE       : Oral
SPECIES OBSERVED        : Rodent - rat
DOSE                    : 96 mg/kg
SEX/DURATION            : female 9-14 day(s) after conception
TOXIC EFFECTS :
   Reproductive - Effects on Newborn - live birth index (measured after birth)
REFERENCE :
   KSRNAM Kiso to Rinsho.  Clinical Report.  (Yubunsha Co., Ltd., 1-5, Kanda
   Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan)  V.1-    1960-
   Volume(issue)/page/year: 7,696,1973

TYPE OF TEST            : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE       : Oral
SPECIES OBSERVED        : Rodent - mouse
DOSE                    : 48 mg/kg
SEX/DURATION            : female 7-12 day(s) after conception
TOXIC EFFECTS :
   Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death,
   e.g., stunted fetus)
REFERENCE :
   KSRNAM Kiso to Rinsho.  Clinical Report.  (Yubunsha Co., Ltd., 1-5, Kanda
   Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan)  V.1-    1960-
   Volume(issue)/page/year: 7,696,1973

TYPE OF TEST            : TDLo - Lowest published toxic dos

Restrict 精麻类化学品

其他信息

  • 用途一:该品具有较强的抗精神病作用,亦有镇静作用,为新型广谱精神病药。适用于急、慢性精神分裂症,对幻觉妄想型、青春型疗效较好。从减轻症状来看,对兴奋躁动、幻觉、妄想、接触被动、拒食等效果满意。
  • 氯氮平
  • Clozapine 是一种有效的5-HT1C受体拮抗剂,作用于5-HT刺激的磷酸肌醇水解,IC50为110 nM。
  • MSDS 信息:8-Chloro-11-(4-methyl-1-piperazinyl)-5H-dibenzo[b,e][1,4]diazepine(5786-21-0).msds
  • 方法一:2-氨基-4-氯二苯胺-2'-羧酸(4''-甲基)哌嗪与三氯氧磷反应得到氯氮平。
  • MOL 文件:5786-21-0.mol
  • 上游原料:三氯氧磷 --> 邻氨基苯甲酸 --> N-甲基哌嗪 --> 四氯化钛 --> 2,5-二氯硝基苯 --> N-苯基邻氨基苯甲酸 --> 2-氨基-4-氯二苯胺
  • Sigma Aldrich:5786-21-0(sigmaaldrich)

系列性分类


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