美沙吡林

美沙吡林用途

甲氧吡啶是一种组胺拮抗剂,是一种具有抗胆碱能活性的吡啶类化学物质。甲基比林可引起靶器官特异性表观遗传改变,如DNA甲基化水平降低。甲基比林诱导大鼠肝癌[1][2]。

美沙吡林名称

[ CAS 号 ]:
91-80-5

[ 中文名 ]:
美沙吡林

[ 英文名 ]:
methapyrilene

[英文别名 ]:

Restryl
Thenylpyramine
Paradormalene
Methapyrilen
Semikon
Pyrinistol
Thionylan
Pyrinistab
Thenylene
metapyrilene

美沙吡林生物活性

[ 描述 ]:

[ 相关类别 ]:

研究领域 >> 癌症

信号通路 >> 神经信号通路 >> mAChR

信号通路 >> 免疫及炎症 >> 组胺受体

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 由mAChR

研究领域 >> 神经疾病

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 组胺受体

[体外研究]

甲基苯丙胺(650μM,72 h)降低了HepRG细胞中转铁蛋白的转录水平,并伴随着转铁蛋白蛋白水平的降低[1]。

[体内研究]

甲基苯丙胺(用水(载体)灌胃,50或150 mg/kg,每日,3天)可诱导大鼠肝毒性并导致门周肝坏死[2]。动物模型：雄性Wistar衍生的AlpK:APfSD(Alderley Park)大鼠[2]剂量：50 mg/kg,150 mg/kg给药：每天用水(载体)灌胃,3天。肝脏中葡萄糖和糖原水平降低。显示50 mg/kg低剂量组尿液中琥珀酸和二甲基甘氨酸水平较高。

美沙吡林物理化学性质

[ 沸点 ]:
173 - 175ºC at 3 mm Hg

[ 分子式 ]:
C₁₄H₁₉N₃S

[ 分子量 ]:
261.38600

[ 精确质量 ]:
261.13000

[ PSA ]:
47.61000

[ LogP ]:
2.71130

[ 外观性状 ]:
无色液体

美沙吡林毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: UT1400000

CHEMICAL NAME :: Pyridine, 2-((2-(dimethylamino)ethyl)-2-thenylamino)-

CAS REGISTRY NUMBER :: 91-80-5

BEILSTEIN REFERENCE NO. :: 0220729

LAST UPDATED :: 199706

DATA ITEMS CITED :: 9

MOLECULAR FORMULA :: C14-H19-N3-S

MOLECULAR WEIGHT :: 261.42

WISWESSER LINE NOTATION :: T6NJ BN2N1&1&1- BT5SJ

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 150 mg/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Behavioral - excitement Behavioral - aggression

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 182 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Behavioral - convulsions or effect on seizure threshold

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 77 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 :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 20 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Behavioral - convulsions or effect on seizure threshold

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - guinea pig

DOSE/DURATION :: 375 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Behavioral - convulsions or effect on seizure threshold

MUTATION DATA

TYPE OF TEST :: Mutation in mammalian somatic cells

TEST SYSTEM :: Rodent - mouse Lymphocyte

DOSE/DURATION :: 100 mg/L

REFERENCE :: ENMUDM Environmental Mutagenesis. (New York, NY) V.1-9, 1979-87. For publisher information, see EMMUEG. Volume(issue)/page/year: 5,420,1983

美沙吡林安全信息

[ 危险品运输编码 ]:
UN 1851

[ 包装等级 ]:
III

[ 危险类别 ]:
6.1(b)