盐酸美沙吡林

盐酸美沙吡林用途

甲吡啉(噻吩基吡拉明)盐酸盐是一种口服活性H1受体抗组胺药和吡啶类抗胆碱药。盐酸美沙比林具有肝毒性,可作为肝毒素在体内引起门静脉周围肝坏死[2]

盐酸美沙吡林名称

[ CAS 号 ]:
135-23-9

[ 中文名 ]:
盐酸美沙吡林

[ 英文名 ]:
Methapyrilene Hydrochloride

[英文别名 ]:

盐酸美沙吡林生物活性

[ 描述 ]:

甲吡啉(噻吩基吡拉明)盐酸盐是一种口服活性H1受体抗组胺药和吡啶类抗胆碱药。盐酸美沙比林具有肝毒性,可作为肝毒素在体内引起门静脉周围肝坏死[2]

[ 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


[体外研究]

甲吡啉盐酸盐(650μM)导致TF下调和FTL上调,而HMOX1水平不变。此外,CD44和SOX9蛋白水平以及PROM1(CD133)和肝干细胞相关标记物的表达增加[1]。甲吡啉盐酸盐(650μM)降低CYP2E1、CYP3A4、NR1l3、ALB、mRNA表达,增加CD133表达[1]。

[体内研究]

盐酸美沙比林(口服灌胃；40或80mg/kg；每周5天；6周)导致经典肝毒性相关标记基因和铁稳态相关基因表达的变化,尤其是大鼠转铁蛋白(Tf)基因显著的剂量依赖性下调和铁蛋白轻链(FTL)基因上调[1]。盐酸美沙比林(口服灌胃；150mg/kg；3天)高剂量引起门静脉周围肝坏死。甲吡啉足以引起肝脏坏死,或亚毒性剂量为50 mg/kg/天[2]。

[参考文献]

[1]. Iryna Kindrat, et al.Effect of methapyrilene hydrochloride on hepatic intracellular iron metabolism in vivo and in vitro. Toxicol Lett. 2017 Nov 5;281:65-73.

[2]. Andrew Craig, et al. Systems toxicology: integrated genomic, proteomic and metabonomic analysis of methapyrilene induced hepatotoxicity in the rat. J Proteome Res. 2006 Jul;5(7):1586-601.

[3]. Shawkat-Muhialdin Jangi, et al. H1 histamine receptor antagonists induce genotoxic and caspase-2-dependent apoptosis in human melanoma cells. Carcinogenesis. 2006 Sep;27(9):1787-96.

盐酸美沙吡林物理化学性质

[ 密度 ]:
1.148g/cm3

[ 沸点 ]:
389.6ºC at 760 mmHg

[ 熔点 ]:
162°

[ 分子式 ]:
C14H20ClN3S

[ 分子量 ]:
297.84700

[ 闪点 ]:
189.4ºC

[ 精确质量 ]:
297.10700

[ PSA ]:
47.61000

[ LogP ]:
3.51330

[ 外观性状 ]:
固体

[ 蒸汽压 ]:
2.82E-06mmHg at 25°C

[ 储存条件 ]:
room temp

盐酸美沙吡林MSDS

详细MSDS(安全技术说明书)

盐酸美沙吡林毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :
UT1750000
CHEMICAL NAME :
Pyridine, 2-((2-(dimethylamino)ethyl)-2-thenylamino)-, monohydrochloride
CAS REGISTRY NUMBER :
135-23-9
LAST UPDATED :
199712
DATA ITEMS CITED :
35
MOLECULAR FORMULA :
C14-H19-N3-S.Cl-H
MOLECULAR WEIGHT :
297.88
WISWESSER LINE NOTATION :
T6NJ BNZN1&1&1- BT5SJ &GH

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Human - man
DOSE/DURATION :
429 ug/kg
TOXIC EFFECTS :
Gastrointestinal - gastritis
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
200 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
150 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
182 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
90 mg/kg
TOXIC EFFECTS :
Behavioral - excitement Behavioral - muscle contraction or spasticity Lungs, Thorax, or Respiration - dyspnea
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
75 mg/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
17500 ug/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - guinea pig
DOSE/DURATION :
14600 ug/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
9100 mg/kg/26W-C
TOXIC EFFECTS :
Tumorigenic - Carcinogenic by RTECS criteria Liver - tumors
TYPE OF TEST :
TD - Toxic dose (other than lowest)
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
18200 mg/kg/26W-C
TOXIC EFFECTS :
Tumorigenic - Carcinogenic by RTECS criteria Liver - tumors
TYPE OF TEST :
TD - Toxic dose (other than lowest)
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
22 gm/kg/64W-C
TOXIC EFFECTS :
Tumorigenic - Carcinogenic by RTECS criteria Liver - tumors
TYPE OF TEST :
TD - Toxic dose (other than lowest)
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
9625 mg/kg/2Y-C
TOXIC EFFECTS :
Tumorigenic - Carcinogenic by RTECS criteria Liver - tumors
TYPE OF TEST :
TD - Toxic dose (other than lowest)
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
4813 mg/kg/2Y-C
TOXIC EFFECTS :
Tumorigenic - equivocal tumorigenic agent by RTECS criteria Liver - tumors
TYPE OF TEST :
TD - Toxic dose (other than lowest)
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
10080 mg/kg/24W-C
TOXIC EFFECTS :
Tumorigenic - equivocal tumorigenic agent by RTECS criteria Liver - tumors
TYPE OF TEST :
Morphological transformation
TYPE OF TEST :
Unscheduled DNA synthesis

MUTATION DATA

TYPE OF TEST :
Cytogenetic analysis
TEST SYSTEM :
Rodent - hamster Lung
DOSE/DURATION :
2 mmol/L
REFERENCE :
MUREAV Mutation Research. (Elsevier Science Pub. B.V., POB 211, 1000 AE Amsterdam, Netherlands) V.1- 1964- Volume(issue)/page/year: 341,77,1994 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOHS - National Occupational Hazard Survey (1974) NOHS Hazard Code - 80458 No. of Facilities: 197 (estimated) No. of Industries: 5 No. of Occupations: 12 No. of Employees: 4170 (estimated) NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - 80458 No. of Facilities: 35 (estimated) No. of Industries: 1 No. of Occupations: 2 No. of Employees: 1698 (estimated) No. of Female Employees: 1135 (estimated)

盐酸美沙吡林安全信息

[ 符号 ]:

GHS06

[ 信号词 ]:
Danger

[ 危害声明 ]:
H301

[ 警示性声明 ]:
P301 + P310

[ 个人防护装备 ]:
Eyeshields;Faceshields;Gloves;type P2 (EN 143) respirator cartridges

[ 危害码 (欧洲) ]:
T

[ 风险声明 (欧洲) ]:
R25

[ 安全声明 (欧洲) ]:
S22;S36;S45

[ 危险品运输编码 ]:
UN 2811 6.1/PG 3

[ WGK德国 ]:
3

[ RTECS号 ]:
UT1750000

[ 包装等级 ]:
III

[ 危险类别 ]:
6.1(b)

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相关化合物

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