Clozapine 氯氮平
CAS 5786-21-0 MFCD00153785
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信息真实价格透明
资金保障
专业采购外包团队在线服务
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现货库存
一流品牌服务
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
GHS Symbol
- 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.....
- 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
- 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;
- 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
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 :
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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
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)