富马酸依美斯汀

富马酸依美斯汀用途

Emedastine difumarate 是一种具有口服活性,选择性和高亲和力的组胺 H1 受体拮抗剂,Ki 值为 1.3 nM。Emedastine difumarate 是一种苯并咪唑衍生物,具有强大的抗过敏特性,可用于过敏性鼻炎,过敏性皮肤疾病和过敏性结膜炎。

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富马酸依美斯汀名称

[ CAS 号 ]:
87233-62-3

[ 中文名 ]:
1-(2-乙氧基乙基)-2-(4-甲基-1-哌嗪基)苯并咪唑富马酸盐

[ 英文名 ]:
emedastine fumarate

[中文别名 ]:

富马酸依美斯汀

[英文别名 ]:

Emedastine

富马酸依美斯汀生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 免疫及炎症 >> 组胺受体

研究领域 >> 炎症/免疫

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 组胺受体

[ 靶点 ]

H1 Receptor:1.3 nM (Ki)

H2 Receptor:49067 nM (Ki)

H3 Receptor:12430 nM (Ki)

[体外研究]

富马酸依美司汀抑制组胺H2受体(Ki=49067nm)和组胺H3受体(Ki=12430nm)[1]。高浓度的富马酸依美司汀(1和10 ng/ml)可显著抑制正常人真皮成纤维细胞产生1型胶原[2]。浓度≥10nm的富马酸依美司汀(1,10,100,1000 nM)抑制CC趋化因子诱导的嗜酸性粒细胞迁移[2]。

[体内研究]

富马酸依美司汀(0.03,0.1,0.3 mg/kg；口服；预处理30 min)可显著抑制组胺诱导的抓挠,剂量分别为0.1和0.3 mg/kg,但不是0.03 mg/kg[3]。预处理富马酸依美司汀(0.03,0.1,0.3mg/kg；口服)可显著抑制P物质和白三烯B引起的抓挠[3]。富马酸依美司汀(0.3 mg/kg,p.o.)对豚鼠被动腹膜过敏反应有显著抑制作用[2]。富马酸依美司汀抑制组胺诱导的离体回肠收缩(IC50=6.1 nM)[2]。动物模型：5-6周龄雄性ICR小鼠[3]剂量：0.03,0.1,0.3mg/kg给药：口服；在瘙痒素注射前30min结果：预处理0.1和0.3mg/kg可显著抑制组胺引起的抓挠。

[参考文献]

[1]. Sharif NA, et al. Emedastine: a potent, high affinity histamine H1-receptor-selective antagonist for ocular use: receptor binding and second messenger studies. J Ocul Pharmacol. 1994 Winter;10(4):653-64.

[2]. Murota H, et al. Emedastine difumarate: a review of its potential ameliorating effect for tissue remodeling in allergic diseases. Expert Opin Pharmacother. 2009 Aug;10(11):1859-67.

[3]. Andoh T, et al. Involvement of blockade of leukotriene B(4) action in anti-pruritic effects of emedastine in mice. Eur J Pharmacol. 2000 Oct 6;406(1):149-52.

富马酸依美斯汀物理化学性质

[ 沸点 ]:
446.6ºC at 760 mmHg

[ 熔点 ]:
148-151°

[ 分子式 ]:
C₂₅H₃₄N₄O₉

[ 分子量 ]:
534.55900

[ 精确质量 ]:
534.23300

[ PSA ]:
182.73000

[ LogP ]:
1.64120

[ 储存条件 ]:
2-8°C

[ 水溶解性 ]:
Soluble in water, sparingly soluble in anhydrous ethanol, very slightly soluble in acetone.

富马酸依美斯汀MSDS

详细MSDS(安全技术说明书)

富马酸依美斯汀毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: DD8870000

CAS REGISTRY NUMBER :: 87233-62-3

LAST UPDATED :: 199503

DATA ITEMS CITED :: 12

MOLECULAR FORMULA :: C17-H26-N4-O.2C4-H4-O4

MOLECULAR WEIGHT :: 534.63

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 :: 1854 mg/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - mydriasis (pupillary dilation) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - respiratory depression

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 39,209,1990

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 643 mg/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - mydriasis (pupillary dilation) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - respiratory depression

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 39,209,1990

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 72 mg/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - mydriasis (pupillary dilation) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - respiratory depression

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 39,209,1990

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 2206 mg/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - respiratory depression

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 39,209,1990

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 609 mg/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - respiratory depression

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 39,209,1990

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 93 mg/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - respiratory depression

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 39,209,1990

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 193 mg/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - lacrimation Behavioral - convulsions or effect on seizure threshold Cardiac - pulse rate increase, without fall in BP

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 39,209,1990

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - guinea pig

DOSE/DURATION :: 744 mg/kg

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

REFERENCE :: ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 34,801,1984 ** OTHER MULTIPLE DOSE TOXICITY DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 22750 mg/kg/13W-I

TOXIC EFFECTS :: Liver - changes in liver weight Kidney, Ureter, Bladder - other changes in urine composition Nutritional and Gross Metabolic - changes in calcium

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 39,215,1990

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 18250 mg/kg/1Y-I

TOXIC EFFECTS :: Liver - other changes Endocrine - changes in pituitary weight Related to Chronic Data - changes in prostate weight

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 39,269,1990

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 6825 mg/kg/13W-I

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Blood - changes in spleen Related to Chronic Data - death

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 39,231,1990

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 16425 mg/kg/1Y-I

TOXIC EFFECTS :: Liver - changes in liver weight Related to Chronic Data - changes in prostate weight Related to Chronic Data - changes in testicular weight

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 39,285,1990

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富马酸依美斯汀安全信息

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

[ RTECS号 ]:
DD8870000

[ 海关编码 ]:
2933990090

富马酸依美斯汀海关

[ 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%

富马酸依美斯汀文献

Efficacy of olopatadine HCI 0.1%, ketotifen fumarate 0.025%, epinastine HCI 0.05%, emedastine 0.05% and fluorometholone acetate 0.1% ophthalmic solutions for seasonal allergic conjunctivitis: a placebo-controlled environmental trial.

Acta Ophthalmol. 87(5) , 549-54, (2009)

We aimed to compare the clinical efficacy and ocular surface variables of olopatadine, ketotifen fumarate, epinastine, emedastine and fluorometholone acetate ophthalmic solutions in preventing the sig...

Emedastine difumarate versus loratadine in chronic idiopathic urticaria: a randomized, double-blind, controlled European multicentre clinical trial.

Eur. J. Dermatol. 16(6) , 649-54, (2006)

Emedastine difumarate (2 mg b.i.d.) was compared to loratadine (10 mg o.d.) in a randomized, double-blind, multicentre trial for 4 weeks in 192 patients with idiopathic chronic urticaria. After one we...

Suplatast tosilate inhibits eosinophil production and recruitment into the skin in murine contact sensitivity.

Clin. Immunol. 108(3) , 257-62, (2003)

Antiallergic drugs and antihistamines have been widely used for controlling mucosal allergic diseases in which eosinophilia is prominent. Although H1-receptor antagonists are effective for treating hi...

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