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富马酸氯马斯汀

富马酸氯马斯汀用途

Clemastine延胡索酸盐是组胺H1受体拮抗剂,IC50为3 nM。

富马酸氯马斯汀名称

[ CAS 号 ]:
14976-57-9

[ 中文名 ]:
富马酸氯马斯汀

[ 英文名 ]:
Clemastine fumarate

[中文别名 ]:

[英文别名 ]:

Tavist,Agasten
MFCD00137486
EINECS 239-055-2
Clemastine fumarate
Clemastine fumarate salt

富马酸氯马斯汀生物活性

[ 描述 ]:

Clemastine延胡索酸盐是组胺H1受体拮抗剂,IC50为3 nM。

[ 相关类别 ]:

信号通路 >> 自噬 >> 自噬

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 组胺受体

信号通路 >> 免疫及炎症 >> 组胺受体

研究领域 >> 神经疾病

[参考文献]

[1]. Seifert, R., et al., Histamine increases cytosolic Ca2+ in dibutyryl-cAMP-differentiated HL-60 cells via H1 receptors and is an incomplete secretagogue. Mol Pharmacol, 1992. 42(2): p. 227-34.

[2]. Schran, H.F., et al., The pharmacokinetics and bioavailability of clemastine and phenylpropanolamine in single-component and combination formulations. J Clin Pharmacol, 1996. 36(10): p. 911-22.

[相关活性小分子]

富马酸氯马斯汀物理化学性质

[ 密度 ]:
1.097 g/cm3

[ 沸点 ]:
116 °C / 24mmHg

[ 熔点 ]:
61 °C

[ 分子式 ]:
C₂₅H₃₀ClNO₅

[ 分子量 ]:
459.962

[ 闪点 ]:
211ºC

[ 精确质量 ]:
459.181244

[ PSA ]:
87.07000

[ LogP ]:
4.75410

[ 外观性状 ]:
白色或近乎于白色结晶粉末

[ 蒸汽压 ]:
1.94E-07mmHg at 25°C

[ 折射率 ]:
1.553

[ 储存条件 ]:
Store at RT

[ 水溶解性 ]:
水溶性：不溶；极微溶：乙醇,甲醇；不溶：二乙醚

富马酸氯马斯汀MSDS

详细MSDS(安全技术说明书)

富马酸氯马斯汀毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: UY0704600

CAS REGISTRY NUMBER :: 14976-57-9

LAST UPDATED :: 199203

DATA ITEMS CITED :: 8

MOLECULAR FORMULA :: C21-H26-Cl-N-O.C4-H4-O4

MOLECULAR WEIGHT :: 460.01

WISWESSER LINE NOTATION :: T5NTJ A1 B2OX1&R&R DG &QV1U1VQ -T

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 3550 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Behavioral - excitement Behavioral - changes in motor activity (specific assay)

REFERENCE :: BCFAAI Bollettino Chimico Farmaceutico. (Societa Editoriale Farmaceutica, Via Ausonio 12, 20123 Milan, Italy) V.33- 1894- Volume(issue)/page/year: 106,467,1967

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 82 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Behavioral - excitement Behavioral - changes in motor activity (specific assay)

REFERENCE :: BCFAAI Bollettino Chimico Farmaceutico. (Societa Editoriale Farmaceutica, Via Ausonio 12, 20123 Milan, Italy) V.33- 1894- Volume(issue)/page/year: 106,467,1967

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 730 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Behavioral - excitement Behavioral - changes in motor activity (specific assay)

REFERENCE :: BCFAAI Bollettino Chimico Farmaceutico. (Societa Editoriale Farmaceutica, Via Ausonio 12, 20123 Milan, Italy) V.33- 1894- Volume(issue)/page/year: 106,467,1967

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 43 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Behavioral - excitement Behavioral - changes in motor activity (specific assay)

REFERENCE :: BCFAAI Bollettino Chimico Farmaceutico. (Societa Editoriale Farmaceutica, Via Ausonio 12, 20123 Milan, Italy) V.33- 1894- Volume(issue)/page/year: 106,467,1967

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 175 mg/kg

TOXIC EFFECTS :: Behavioral - hallucinations, distorted perceptions Behavioral - muscle contraction or spasticity Gastrointestinal - nausea or vomiting

REFERENCE :: BCFAAI Bollettino Chimico Farmaceutico. (Societa Editoriale Farmaceutica, Via Ausonio 12, 20123 Milan, Italy) V.33- 1894- Volume(issue)/page/year: 106,467,1967

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: >50 mg/kg

TOXIC EFFECTS :: Behavioral - hallucinations, distorted perceptions Behavioral - muscle contraction or spasticity Gastrointestinal - nausea or vomiting

REFERENCE :: BCFAAI Bollettino Chimico Farmaceutico. (Societa Editoriale Farmaceutica, Via Ausonio 12, 20123 Milan, Italy) V.33- 1894- Volume(issue)/page/year: 106,467,1967

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 1 gm/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,230,1982

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 19 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Behavioral - excitement Behavioral - changes in motor activity (specific assay)

REFERENCE :: BCFAAI Bollettino Chimico Farmaceutico. (Societa Editoriale Farmaceutica, Via Ausonio 12, 20123 Milan, Italy) V.33- 1894- Volume(issue)/page/year: 106,467,1967

富马酸氯马斯汀安全信息

[ 危险品运输编码 ]:
NONH for all modes of transport

[ RTECS号 ]:
UY0704600

[ 海关编码 ]:
2933990090

富马酸氯马斯汀上下游产品

富马酸氯马斯汀上游产品

富马酸氯马斯汀下游产品

富马酸氯马斯汀海关

[ 海关编码 ]: 2933990090

[ 中文概述 ]:
2933990090. 其他仅含氮杂原子的杂环化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%

[ 申报要素 ]: 品名, 成分含量, 用途, 乌洛托品请注明外观, 6－己内酰胺请注明外观, 签约日期

[ Summary ]:
2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

富马酸氯马斯汀文献

Salt effects in electromembrane extraction.

J. Chromatogr. A. 1347 , 1-7, (2014)

Electromembrane extraction (EME) was performed on samples containing substantial amounts of NaCl to investigate how the presence of salts affected the recovery, repeatability, and membrane current in ...

Antiallergic and antiasthmatic effects of a novel enhydrazinone ester (CEE-1): inhibition of activation of both mast cells and eosinophils.

J. Pharmacol. Exp. Ther. 350(2) , 444-54, (2014)

Activation of mast cells and eosinophils is a fundamental process in the pathophysiology of allergic diseases. We have previously reported that the novel enhydrazinone ester CEE-1 (ethyl 4-phenylhydra...

A screen of approved drugs and molecular probes identifies therapeutics with anti-Ebola virus activity.

Sci. Transl. Med. 7 , 290ra89, (2015)

Currently, no approved therapeutics exist to treat or prevent infections induced by Ebola viruses, and recent events have demonstrated an urgent need for rapid discovery of new treatments. Repurposing...

更多文献

富马酸氯马斯汀相关知识

富马酸氯马斯汀片_说明书_禁忌_富马酸氯马斯汀副作用

2019-01-10 17:18:24

导读：富马酸马斯汀（Clemastine Fumarate）是瑞士山道士（Sandoz）公司六十年代开发成功的抗组胺药。其后，在美国、日本、德国等陆续投放市场。本品是一个典型的，有代表性的第二代H1受体拮抗剂，临床上用于治疗由组胺引了的各种过敏性疾病，是目前世界上公认的最好的抗组胺药之一。经国外四...